A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A family of hexahydropyridines.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
Agents inhibiting the effect of narcotics on the central nervous system.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.
An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
Compounds with BENZENE fused to AZEPINES.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.
Purine bases found in body tissues and fluids and in some plants.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
A group of compounds that contain the structure SO2NH2.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)
Seven membered heterocyclic rings containing a NITROGEN atom.
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
An integrin beta subunit of approximately 85-kDa in size which has been found in INTEGRIN ALPHAIIB-containing and INTEGRIN ALPHAV-containing heterodimers. Integrin beta3 occurs as three alternatively spliced isoforms, designated beta3A-C.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
Elements of limited time intervals, contributing to particular results or situations.
A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
The observable response an animal makes to any situation.
Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.
A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
Compounds with a BENZENE fused to IMIDAZOLES.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Injections into the cerebral ventricles.
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
Use of electric potential or currents to elicit biological responses.
Peptides composed of between two and twelve amino acids.
A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
Established cell cultures that have the potential to propagate indefinitely.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).
A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.
Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.
Cell surface proteins that bind CALCITONIN GENE-RELATED PEPTIDE with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the CENTRAL NERVOUS SYSTEM and the periphery. They are formed via the heterodimerization of the CALCITONIN RECEPTOR-LIKE PROTEIN and RECEPTOR ACTIVITY-MODIFYING PROTEIN 1.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.
Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.
A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
The most common inhibitory neurotransmitter in the central nervous system.
AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.
A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.
A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.
A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
The physical activity of a human or an animal as a behavioral phenomenon.
The rate dynamics in chemical or physical systems.
Drugs that bind to and activate dopamine receptors.
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)
Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
A subclass of serotonin receptors that form cation channels and mediate signal transduction by depolarizing the cell membrane. The cation channels are formed from 5 receptor subunits. When stimulated the receptors allow the selective passage of SODIUM; POTASSIUM; and CALCIUM.
A family of biologically active peptides sharing a common conserved C-terminal sequence, -Phe-X-Gly-Leu-Met-NH2, where X is either an aromatic or a branched aliphatic amino acid. Members of this family have been found in mammals, amphibians, and mollusks. Tachykinins have diverse pharmacological actions in the central nervous system and the cardiovascular, genitourinary, respiratory, and gastrointestinal systems, as well as in glandular tissues. This diversity of activity is due to the existence of three or more subtypes of tachykinin receptors.
A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ B with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the BRONCHI.
The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.
A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.
A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
Proteins prepared by recombinant DNA technology.
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.
A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.
Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
An angiotensin receptor subtype that is expressed at high levels in fetal tissues. Many effects of the angiotensin type 2 receptor such as VASODILATION and sodium loss are the opposite of that of the ANGIOTENSIN TYPE 1 RECEPTOR.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.
A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.
Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.
A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.
A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.
Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.
A subtype of BRADYKININ RECEPTOR that is induced in response to INFLAMMATION. It may play a role in chronic inflammation and has a high specificity for KININS lacking the C-terminal ARGININE such as des-Arg(10)-kallidin and des-Arg(9)-bradykinin. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
Compounds that inhibit the action of prostaglandins.
Drugs that selectively bind to and activate beta-adrenergic receptors.
A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.
A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.

(+/-)-Pindolol acts as a partial agonist at atypical beta-adrenoceptors in the guinea pig duodenum. (1/33)

The agonistic and antagonistic effects of (+/-)-pindolol (1-(1H-indol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanol) were estimated to clarify whether (+/-)-pindolol acts as a partial agonist on atypical beta-adrenoceptors in the guinea pig duodenum. (+/-)-Pindolol induced concentration-dependent relaxation with a pD2 value of 5.10 +/- 0.03 and an intrinsic activity of 0.83 +/- 0.03. However, the relaxations to (+/-)-pindolol were not antagonized by the non-selective beta1- and beta2-adrenoceptor antagonist (+/-)-propranolol (1 microM). In the presence of (+/-)-propranolol (1 microM), the non-selective beta1-, beta2- and beta3-adrenoceptor antagonist (+/-)-bupranolol (30 microM) induced a rightward shift of the concentration-response curves for (+/-)-pindolol (apparent pA2 = 5.41 +/- 0.06). In the presence of (+/-)-propranolol, (+/-)-pindolol (10 microM) weakly but significantly antagonized the relaxant effects to catecholamines ((-)-isoprenaline, (-)-noradrenaline and (-)-adrenaline), a selective beta3-adrenoceptor agonist BRL37344 ((R*,R*)-(+/-)-4-[2-[(2-(3-chlorophenyl)-2-hydroxyethyl) amino]propyl]phenoxyacetic acid sodium salt) and a non-conventional partial beta3-adrenoceptor agonist (+/-)-CGP12177A([4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H -benzimidazol-2-one] hydrochloride). These results demonstrate that (+/-)-pindolol possesses both agonistic and antagonistic effects on atypical beta-adrenoceptors in the guinea pig duodenum.  (+info)

Further evidence that (+/-)-carteolol-induced relaxation is mediated by beta2-adrenoceptors but not by beta3-adrenoceptors in the guinea pig taenia caecum. (2/33)

The properties of the beta1- and beta2-adrenoceptor partial agonist (+/-)-carteolol were investigated against the beta2- and beta3-adrenoceptors of the taenia caecum of the guinea pig. (--)-Isoprenaline and (+/-)-carteolol induced concentration-dependent relaxation in this tissue. The non-selective beta1- and beta2-adrenoceptor antagonist (+/-)-propranolol (10-100 nM), the selective beta2-adrenoceptor antagonist ICI 118,551 (10-100 nM) and the non-selective beta1-, beta2- and beta3-adrenoceptor antagonist (+/-)-bupranolol (10-100nM), caused a concentration-dependent rightward shift of the concentration-response curves for (--)-isoprenaline and (+/-)-carteolol. Schild regression plot analyses carried out for (+/-)-propranolol against (--)-isoprenaline and (+/-)-carteolol gave pA2 values of 8.35 and 8.24, respectively. Schild plot analyses of ICI 118,551 against (--)-isoprenaline and (+/-)-carteolol gave pA2 values of 8.47 and 8.41, respectively. Schild plot analyses of (+/-)-bupranolol against (--)-isoprenaline and (+/-)-carteolol gave pA2 values of 8.47 and 8.53, respectively. Slopes of the Schild plots were not significantly different from unity. These results suggest that the relaxant effects of (+/-)-carteolol in the guinea pig taenia caecum are mediated by beta2-adrenoceptors but not by beta3-adrenoceptors.  (+info)

Oestradiol and progesterone change beta3-adrenergic receptor affinity and density in brown adipocytes. (3/33)

OBJECTIVE: To check if the oestradiol- and progesterone-driven reduction in noradrenaline responsiveness of brown adipocytes is due to a reduction in either the density or the affinity of beta3-adrenoceptors (beta3-AR). beta1/beta2-AR were also studied. DESIGN: Four groups of animals were considered. (i) control rats at thermoneutrality, (ii) cold-acclimated rats, to determine beta-AR under continuous sympathetic stimulation, which is known to decrease noradrenaline responsiveness, (iii) oestradiol- and (iv) progesterone-treated cold-acclimated rats to determine hormonal effects on beta-AR populations in thermogenically active brown adipocytes. METHODS: Oestradiol and progesterone were chronically elevated by means of s.c. Silastic implants. Densities and affinities of beta-AR populations were determined by binding studies using [3H]CGP-12177 as radioligand. RESULTS: Two populations of low and high binding affinities (K(d) 1.6 and 27.3 nmol/l) corresponding to beta3- and beta1/beta2-AR respectively were found at thermoneutrality. beta3-AR density was higher than that of beta1/beta2-AR (B(max) 419 and 143 fmol/mg protein respectively). Cold-acclimated rats showed a reduction of beta3-AR binding capacity (B(max) 308 fmol/mg protein). Oestradiol and progesterone reduced the density of beta3-AR to 167 and 185 fmol/mg protein respectively, while increasing their affinity for [3H]CGP-12177 (K(d) 9.5 and 4.0 nmol/l vs 16 nmol/l in cold-acclimated untreated rats). The density of beta1/beta2-AR was also reduced after oestradiol treatment (B(max) 51 fmol/mg protein). CONCLUSIONS: Both oestradiol and progesterone reduce the density of beta3-AR in brown adipose tissue (BAT) while increasing their affinity for [3H]CGP-12177. Oestradiol also reduces the density of beta1/beta2-AR whereas cold-acclimation reduces the density of beta3-AR.  (+info)

Mouse beta 3a- and beta 3b-adrenoceptors expressed in Chinese hamster ovary cells display identical pharmacology but utilize distinct signalling pathways. (4/33)

1. This study characterizes the mouse beta(3a)-adrenoceptor (AR) and the splice variant of the beta(3)-AR (beta(3b)-AR) expressed in Chinese hamster ovary cells (CHO-K1). 2. Stable clones with high (approximately 1200), medium (approximately 500) or low receptor expression (approximately 100 fmol mg protein(-1)) were determined by saturation binding with [(125)I]-(-)-cyanopindolol. Competition binding studies showed no significant differences in affinity of beta-AR ligands for either receptor. 3. Several functional responses of each receptor were measured, namely extracellular acidification rate (EAR; cytosensor microphysiometer), cyclic AMP accumulation, and Erk1/2 phosphorylation. The beta(3)-AR agonists BRL37344, CL316243, GR265162X, L755507, SB251023, the non-conventional partial beta-AR agonist CGP12177 and the beta-AR agonist (-)-isoprenaline caused concentration-dependent increases in EAR in cells expressing either splice variant. CL316243 caused concentration-dependent increases in cyclic AMP accumulation and Erk1/2 phosphorylation in cells expressing either receptor. 4. PTX treatment increased maximum EAR and cyclic AMP responses to CL316243 in cells expressing the beta(3b)-AR but not in cells expressing the beta(3a)-AR at all levels of receptor expression. 5. CL316243 increased Erk1/2 phosphorylation with pEC(50) values and maximum responses that were not significantly different in cells expressing either splice variant. Erk1/2 phosphorylation was insensitive to PTX or H89 (PKA inhibitor) but was inhibited by LY294002 (PI3K gamma inhibitor), PP2 (c-Src inhibitor), genistein (tyrosine kinase inhibitor) and PD98059 (MEK inhibitor). 6. The adenylate cyclase activators forskolin or cholera toxin failed to increase Erk1/2 levels although both treatments markedly increased cyclic AMP accumulation in both beta(3a)- or beta(3b)-AR transfected cells. 7. These results suggest that in CHO-K1 cells, the beta(3b)-AR, can couple to both G(s) and G(i) to stimulate and inhibit cyclic AMP production respectively, while the beta(3a)-AR, couples solely to G(s) to increase cyclic AMP levels. However, the increase in Erk1/2 phosphorylation following receptor activation is not dependent upon coupling of the receptors to G(i) or the generation of cyclic AMP.  (+info)

Physiological antagonism between ventricular beta 1-adrenoceptors and alpha 1-adrenoceptors but no evidence for beta 2- and beta 3-adrenoceptor function in murine heart. (5/33)

1. Murine left atrium lacks inotropic beta(2)-adrenoceptor function. We investigated whether beta(2)-adrenoceptors are involved in the cardiostimulant effects of (-)-adrenaline on spontaneously beating right atria and paced right ventricular myocardium of C57BL6 mice. We also studied a negative inotropic effect of (-)-adrenaline. 2. Sinoatrial tachycardia, evoked by (-)-adrenaline was resistant to blockade by beta(2)-selective ICI 118,551 (50 nM) but antagonized by beta(1)-selective CGP 20712A (300 nM). This pattern was unaffected by pretreatment with pertussis toxin (PTX, 600 microg kg(-1) i.p. 24 h) which reversed carbachol-evoked bradycardia to tachycardia. 3. Increases of ventricular force by (-)-adrenaline and (-)-noradrenaline were not blocked by ICI 118,551 but antagonized by CGP 20712A. 4. Under blockade of beta-adrenoceptors, (-)-adrenaline and (-)-noradrenaline depressed ventricular force (-logIC(50)M=7.7 and 6.9). The cardiodepressant effects of (-)-adrenaline were antagonized by phentolamine (1 microM) and prazosin (1 microM) but not by (-)-bupranolol (1 microM). Prazosin potentiated the positive inotropic effects of (-)-adrenaline (in the absence of beta-blockers) from -logEC(50)M=6.2 - 6.8. 5. PTX-treatment reduced carbachol-evoked depression of ventricular force in the presence of high catecholamine concentrations. Inhibition of ventricular function of G(i) protein was verified by 82% reduction of in vitro ADP-ribosylation. PTX-treatment tended to increase the positive inotropic potency of (-)-adrenaline under all conditions investigated, including the presence of ICI 118,551. 6. (-)-Adrenaline causes murine cardiostimulation through beta(1)-adrenoceptors but not through beta(2)-adrenoceptors. The negative inotropic effects of (-)-adrenaline are mediated through ventricular alpha(1)-adrenoceptors but not through beta(3)-adrenoceptors. Both G(i) protein and alpha(1)-adrenoceptors restrain (-)-adrenaline-evoked increases in right ventricular force mediated through beta(1)-adrenoceptors.  (+info)

Evidence against beta 3-adrenoceptors or low affinity state of beta 1-adrenoceptors mediating relaxation in rat isolated aorta. (6/33)

1 The presence of beta(3)-adrenoceptors and the low affinity state of the beta(1)-adrenoceptor (formerly "putative beta(4)-adrenoceptor") was investigated in ring preparations of rat isolated aorta preconstricted with phenylephrine or prostaglandin F(2alpha) (PGF(2alpha)). Relaxant responses to isoprenaline, selective beta(3)-adrenoceptor agonists (BRL 37344, SR 58611A, CL 316243) and non-conventional partial agonists (CGP 12177A, cyanopindolol, pindolol) were obtained. 2 In phenylephrine-constricted, but not PGF(2alpha)-constricted rings, relaxations to isoprenaline showed a propranolol-resistant component. 3 In phenylephrine-constricted rings, relaxations to BRL 37344 (pEC(50), 4.64) and SR 58611A (pEC(50), 4.94) were not antagonized by the selective beta(3)-adrenoceptor antagonist SR 59230A (< or =1 microM). CL 316243 (< or =100 microM) failed to produce relaxation. In PGF(2alpha)-constricted rings only SR 58611A produced relaxation, which was not affected by SR 59230A (< or =3 microM). 4 Non-conventional partial agonists produced relaxation in phenylephrine-constricted but not PGF(2alpha)-constricted rings. The relaxation to CGP 12177A was unaffected by SR 59230A (< or =1 microM) or by CGP 20712A (10 microM), reported to block the low affinity state of the beta(1)-adrenoceptor. 5 beta-adrenoceptor antagonists also produced relaxation in phenylephrine-constricted rings with an order of potency of (pEC(50) values): bupranolol (5.5) approximately 38;SR 59230A (5.47) approximately 38;cyanopindolol (5.47)>pindolol (5.30)>alprenolol (5.10)>propranolol (4.83)>ICI 118551 (4.60)>CGP 12177A (4.38) approximately 38;CGP 20712A (4.35). Bupranolol (100 microM), alprenolol (30 microM), propranolol (100 microM) and SR 59230A (10 microM) produced no relaxation in PGF(2alpha)-constricted rings. 6 These results provide no evidence for the presence of functional beta(3)-adrenoceptors or the low affinity state of the beta(1)-adrenoceptor in rat aorta.  (+info)

