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.

Functional and molecular biological evidence for a possible beta3-adrenoceptor in the human detrusor muscle. (1/144)

The possible existence of a beta3-adrenergic receptor (beta3-AR) in the human detrusor muscle was investigated by in vitro functional studies and analysis of mRNA expression. Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of the human detrusor. The rank order for their relaxing potencies was isoprenaline (pD2 6.37+/-0.07) > or = noradrenaline (pD2 6.07+/-0.12) > or = adrenaline (pD2 5.88< or =0.11). Neither dobutamine (beta1- and beta2-AR agonist) nor procaterol (beta2-AR agonist) produced any significant relaxation at concentrations up to 10(-5) M. BRL37344A, CL316243 and CGP-12177A (beta3-AR agonists), relaxed the preparations significantly at concentrations higher than 10(-6) M. The pD2 values for BRL37344A, CL316243 and CGP-12177A were 6.42+/-0.25, 5.53+/-0.09 and 5.74+/-0.14, respectively. CGP-20712A (10(-7) - 10(-5) M), a beta1-AR antagonist, did not affect the isoprenaline-induced relaxation. On the other hand, ICI-118,551, a beta2-AR antagonist, produced a rightward parallel shift of the concentration-relaxation curve for isoprenaline only at the highest concentration used (10(-5) > M) and its pKB value was 5.71+/-0.19. Moreover, SR58894A (10(-7) - 10(-5) M), a beta3-AR antagonist, caused a rightward shift of the concentration-relaxation curve for isoprenaline in a concentration-dependent manner. The pA2 value and slope obtained from Schild plots were 6.24+/-0.20 and 0.68+/-0.31. The beta1-, beta2- and beta3-AR mRNAs were all positively expressed in detrusor smooth muscle preparations in a reverse transcription polymerase chain reaction assay. In conclusion, the present results provide the first evidence for the existence of the beta3-AR subtype in the human detrusor. They also suggest that the relaxation induced by adrenergic stimulation of the human detrusor is mediated mainly through beta3-AR activation.  (+info)

Inhibition of beta(2)-adrenergic and muscarinic cholinergic receptor endocytosis after depletion of phosphatidylinositol bisphosphate. (2/144)

Recent evidence supporting a role for phosphoinositides in the endocytosis of phospholipase C-coupled receptors has prompted an investigation of whether there exists a similar requirement for the internalization of adenylyl cyclase-linked receptors. When 1321N1 astrocytoma cells, which possess both muscarinic cholinergic receptors (mAChRs) that couple to phospholipase C and beta-adrenergic receptors (beta(2)-ARs) linked to adenylyl cyclase, were pretreated with wortmannin (WT) at a concentration known to inhibit phosphatidylinositol 4-kinase activity, the labeling of both phosphatidylinositol 4-phosphate and phosphatidylinositol 4, 5-bisphosphate (PIP(2)) was reduced. Stimulation of phosphoinositide breakdown by activation of mAChRs in WT-pretreated cells led to a further depletion of PIP(2). As previously demonstrated for SH-SY5Y neuroblastoma, inclusion of WT inhibited the endocytosis of mAChRs in 1321N1 cells by >85%. In contrast, the internalization of beta(2)-ARs was only partially ( approximately 30%) prevented. However, when the concentration of PIP(2) was further reduced by exposure of WT-pretreated 1321N1 cells to a muscarinic agonist, the endocytosis of beta(2)-ARs was substantially inhibited (>70%). Lower concentrations of WT (100 nM) that were sufficient to fully inhibit phosphatidylinositol 3-kinase activity had no effect on either phosphoinositide synthesis or receptor endocytosis. The results indicate that the agonist-induced endocytosis of an adenylyl cyclase-linked receptor such as the beta(2)-AR, like that of the phospholipase C-coupled mAChR, is dependent on the synthesis of phosphoinositides and, in particular, that of PIP(2).  (+info)

G(i) protein-mediated functional compartmentalization of cardiac beta(2)-adrenergic signaling. (3/144)

In contrast to beta(1)-adrenoreceptor (beta(1)-AR) signaling, beta(2)-AR stimulation in cardiomyocytes augments L-type Ca(2+) current in a cAMP-dependent protein kinase (PKA)-dependent manner but fails to phosphorylate phospholamban, indicating that the beta(2)-AR-induced cAMP/PKA signaling is highly localized. Here we show that inhibition of G(i) proteins with pertussis toxin (PTX) permits a full phospholamban phosphorylation and a de novo relaxant effect following beta(2)-AR stimulation, converting the localized beta(2)-AR signaling to a global signaling mode similar to that of beta(1)-AR. Thus, beta(2)-AR-mediated G(i) activation constricts the cAMP signaling to the sarcolemma. PTX treatment did not significantly affect the beta(2)-AR-stimulated PKA activation. Similar to G(i) inhibition, a protein phosphatase inhibitor, calyculin A (3 x 10(-8) M), selectively enhanced the beta(2)-AR but not beta(1)-AR-mediated contractile response. Furthermore, PTX and calyculin A treatment had a non-additive potentiating effect on the beta(2)-AR-mediated positive inotropic response. These results suggest that the interaction of the beta(2)-AR-coupled G(i) and G(s) signaling affects the local balance of protein kinase and phosphatase activities. Thus, the additional coupling of beta(2)-AR to G(i) proteins is a key factor causing the compartmentalization of beta(2)-AR-induced cAMP signaling.  (+info)

Isoeugenolol: a selective beta1-adrenergic antagonist with tracheal and vascular smooth muscle relaxant properties. (4/144)

Isoeugenolol (1.0, 3.0, 5.0 mg/kg, i.v.) produced a dose-dependent bradycardia and a decrease in blood pressure in anesthetized Wistar rats. Isoeugenolol inhibited the tachycardia effects induced by (-)isoproterenol, but had no blocking effect on the arterial pressor responses induced by (-)phenylephrine. In isolated guinea pig tissues, isoeugenolol antagonized (-)isoproterenol-induced positive inotropic and chronotropic effects on the atria and tracheal relaxations in a concentration-dependent manner. The apparent pA2 values for isoeugenolol on right atria, left atria and trachea were 7.63+/-0.03, 7.89+/-0.12 and 6.12+/-0.05, respectively, indicating that isoeugenolol was a highly selective beta1-adrenoceptor blocker. On the other hand, isoeugenolol produced a mild direct cardiac depression at high concentration and was without intrinsic sympathomimetic activity (ISA). In isolated rat thoracic aorta, isoeugenolol relaxed more potently the contractions induced by (-)phenylephrine (10 microM) and 5-HT (10 microM) than those by high K+ (75 mM). In isolated guinea pig trachea, isoeugenolol attenuated the carbachol (1 microM)-con-tracted trachea more significantly than those contracted with high K+. Furthermore, the binding characteristics of isoeugenolol and various beta-adrenoceptor antagonists were evaluated in [3H]CGP-12177 binding to rat ventricle, lung and interscapular brown adipose tissue (IBAT) membranes. The -log IC50 values of isoeugenolol for predominate beta1-, beta2- and beta3-adrenergic receptor sites were 5.82+/-0.09, 4.74+/-0.05 and 4.73+/-0.12, respectively. In conclusion, isoeugenolol was found to be a highly selective beta1-adrenoceptor antagonist with tracheal and vascular smooth muscle relaxant activities, but was devoid of alpha-adrenoceptor-blocking action.  (+info)

Dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization. (5/144)

The use of dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization was investigated in 20 men. At 2.5, 5, and 10 microg x kg(-1) x min(-1), dobutamine induced significant increases in energy expenditure, lipid oxidation, and lipolysis. The beta(1)-adrenoceptor antagonist atenolol (bolus: 42.5 microg/kg, infusion: 1.02 microg x kg(-1) x min(-1)) blocked all dobutamine-induced effects on thermogenesis and lipid utilization. All parameters remained at levels comparable to those during saline infusion. The dose of atenolol used did not inhibit beta(2)-adrenoceptor-specific changes in energy expenditure, lipid oxidation, and lipolysis during salbutamol infusion (85 ng x kg(-1) x min(-1)). This indicates that atenolol was specific for beta(1)-adrenoceptors and did not camouflage concomitant beta(2)-adrenoceptor stimulation during dobutamine infusion. Therefore, we conclude that dobutamine can be used as a selective beta(1)-adrenoceptor agonist at dosages +info)

Selective beta1-adrenoceptor blockade enhances the activity of the stimulatory G-protein in human atrial myocardium. (6/144)