Role of nitric oxide in beta3-adrenoceptor activation on basal tone of internal anal sphincter. (7/33)

Effects of activation of beta3-adrenoceptor (beta3-AR) have not been determined in the spontaneously tonic smooth muscle of the internal anal sphincter (IAS). The effects of disodium (R,R)-5-[2-[2-3-chlorophenyl)-2-hydroxyethyl]-amino]propyl]-1,3-benzodioxole-2,2- dicarboxylate (CL 316243), a selective beta3-AR agonist, on the basal smooth muscle tone and direct release of nitric oxide (NO) by circular smooth muscle strips of the opossum IAS were determined. We also examined the presence of endothelial nitric oxide synthase (eNOS) protein by Western blot studies. CL 316243 produced a concentration-dependent relaxation of the smooth muscle that remained unmodified by different neurohumoral antagonists. The smooth muscle relaxation by CL 316243 was selectively antagonized by L 748337, a beta3-AR antagonist. Such relaxation was several times longer than by isoproterenol. The effect of CL 316243 was significantly attenuated by a nonselective NOS inhibitor N(omega)-nitro-l-arginine (l-NNA) and by putative inhibitor of eNOS l-N5-(1-iminoethyl)-ornithine dihydrochloride (l-NIO). Inhibitors of iNOS [N-(3-aminomethyl)benzyl acetamide 2HCl] and nNOS [1-[2-(trifluoromethylphenyl)imidazole]] had no effect on this relaxation. Relaxation of the IAS smooth muscle induced by CL 316243 was accompanied by an increased release of NO; this was attenuated by l-NNA and l-NIO. In addition, Western blot studies revealed the presence of eNOS in the circular smooth muscle of the IAS. These data demonstrate potent and protracted IAS smooth muscle relaxation by beta3-AR activation, which is partly transduced via NOS, possibly smooth muscle eNOS. Multiple signal-transduction pathways including NOS activation may explain the characteristic IAS relaxation by beta3-AR activation. The studies may have therapeutic implications in anorectal motility disorders.  (+info)

White adipose tissue contributes to UCP1-independent thermogenesis. (8/33)

Beta3-adrenergic receptors (AR) are nearly exclusively expressed in brown and white adipose tissues, and chronic activation of these receptors by selective agonists has profound anti-diabetes and anti-obesity effects. This study examined metabolic responses to acute and chronic beta3-AR activation in wild-type C57Bl/6 mice and congenic mice lacking functional uncoupling protein (UCP)1, the molecular effector of brown adipose tissue (BAT) thermogenesis. Acute activation of beta3-AR doubled metabolic rate in wild-type mice and sharply elevated body temperature and BAT blood flow, as determined by laser Doppler flowmetry. In contrast, beta3-AR activation did not increase BAT blood flow in mice lacking UCP1 (UCP1 KO). Nonetheless, beta3-AR activation significantly increased metabolic rate and body temperature in UCP1 KO mice, demonstrating the presence of UCP1-independent thermogenesis. Daily treatment with the beta3-AR agonist CL-316243 (CL) for 6 days increased basal and CL-induced thermogenesis compared with naive mice. This expansion of basal and CL-induced metabolic rate did not require UCP1 expression. Chronic CL treatment of UCP1 KO mice increased basal and CL-stimulated metabolic rate of epididymal white adipose tissue (EWAT) fourfold but did not alter BAT thermogenesis. After chronic CL treatment, CL-stimulated thermogenesis of EWAT equaled that of interscapular BAT per tissue mass. The elevation of EWAT metabolism was accompanied by mitochondrial biogenesis and the induction of genes involved in lipid oxidation. These observations indicate that chronic beta3-AR activation induces metabolic adaptation in WAT that contributes to beta3-AR-mediated thermogenesis. This adaptation involves lipid oxidation in situ and does not require UCP1 expression.  (+info)

The P2X₇ receptor is an ATP-gated cation channel expressed by a number of cell types, including osteoblasts. Genetically modified mice with loss of P2X₇ function exhibit altered bone formation. Moreover, activation of P2X₇ in vitro stimulates osteoblast differentiation and matrix mineralization, although the underlying mechanisms remain unclear. Because osteogenesis is associated with enhanced cellular metabolism, our goal was to characterize the effects of nucleotides on metabolic acid production (proton efflux) by osteoblasts. The P2X₇ agonist 2,3-O-(4-benzoylbenzoyl)ATP (BzATP; 300 μM) induced dynamic membrane blebbing in MC3T3-E1 osteoblast-like cells (consistent with activation of P2X₇ receptors) but did not induce cell death. Using a Cytosensor microphysiometer, we found that 9-min exposure to BzATP (300 μM) caused a dramatic increase in proton efflux from MC3T3-E1 cells (∼2-fold), which was sustained for at least 1 h. In contrast, ATP or UTP (100 μM), which activate P2 receptors
Harnessing the potential of cells as complex biosensors promises the potential to create sensitive and selective detectors for discrimination of biodefense agents. Here we present toxin detection and suggest discrimination using cells in a multianalyte microphysiometer (MMP) that is capable of simultaneously measuring flux changes in four extracellular analytes (acidification rate, glucose uptake, oxygen uptake, and lactate production) in real-time. Differential short-term cellular responses were observed between botulinum neurotoxin A and ricin toxin with neuroblastoma cells, alamethicin and anthrax protective antigen with RAW macrophages, and cholera toxin, muscarine, 2,4-dinitro-phenol, and NaF with CHO cells. These results and the post exposure dynamics and metabolic recovery observed in each case suggest the usefulness of cell-based detectors to discriminate between specific analytes and classes of compounds in a complex matrix, and furthermore to make metabolic inferences on the cellular effects
The goal of this work is development of a fast and repeatable optical assay that uses a novel combination of fluorophores and endogenous contrast to report on the metabolic phenotype of cancers in vivo. The proportions of ATP generated by glycolysis and oxidative phosphorylation relate to inherent tumor behaviors that affect treatment response. The need for instruments measuring metabolic endpoints is demonstrated by the widespread use of Seahorse extracellular flux analyzers in cancer research. The assays provide valuable insight into two primary arms of cellular metabolism by reporting on extracellular acidification rate (ECAR) related to glycolysis and oxygen consumption rate (OCR) related to mitochondrial respiration [1]. The ratio OCR/ECAR obtained by Seahorse was used to compare a panel of breast cancer cell lines and show that basal subtypes were often highly glycolytic, which suggested better therapeutic outcome [2]. While the Seahorse is an excellent research tool, the technique ...
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Structure, properties, spectra, suppliers and links for: {4-[(2R)-2-{[(2R)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino}propyl]phenoxy}acetic acid.
WATERNT Program (v1.01) was used to estimate the water solubility of the test substance 2-[[4-[bis(2-hydroxyethyl)amino]-o-tolyl]azo] -5-nitrobenzonitrile (CAS no. 12236-25-8). The estimated water solubility of the test substance 2-[[4-[bis(2-hydroxyethyl)amino]-o-tolyl]azo]-5-nitrobenzonitrile (CAS no. 12236-25-8) at 25 deg C was 61.338 mg/l. Based on the estimated value, the test substance 2-[[4-[bis(2-hydroxyethyl)amino]-o-tolyl]azo]-5-nitrobenzonitrile (CAS no. 12236-25-8) was considered to be slightly soluble in water. ...
TY - JOUR. T1 - A potent juvenile hormone mimic, 1-(4′-ethylphenoxy)-6,7-epoxy-3,7-dimethyl-2-octene, labeled with tritium in either the ethylphenyl- or geranyl-derived moiety. AU - Kamimura, Hideo. AU - Hammock, Bruce D.. AU - Yamamoto, Izuru. AU - Casida, John E.. PY - 1972. Y1 - 1972. N2 - Reduction of citral with sodium borotritide, conversion of the alcohol product to the bromo derivative, formation of the ether by reaction with 4-ethyl-phenol, and epoxidation yields 1-(4′-ethylphenoxy)-6,7 - epoxy - 3,7 - dimethyl - 2 - octene-1 -3H. Alternatively, tritiation of 4-ethylphenol with tritium water in sulfuric acid, reaction of the recovered phenol with geranyl bromide, and epoxidation yields 1 - (4′-ethylphen-3H-oxy)-6,7-epoxy-3,7-dimethyl-2-octene. the products have a high specific activity (33 to 654 mCi per mmol) and are useful in studies on the degradation and mode of action of this potent juvenile hormone mimic.. AB - Reduction of citral with sodium borotritide, conversion of the ...
91051-78-4 - Fatty acids, tallow, 2-(bis(2-hydroxyethyl)amino)ethyl esters - Searchable synonyms, formulas, resource links, and other chemical information.
61361-60-2 - KBPURVPYVJJZGS-UHFFFAOYSA-N - Phenol, 2-(((2-hydroxyethyl)amino)methyl)-4-nitro- - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Interconnected RNA processing mechanisms ensure the fidelity of non-conventional mRNA splicing during the unfolded protein response.
This course is designed for graduate students with an interest in using primary research literature to discuss and learn about current research around non-conventional light stable isotope geochemistry.
Volume-specific proton flux is measured in a closed system as the time derivative of proton concentration, expressed in units [pmol·s-1·mL-1]. Proton flux can be measured in an open system at steady state, when any acidification of the medium is compensated by external supply of an equivalent amount of base. The extracellular acidification rate (ECAR) is the change of pH in the incubation medium over time, which is zero at steady state. Volume-specific proton flux is comparable to volume-specific oxygen flux [pmol·s-1·mL-1], which is the (negative) time derivative of oxygen concentration measured in a closed system, corrected for instrumental and chemical background. pH is the negative logarithm of proton activity. Therefore, ECAR is of interest in relation to acidification issues in the incubation buffer or culture medium. The physiologically relevant metabolic proton flux, however, must not be confused with ECAR ...
Platelets show decreased glycolytic rate in asthma.(A) Extracellular acidification rate (ECAR) trace in asthmatic (filled squares) and healthy controls (open sq
3-[Acetyl(pentyl)amino]propyl acetate | C12H23NO3 | CID 582542 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
[65 Pages Report] Check for Discount on [3-[(ethylimidocarbonyl)amino]propyl]trimethylammonium iodide Global Market and Forecast Research report by ChemReport. DescriptionWe provide independent and unbiased information on manufacturers, prices, production...
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Page 3-Images and discussion of techniques which fall outside the other categories or cover more than one... Please be descriptive in your titles!
Sigma-Aldrich offers abstracts and full-text articles by [R Mitchell Baldwin, Margaret Bejide, Laura Trinkle-Mulcahy, Jocelyn Côté].
Title:Non-Conventional Desulfurization of Fuels and Biofuels: A Review. VOLUME: 13 ISSUE: 2. Author(s):Debarpita Ghosal* and Sankhajit Pal. Affiliation:Department of Chemical Engineering, C.V. Raman College of Engineering, Bhubaneswar, Odisha- 752054, Department of Chemical Engineering, C.V. Raman College of Engineering, Bhubaneswar, Odisha- 752054. Keywords:Desulfurization, fuel, biofuel, non-conventional processes, aromatics, microfibrous material.. Abstract:Sulphur compounds in fuel cause major environmental pollution. Hence, the desulphurization of fuel has become a tremendous concern. Aside from the standard hydrodesulphurization method, many new processes have gained attention. Our present work discusses varied non-conventional desulphurization techniques likeaerobic desulphurization, adsorbent desulphurization, membrane desulphurization, extractive desulphurization, etc. These strategies in conjunction with their pros and cons are mentioned well.. ...
You are viewing an interactive 3D depiction of the molecule (3z)-4-{[(2s)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}-3-[4-methyl-6-(4-morpholinyl)-1,3-dihydro-2h-benzimidazol-2-ylidene]-2(3h)-pyridinone (C24H17ClN5O3) from the PQR.
TY - JOUR. T1 - Analyses of Avascular Mutants Reveal Unique Transcriptomic Signature of Non-conventional Endothelial Cells. AU - Pak, Boryeong. AU - Schmitt, Christopher E.. AU - Choi, Woosoung. AU - Kim, Jun Dae. AU - Han, Orjin. AU - Alsiö, Jessica. AU - Jung, Da Woon. AU - Williams, Darren R.. AU - Coppieters, Wouter. AU - Stainier, Didier Y.R.. AU - Jin, Suk Won. PY - 2020/11/23. Y1 - 2020/11/23. N2 - Endothelial cells appear to emerge from diverse progenitors. However, to which extent their developmental origin contributes to define their cellular and molecular characteristics remains largely unknown. Here, we report that a subset of endothelial cells that emerge from the tailbud possess unique molecular characteristics that set them apart from stereotypical lateral plate mesoderm (LPM)-derived endothelial cells. Lineage tracing shows that these tailbud-derived endothelial cells arise at mid-somitogenesis stages, and surprisingly do not require Npas4l or Etsrp function, indicating that ...
TY - JOUR. T1 - Decreased FBP1 expression rewires metabolic processes affecting aggressiveness of glioblastoma. AU - Son, Beomseok. AU - Lee, Sungmin. AU - Kim, Hyunwoo. AU - Kang, Hyunkoo. AU - Jeon, Jaewan. AU - Jo, Sunmi. AU - Seong, Ki Moon. AU - Lee, Su Jae. AU - Youn, Hye Sook. AU - Youn, Bu Hyun. PY - 2020/1/2. Y1 - 2020/1/2. N2 - Radiotherapy is a standard treatment option for patients with glioblastoma (GBM). Although it has high therapeutic efficacy, some proportion of the tumor cells that survive after radiotherapy may cause side effects. In this study, we found that fructose 1,6-bisphosphatase 1 (FBP1), a rate-limiting enzyme in gluconeogenesis, was downregulated upon treatment with ionizing radiation (IR). Ets1, which was found to be overexpressed in IR-induced infiltrating GBM, was suggested to be a transcriptional repressor of FBP1. Furthermore, glucose uptake and extracellular acidification rates were increased upon FBP1 downregulation, which indicated an elevated glycolysis ...
N-[3-[Bis-(2-hydroxyethyl)amino]propyl]hexadecan-1-amide/ACM66161657 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
N-{3-oxo-3-[(1,2,2,6,6-pentamethylpiperidin-4-yl)amino]propyl}furan-2-carboxamide | C18H29N3O3 | CID 1502175 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
There are close to 28 million nurses around the world who comprise a global workforce that delivers about 90 percent of primary healthcare, including frontline response to the COVID-19 pandemic. Ensuring their optimal contribution and continued well-being amid the myriad consequences of COVID-19 will increase the potential for measurable and improved health outcomes.. ...
The main subject is the equilibrium and the evolution of 2D and 3D dry soap-like |br /|foams. A star-triangle equivalence is proved using geometrical methods and |br /|invariance by inversion transformations. This equivalence states that triangular bubbles can be freely exchanged with threefold stars without perturbing the overall equilibrium; a star is a set of three edges ending at a central vertex. Considering an equilibrated foam in contact with a solid, curved and smooth, surface and considering the trace of the films on the surface as a non-conventional 2D foam, the equilibrium equations are established for this 2D foam, generalising the standard case of flat Hele-Shaw cells. The invariance of the vertex equilibrium conditions by conformal transformations is proved. As an application, the configurations of foams in thin interstices between two non parallel plates is analysed in details. Normal incidence and Laplaces law lead to an approximate equation relating the plate profile to a conformal map
|.. ۞ Refactoring a double negative to make it a single positive conditional if ( !item.isNotFound() )item.is found as Double-Negative Regulatory T Cells: non-conventional regulators signaling pathways influencing SLF and c-Kit-mediated survival and proliferation. The Isolation Kit is developed for the isolation of CD4-CD8-CD56-CD3+TCRα/β+ T cells from PBMCs in peripheral blood lymphocytes. To examine the…
Absynth Biologics discovers and develops vaccines and antibodies to prevent and treat bacterial infections based on proprietary, non-conventional platform for identifying novel protein antigen that harness the immune system and that use a dual-action mechanism. ...
Tan CK., Davies M.J, McCluskey DK., Munro IR., Nweke MC., Tracey MC., Szita N., Electromagnetic stirring in a microbioreactor with non-conventional chamber morphology and implementation of multiplexed mixing, Journal of Chemical Technology and Biotechnology (2015) 1927- ...
2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydrofuran-2-yl]methyl (3R)-3-hydroxy-4-({3-oxo-3-[(2-sulfanylethyl)amino]propyl}amino)-2,2-dimethyl-4-oxobutyl dihydrogen ...
N,N-butane-1,4-diylbis[1-hydroxy-N-(3-{[(1-hydroxy-6-oxo-1,6-dihydropyridin-2-yl)carbonyl]amino}propyl)-6-oxo-1,6-dihydropyridine-2-carboxamide ...
A comparative study of application of different non-conventional filters on electroencephalogram., Gauri Shanker Gupta, Maanvi Bhatnagar, Shikhar Kumar, Rakesh Kumar Sinha
Upon liver injury, hepatic stellate cells (HSCs) transdifferentiate to migratory, proliferative and extracellular matrix-producing myofibroblasts (e.g., activated HSCs; aHSCs) causing liver fibrosis. HSC activation is associated with increased glycolysis and glutaminolysis. Here, we compared the contribution of glycolysis, glutaminolysis and mitochondrial oxidative phosphorylation (OXPHOS) in rat and human HSC activation. Basal levels of glycolysis (extracellular acidification rate ~3-fold higher) and particularly mitochondrial respiration (oxygen consumption rate ~5-fold higher) were significantly increased in rat aHSCs, when compared to quiescent rat HSC. This was accompanied by extensive mitochondrial fusion in rat and human aHSCs, which occurred without increasing mitochondrial DNA content and electron transport chain (ETC) components. Inhibition of glycolysis (by 2-deoxy-D-glucose) and glutaminolysis (by CB-839) did not inhibit rat aHSC proliferation, but did reduce Acta2 (encoding α-SMA) ...
Lookchem Provide Cas No.118474-59-2 Basic information: Properties,Safety Data,Sds and Other Datebase. We also Provide Trading Suppliers & Manufacture for 118474-59-2 10-{3-[(2-aminoethyl)amino]propyl}-3,6-bis(dimethylamino)acridinium platinum(2+) chloride (1:1:3).
3. Invest to get the best quality human resources. Finding and retaining skilled workers is a major challenge for companies operating in Africa. Securing a supply of the best local people, recruiting in the diaspora, transferring skills from other parts of your company and working hard to retain key staff will be an essential element of success, notes E&Y.. 4. Expand from strategic economic hubs and think about non-conventional market groupings. Some African countries are much more developed than others when it comes to infrastructure, financial services and the availability of skilled labour. Investors should consider setting up their base in these countries for expansion into the rest of the continent.. Expansion plans should also look at non-conventional regional market groupings such as urban corridors, cultural affinities and regional economic communities in order to build critical mass and drive higher returns more quickly, says the report. ...
Molecular Caging (MC) processed dosage forms for various sustained release formulations applicable to solid, liquid, gel, and for oral or parenteral administrations. Micro and nano particles/capsules and non-conventional delivery systems ...
Its unfair that you decided to single out for a reason Edwin Casimero. He is a staunch supporter of that school of thought according to which the causes of most of the ailments that befell us are linked with the defectuous way in which most of us nourish ourselves. Hence his plea for raw, fruitarianism etc. You could not have failed to notice that he is a staunch enemy of junk food. The truth is that most what Casimero claims makes sense... True, his is an intuitionist, non-conventional approach that spits in the face of the establishment. But sooner or later, most of his daring theories prove to be right. I am not sure that cancer is a fungus (as he claims), perhaps it is up to a certain point, yet according to a recent New Scientist article, Alzheimer is a form of diabetes caused by the flawed way we feed ourselves (well, at least most of us) too much sugar and carbs, gluten and bad quality highly processed saturated oils ...
There are many alternative views on cancer treatment. This category is dedicated to non-conventional treatment of cancer and information on alternative methods of dealing with chemotherapy and radiation.
Most eukaryotic proteins are secreted through the conventional endoplasmic reticulum (ER)-Golgi secretory pathway. However, cytoplasmic, nuclear and signal-peptide-containing proteins have been shown to reach the cell surface by non-conventional transport pathways. The mechanisms and molecular compo …