1. Chronic selective beta1-adrenoceptor (beta1AR) blocker treatment enhances the sensitivity of beta2-adrenoceptor (beta2AR) in human heart (Hall et al., 1990; 1991). To clarify the mechanism of the cross-sensitization between beta1AR and beta2AR, we determined whether the stimulatory G-protein (G(s)alpha) function is increased in atria from beta1AR-blocker treated patients compared with non-beta-blocked patients, and investigated whether this change is caused by an alteration of post-translational modification of Gsalpha protein. 2. G(s)alpha function was determined by reconstitution of human atrial G(s)alpha into S49 cyc- cell membranes. In the reconstitution system, GTPgammaS stimulated cyclic AMP generation in a dose-dependent manner. Upon 10(-4) M GTPgammaS stimulation, G(s)alpha activity in the beta1AR-blocker, atenolol, treated group (78.2+/-10. 3 pmol cyclic AMP mg(-1) min(-1) 10(-3)) was 65% higher than that in non-beta-blocked patients (47.3+/-6.3 pmol cyclic AMP mg(-1) min(-1) 10(-3), n=15, P=0.02). 3. Isoelectric point (pI) valu G(s)alpha were measured by two dimensional gel electrophoresis (2D-E) and the amount of each isoform quantified by image analysis of a Western blot of the gel using specific antibody. Multiple isoforms of G(s)alpha were detected by 2D-E with different pI values. There were no significant differences between the groups of patients in either pI values or the proportions of the acidic isoforms of G(s)alpha to the main basic form (n=12, P>0.05). 4. The results suggest that chronic beta1AR-blockade enhances Gsalpha function in human atrium, and this may account in part for the hypersensitivity of beta2AR and other Gs-coupled receptors during beta1AR-blockade. The increased G(s)alpha function is unlikely to be caused directly by blockade of protein kinase A phosphorylation of G(s)alpha protein.  (+info)

Enhancement by epinephrine of benzylpenicillin transport in rat small intestine. (7/144)

The perfusion of rat small intestinal lumen with epinephrine (0.1 mM) resulted in a significant increase in the amount of benzylpenicillin (BP) transported from the mucosal to the serosal side. In this study, the perfusion of the lumen with phenylephrine, clonidine, dobutamine, or salbutamol had no effect on BP transport. However, the combinations of phenylephrine and isoproterenol, clonidine and isoproterenol, and phenylephrine and salbutamol increased the BP transport to a similar extent as that observed with epinephrine alone. Tolazolin or propranolol inhibited the epinephrine-induced increase in BP transport. An increase in the intracellular concentration of cAMP in conjunction with specific activation of either alpha(1)- or alpha(2)-adrenoceptors induced an increase in BP transport similar to that observed in response to epinephrine alone. Staurosporine or N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide abolished the epinephrine-induced increase in BP transport. Peptides or either zwitterionic or anionic cephalosporins also blocked the effect of epinephrine on BP transport. The extent of BP uptake into brush border or basolateral membrane vesicles prepared from epinephrine-perfused intestinal loops was markedly greater than that into vesicles prepared from control loops. The perfusion of intestinal lumen with carbonyl cyanide p-trifluoromethoxy phenylhydrazone, amiloride, or ouabain inhibited epinephrine-induced BP transport. These results indicate that the interaction of epinephrine with both beta(2)-adrenoceptors and either alpha(1)- or alpha(2-)adrenoceptors markedly stimulates the BP transport, an effect likely mediated by the enhancement of the function in the brush border membrane of intestinal epithelial cells coupled with the generation of an H(+) gradient.  (+info)

Negative inotropic effects of isoprenaline on isolated left atrial assays from aged transgenic mice with cardiac over-expression of human beta(2)-adrenoceptors. (8/144)

The action of isoprenaline has been evaluated in an isolated, left atrial assay, from aged transgenic mice with cardiac-specific over-expression of the beta(2)-adrenoceptor. In the assay, isoprenaline produced a negative inotropic concentration-response curve that was not altered by incubation with CGP-20712A (1 microM), a beta(1)-adrenoceptor antagonist. However, after incubation with ICI-118,551 (300 nM), a selective beta(2)-adrenoceptor antagonist, isoprenaline produced a positive inotropic concentration-effect curve that was located to the left of the negative inotropic curve. This suggests that the negative inotropic effect was mediated by a homogenous population of negatively-coupled beta(2)-adrenoceptors. In the presence of CGP-20712A (300 nM), the positive curve was shifted to the right, suggesting that the positive inotropic effect was mediated, at least in part, by beta(1)-adrenoceptors. These results differ substantially from those previously obtained in young transgenic mice. An outline of an explanatory model, based on a concept of over-expressed receptors 'stealing' G-proteins, is suggested.  (+info)

Normal apoptosis occurs continuously in the olfactory neuroepithelium of adult vertebrates, making it a useful model for studying neuronal apoptosis. Here we demonstrate that overexpression of the anti-apoptotic Bag-1 gene in olfactory neuronal cells confers a strong resistance to apoptosis. Conversely decreased levels of Bag-1 were found to precede a massive wave of olfactory neuronal apoptosis triggered by synaptic target ablation. We show that the decrease is brought about by ubiquitination and subsequent degradation of the Bag-1 protein. The ring finger protein Siah-2 is a likely candidate for the ubiquitination reaction since Siah-2 mRNA accumulated in lesioned olfactory neuroepithelium and overexpression of Siah-2 stimulated Bag-1 ubiquitination and degradation in transient expression assays. These results together identify destabilization of Bag-1 as a necessary step in olfactory neuronal apoptosis. ...
InChI=1S/C23H40N2O4/c1-5-6-7-8-9-10-11-23(27)25-15-19-12-13-21(22(14-19)28-4)29-17-20(26)16-24-18(2)3/h12-14,18,20,24,26H,5-11,15-17H2,1-4H3,(H,25,27 ...
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Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.
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Effects of depexamine may be suppressed by concomitant use with ß2-adrenergic and dopamine receptor antagonists requires ... a novel agonist at peripheral dopamine receptors and beta 2-adrenoceptors". British Journal of Pharmacology. 85 (3): 599-608. ... It is not an α-adrenergic agonist, does not cause vasoconstriction, and is not a pressor agent. As of 2004 there was some ... Dopexamine stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ...
... 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/ ...
... beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, beta adrenergic receptor antagonists. ... Beta-Adrenoceptor Antagonists (Beta-Blockers); "CV Pharmacology , Beta-Adrenoceptor Antagonists (Beta-Blockers)". Archived from ... Beta blockers, due to their antagonism at beta-1 adrenergic receptors, inhibit both the synthesis of new melatonin and its ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 ...
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 66 (2): 283-286. ISSN 1534-7796. PMID 15039516. (subscription required) Lee, H. S.; Kwon, K. Y.; Alphs, L. D.; Meltzer, H. Y. ( ... 157 (2): 569-593. doi:10.1111/j.1749-6632.1969.tb12908.x. ISSN 1749-6632. Siegler EL, Tamres D, Berlin JA, Allen-Taylor L, ...
... causes decreased heart rate and are thought to function as beta blockers, antagonists for the beta-1 and beta-2 adrenergic ... of three-finger fold toxins creates ligands with original pharmacological profiles for muscarinic and adrenergic receptors". ... a family of G-protein-coupled receptors. Muscarinic toxins can be either receptor agonists or receptor antagonists, and in some ... "Crystal structures of free and antagonist-bound states of human α9 nicotinic receptor extracellular domain". Nature Structural ...
... β2-adrenoceptor antagonist) is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high ... ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... an antagonist for β2 and for β1 or β3 adrenoceptors) like the non-selective betablocker Propranolol. ... Fitzgerald, JD; Wale, JL (1983). "The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)". J Cardiovasc ...
... denotes selective antagonist to the receptor. compound-6FA, PAM at intracellular binding site Beta-2 adrenergic receptor has ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... "Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta- ...
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... is an adrenergic antagonist which blocks the Beta-3 adrenergic receptors of cells, with either high specificity (an antagonist ... "Potent and selective human beta(3)-adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics ... SR 59230A Carvedilol Betablocker Beta-3 adrenergic receptor Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, ... A Beta-3 adrenergic antagonist (β3-adrenoceptor antagonist) ... an antagonist for β3 and for β1 or β2 adrenoceptors) like the ...
Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused ... the beta-2 adrenergic receptor and rhodopsin). Below this primary (orthosteric) binding pocket lies a secondary (allosteric) ... December 2003). "Progress in pursuit of therapeutic A2A antagonists: the adenosine A2A receptor selective antagonist KW6002: ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ...
Like other alpha-1 receptor antagonists, it has a role in the peri-operative management of pheochromocytoma. Doxazosin is ... Doxazosin is usually added to other antihypertensive therapy such as calcium channel antagonists, diuretics, beta- ... It is a α1-selective adrenergic blocker in the quinazoline class of compounds. Doxazosin was patented in 1977 and came into ... "Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?". Journal of Hypertension. ...
... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in ... receptor". Hein, Lutz; Altman, John D.; Kobilka, Brian K. (1999). "Two functionally distinct α2-adrenergic receptors regulate ...