The Energy Statistics Database contains comprehensive energy statistics on the production, trade, conversion and final consumption of primary and secondary; conventional and non-conventional; and new and renewable sources of energy. The Energy Statistics dataset, covering the period from 1990 onwards, is available at UNdata. For data prior to 1990, please refer to http://unstats.un.org/unsd/energy/edbase.htm ...
Harnessing AWRI s yeast and bacterial research to shape next-gen Chardonnay Part 1: Wild and non-conventional yeast - Christopher Curtin, Jennifer Bellon, Eveline Bartowsky, Paul Henschke, Paul Chambers, Markus Herderich and Isak Pretorius ...
While our ability to accurately diagnose and treat allergic disease has benefited from scientific understanding of what happens during an allergic reaction, a number of tests and treatments have been promoted in the absence of any scientific rationale. Some non-conventional approaches to disease also claim that various disorders unrelated to allergy have an immune basis.…
Ourea style is designed for an everyday active and refined lifestyle, combining both classic and non-conventional elements in its character. Large and discreet, the Spei comes with an adjustable shoulder strap and sleek statement magnetic fastenings placed on the middle closure of the bag. The Ourea is inspired by the
Thiamine-dependent enzymes (TDEs) control metabolic pathways that are frequently altered in cancer and therefore present cancer-relevant targets. We have previously shown that the recombinant enzyme thiaminase cleaves and depletes intracellular thiamine, has growth inhibitory activity against leukemia and breast cancer cell lines, and that its growth inhibitory effects were reversed in leukemia cell lines by rapamycin. Now, we first show further evidence of thiaminase therapeutic potential by demonstrating its activity against breast and leukemia xenografts, and against a primary leukemia xenograft. We therefore further explored the metabolic effects of thiaminase in combination with rapamycin in leukemia and breast cell lines. Thiaminase decreased oxygen consumption rate and increased extracellular acidification rate, consistent with the inhibitory effect of acute thiamine depletion on the activity of the TDEs pyruvate dehydrogenase and 2-oxoglutarate dehydrogenase complexes; these effects were
I obtained my PhD on Fluids Thermodynamics Engineering in 2012, at the TERMOCAL research group (Universidad de Valladolid). During this period I worked on the experimental determination of the density of non-conventional fuel gas mixtures by using a single sinker densimeter with magnetic coupling. These experimental results were important for the further development of the current equation of state for natural gas, in order to introduce the use of biogas and other non-conventional fuel gases. I also had the opportunity to develop part of my work at two top research institutes: the Lehrstuhl für Thermodynamik, at Ruhr Universität Bochum (Germany), where I carried out measurements of the sorption of gases in polyols and MOF samples by using a gravimetric sorption analyzer; and the National Institute of Standards and Technology (NIST) Boulder (USA), where I characterized the thermodynamic behavior of a new fluid for use in refrigeration and organic Rankine cycles. In addition, during my PhD, I ...
Non Conventional Aquatint V:. Date: May 4, 2017. Temperature: 71 F. Humidity: moderate. Researchers: Claire Crews and Sam Guerin. How does Neutralizer sprayed onto aquatinted plate effect the aquatint medium?. For this experiment we sprayed aquatint medium to cover the entire plate (sprayed for 3 minutes at a distance of 18″ with the nozzle open 2 turns), then immediately sprayed an area with neutralizer at 6″ for 3 seconds. Neutralizer caused aquatint medium to move to edges of sprayed area and drip to bottom of plate, creating some stopped out areas and some stippled areas.. Even coverage of aquatint medium on plate:. ...
One unique example of RNA processing is non-conventional splicing of RNAs, which is an essential step during transfer RNA (tRNA) maturation. tRNAs are transcribed as precursor transcripts (pre-tRNA) and are subjected to multiple posttranscriptional processing events before they can fulfil their function. Intron-containing pre-tRNAs undergo non-conventional splicing-a cytosolic, enzyme-catalysed processing reaction. The splicing of pre-tRNAs occurs in two steps: The intron is first excised by a splicing endonuclease and the resulting tRNA exon halves are ligated by tRNA ligase to form a fully matured functional tRNA. Because eukaryotic tRNA introns disrupt the anticodon stem-loop structure, the removal of these introns is an essential process ...
Tosin Onabanjo is a Research Fellow in Energy Systems at Cranfield University, UK. Her research is actively contributing to the development of the Nano-Membrane Toilet, a project funded by the Bill and Melinda Gates Foundation and designed for people lacking access to modern sanitation. Here, she shares how a microbe Saccharomyces cerevisiae, popularly known as bakers yeast, influenced her non-conventional multidisciplinary career path. Meet Tosin on her Soapbox on Saturday, 9th July in Milton Keynes, as she speaks on The Role of Microbiomes in the Energy Economy.. SS: How did you get to your current position?. TO: I have a non-conventional career path! I started out as a Microbiologist with the intention to become a medical doctor. I got fascinated by microbes and their applications, so I completed my Bachelors in Microbiology at Olabisi Onabanjo University, Nigeria and went on to get a Masters degree in Biotechnology at University of Hertfordshire, UK. Prior to my Masters degree, I ...
It is no secret that over the past two months, Goldman has commenced a full endorsement of Nominal GDP targetting as a method to stimulate the economy, not to mention Wall Streets bonus pool, after Ben Bernanke completely ignored Hatzius advice to reduce the Interest on Overnight Excess Reserve rate as well as subsequent pleading for a start of MBS LSAP. Mathematics once again aside, and as we demonstrated, the math works out to an non-trivial incremental $10 trillion in debt through 2016 on top of what will be issued, to catch up with the GDP growth run rate and to eliminate the excess slack in the economy, the question is whether NGDP would achieve any tangible stimulus at all, or merely reduce the Feds ever smaller arsenal of non-conventional means to boost the economy by one more approach. The attached rhetorical Q&A just released by Goldman seeks to answer that and any other left over questions one may have on NGDP as a policy measure, and further puts out the inverse strawman argument that it
The point is that the practice of medicine, whether conventional or non-conventional is always dependent upon the context of the culture within which it is practiced. That means that each culture has criteria upon which it decides whether something is effective or not effective. And there are no 100 per cent reliable criteria to determine whether one particular treatment will benefit each individual who undertakes it. At the moment, the litmus test for medicine in the west, is a scientific trial. However these trials are unreliable. I have friend with MS who has been presribed a cocktail of drugs, all of which are useless. When researching the efficacy of these drugs I discovered none of them had been trialed by the drug companies on unhealthy frail individuals taking many other prescription drugs, the very people they would be presribed to. Instead, drug trials are aimed first of all, at very healthy people who take no drugs at all. The target population in these situations receives a drug ...
Alternative fuel sources come in all shapes and sizes. But if you are confused about what they are, here is a short definition. Alternative fuels are non-conventional or advanced sources of fuel; substances that can be used as fuel sources that are not conventional.
She has carved a permanent place in the showbiz world by taking non-conventional route from portraying a hot-headed don in Fukrey...
The Energy Statistics Database contains comprehensive energy statistics on the production, trade, conversion and final consumption of primary and secondary; conventional and non-conventional; and new and renewable sources of energy. The Energy Statistics dataset, covering the period from 1990 onwards, is available at UNdata. For data prior to 1990, please refer to http://unstats.un.org/unsd/energy/edbase.htm ...
Mazes are usually two-dimensional. I wanted to create a three-dimensional one, said the always non-conventional Danish architect Bjarke Ingels at the launch of his new BIG Maze at the National Building Museum (NBM) in Washington, D.C.read more. ...
"Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... SR 59230A is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 ... Bellantuono V, Cassano G, Lippe C (August 2008). "The adrenergic receptor subtypes present in frog (Rana esculenta) skin". Comp ...
... is a short-acting beta adrenergic receptor antagonist. Acylation of glycidol (2) with the acid chloride 1 produces ... 1. Novel .beta.-blockers with ultrashort duration of action". Journal of Medicinal Chemistry. 27 (8): 1007. doi:10.1021/ ... 81 (3): 309-22. PMID 8235065. Kam, Sheung Tsam; Matier, William L.; Mai, Khuong X.; Barcelon-Yang, Cynthia; Borgman, Robert J ... the ester 3. Reaction of that intermediate with amine 4, obtained by reaction of 1,1-dimethylethylenediamine with urea, gives ...
"Death temporally related to the use of a Beta adrenergic receptor antagonist in cocaine associated myocardial infarction". ... "Reflections on beta-adrenergic receptor blockers and cocaine use. A case in point". Revista Española De Cardiología. 62 (4): ... Schurr, James W.; Gitman, Brenda; Belchikov, Yuly (2014-12-01). "Controversial therapeutics: the β-adrenergic antagonist and ... "Potentiation of Cocaine-Induced Coronary Vasoconstriction by Beta-Adrenergic Blockade". Annals of Internal Medicine. 112 (12): ...
... is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 ... "Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... "Administration of a selective β2 adrenergic receptor antagonist exacerbates neuropathology and cognitive deficits in a mouse ...
... bronchodilation Subtype unspecific β antagonists (beta blockers) can be used to treat: heart arrhythmia - decrease the output ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 There is no α1C receptor. There was a subtype known as C, but ... and β-Adrenergic Receptors Theory of receptor activation Desensitization of β1 receptors. ... Sep 2010). "Ghrelin secretion stimulated by {beta}1-adrenergic receptors in cultured ghrelinoma cells and in fasted mice". ...
... denotes selective antagonist to the receptor. compound-6FA, PAM at intracellular binding site Beta-2 adrenergic receptor has ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ...
Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic ... is a beta-adrenergic receptor, and also denotes the human gene encoding it. Actions of the β3 receptor include Enhancement of ... Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through ...
... adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics. 290 (2): 649-55. PMID 10411574. v ... β3-adrenoceptor antagonist) is an adrenergic antagonist which blocks the Beta-3 adrenergic receptors of cells, with either high ... SR 59230A Carvedilol Betablocker Beta-3 adrenergic receptor Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, ... an antagonist for β3 and for β1 or β2 adrenoceptors) like the non-selective betablocker Carvedilol. ...
... is a beta adrenergic receptor antagonist. Curtis-Prior, PB; Gadd, AL (1990). "Beta-adrenoceptor antagonists and human ... 42 (3): 220-2. doi:10.1111/j.2042-7158.1990.tb05395.x. PMID 1974626. S2CID 85573776. v t e v t e. ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Chlorprothixene is an antagonist of the following receptors: 5-HT2, 5-HT6, 5-HT7: antipsychotic effects, sedation/anxiolysis, ... I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes". Methods Find ...
... is a beta adrenergic receptor antagonist. Mostaghim, R; Maddox, YT; Ramwell, PW (1986). "Endothelial potentiation ... of relaxation response to beta adrenoceptor blocking agents". The Journal of Pharmacology and Experimental Therapeutics. 239 (3 ...
... is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high specificity (an antagonist ... ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... A Beta-2 adrenergic antagonist (β2-adrenoceptor antagonist) ... "The pharmacology of a beta 2-selective adrenoceptor antagonist ... which is selective for β2 adrenoceptors) like Butaxamine and ICI-118,551, or non-specifically (an antagonist for β2 and for β1 ...
... is a beta adrenergic receptor antagonist. The methyl group on a sulfoxide is sufficiently acidic to substitute for ... "Studies on the mechanism of the acute antihypertensive and vasodilator actions of several beta-adrenoceptor antagonists". J. ... Bromination followed by condensation with 4-(4-methoxyphenyl)butan-2-amine (not PMA) gives the aminoketone 3. Successive ...
... carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular ... Bronchospasms and low blood sugar because at high doses drug can be an antagonist for β2 adrenergic receptors located in lung ... Smith C, Teitler M (April 1999). "Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors" (PDF). ... 15 (1). Bristow, M. R.; Hershberger, R. E.; Port, J. D.; Minobe, W.; Rasmussen, R. (1989). "Beta 1- and beta 2-adrenergic ...
"Three-dimensional models for beta-adrenergic receptor complexes with agonists and antagonists". Journal of Medicinal Chemistry ... In 1984 the β3 receptor was described as the third group of beta receptors in adipose tissue. This led to the development of ... Beta-adrenergic agonist Beta2-adrenergic agonist "Betmiga , European Medicines Agency". www.ema.europa.eu. Retrieved 2018-10-02 ... β2 adrenergic receptors to prevent over-activation by opposing the classical inotropic effect of β1 and β2 adrenergic receptors ...
... and β-adrenergic receptor antagonist. Alpha blocker Beta blocker Palluk R, Hoefke W, Gaida W, Mierau J, Bechtel WD (July 1986 ... "Interactions of MEN 935 (adimolol), a long acting beta- and alpha-adrenolytic antihypertensive agent, with postsynaptic alpha- ... 333 (3): 277-83. doi:10.1007/bf00512941. PMID 3020439. S2CID 24300936. v t e v t e. ...
January 2016). "Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive ... The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment ... Indication is more precautious as well when other muscarinic antagonists are used that are not selective. In addition, ... receptor. The receptors are located in the kidneys, urinary tract and bladder tissue. Upon binding, the β3 receptor undergoes a ...
"Identification of adenylate cyclase-coupled beta-adrenergic receptors with radiolabeled beta-adrenergic antagonists". ... NRGs bind to the ERBB receptors to promote phosphorylation of specific tyrosine residues on the C-terminal link of the receptor ... Neuregulins are ligands of the ERBB-family receptors, while NRG1 and NRG2 are able to bind and activate both ERBB3 and ERBB4, ... NRGs bind to the ERBB3 and ERBB4 tyrosine kinase receptors; they then form homodimers or heterodimers, often consisting of ...
... carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular ... Schliep HJ, Harting J (1984). "Beta 1-selectivity of bisoprolol, a new beta-adrenoceptor antagonist, in anesthetized dogs and ... "Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors" (PDF). Cardiovasc Drugs Ther. 13 (2): 123-6. ... Bristow M. R.; Hershberger R. E.; Port J. D.; Minobe W.; Rasmussen R. (1989). "Beta 1- and beta 2-adrenergic receptor-mediated ...
... is a beta adrenergic receptor antagonist. Stephenson, KA; Wilson, AA; Meyer, JH; Houle, S; Vasdev, N (2008). "Facile ... Synthesis, radiolabeling, and ex vivo biodistribution of 18F-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol ...
Beta blockers) β1-selective antagonists include: Acebutolol (in hypertension, angina pectoris and arrhythmias) Atenolol (in ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic ... The beta-1 adrenergic receptor (β1 adrenoceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the ... "The cardiac beta-adrenergic receptor. Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by ...
September 2018). "β3-adrenergic receptor activation induces TGFβ1 expression in cardiomyocytes via the PKG/JNK/c-Jun pathway". ... Bond RA, Clarke DE (November 1988). "Agonist and antagonist characterization of a putative adrenoceptor with distinct ... pharmacological properties from the alpha- and beta-subtypes". British Journal of Pharmacology. 95 (3): 723-34. doi:10.1111/j. ... BRL-37344 is a drug which acts as a selective agonist of the β3 adrenergic receptor, which has been investigated for various ...
J. W. Black; A. F. Crowther; R. G. Shanks; A. C. Dornhorst (1964). "A new adrenergic beta-receptor antagonist". The Lancet. 283 ... he called beta adrenotropic receptor (now β-adrenoceptor or β-adrenergic receptor). ″This concept of two fundamental types of ... he called alpha adrenotropic receptor (now α-adrenoceptor or α-adrenergic receptor), while the receptor with the second rank ... that both are beta type receptors. … It is suggested that this terminology be extended to the realm of adrenergic blocking ...
For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta ... angiotensin II receptor antagonists, calcium-channel blockers, and thiazide diuretics are generally preferred over beta ... Nebivolol while selectively blocking beta(1) receptor acts as a beta(3)-agonist. β3 receptors are found in the gallbladder, ... It works by blocking β1-adrenergic receptors in the heart and dilating blood vessels. Nebivolol was patented in 1983 and came ...