The adrenergic receptors exert opposite physiologic effects in the vascular smooth muscle under activation: alpha-1 receptors. ... Antagonists of alpha-1 receptors (doxazosin, prazosin) cause vasodilation (a decrease in vascular smooth muscle tone with ... Agonism of beta-2 receptors causes vasodilation and low blood pressure (i.e. the effect is opposite of the one resulting from ... Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). ...
... 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. ... Wellstein A, Palm D, Belz GG (1986). "Affinity and selectivity of beta-adrenoceptor antagonists in vitro". J. Cardiovasc. ...
... 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 ... Schliep HJ, Harting J (1984). "Beta 1-selectivity of bisoprolol, a new beta-adrenoceptor antagonist, in anesthetized dogs and ... Smith C, Teitler M (April 1999). "Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors" (PDF). ...
... is a beta adrenergic receptor antagonist. Allen, JD; Shanks, RG (1974). "Effects of tiprenolol, practolol and ... 51 (2): 179-85. doi:10.1111/j.1476-5381.1974.tb09645.x. PMC 1776753. PMID 4155971. v t e v t e. ...
... 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. ...
Lohse MJ, Benovic JL, Codina J, Caron MG, Lefkowitz RJ (June 1990). "beta-Arrestin: a protein that regulates beta-adrenergic ... and neutral antagonists are ligands that do not affect the equilibrium. It is not yet known how exactly the active and inactive ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... is a receptor that can bind with stimulative signal molecules, while inhibitory hormone receptor (Ri) is a receptor that can ...
Asapiprant (S-555739) and Laropiprant are selective receptor antagonists of DP1 whereas Vidupiprant is a receptor antagonist ... also known as β-Adrenergic receptor kinase 2 [BARK1]) and arrestin 2 (also known as Arrestin beta 1 [ARRB1]). These agents act ... Prostaglandin receptors Prostanoid receptors Prostaglandin DP2 receptor Eicosanoid receptor GRCh38: Ensembl release 89: ... is primarily a receptor for prostaglandin D2 (PGD2). The receptor is a member of the Prostaglandin receptors belonging to the ...
... 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 ...
"Three-dimensional models for beta-adrenergic receptor complexes with agonists and antagonists". Journal of Medicinal Chemistry ... The β3 (beta 3) adrenergic receptor agonist or β3-adrenoceptor agonist, also known as β3-AR agonist, are a class of medicine ... Coman, Oana Andreia; Păunescu, H.; Ghiţă, Isabel; Coman, L.; Bădărăru, Anca; Fulga, I. (2009). "Beta 3 adrenergic receptors: ... In 1984 the β3 receptor was described as the third group of beta receptors in adipose tissue. This led to the development of ...
Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... Phenibut is a GABAB receptor agonist, as well as an antagonist at α2δ subunit-containing voltage-dependent calcium channels ( ... Beta-receptor blockers such as propranolol and oxprenolol, although not anxiolytics, can be used to combat the somatic symptoms ... beta blockers also can have an antianxiety effect. The alpha1 antagonist prazosin could be effective for PTSD The Alpha-2 ...
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 selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker. ICI binds to the β2 subtype with ... "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 ...
Antibodies against the Alpha 1 adrenergic receptor and muscarinic acetylcholine M4 receptor[4][5][6]. ... Vasopressin receptor antagonist Helps retain water, Increase blood volume Desmopressin (DDAVP) [95] ... December 2007). "[A multicenter study on treatment of autonomous nerve-mediated syncope in children with beta-receptor blocker ... Alpha-1 adrenergic receptor agonist Constrict the peripheral blood vessels aiding venous return. Midodrine[17][89][90][91] ...
As a non-selective alpha receptor antagonist, it will also affect both the postsynaptic alpha 1 and presynaptic alpha 2 ... Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of ... Clinically, non-selective alpha antagonists block alpha receptors (but do not differentiate between alpha-1 and alpha-2). They ... Phenoxybenzamine also has irreversible antagonist/weak partial agonist properties at the serotonin 5-HT2A receptor. Due to its ...
Cite journal requires ,journal= (help) Pauwels PJ (September 1997). "5-HT 1B/D receptor antagonists". Gen Pharmacol. 29 (3): ... "Agonist activity of sumatriptan and metergoline at the human 5-HT1D beta receptor: further evidence for a role of the 5-HT1D ... Pertz H, Eich E (1999). "Ergot Alkaloids and their Derivatives as Ligands for Serotoninergic, Dopaminergic, and Adrenergic ... Hutcheson JD, Setola V, Roth BL, Merryman WD (November 2011). "Serotonin receptors and heart valve disease--it was meant 2B". ...
"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 ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... GnRH antagonists (e.g., cetrorelix). *Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone ... 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, ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ...
... fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is evidence that it may have ... Antagonists. *Typical antipsychotics: Butaclamol. *Chlorpromazine. *Chlorprothixene. *Flupentixol (flupenthixol) (+melitracen) ... 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 ...
... and dopamine D3 receptors.[31][32] It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B ... Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the ... α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2B, and dopamine D2 receptors, and weak affinity for the 5-HT1E, 5-HT2A, 5-HT ...
Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... Antagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol ... receptor". Naunyn-Schmiedeberg's Archives of Pharmacology. 357 (1): 17-24. PMID 9459568. doi:10.1007/PL00005133.. ... 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, ... dopamine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, and 5-HT (serotonin) antagonists. ... Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ...
Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, ... beta-Ergocryptine. CH(CH3)2. CH(CH3)CH2CH3 (S). Isoleucine ... Adrenergic receptor modulators. α1. *Agonists: 6-FNE. * ... a 5-HT2A/2C antagonist.[15] The selectivity and affinity of ergolines for certain 5-HT receptors can be improved by introducing ... The antagonist or agonist behavior of the ergolines are substrate dependent and mixed agonist/antagonist behaviors of ergoline ...
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 ...
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 ...
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 ... Retrieved 2 September 2016.. *^ a b c d e f g h i j "Cymbalta (duloxetine delayed-release) Capsules for Oral Use. Full ...
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] ... 2,5-DMA is the alpha-methyl homologue of 2C-H and could be called "DOH" under the DO naming scheme. ...
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. ...
Hydroxyzine - Antihistamine, 5-HT2A receptor antagonist.. *Propranolol - Sympatholytic, beta blocker.. *Clonidine - ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ... 19 (2): 107-116.. ,access-date=. requires ,url=. (help). *^ a b Scott, E. L. (2011, September 6). Anxiety Disorders With ... 88 (2): 73-7. PMC 1295099 . PMID 7769598.. *^ Morissette, Sandra Baker; Tull, Matthew T.; Gulliver, Suzy Bird; Kamholz, Barbara ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... However, if MDPEA were either used in high enough of doses (e.g., 1-2 grams), or in combination with a monoamine oxidase ... 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, ...
Antagonists: Δ1-9-G129R-hPRL. *Δ1-14-G129R-hPRL. *G120K-hGH. *G129R-hPRL ... 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 ... The majority of targets selected for drug discovery efforts are proteins, such as G-protein-coupled receptors (GPCRs) and ...
... 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 ...
... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor,antagonists,using,CypHer5E, ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Adjuvants, Anesthesia. Muscarinic Antagonists. ... Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. ... SGRQ-C is a health related quality of life questionnaire consisting of 40 items divided into two components: 1) symptoms, 2) ...
Adrenergic beta-2 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Adjuvants, Anesthesia. ... Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. Tocolytic ... However, to ensure comparability with the TDI paper version, all TDI values were divided by 2 before the analysis. If data was ... However, to ensure comparability with the TDI paper version, all TDI values were divided by 2 before the analysis. If data was ...
Hormones, Hormone Substitutes, and Hormone Antagonists. Adrenergic beta-2 Receptor Agonists. Adrenergic beta-Agonists. ... Treatment with inhaled anticholinergic agents or long-acting beta agonists (LABA) and combination of the LABA formoterol and ... Each visit day lung function, heart function and breathlessness measurements at baseline, then they will receive 2 puffs of ... Measurement were performed at rest for 5 minutes to obtain a steady state and the last 2 minutes were taken for analysis as an ...
Adrenergic beta-2 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Anticonvulsants. ... Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. ... The objective of this study is to compare the benefits of combination long-acting beta-agonist/inhaled corticosteroid therapy ... long acting beta-agonists (e.g. formoterol, salmeterol), methylxanthines (e.g. theophylline), or combination therapy with a ...
Histamine H(1) receptor (H(1)R) antagonists are very effective drugs alleviating the symptoms of allergic reactions. Here we ... Receptors, Adrenergic, beta-2 / chemistry * Receptors, Dopamine D3 / chemistry * Receptors, Histamine H1 / chemistry* ... Histamine H(1) receptor (H(1)R) antagonists are very effective drugs alleviating the symptoms of allergic reactions. Here we ... This region is not conserved in other aminergic receptors, demonstrating how minor differences in receptors lead to pronounced ...