Straube T, Frey JU (2003). "Involvement of beta-adrenergic receptors in protein synthesis-dependent late long-term potentiation ... an antagonist to the NMDA receptor, which prevented LTP in this pathway.[24] Conversely, LTP in the mossy fiber pathway is NMDA ... β-adrenergic receptor agonists such as norepinephrine may alter the protein synthesis-dependent late phase of LTP.[51] Nitric ... "Selective impairment of learning and blockade of long-term potentiation by an N-methyl-D-aspartate receptor antagonist, AP5". ...
"Dobutamine increases alveolar liquid clearance in ventilated rats by beta-2 receptor stimulation". Am. J. Respir. Crit. Care ... Dobutamine is predominantly a β1-adrenergic agonist, with weak β2 activity, and α1 selective activity, although it is used ... isomer is a potent β1 agonist and α1 antagonist, while the (−) isomer is an α1 agonist. The administration of the racemate ... Since it does not act on dopamine receptors to inhibit the release of norepinephrine (another α1 agonist), dobutamine is less ...
Straube T, Frey JU (2003). "Involvement of beta-adrenergic receptors in protein synthesis-dependent late long-term potentiation ... an antagonist to the NMDA receptor, which prevented LTP in this pathway. Conversely, LTP in the mossy fiber pathway is NMDA ... Additionally, β-adrenergic receptor agonists such as norepinephrine may alter the protein synthesis-dependent late phase of LTP ... As mentioned previously, AMPA receptors are the brain's most abundant glutamate receptors and mediate the majority of its ...
Adrenergic receptor Alpha blocker Antagonist Beta blocker List of adrenergic drugs Propanolol Sympathetic nervous system ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group ... The α-adrenergic antagonists have different effects from the β-adrenergic antagonists. Adrenergic ligands are endogenous ...
... is a first generation, non-selective beta blocker in the class of β-adrenergic receptor antagonists. On the receptor ... "Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO ... "The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan ... The rationale behind this strategy has its basis in the fact that pindolol is an antagonist of the serotonin 5-HT1A receptor. ...
Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, ... Beta-Adrenoceptor Antagonists (Beta-Blockers); "CV Pharmacology , Beta-Adrenoceptor Antagonists (Beta-Blockers)". Archived from ... β2 and β3 receptors. β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors are ... β3-adrenergic receptors are located in fat cells. Beta receptors are found on cells of the heart muscles, smooth muscles, ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... norepinephrine then acting on lipolysis-inducing beta receptors.. Muscle mass[edit]. Males typically have more skeletal muscle ...
transmembrane signaling receptor activity. • Wnt-activated receptor activity. • G-protein coupled receptor activity. ... amyloid-beta binding. • signal transducer activity. • Wnt-protein binding. • protein binding. • protein kinase binding. • ... "Purification and molecular cloning of a secreted, Frizzled-related antagonist of Wnt action". Proc. Natl. Acad. Sci. U.S.A. 94 ... "Frizzled Receptors: FZD5". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ...
... α1-adrenergic receptor antagonist (Ki = 75 nM and 86 nM, respectively).[12] It possesses low or no affinity for the 5-HT1A, 5- ... Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... α2-adrenergic receptor (Ki = 730 nM),[12] likely acting as an antagonist there as well. ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ...
... fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is evidence that it may have ... some alpha-1 [7] and alpha-2 adrenoceptor antagonist activity.[5] D1 receptor stimulation activates adenylyl cyclase and raises ... Concomitant use of fenoldopam with a beta-blocker should be avoided if possible, as unexpected hypotension can result from beta ... Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial ...
February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT ... It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and dopamine D2, and as a partial ...
... a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. ... Antagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol ... Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (1998). „[3H]Rauwolscine: an antagonist radioligand for the ...
... a new antipsychotic with combined dopamine and serotonin receptor antagonist activity". J Pharmacol Exp Ther 275 (1): 101-13. ... Antagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol ... H1 Antagonist (Ki = 47 nM). *α1-adrenergic Antagonist (Ki = 10 nM) ... Smatra se da deluje kao antagonist na tim receptorima.[8][9] Ziprasidon takođe pokazuje umerenu inhibiciju sinaptičkog ponovnog ...
... captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist.[2] It produces ... Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... enhances hypothalamic BDNF expression in vivo by synergistic 5-HT2c receptor antagonism and sigma-1 receptor agonism". J. ...
General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ... Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ... H2-receptor antagonists, cytoprotectants, prostaglandin analogues. *Lower digestive tract: laxatives, antispasmodics, ... Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ...
These substances are neuroleptic and are either an antagonist of dopamine at the postsynaptic level at the D2 receptor site or ... beta-Ergocryptine. CH(CH3)2. CH(CH3)CH2CH3 (S). Isoleucine ... Adrenergic receptor modulators. α1. *Agonists: 6-FNE. * ... Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, ... a 5-HT2A/2C antagonist.[15] The selectivity and affinity of ergolines for certain 5-HT receptors can be improved by introducing ...
Re dhe vetëm beta receptor antagonist adrenergic, dichloroisoproterenol, gjithashtu ishte e pershkruara me larte dhe do të ... Alquist kishte raportuar më parë se efektet adrenergic mund të klasifikohen si alfa ose beta varësi të potencë relative të ... për shkak të efekteve beta adrenergic siç tregohet nga potencies relative e-isoproterenol l,-l epinephrine dhe-l norepinephrina ... për të treguar se efektet catecholamine në formimin AMP ciklike janë për shkak të efekteve përmes receptorit beta adrenergic. ...
Angiotensin II receptor antagonist. *ACE inhibitor. *Alpha-adrenergic agonist. *Beta blocker. *Dopamine agonist ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ... Drug classes that share a common molecular mechanism of action by modulating the activity of a specific biological target.[3] ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Receptor/signaling modulators. GABA receptor modulators. GABAA receptor positive modulators. Ionotropic glutamate receptor ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ...
... with gamma decay following rapidly after beta decay: I. 53. 131. ⟶. β. +. ν. ¯. e. +. Xe. ∗. 54. 131. +. 606. keV. {\ ... Meta-[I-131]iodobenzylguanidine is a radio-labeled analog of the adrenergic blocking agent guanethidine.[37] Radioactivity is ... displaystyle {\ce {^{131}_{53}I-,\beta +{\bar {\nu }}_{e}+{^{131}_{54}Xe^{\ast }}+606keV}}}. Xe. ∗. 54. 131. ⟶. Xe. 54. 131. + ... Beta decay also produces an antineutrino, which carries off variable amounts of the beta decay energy. The electrons, due to ...
... an alpha-2 adrenergic agonist Irbesartan, an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker ... Vasopressin receptor antagonists, such as conivaptan Acetazolamide, a carbonic anhydrase inhibitor Lithium was previously used ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 19 (3): 759-762. ISSN 0145-6008. PMID 7573805. Fichman, M. P.; Kleeman, C. R.; Bethune, J. E. (1970-01-01). "Inhibition of ...
Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors.[22] ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ...
Beta blockers. *Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... "Combining opioid and adrenergic mechanisms for chronic pain". Postgraduate Medicine. 126 (4): 98-114. doi:10.3810/pgm.2014.07. ... Partial agonist at the mu opioid receptor; agonist at delta opioid receptor; antagonist at kappa opioid receptor.. Sublingual, ... Full agonist at kappa opioid receptors, partial agonist/antagonist at the mu opioid receptors.[39]. IM, IV, SC.. Protein ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... History: 2,5-DMA was first synthesized in Tuckahoe, New York by Richard Baltzly and Johannes S. Buck in 1939.[3] ... History: Experiments on psychiatric patients who were given 3,4-DMA at dosages of 70 mg to 700 mg by IV injection took place at ...
Beta blockers. *Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... but other drugs such as CB1 receptor antagonists exist in this class too.[25][26] Drugs used to treat sleep disorders such as ... on adrenergic receptors.[83] It is most usually marketed as the hydrochloride or sulfate salt. ...
5-HT2A receptor antagonist.. *Propranolol - Sympatholytic, beta blocker.. *Clonidine - Sympatholytic, α2-adrenergic receptor ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ... 46 (3): 424-9. doi:10.1345/aph.1Q405. PMID 22395254.. *^ Rif S. El-Mallakh; S. Nassir Ghaemi (2 April 2007). Bipolar Depression ... 11 (3): 171-83. doi:10.2165/00148581-200911030-00003. PMID 19445546.. *^ Schacter, Daniel L.; Gilbert, Daniel T.; Wegner, ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... 3,4-Methylenedioxyphenethylamine ("3,4-MDPEA" or just "MDPEA"), also known as homopiperonylamine, is a substituted ... InChI=1S/C9H11NO2/c10-4-3-7-1-2-8-9(5-7)12-6-11-8/h1-2,5H,3-4,6,10H2 ...
See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... Serotonin antagonists and reuptake inhibitors *Etoperidone. *Nefazodone. *Trazodone. *Tricyclic antidepressants *Amitriptyline ... InChI=1S/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ... InChI=1/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ...
Beta blockers. *Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... α-Adrenergic receptor agonists[edit]. Main article: α-Adrenergic receptor agonist. Common or widely marketed[edit]. * ... Pseudoephedrine acts indirectly on the adrenergic receptor system, whereas phenylephrine and oxymetazoline are direct agonists ... α1-adrenergic receptor since they mediate vasoconstriction and constricting nasal vasculature causes decongestion of nasal ...
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Frequent infusions of beta-lactam antibiotics without exceeding total daily dose would help to keep the antibiotics level above ... and H2 antagonist are useful in a person with risk factors of developing upper gastrointestinal bleeding (UGIB) such as on ... the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I-like receptors. Invariably, the ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Galanin receptor 1 (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.[5] ... "Galanin Receptors: GAL1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it. *v ...
... compounds will be screened for their ability to inhibit or stimulate that receptor (see antagonist and agonist): if the target ... on beta blockers and cimetidine, and the discovery of statins by Akira Endo.[15] Another champion of the approach of developing ... who pioneered the first inhaled selective beta2-adrenergic agonist for asthma, the first inhaled steroid for asthma, ranitidine ... 9 (3): 203-14. doi:10.1038/nrd3078. PMID 20168317. S2CID 1299234.. *^ a b c d Current Model for Financing Drug Development: ...
... is a non-cardioselective beta blocker, that is, it blocks beta-1 receptors as well as beta-2 receptors. The latter ... Levobunolol (trade names AKBeta, Betagan, Vistagan, among others) is a non-selective beta blocker. It is used topically in the ... Further information: Beta blocker § Adverse effects. The most common side effect is eye irritation felt as stinging or burning ... Like other beta blockers, and unlike the anti-glaucoma medication pilocarpine, levobunolol has no effect on accommodation and ...
CRF1 and NK1 receptor antagonists". European Neuropsychopharmacology. Elsevier. 16 (7): 521-537. doi:10.1016/j.euroneuro. ... "Interaction between the antidepressant-like behavioral effects of beta adrenergic agonists and the cyclic AMP PDE inhibitor ... 1997). "Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites". J Pharmacol Exp ... Cusack B, Nelson A, Richelson E. (1994). "Binding of antidepressants to human brain receptors: focus on newer generation ...
Receptors, Adrenergic, beta-3 / genetics * Receptors, Adrenergic, beta-3 / physiology* * Syndrome * Translational Medical ... a paucity of public domain tools for the study of the drug target and aspects of receptor agonists as drugs had to be addressed ... Keywords: Drug development; Mirabegron; Species differences; Translational pharmacology; Urinary bladder; β(3)-Adrenoceptor. ...
Adrenergic alpha-1 Receptor Antagonists. Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. ... Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. To Top ... At Visits 2, 3, 4, and 5, subjects will complete the IPSS, EQ-5D-5L, OAB-q, PPBC, and TS-VAS. Maximum urinary flow (Qmax) will ... Change from Baseline to Week 12 (End of Treatment) in mean number of micturitions per day based on a 3-day diary [ Time Frame: ...
Adrenergic beta-Antagonists / administration & dosage* * Adult * Body Weight / drug effects * Circadian Rhythm ... Objective: Our objective was to test the safety and metabolic effects of a novel beta(3)-adrenoreceptor agonist (TAK-677) in ... 3-((2R)-(((2R)-3-chlorophenyl)-2-hydroxyethyl)amino)propyl)-1H-indol-7-yloxy)acetic acid ...
Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Muscarinic Antagonists. Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Comparisons of the Impact of Beta-3 Agonist Versus Antimuscarinics on Psychological Distress, Sexual Function, Bladder Wall ...
... adrenergic receptor antagonists. J Pharmacol Exp Ther. 1999;290:649-55.PubMedGoogle Scholar ... Differential distribution of beta-adrenergic receptor subtypes in blood vessels of knockout mice lacking beta(1)- or beta(2)- ... Beta3-adrenergic receptor subtype signaling in senescent heart: nitric oxide intoxication or "endogenous" beta blockade for ... Functional beta-adrenergic receptor signalling on nuclear membranes in adult rat and mouse ventricular cardiomyocytes. ...
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); DRB57K47QC (Celiprolol); Y41JS2NL6U (Bisoprolol). ... 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); 0 (Cytokines); 0 (Interleukin-6); 0 (Lipids); ... 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Vasodilator Agents); 268B43MJ25 (Uric Acid); 2TN51YD919 (Hypoxanthine); ... 0 (Adrenergic beta-Antagonists); 0 (Propanolamines); 67P356D8GH (Acebutolol); 820484N8I3 (Histamine); DRB57K47QC (Celiprolol); ...
Info Adrenergic Agents. * Info Adrenergic Antagonists. * Info Adrenergic beta-3 Receptor Antagonists ... 1 result for Category equals ADRENERGIC BETA-3 RECEPTOR ANTAGONISTS. Property. Value. ... 3-(2-Ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate View Synonyms. View Structure. ...
Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic ... is a beta-adrenergic receptor, and also denotes the human gene encoding it. Actions of the β3 receptor include Enhancement of ... Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through ...
... adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics. 290 (2): 649-55. PMID 10411574. v ... β3-adrenoceptor antagonist) is an adrenergic antagonist which blocks the Beta-3 adrenergic receptors of cells, with either high ... SR 59230A Carvedilol Betablocker Beta-3 adrenergic receptor Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, ... an antagonist for β3 and for β1 or β2 adrenoceptors) like the non-selective betablocker Carvedilol. ...
Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Muscarinic Antagonists. Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Regular use of any inducer of liver metabolism (e.g. barbiturates, rifampin) in the 3 months prior to admission to the Clinical ... History of smoking more than 10 cigarettes (or equivalent amount of tobacco) per day within 3 months prior to admission to the ...
Alpha- or beta-adrenergic antagonists did not attenuate the initial rise in PRA. The PRA increased again after 48 hours of ... Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog.. C R Ayers ... At the end of the chronic isoproterenol infusion period, beta-adrenergic receptor refractoriness was demonstrated, as PRA did ... Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog. ...
... surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, ... adrenergic receptor. Science 245: 1118-1121. Hadcock JR and Malbon CC (1988) Down‐regulation of betaadrenergic receptors: ... Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. In: Hardman JG and Limbird L (eds) ... 1996) The betaadrenergic receptor is a substrate for the insulin receptor tyrosine kinase. Journal of Biological Chemistry 271 ...
... beta3 adrenoceptor antagonist (CAS 1135278-41-9), with ,99% purity. Water soluble compound. Join researchers using our high ... Neuroscience Neurotransmission Receptors / Channels GPCR Adrenergic Receptors Share by email SR 59230A hydrochloride, beta3 ... Agonists, activators, antagonists and inhibitors. Cell lines and Lysates. Multiplex Assays. By research area. Cancer. ... Functional identification of rat atypical beta-adrenoceptors by the first beta 3-selective antagonists, ...
For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor,antagonists,using,CypHer5E, ... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ...
... adrenergic receptor antagonists.. Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, Cascieri MA, Weber AE. ... Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.. Weber AE, Mathvink RJ, Perkins L, ... of the efficacy of glucagon receptor antagonists in murine liver expressing the human glucagon receptor. ... A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects.. Qureshi SA, Rios Candelore M, Xie D, Yang ...
Atenolol contraindication digoxin 0. Beta-adrenergic blockers propranolol, 5-10 mg q8 to 12h PO; atenolol, 6. ... At higher dosages, atenolol may affect beta2 receptors in the contraindication of atenolol, which may affect breathing. ... Data from other beta-blocker trials suggest that if there is any question concerning the use of IV beta-blocker or clinical ... Beta blockers are one of several antihypertensive drug classes associated with ED. Nebivolol is a beta blocker with ...
... adrenergic receptor antagonists, compositions comprising .alpha.-adrenergic receptor antagonists that are optionally ... 2-((.beta.-(4-Hydroxyphenyl) ethyl) t-butoxycarbonylaminomethyl)-1-tetralone. 2-((.beta.-(3-(4-Hydroxyphenyl) ethyl) ... adrenergic receptor antagonists: NO.sub.n -.alpha.-antagonists where n is 1 or 2. The .alpha.-adrenergic antagonists can be ... adrenergic receptor antagonists or the modifications of .alpha.-adrenergic receptor antagonists to be directly or indirectly ...
4. What is the role played by beta-agonists in the treatment of the overactive bladder?. β3-adrenergic receptor agonists ... This is a long-acting M3 receptor-specific muscarinic receptor antagonist, which allows for a single daily dose. Its use to ... with a predominant expression of β3 receptors in the detrusor muscle. Activation of β3 adrenergic receptors causes relaxation ... β3 adrenergic receptor agonists have the effect of improving symptoms related to overactive bladder. Patients who may benefit ...
The effects of various adrenergic beta receptor agonists and antagonists on lipolysis (measured as glycerol release) in human ... Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs.. M Frisk-Holmberg and ... Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs.. M Frisk-Holmberg and ... Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs.. M Frisk-Holmberg and ...
Beta-arrestin-dependent activation of Ca(2+)/calmodulin kinase II after beta(1)-adrenergic receptor stimulation. J Cell Biol. ... Isoform-specific antagonists of exchange proteins directly activated by cAMP. Proc Natl Acad Sci U S A. 2012;109(45):18613- ... β-arrestin 1 regulates β2-adrenergic receptor-mediated skeletal muscle hypertrophy and contractility. Skelet Muscle. 2018;8(1): ... Beta-arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic beta cells. Proc Natl ...
... adrenergic receptor-mediated diseases, conditions, or disorders in a mammal which methods comprise administering to the mammal ... beta..sub.3 adrenergic receptor agonists of structural Formula (I), ##STR1##the stereoisomers and prodrugs thereof, and the ... pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R.sub.1, R.sub.2, R.sub.3, R.sub ... a glucocorticoid receptor agonist or antagonist, an orexin receptor antagonist, a urocortin binding protein antagonist, a ...
ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 ... "Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... "Administration of a selective β2 adrenergic receptor antagonist exacerbates neuropathology and cognitive deficits in a mouse ...
"Death temporally related to the use of a Beta adrenergic receptor antagonist in cocaine associated myocardial infarction". ... "Reflections on beta-adrenergic receptor blockers and cocaine use. A case in point". Revista Española De Cardiología. 62 (4): ... Schurr, James W.; Gitman, Brenda; Belchikov, Yuly (2014-12-01). "Controversial therapeutics: the β-adrenergic antagonist and ... "Potentiation of Cocaine-Induced Coronary Vasoconstriction by Beta-Adrenergic Blockade". Annals of Internal Medicine. 112 (12): ...
Removal of extracellular Ca2+ or addition of the Ca2+ channel antagonists nifedipine and verapamil almost totally abolished ... The beta-adrenergic receptor-induced inhibition was prevented by pertussis toxin and could not be reproduced by forskolin, ... Activation of beta-adrenergic receptors inhibits Ca2+ entry-mediated generation of inositol phosphates in the guinea pig ... Activation of beta-adrenergic receptors inhibits Ca2+ entry-mediated generation of inositol phosphates in the guinea pig ...
... beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist ... A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic ... beta-1; Adrenergic Receptor, beta-1; Receptor, Adrenergic, beta-1; Adrenergic Receptor, beta 1; Adrenergic Receptors, beta-1; ... Adrenergic beta 1 Receptors; Receptor, beta-1 Adrenergic; Receptors, Adrenergic beta-1; Receptors, beta 1 Adrenergic; beta 1 ...
... adrenergic receptor: a salt bridge linking extracellular loops 2 and 3. Small-molecule drugs that bind within the transmembrane ... The peptide adopts a beta-turn conformation and sits in the major groove of the RNA. Specific contacts are apparent between ... core and exhibit different efficacies towards G-protein activation (agonist, neutral antagonist and inverse agonist) also ... Solution mapping of T cell receptor docking footprints on peptide-MHC PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE ...
Beta-adrenergic antagonist:. 1. Beta adrenergic receptor blockade improves?. 2. Mechanisms for doing this? ... 1. Beta blockers improve overall prognosis and ventricular function. 2. They do this (above) by reducing potential for sudden ... Beta agonist: stimulates the heart, can be used short term. 4. Amrinone potentiates dobutamine --, additional stimulation ... 3. If BP is high, add nitroprusside to Dopamine and it wont bottom out because the increase in CO is much much greater than the ...
β3-adrenoceptor - Adrenoceptors. Detailed annotation on the structure, function, physiology, pharmacology and ... 2004) Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in ... adrenergic receptor antagonists. J. Pharmacol. Exp. Ther., 290 (2): 649-55. [PMID:10411574] ... and beta3-adrenergic receptors generates a beta-adrenergic signaling unit with distinct functional properties. J. Biol. Chem., ...
Dual inhibition of beta-adrenergic and angiotensin II receptors by a single antagonist: a functional role for receptor-receptor ... beta-2 adrenergic receptor , beta-2 adrenoreceptor , beta 2-AR , Adrb-2 , adrenoceptor beta 2, surface , adrenergic receptor ... 2002) Beta 1/beta 2-adrenergic receptor heterodimerization regulates beta 2-adrenergic receptor internalization and ERK ... 1988) Structural basis of beta-adrenergic receptor subtype specificity studied with chimeric beta 1/beta 2-adrenergic receptors ...
... and it is probably not surprising that a beta-adrenergic antagonist should have similarities of this type.. Open image in new ... where we display the Tanimoto similarity to all metabolites for the beta-(adrenergic receptor) blocker propranolol. All ... 3.School of Computer ScienceThe University of ManchesterManchesterUK. *4.Manchester Business SchoolThe University of Manchester ... Journal of Cheminformatics, 3, 30. doi: 10.1186/1758-2946-3-30.PubMedCentralPubMedGoogle Scholar ...
  • The effects of various adrenergic beta receptor agonists and antagonists on lipolysis (measured as glycerol release) in human adipose tissue in vitro were studied. (aspetjournals.org)
  • Stereoisomers of beta-adrenergic agonists and antagonists were 9- to 300-fold more potent than their corresponding (+) stereoisomers. (duke.edu)
  • Modulation of the activity of central serotoninergic neurons by novel serotonin1A receptor agonists and antagonists: a comparison to adrenergic and dopaminergic neurons in rats. (aspetjournals.org)
  • These SNPs also have the potential to alter response to medications when polymorphisms affect drug targets (e.g., beta-receptors), especially with regards to adrenergic agonists and antagonists. (ebmconsult.com)
  • The majority of the available literature on beta receptor antagonists and infantile hemangiomas pertains to propranolol. (jddonline.com)
  • Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood-brain barrier, has not been investigated for this purpose. (frontiersin.org)
  • Propranolol is a non-selective beta-adrenergic antagonist that has good penetration of the blood-brain barrier ( 21 ). (frontiersin.org)
  • METHODS: Burn mice were randomized to receive daily injections of propranolol (nonselective 1/ 2 antagonist), nadolol (long-acting 1/ 2 antagonist), butoxamine (selective 2 antagonist), or SR59230A (selective 3 antagonist) for 6 days after burn. (bireme.br)
  • RESULTS: Although propranolol improved early and late erythroblasts, only butoxamine and selective 3-antagonist administrations were positively reflected in the peripheral blood hemoglobin and red blood cells count. (bireme.br)
  • In order to evaluate the involvement of monoaminergic system, rats were pretreated with the inhibitor of brain serotonin stores p-chlorophenylalanin (PCPA), dopamine (SCH23390 and sulpiride), and adrenoceptor (prazosin and propranolol) antagonists. (bireme.br)
  • The beta-adrenergic antagonist, (-) propranolol, potently competed for the binding sites, causing half-maximal inhibition of binding at 9 nM. (duke.edu)
  • the pI50 for propranolol was approximately 6 (as expected for the beta 3-receptor). (nih.gov)
  • Schild plots for propranolol inhibition of norepinephrine-, isoprenaline-, BRL-37344- and CGP-12177-induced thermogenesis yielded similar pA2 (the negative logarithm of the inhibitory constant for an antagonist, as calculated from a series of agonist dose-response curves at different antagonist concentrations) (approximately 5.5), for interaction with either agonist, implying that the same receptor was stimulated by all agonists. (nih.gov)
  • Dopamine receptor agonists.iii. (bireme.br)
  • Dopamine receptor antagonists.iv. (bireme.br)
  • Structurally related compounds devoid of beta-adrenergic activity such as dopamine, dihydroxymandelic acid, normetanephrine, pyrocatechol, and phentolamine did not effectively compete for the binding sites. (duke.edu)
  • Different mechanisms mediated by dopamine D1 and D2 receptors are involved etiologically in activity-stress gastric lesion of the rat. (aspetjournals.org)
  • Biased signaling agonist of Dopamine D3 receptor induces receptor internalization independent of β-Arrestin recruitment. (bioportfolio.com)
  • 3: The method of claim 1, wherein the agents comprise at least two of a Gi-coupled dopamine D2 receptor agonist, a Gs-coupled .beta.1 adrenergic receptor antagonist, or a Gq-coupled .alpha.1 adrenergic receptor blocker. (patents.com)
  • β(3)-Adrenoceptor. (nih.gov)
  • Nebivolol, a vasodilating selective beta(1)-blocker, is a beta(3)-adrenoceptor agonist in the nonfailing transplanted human heart. (springer.com)
  • Human atrial β(1L)-adrenoceptor but not β 3 -adrenoceptor activation increases force and Ca(2+) current at physiological temperature. (springer.com)
  • A Beta-3 adrenergic antagonist (β3-adrenoceptor antagonist) is an adrenergic antagonist which blocks the Beta-3 adrenergic receptors of cells, with either high specificity (an antagonist which is selective for β3 adrenoceptors) like L-748,328, L-748,337 and SR 59,230A or non-specifically (an antagonist for β3 and for β1 or β2 adrenoceptors) like the non-selective betablocker Carvedilol. (wikipedia.org)
  • The beta-3 adrenergic receptor (β3-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it. (wikipedia.org)
  • Potent, selective β 3 adrenoceptor antagonist (IC 50 values are 40, 408 and 648 nM for β 3, β 1 and β 2 , respectively). (abcam.com)
  • The principal actions of cocaine on the cardiovascular system are from alpha- and beta-1-adrenoceptor stimulation resulting in increased heart rate, systemic arterial pressure, and myocardial contractility, which are major determinants of myocardial oxygen demand. (wikipedia.org)
  • ICI binds to the β 2 subtype with at least 100 times greater affinity than β 1 or β 3 , the two other known subtypes of the beta adrenoceptor. (wikipedia.org)
  • ICI 118,551 hydrochloride is a highly selective β 2 -adrenoceptor antagonist. (abmole.com)
  • Coexisting beta-adrenoceptor subtypes: significance for thermogenic process in brown fat cells. (nih.gov)
  • Our work reported in this review focuses on a potential new target for tocolytic drugs, the β 3 -adrenoceptor (ADRB3). (biomedcentral.com)
  • β(3)-Adrenoceptor agonists increase bladder capacity and prolong micturition interval. (unboundmedicine.com)
  • It is assumed that β(3)-adrenoceptor agonists could exert an inhibitory effect on bladder afferent through β(3)-adrenoceptors in the urothelium and detrusor, which eventually improve the symptom of urgency. (unboundmedicine.com)
  • Mirabegron is a potent and selective β(3)-adrenoceptor agonist. (unboundmedicine.com)
  • α(1)-Adrenoceptor antagonists (α(1)-blockers) have become a mainstay of male lower urinary tract symptoms treatment. (unboundmedicine.com)
  • Alpha 2-adrenoceptor antagonists block the stimulant effects of cocaine in mice. (isni.org)
  • title=Genetic variation of the beta(2)-adrenoceptor: its functional and clinical importance in bronchial asthma. (enacademic.com)
  • DESIGN AND METHODS: We determined the B2BKR genotype of 90 patients with essential hypertension and echocardiographically diagnosed LV hypertrophy, included in a double-blind study to receive treatment for 48 weeks with either the angiotensin II type 1 (AT1) receptor antagonist irbesartan or the beta1-adrenoceptor antagonist atenolol. (diva-portal.org)
  • Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through the action of the G proteins of the type Gs. (wikipedia.org)
  • The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. (curehunter.com)
  • The adrenergic system is the one that uses neurohormones and neurotransmitters called epinephrine (adrenaline) and norepinephrine (noradrenaline). (study.com)
  • While both norepinephrine and epinephrine act on beta receptors, it is mainly epinephrine that is in charge of stimulating beta receptors, so we'll ignore norepinephrine for simplicity's sake. (study.com)
  • There are three major types of beta receptors stimulated by epinephrine: beta-1, beta-2, and beta-3. (study.com)
  • When epinephrine stimulates beta-1 receptors, the heart rate increases, and the force of contraction of the heart increases as well. (study.com)
  • When epinephrine stimulates beta-2 receptors, the airways and the blood vessels (especially in skeletal muscle) dilate. (study.com)
  • Some medications can block the effects of epinephrine on beta receptors. (study.com)
  • 3. _____ Drugs that block the action of norepinephrine and epinephrine on alpha receptors (alpha adrenergic antagonists or alpha-blockers) dilate most blood vessels. (coursehero.com)
  • Cardioselective beta-1-adrenergic antagonists such as atenolol work by selectively binding to the beta-1 adrenergic receptors found in vascular smooth muscle and the heart, blocking the positive inotropic and chronotropic actions of endogenous catecholamines such as isoproterenol, norepinephrine, and epinephrine, thereby inhibiting sympathetic stimulation. (statpearls.com)
  • Beta blockers block the action of endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors , of the sympathetic nervous system , which mediates the fight-or-flight response . (netlibrary.net)
  • Beta receptors are found on cells of the heart muscles, smooth muscles , airways , arteries , kidneys , and other tissues that are part of the sympathetic nervous system and lead to stress responses, especially when they are stimulated by epinephrine (adrenaline). (netlibrary.net)
  • Beta blockers interfere with the binding to the receptor of epinephrine and other stress hormones, and weaken the effects of stress hormones. (netlibrary.net)
  • Non-specific agonists have a far weaker effect on beta-receptors than specific beta agonists such as epinephrine, Albuterol or Clenbuterol . (thinksteroids.com)
  • To understand the main differences between cardioselective and non-cardioselective beta blockers, we need to make sure you know some very basic concepts pertaining to adrenergic pharmacology. (study.com)
  • Large differences exist in the pharmacology of agents within the class, thus not all beta blockers are used for all indications listed below. (netlibrary.net)
  • title=Molecular pharmacology and modeling of vasopressin receptors. (enacademic.com)
  • in normal heart, ß 3 -ARs may mediate a moderate negative inotropic effect, but in heart failure, it may protect against adverse effects of excessive catecholamine stimulation by action on excitation-contraction coupling, electrophysiology, or remodelling. (springer.com)
  • ß(3) adrenergic stimulation of the cardiac Na+−K + pump by reversal of an inhibitory oxidative modification. (springer.com)
  • Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog. (ahajournals.org)
  • 2004) Characterization of agonist stimulation of cAMP‐dependent protein kinase and G protein‐coupled receptor kinase phosphorylation of the beta2‐adrenergic receptor using phosphoserine‐specific antibodies. (els.net)