The recently determined X-ray structure of the beta(2)-adrenergic receptor o … ... Due partly to the lack of reliable receptor structures, drug discovery efforts have been largely ligand-based. ... Aminergic G protein-coupled receptors (GPCRs) have been a major focus of pharmaceutical research for many years. ... Structure-based discovery of beta2-adrenergic receptor ligands Proc Natl Acad Sci U S A. 2009 Apr 21;106(16):6843-8. doi: ...
Orthosteric β-adrenergic receptor antagonists, known as beta-blockers, are amongst the most prescribed drugs in the world and ... such as the nine adrenergic receptors. Allosteric ligands may bind to less-conserved regions of these receptors and therefore ... Mechanism of intracellular allosteric beta 2AR antagonist revealed by X-ray crystal structure.. Liu, X., Ahn, S., Kahsai, A.W. ... The majority of GPCR crystal structures published to date were obtained with receptors bound to orthosteric antagonists, and ...
The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. ... Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. ... "beta2AR antagonists and beta2AR gene deletion both promote skin wound repair processes.". Pullar C.E., Le Provost G.S., OLeary ... "Antithetic regulation by beta-adrenergic receptors of Gq receptor signaling via phospholipase C underlies the airway beta- ...
1994) Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor. Mol Pharmacol 45:390-394. ... 1982) Adrenergic receptors in the heart. Annu Rev Physiol 44:475-484. ... 2016) Dihydromunduletone is a small-molecule selective adhesion G protein-coupled receptor antagonist. Mol Pharmacol 90:214-224 ... 2011) Crystal structure of the β2 adrenergic receptor-Gs protein complex. Nature 477:549-555. ...
Leukotriene receptor antagonists; Methyl xanthines; Omalizumab; Pathophysiology ... Beta-2 adrenergic receptor agonists; Cromones; Glucocorticoids; ... Advanced Search Search Help About NIOSHTIC-2 Feedback Terms: ... NIOSHTIC-2 Publications Search. Search Results. New Search. ...
Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline . ... In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors ... Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. ... Antagonist. Curator comments. Reported antagonism of doxofyllin at adenosine A(2A) receptors was observed only at the highest ...
Glycopyrronium bromide is a muscarinic receptor antagonist. It blocks muscarinic receptors in muscle cells in the airways. ... A main study involved 3,092 patients whose asthma was not well controlled on a combination of a long-acting beta-2 agonist and ... Because these receptors help control the contraction of the airway muscles, blocking them causes the muscles to relax, helping ... In patients whose asthma is not controlled well enough on a combination of an inhaled long-acting beta-2 agonist and high-dose ...
... β2-adrenoceptor antagonist) is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high ... ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... an antagonist for β2 and for β1 or β3 adrenoceptors) like the non-selective betablocker Propranolol. ... Fitzgerald, JD; Wale, JL (1983). "The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)". J Cardiovasc ...
Randomised trial of effects of calcium antagonists compared with diuretics and beta-blockers on cardiovascular morbidity and ... Effects of the angiotensin receptor blocker azilsartan medoxomil versus olmesartan and valsartan on ambulatory and clinic blood ... Altered beta-2 adrenergic receptor gene expression in human clinical hypertension. Biol Res Nurs. 2009 Jul. 11(1):17-26. [ ... Epstein M. Calcium antagonists and renal disease. Kidney Int. 1998 Nov. 54(5):1771-84. [Medline]. ...
Randomised trial of effects of calcium antagonists compared with diuretics and beta-blockers on cardiovascular morbidity and ... Effects of the angiotensin receptor blocker azilsartan medoxomil versus olmesartan and valsartan on ambulatory and clinic blood ... Altered beta-2 adrenergic receptor gene expression in human clinical hypertension. Biol Res Nurs. 2009 Jul. 11(1):17-26. [ ... Epstein M. Calcium antagonists and renal disease. Kidney Int. 1998 Nov. 54(5):1771-84. [Medline]. ...
"Potent and selective human beta(3)-adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics ... Beta-3 adrenergic receptor has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... The beta-3 adrenergic receptor (β3-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic receptor Beta Blocker GRCh38: Ensembl release 89: ...
Analysis of Drug Design for a Selection of G Protein-Coupled Neuro- Receptors Using Neural Network Techniques pp. 202-211(10) ... Ligand and Structure Based Models for the Identification of Beta 2 Adrenergic Receptor Antagonists pp. 222-236(15) Authors: ... Interaction studies of Withania somniferas key metabolite Withaferin A with different receptors associated with cardiovascular ...
... receptor,for,functional,screening,biological,advanced biology technology,biology laboratory technology,biology device ... INTRODUCTION ...Many G-protein coupled receptors (GPCRs) trigger upon binding of an a...One of the methods of choice (reviewed ... TSH-Receptor. This system can be used to detect either agonists or antagonists. Surmountable antagonists as well as non- ... Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000. 11. The use of CypHer5 ...