  • Upon agonist stimulation, a fluorescent signal is observed as the CypHer5E-antibody conjugate is internalized alongside the receptor into acidic endosomal vesicles. (bio-medicine.org)
  • Excessive stimulation of beta-1 receptors can lead to irregular heart rhythms, or arrhythmias. (study.com)
  • Beta-1 stimulation also causes the release of an enzyme called renin from the kidneys. (study.com)
  • Effects on atrial repolarization of the interaction between K+ channel blockers and muscarinic receptor stimulation. (aspetjournals.org)
  • Direct stimulation of these receptors appear to decrease blood pressure independent of the central alpha-2 adrenergic effects. (infectiousdiseaseadvisor.com)
  • In conclusion, these data suggest that chronic ethanol feeding increased phosphodiesterase 4 activity in adipocytes, resulting in decreased accumulation of cAMP in response to beta-adrenergic activation and a suppression of beta-adrenergic stimulation of lipolysis. (dundee.ac.uk)
  • CypHer5E, consequently, can be used to screen for novel antagonists of known receptors and for potential ligands of non-G-protein coupled receptors (5) and orphan receptors. (bio-medicine.org)
  • Further, receptor models incorporating a flexible TM-V backbone allow reliable prediction of binding affinities for a set of diverse ligands, suggesting potential utility of this approach to design of effective and subtype-specific agonists for adrenergic receptors. (pubmedcentralcanada.ca)
  • Bile acids: natural ligands for an orphan nuclear receptor. (nature.com)
  • Ligands targeting the σ receptor are in clinical trials for treatment of Alzheimer's disease, ischemic str. (bioportfolio.com)
  • 2-(4,5-dihydro-1H-imidazol-2-yl)indazole (indazim) derivatives as selective I(2) imidazoline receptor ligands. (isni.org)
  • Endothelial beta3-adrenoreceptors mediate nitric oxide-dependent vasorelaxation of coronary microvessels in response to the third-generation beta-blocker nebivolol. (springer.com)
  • Beta-adrenergic receptors are G-protein linked and mediate the adenylate cyclase cascade in targeted cells. (jddonline.com)
  • Spinal nonadrenergic imidazoline receptors do not mediate the antinociceptive action of intrathecal clonidine in the rat. (aspetjournals.org)
  • Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. (abcam.com)
  • β(3)-Adrenoceptors are predominantly expressed in the human bladder and mediate relaxation of detrusor muscle. (unboundmedicine.com)
  • As a result, efforts to develop new antidepressant treatments included an emphasis on developing compounds that specifically did not have antagonist effects at muscarinic cholinergic receptors [17]. (google.com)
  • Here, we aimed to examine the contribution of adrenergic/cholinergic/opioid receptors to the antinociceptive effects of ESL in a trigeminal pain model, as these neurotransmitter systems are known to have an important role in the modulation of trigeminal nociception. (ac.rs)
  • The involvement of adrenergic/cholinergic/opioid receptors was evaluated by intraperitoneally pretreating mice with an appropriate antagonist immediately after peroral application of ESL. (ac.rs)
  • Benzodiazepine-withdrawal-induced gastric emptying disturbances in rats: evidence for serotonin receptor involvement. (aspetjournals.org)
  • Food restriction had no effect on receptor characteristics, and treatment of diabetic rats with insulin prevented any downregulation of cardiac bAR or aAR. (diabetesjournals.org)
  • Hajinezhad M R, Shohreh B. Possible Involvement of Beta-Adrenergic Receptors on Nociceptin/Orphanin FQ Induced Food Consumption in Male Rats, Zahedan J Res Med Sci. (zjrms.com)
  • The aim of this study was to determine the possible interaction between beta adrenergic and N/OFQ receptors on food consumption in male rats. (zjrms.com)
  • The results obtained from previous studies have shown that beta-receptor antagonists stimulate food consumption in rats [ 3 ]. (zjrms.com)
  • High dosages of beta adrenergic receptor agonists induce cardiomyocyte necrosis and interstitial fibrosis in rats [ 5 ]. (zjrms.com)
  • In response to beta-adrenergic activation, the early peak of cAMP accumulation was suppressed after ethanol feeding, although the basal cAMP concentration in adipocytes did not differ between pair- and ethanol-fed rats. (dundee.ac.uk)
  • Our objective was to test the safety and metabolic effects of a novel beta(3)-adrenoreceptor agonist (TAK-677) in humans. (nih.gov)
  • Beta blockers (β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, or beta adrenergic receptor antagonists ) are a class of drugs that are particularly used for the management of cardiac arrhythmias , protecting the heart from a second heart attack ( myocardial infarction ) after a first heart attack (secondary prevention), [1] and, in certain cases, hypertension . (netlibrary.net)
  • The beta-2 adrenergic receptor (β 2 adrenoreceptor), also known as ADRB2 , is an beta-adrenergic receptor , and also denotes the human gene encoding it. (enacademic.com)
  • Alprenolol is a nonspecific beta-adrenergic inhibitor with additional antagonist effects on serotonin 5HT-1a receptors. (jddonline.com)
  • Ligand-directed serotonin 5-HT receptor desensitization, β-arrestin recruitment, and sensitization. (bioportfolio.com)
  • Chronic intrarenal isoproterenol administration produced a similar increase in PRA, which peaked at 3-5 hours and then returned to control levels. (ahajournals.org)
  • At the end of the chronic isoproterenol infusion period, beta-adrenergic receptor refractoriness was demonstrated, as PRA did not increase significantly in response to a fourfold increase in the dose of isoproterenol. (ahajournals.org)
  • Twelve replicate wells contained a known agonist, isoproterenol, and four replicate wells contai ned a known antagonist, alprenolol, each diluted in 0.01% DMSO. (bio-medicine.org)
  • Here we show that while the carazolol pocket captured in the β 2 AR crystal structure accommodates (-)-isoproterenol and other agonists without steric clashes, a finite movement of the flexible extracellular part of TM-V helix (TM-Ve) obtained by receptor optimization in the presence of docked ligand can further improve the calculated binding affinities for agonist compounds. (pubmedcentralcanada.ca)
  • In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta 2 -adrenergic receptors compared to isoproterenol. (centerwatch.com)
  • In experiments 4 effects of isoproterenol (0.5 mg/kg) and Nociceptin antagonist (8 mg/kg) on food consumption was investigated. (zjrms.com)
  • Isoproterenol is a non-selective beta adrenergic agonist. (zjrms.com)
  • In the peripheral nervous system, as well as the brain, isoproterenol appears to have only beta-adrenergic activity. (zjrms.com)
  • Peripheral, but not central anorectic effect of isoproterenol is mediated by beta adrenergic receptors. (zjrms.com)
  • Receptor subtypes involved in dual effects induced by prostaglandin E2 in circular smooth muscle from dog colon. (aspetjournals.org)
  • Thus, despite the fact that different beta-receptor subtypes coexist in the tissue, we find no evidence for the participation of beta 1- or beta 2-receptors in the thermogenic response. (nih.gov)
  • title=Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. (enacademic.com)
  • 8 PKA also inhibits the excitatory Gq coupled pathway by phosphorylating the inositol trisphosphate receptor and phospholipase C resulting in inhibition of intracellular calcium release. (soxanddawgs.com)
  • Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs. (aspetjournals.org)
  • The beta-adrenergic receptor-induced inhibition was prevented by pertussis toxin and could not be reproduced by forskolin, indicating that cAMP was not involved. (aspetjournals.org)
  • Accumulation of inositol phosphates triggered by high K+ was insensitive to the beta-adrenergic receptor inhibition. (aspetjournals.org)
  • Propranolol's efficacy is most probably attributable to its inhibition of vasodilation and angiogenesis-functions associated with beta-2 blockade. (jddonline.com)
  • Dexmedetomidine is a potent alpha-2 adrenergic agonist that binds to the alpha-2 adrenergic receptor subtype A at the LC, resulting in almost complete inhibition of the LC, which has a sedative effect ( 5 , 6 ). (frontiersin.org)
  • This can be calculated for a given antagonist by determining the concentration of antagonist needed to elicit half inhibition of the maximum biological response of an agonist . (lookformedical.com)
  • beta3-adrenergic receptor activation increases human atrial tissue contractility and stimulates the L-type Ca2+ current. (springer.com)
  • Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. (els.net)
  • The sympathetic autonomic response is mediated by adrenergic receptors, the targets of intrinsic catecholamines. (jddonline.com)
  • The pathophysiology of delirium is not fully understood, but several neurotransmitters are known to play an important role, including catecholamines ( 2 , 3 ). (frontiersin.org)
  • They also provide an experimental approach to the study of states of altered sensitivity to catecholamines at the receptor level in man. (duke.edu)
  • α adrenergic receptors , preventing adrenaline and noradrenaline from binding. (lookformedical.com)
  • Noradrenaline, once released into the synaptic space, interacts with adrenergic receptors on the surface of adipocytes (also known as plain old fat cells). (thinksteroids.com)
  • Our screens identified several classes of molecules that include inhibitors of the bromodomain and extra-terminal (BET) family of proteins and agonists of the beta-2 adrenergic receptor. (biomedcentral.com)
  • Animal and human evidence indicates a potential therapeutic benefit for β-adrenergic receptor antagonists, selective cyclooxygenase inhibitors, and anti-fibrinolytics administered through the perioperative period. (edu.au)
  • These are added to enhance anabolic effects (human growth hormone, insulin-like growth factor 1 and insulin), to enhance fat and water loss (diuretics, thyroid hormones, beta-2-adrenergic receptor agonists and amphetamines), to counteract negative side-effects of AAS (aromatase inhibitors and estrogen receptor antagonists) and to reactivate endogenous testosterone production at the end of a cycle (gonadotropins). (taylorhooton.org)
  • Potent and selective human beta(3)-adrenergic receptor antagonists. (springer.com)
  • To identify directly and to quantitate these beta-adenergic receptors in human lymphocytes, (-) [3H] alprenolol, a potent beta-adrenergic antagonist, was used to label binding sites in homogenates of human mononuclear leukocytes. (duke.edu)
  • RP 73870, a gastrin/cholecystokinin-B receptor antagonist with potent anti-ulcer activity in the rat. (aspetjournals.org)
  • S 16118 (p-guanidobenzoyl-[Hyp3,Thi5,D-Tic7,Oic8]bradykinin) is a potent and long-acting bradykinin B2 receptor antagonist, in vitro and in vivo. (aspetjournals.org)
  • Vibegron is a potent and selective beta 3 adrenergic receptor agonist. (abmole.com)
  • Nebivolol selective beta(1)-blocker and beta(3)-agonist. (wikipedia.org)
  • Beta blockers are one of several antihypertensive drug classes associated with ED. Nebivolol is a beta blocker with vasodilating properties mediated through endothelial release of nitric oxide contraindication of atenolol facilitates penile erection. (soxanddawgs.com)
  • Antagonism of this activity by beta-blocker agents like atenolol can thus cause increased bronchoconstriction. (soxanddawgs.com)
  • A beta blocker sounds about right. (study.com)
  • Hence the name beta blocker, beta antagonist, or beta-adrenergic antagonist. (study.com)
  • Befunolol is a beta blocker introduced in 1983 by Kakenyaku Kakko. (drugbank.ca)
  • Ser49Gly leads to impaired down-regulation of the beta-1 receptor, and Arg389Gly leads to higher signal transduction.11, 12 Therefore, carriers of either variant have enhanced ß1-receptor activity and are more sensitive to beta-blocker therapy. (ebmconsult.com)
  • A β2adrenergic receptor antagonist screen was performed using the LOPAC ™ compound library, which consists of 640 well-characterized, pharmaceutically diverse compounds with known drug or drug-like activity. (bio-medicine.org)
  • The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 was able to identify all specific β2-adrenergic receptor antagonists and additional structurally related compounds present in the LOPAC compound library. (bio-medicine.org)
  • adrenergic receptor antagonists that are optionally substituted with at least one NO or NO.sub.2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females. (patentgenius.com)
  • 3. The composition of claim 1, further comprising one or more of a medicament, a denervating agent, a sympathetic denervating agent, a parasympathetic nerve specific denervating agent, a neuroblocking agent, and a highly specific neuroblocking agent. (freepatentsonline.com)
  • All of these agents work centrally to reducing the sympathetic outflow by agonizing the central alpha-2 adrenergic receptors in the brain. (infectiousdiseaseadvisor.com)
  • Clenbuterol will interact directly with the beta-receptor with or without sympathetic activity in a dose dependent manner. (thinksteroids.com)
  • This means it stimulates the sympathetic nervous system by activating receptors in the body that cause you to burn more energy. (steroidly.com)
  • The relative cardiospecificity of selective beta-1 antagonists renders them less likely candidates for dermatological application, though a recently published paper reports the successful replacement of propanolol therapy with atenolol in 2 patients. (jddonline.com)
  • adrenergic receptor antagonist, wherein the imidazoline .alpha. (patentgenius.com)
  • Imidazoline receptors are located in the ventrolateral medulla of the brain as well as other tissues and likely plays a role in the clinical effects/toxicity of these agents. (infectiousdiseaseadvisor.com)
  • 3H]2-(2-benzofuranyl)-2-imidazoline: a new selective high affinity radioligand for the study of rabbit brain imidazoline I2 receptors. (isni.org)
  • Atenolol is a second-generation beta-1-selective adrenergic antagonist indicated in the treatment of hypertension, angina pectoris, and acute myocardial infarction. (statpearls.com)
  • Mirabegron, a beta-3 adrenergic receptor agonist, another alternative to nonselective antimuscarinic drugs, appears to be less likely to cause dry mouth. (thedoctorweighsin.com)
  • A Japanese phase 3 study showed that mirabegron has excellent efficacy and safety for treating overactive bladder. (unboundmedicine.com)
  • Mirabegron is a beta-3 adrenergic receptor agonist and its activation of these receptors relaxes the detrusor muscle during the storage phase of the urinary bladder fill-void cycle, thereby increasing bladder capacity. (pharmacistactivist.com)
  • Thus, prospective studies in animals and patients at different stages of heart failure should lead to identify the best therapeutic window to use ß 3 -AR agonists and/or antagonists. (springer.com)
  • ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β 2 adrenergic receptor, as few other specific antagonists for this receptor are known. (wikipedia.org)
  • 1 In light of this new clinical application for betablockade in pediatric dermatology, this succinct review of the properties and current applications of available beta-adrenergic antagonists, as well as the established treatments for infantile hemangioma will serve as an overview for consideration of therapeutic options in managing infantile hemangiomas. (jddonline.com)
  • Moreover, over the past two decades of antidepressant drug development, the muscarinic antagonist effects of early antidepressant drugs (i.e., the tricyclic antidepressant agents) were viewed almost exclusively as producing unwanted side effects without contributing at all to therapeutic effects [ 14-16 ]. (google.com)
  • In therapeutic doses, these agents have little effect on peripheral alpha-2 adrenergic receptors. (infectiousdiseaseadvisor.com)
  • Equally, the similarity in the symptomatic, circulatory, and electrocardiographic response to the intravenous and oral preparations suggests that metabolic breakdown products are probably of therapeutic importance only in so far as they antagonize beta-receptor activity. (bmj.com)
  • Comparisons of the Impact of Beta-3 Agonist Versus Antimuscarinics on Psychological Distress, Sexual Function, Bladder Wall Thickness and Blood Flow in Women With Overactive Bladder Syndrome: a Randomized Controlled Study. (clinicaltrials.gov)
  • Tolterodine and oxybutynin, drugs for the treatment of overactive bladder, were cited in 4 and 3 studies, respectively. (thedoctorweighsin.com)
  • Recent studies suggest that antimuscarinics might suppress bladder afferent activity by blocking muscarinic receptors in the urothelium, myofibroblasts and detrusor, thereby improving overactive bladder symptoms. (unboundmedicine.com)
  • Identification of beta-adrenergic receptors in human lymphocytes by (-) (3H) alprenolol binding. (duke.edu)
  • Binding of (-) [3H] alprenolol to these sites demonstrated the kinetics, affinity, and stereospecificity expected of binding to adenylate cyclase-coupled beta-adrenergic receptors. (duke.edu)
  • Binding was rapid (t1/2 less than 30 s) and rapidly reversible (t1/2 less than 3 min) at 37 degrees C. Binding was a saturable process with 75 +/- 12 fmol (-) [3H] alprenolol bound/mg protein (mean +/- SEM) at saturation, corresponding to about 2,000 sites/cell. (duke.edu)
  • Half-maximal saturation occurred at 10 nM (-) [3H] alprenolol, which provides an estimate of the dissociation constant of (-) [3H] alprenolol for the beta-adrenergic receptor. (duke.edu)
  • The second rise in PRA was increased by 30% with alpha-adrenergic blockade. (ahajournals.org)
  • Utilizing the scald burn injury model, we studied erythropoietin-independent late maturation stages and the effect of 1/ 2, -2, or -3 blockade in burn mediated erythropoietin-resistant anemia. (bireme.br)
  • von Homeyer P, Schwinn D. Pharmacogenomics of ß-adrenergic Receptor Physiology and Response to ß-Blockade. (ebmconsult.com)
  • The titratability and rapid offset of action of esmolol in such patients may broaden the clinical applicability of the adjunctive cardioprotective effect of beta-receptor blockade in the current era of reperfusion therapy for myocardial infarction. (onlinejacc.org)
  • moreover, a paucity of public domain tools for the study of the drug target and aspects of receptor agonists as drugs had to be addressed. (nih.gov)
  • Adrenergic beta receptor blocking drugs inhibited catecholamineinduced lipolysis competitively. (aspetjournals.org)
  • Newer drugs, such as darifenacin and solifenacin are M3 selective receptor antagonists and may be more bladder-specific and have fewer side effects such as dry mouth. (thedoctorweighsin.com)
  • Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs: May potentiate effect. (nih.gov)
  • For the treatment of primary hypertension, in comparison with other first-line anti-hypertensive drugs, first-line beta-blockers are not as effective in preventing stroke and total cardiovascular events as first-line diuretics , drugs inhibiting the renin-angiotensin system and calcium channel blockers . (netlibrary.net)
  • Antagonizing the anticonvulsant effect of ethanol using drugs acting at the benzodiazepine/GABA receptor complex. (isni.org)
  • Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. (mdibl.org)
  • CypHer5 has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor expressing cells (2). (bio-medicine.org)
  • Agonist and antagonist controls were placed symmetrically in columns 1 and 12 of each plate. (bio-medicine.org)
  • Moreover, the polymorphisms may change how a patient responds to drug therapy, specifically beta-agonist and antagonist therapies. (ebmconsult.com)
  • In addition, we determined the effect of a 48-h treatment with a β3-AR agonist and antagonist on expression of these marker genes . (bvsalud.org)
  • The norepinephrine provided by the LC acts at the medial septal area (MSA) and the medial preoptic area (MPOA) to activate waking-active neurons ( via alpha-1 adrenergic receptors) and inhibit sleep-active neurons ( via alpha-2 adrenergic receptors). (frontiersin.org)
  • Beta adrenergic receptors physiologically inhibit food intake in mammals. (zjrms.com)
  • A method of treating an ocular disorder in a subject includes administering to the subject subtherapeutic amounts of two or more agents that inhibit and/or blocks the activation of Gs- or Gq-protein coupled receptors or Gs- or Gq-signaling cascade in ocular cells of the subject, and/or activates Gi-protein coupled receptors, which is induced or triggered by light induced all-trans-retinal generation. (patents.com)
  • (D) They are used to stabilize the detrusor muscle, through binding and blocking muscarinic receptors. (scielo.br)
  • When the bladder becomes full, the stretch receptors of the detrusor muscle send a signal to the pons, which in turn notifies the brain. (medscape.com)
  • Rodent major pelvic ganglion (MPG) is known to have crucial role in controlling non-voiding detrusor contraction, and also reported to contain beta-3 adrenergic receptor. (auanet.org)
  • Rabbit, a relevant model for the study of cardiac beta 3-adrenoceptors. (springer.com)
  • Individuals with cocaine overdose should be transported immediately to the nearest emergency department, preferably by ambulance in case cardiac arrest occurs en route. (wikipedia.org)
  • Beta-1 adrenergic receptors have an important role in cardiac function. (jddonline.com)
  • Furthermore, the lack of change in cardiac MCR suggests that the adrenergic receptor alterations are not the result of nonspecific abnormalities of protein synthesis in the diabetic heart. (diabetesjournals.org)
  • Further studies are required to establish the physiologic significance of these receptor alterations, but these data support the hypothesis that altered adrenergic receptor properties may underlie, at least in part, the chronotropic and inotropic abnormalities of cardiac performance that are associated with the diabetic state. (diabetesjournals.org)
  • PARP-inhibitor treatment prevents hypertension induced cardiac remodeling by favorable modulation of heat shock proteins, Akt-1/GSK-3? (jove.com)
  • competitively antagonizes the cardiac actions of adenosine at the cell surface receptors . (lookformedical.com)
  • Rate-pressure product decreased by 33% and cardiac index by 14% during esmolol treatment, but pulmonary capillary wedge pressure was not significantly altered by drug infusion (19 ± 3 mm Hg at baseline versus 19 ± 5 during treatment, p = NS). (onlinejacc.org)
  • While detailed knowledge of ligand-receptor interactions would be instrumental in design of new and improved clinical candidates, the insight into spatial structure of GPCR has been limited to ab initio models ( Goddard and Abrol 2007 ) or models based on rhodopsin crystal structure ( Palczewski and others 2000 ). (pubmedcentralcanada.ca)
  • Beta adrenergic receptors (or β receptors) belong to the guanine nucleotide-binding G protein-coupled receptor (GPCR) superfamily. (zjrms.com)
  • As model systems we utilize the so called adrenergic receptors for adrenaline and related molecules. (duke.edu)
  • It also has the effect of increasing circulating adrenaline (Adr), the body's chief beta-2 agonist. (thinksteroids.com)
  • Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions. (els.net)
  • When this effect ceases due to metabolism of cocaine, depletion of associated neurotransmitters, and receptor down-regulation (tachyphylaxis), the cocaine user may experience dysphoria, or a "crash" after the initial high. (wikipedia.org)
  • Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes. (abcam.com)
  • Functional identification of rat atypical beta-adrenoceptors by the first beta 3-selective antagonists, aryloxypropanolaminotetralins. (abcam.com)
  • Albuterol acts as a functional antagonist to relax the airway irrespective of the spasmogen involved, thus protecting against all bronchoconstrictor challenges. (centerwatch.com)
  • [5] β 2 -adrenergic receptors are located mainly in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle, and skeletal muscle. (netlibrary.net)
  • Agonist-induced and shear stress-induced nitric oxide-mediated vasodilation are decreased in the skeletal muscle circulation of patients with heart failure when compared with age-matched normal subjects (3,4) . (onlinejacc.org)
  • 2. ____ Vascular smooth muscle cells of most blood vessels have alpha receptors, and activation of vascular smooth muscle alpha receptors causes vasoconstriction. (coursehero.com)
  • 4. ____ Some blood vessels have beta receptors, and activation of vascular smooth muscle beta receptors causes vasodilation. (coursehero.com)
  • Adding to its complex toxicity, cocaine targets muscarinic acetylcholine, N-methyl-D-aspartate (NMDA), sigma, and kappa-opioid receptors. (wikipedia.org)
  • Effect of intracerebroventricular beta-funaltrexamine on mu opioid receptors in the rat brain: consideration of binding condition. (aspetjournals.org)
  • lol and beta(1)-selective, metoprolol), muscarinic (atropine), nicotinic (mecamylamine) and opioid receptors (naloxone). (ac.rs)
  • Additionally, the role of peripheral alpha(2)-adrenergic, beta(1)-adrenergic, muscarinic and opioid receptors was evaluated by co-injecting ESL with an antagonist into the perinasal area. (ac.rs)
  • Significance: This study suggests that ESL's efficacy against trigeminal nociception is mediated by peripheral (and possibly central) alpha(2)-adrenergic, muscarinic and opioid receptors, as well as central beta(1)-adrenergic receptors. (ac.rs)
  • Three types of beta receptors are known, designated β 1 , β 2 and β 3 receptors. (netlibrary.net)
  • To prime albuterol sulfate inhalation aerosol, release 3 sprays into the air away from the face. (nih.gov)
  • Beta-blockers: May decrease effectiveness of Albuterol sulfate inhalation aerosol and produce severe bronchospasm. (nih.gov)
  • Albuterol sulfate is a beta 2 -adrenergic agonist. (rxlist.com)
  • 9, 10 In patients with intermittent asthma an inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol is preferred (Step 1). (dentalcare.com)
  • The patient experiences prompt relief with inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol. (dentalcare.com)
  • Albuterol sulfate, chemically known as (1,3-benzenedimethanol, α'-[[(1,1dimethylethyl) amino] methyl]-4-hydroxy, sulfate (2:1)(salt), (±)- is a relatively selective beta 2 -adrenergic bronchodilator. (rxlist.com)
  • Recent studies have examined the effectiveness of alpha-2 adrenergic agonists for controlling delirium and agitation. (frontiersin.org)
  • Rauwolscine is an alpha-2 adrenergic receptor antagonist with little to no activity on alpha-1. (drsharma.ca)
  • However, in overdose, peripheral agonism of the alpha-2 adrenergic receptor may occur with a resultant transient increase in blood pressure. (infectiousdiseaseadvisor.com)
  • etoprolol and atenolol are beta-blockers used to treat high blood pressure hypertension heart pain angina congestive heart failure, hyperthyroidism, abnormal heart rhythms, contraindication of atenolol some neurologic conditions. (soxanddawgs.com)
  • Hypertension and coronary artery disease are the most common and strongest risk factors conferring a 2- to 3-fold increased risk [ 8 ]. (hindawi.com)
  • In Part I we found that the CYP2C9 genotype appears to influence the diastolic blood pressure response to the angiotensin II-receptor antagonist irbesartan in patients with hypertension and left ventricular hypertrophy. (diva-portal.org)
  • This characteristic makes it ideal for monitoring the translocation of cell surface receptors into the endosomal pathway. (bio-medicine.org)
  • 2) NA then binds to adrenergic receptors on the surface of all tissues that contain these receptors. (thinksteroids.com)
  • 3) As NA binds to beta-adrenergic receptors, stimulatory guanine nucleotide regulatory proteins(Gs-proteins) within the cell membrane activate the enzyme adenylate cyclase. (thinksteroids.com)
  • It may be reduced to 5 alpha-dihydrotestosterone, which binds more avidly to the androgen receptor than testosterone. (taylorhooton.org)
  • We have investigated the effect of beta-3 adrenergic receptor agonist (CL-316,243) on micromotion of major pelvic ganglion disconnected rat bladder. (auanet.org)
  • Human lymphocytes are known to posessess a catecholamine-responsive adenylate cyclase which has typical beta-adrenergic specificity. (duke.edu)
  • A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS and a variety of other G-PROTEIN-COUPLED RECEPTORS. (bioportfolio.com)
  • β3 receptors are found in the gallbladder, urinary bladder, and in brown adipose tissue. (wikipedia.org)
  • Operating via heterotrimeric G proteins, adrenergic receptors constitute one of the most intensely studied classes of membrane proteins, whose expression and function are subject to regulation at many different levels, including transcriptional, posttranscriptional and posttranslational. (els.net)
  • Hadcock JR and Malbon CC (1988) Down‐regulation of beta‐adrenergic receptors: agonist‐induced reduction in receptor mRNA levels. (els.net)
  • Kallal L, Gagnon AW, Penn RB and Benovic JL (1998) Visualization of agonist‐induced sequestration and down‐regulation of a green fluorescent protein‐tagged beta2‐adrenergic receptor. (els.net)
  • Kohout TA and Lefkowitz RJ (2003) Regulation of G protein‐coupled receptor kinases and arrestins during receptor desensitization. (els.net)
  • Krupnick JG and Benovic JL (1998) The role of receptor kinases and receptors in G‐protein‐coupled receptor regulation. (els.net)
  • Shenoy SK, McDonal PH, Kohout TA and Lefkowitz RJ (2001) Regulation of receptor fate by ubiquitination of activated beta2‐adrenergic receptor and beta‐arrestin. (els.net)
  • Beta adrenergic receptors and N/OFQ are involved in the regulation of food intake through central and peripheral mechanisms. (zjrms.com)
  • Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. (nature.com)
  • Receptors with the Gly16 variant have enhanced down-regulation of the beta-2 receptor. (ebmconsult.com)
  • Agonist-induced internalization of G protein-coupled receptors (GPCRs) is a significant step in receptor kinetics and is known to be involved in receptor down-regulation. (bioportfolio.com)
  • Beta-3 is involved in the regulation of lipolysis and thermogenesis. (abcam.com)
  • Beta blockers are known primarily for their reductive effect on heart rate, although this is not the only mechanism of action of importance in congestive heart failure. (netlibrary.net)
  • CysLT1 receptor is a target for extracellular nucleotide- induced heterologous desensitization: a possible feedback mechanism in. (lookformedical.com)
  • Mechanism of action - non-selectively antagonizes beta-1 and beta-2 adrenergic receptors c. (antiessays.com)
  • The assembly of the signaling complex provides a mechanism that ensures specific and rapid signaling by this G protein-coupled receptor. (enacademic.com)
  • Bucindolol is a nonspecific beta-adrenergic inhibitor with slight alpha-adrenergic antagonistic properties. (jddonline.com)
  • Carteolol is a nonspecific beta-adrenergic inhibitor. (jddonline.com)
  • Ro40-2148 Solabegron (GW-427,353) Vibegron (MK-4618) L-748,328 L-748,337 SR 59230A was thought to be a selective β3 antagonist but later found to also be an antagonist of the α1 receptor. (wikipedia.org)
  • The 2.4 Å crystal structure of the β 2 -adrenergic receptor (β 2 AR) in complex with the high-affinity inverse agonist (-)-carazolol provides a detailed structural framework for the analysis of ligand recognition by adrenergic receptors. (pubmedcentralcanada.ca)
  • Structural basis for σ receptor ligand recognition. (bioportfolio.com)
  • May increase bladder capacity through beta-adrenergic receptors on the bladder. (arhp.org)
  • The bladder and urethra are innervated by 3 sets of peripheral nerves arising from the autonomic nervous system (ANS) and somatic nervous system. (medscape.com)
  • Beta-3 adrenergic receptor agonist is known to alleviate rodent bladder microcontractions by inhibiting afferent pathway. (auanet.org)
  • We could observe that beta-3 adrenergic receptor agonist have effect in alleviating micromotions of MPG disconnected rat bladder. (auanet.org)
  • These results also suggest that the major action point of the beta 3 adrenergic receptor agonist is in the bladder. (auanet.org)
  • Actions of the β3 receptor include Enhancement of lipolysis in adipose tissue. (wikipedia.org)
  • The results indicate that the adrenergic reciptor mediating lipolysis in human adipose tissue is of type beta-1. (aspetjournals.org)
  • These receptors are found in gallbladder and brown adipose tissues. (jddonline.com)
  • The possible significance of the coexisting beta 1-, beta 2-, and beta 3-adrenoceptors in brown adipose tissue for the thermogenic response was investigated. (nih.gov)
  • This produces a generalized effect because alpha receptors, particularly alpha-2 receptors, decrease lipolysis and beta receptors increase lipolysis. (thinksteroids.com)
  • Chronic ethanol feeding decreased beta-adrenergic receptor-stimulated lipolysis, but had no effect on basal lipolysis. (dundee.ac.uk)
  • Chronic ethanol feeding also decreased beta-adrenergic receptor-stimulated protein kinase A activation and phosphorylation of its downstream proteins, perilipin A and hormone-sensitive lipase, the primary lipase-mediating lipolysis. (dundee.ac.uk)
  • Table 2 discusses clinical outcomes as they relate to each ß-receptor polymorphism. (ebmconsult.com)
  • Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs) (4). (bio-medicine.org)
  • The focus of work in this laboratory is on the elucidation of the molecular properties and regulatory mechanisms controlling the function of G protein-coupled receptors. (duke.edu)
  • Exposure of G protein-coupled receptors (GPCRs) to agonists can desensitize receptor signaling and lead to drug tolerance, whereas, inverse agonists may sensitize signaling. (bioportfolio.com)
  • 1988) Molecular cloning and expression of the cDNA for the hamster alpha 1‐adrenergic receptor. (els.net)
  • Furthermore, we investigated the NE-induced expression of the apoptosis marker genes Akt and p38MAPK, their phosphorylated counterparts p-Akt and p-p38MAPK, caspase-3 , Bcl-2, and Bax. (bvsalud.org)
  • β3-AR overexpression was found to increase CM apoptosis , accompanied by an increased expression of caspase-3 , bax/bcl-2, and p-p38MAPK. (bvsalud.org)
  • Activation of beta-adrenergic receptors inhibits Ca2+ entry-mediated generation of inositol phosphates in the guinea pig myometrium, a cyclic AMP-independent event. (aspetjournals.org)
  • The nociceptin/orphanin FQ (N/OFQ) peptide is the endogenous ligand for the N/OFQ peptide (NOP) receptor. (zjrms.com)