Structure of a beta(1)-adrenergic G-protein-coupled receptor.Google Scholar ... Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography.Google Scholar ... The 2.6 Angstrom Crystal Structure of a Human A(2A) Adenosine Receptor Bound to an Antagonist. Science 322:1211-1217.PubMed ... These compounds primarily target the cannabinoid receptors 1 (CB1) and Cannabinoid receptors 2 (CB2). This chapter focuses on ...
Muscarinic receptor antagonists and long-acting beta-2-adrenergic agonists are commonly combined in the management of COPD. ... Glycopyrronium is a muscarinic-receptor antagonist. It works by blocking some receptors called muscarinic receptors, which ... Indacaterol is a long-acting beta-2 agonist. It works by attaching to beta-2-adrenergic receptors found in the muscles of many ... When inhaled, indacaterol reaches the receptors in the airways and activates them. This causes the muscles of the airways to ...
An ADRENERGIC BETA-2 RECEPTOR AGONIST with a prolonged duration of action. It is used to manage ASTHMA and in the treatment of ... A scopolamine derivative and CHOLINERGIC ANTAGONIST that functions as a BRONCHODILATOR AGENT. It is used in the treatment of ... The disease is characterized by hypersecretion of mucus accompanied by a chronic (more than 3 months in 2 consecutive years) ...
An ADRENERGIC BETA-2 RECEPTOR AGONIST with a prolonged duration of action. It is used to manage ASTHMA and in the treatment of ... GSK233705 is a high-affinity specific muscarinic receptor (mAChR) antagonist which is being developed for once daily treatment ... A scopolamine derivative and CHOLINERGIC ANTAGONIST that functions as a BRONCHODILATOR AGENT. It is used in the treatment of ... COPD) at discharged in 2 Edmonton EDs. Patients will all be provided with evidence-based discharge (prednisone and an ...
An ADRENERGIC BETA-2 RECEPTOR AGONIST with a prolonged duration of action. It is used to manage ASTHMA and in the treatment of ... GSK233705 is a high-affinity specific muscarinic receptor (mAChR) antagonist which is being developed for once daily treatment ... A scopolamine derivative and CHOLINERGIC ANTAGONIST that functions as a BRONCHODILATOR AGENT. It is used in the treatment of ... The disease is characterized by hypersecretion of mucus accompanied by a chronic (more than 3 months in 2 consecutive years) ...
Randomised trial of effects of calcium antagonists compared with diuretics and beta-blockers on cardiovascular morbidity and ... Effects of the angiotensin receptor blocker azilsartan medoxomil versus olmesartan and valsartan on ambulatory and clinic blood ... Which medications in the drug class Beta-Blockers, Beta-1 Selective are used in the treatment of Hypertension? ... Beta-blocker plus ARB or ACEI plus diuretic plus spironolactone regardless of BP; CCB can be added if needed for BP control ...
Trace amine associated receptor 1 and movement control. 2008, Pubmed Wellner-Kienitz, Overexpression of beta 1 and beta 2 ... adrenergic receptors in rat atrial myocytes. Differential coupling to G protein-gated inward rectifier K(+) channels via G(s) ... Trace amine-associated receptors form structurally and functionally distinct subfamilies of novel G protein-coupled receptors. ... Trace amine-associated receptor 1 (TAAR1) is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous ...
Comparable effect of a leukotriene receptor antagonist and long-acting beta2-adrenergic agonist in cough variant asthma pp. e78 ... Beta2-adrenergic receptor haplotype/polymorphisms and asthma susceptibility and clinical phenotype in a Chinese Han population ...
... a beta-adrenergic receptor antagonist. The beta-mediated regulation of alpha 2-receptor sensitivity at brain norepinephrine ... beta-Adrenergic regulation of alpha 2-adrenergic receptors in the central nervous system ... Incubation of rat cerebral cortical slices with the beta-adrenergic agonist isoproterenol causes an increase in alpha 2- ... adrenergic receptor binding in addition to a decrease in beta-adrenergic receptor binding. The effects are rapid and reversible ...
Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. ... The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer- ... beta-Endorphin / pharmacology. Chemical. Reg. No./Substance: 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/ ... Adrenergic alpha-Agonists / pharmacology. Adrenergic alpha-Antagonists / pharmacology. Animals. Chickens / physiology*. ...
... catecholamines in the culture medium and thus appear to reflect spontaneous beta 2AR activity and direct antagonist-receptor ... Inverse agonist activity of beta-adrenergic antagonists.. P Chidiac, T E Hebert, M Valiquette, M Dennis and M Bouvier ... Inverse agonist activity of beta-adrenergic antagonists.. P Chidiac, T E Hebert, M Valiquette, M Dennis and M Bouvier ... Inverse agonist activity of beta-adrenergic antagonists.. P Chidiac, T E Hebert, M Valiquette, M Dennis and M Bouvier ...
  • Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). (bio-medicine.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)
  • 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)
  • Agonist and antagonist controls were placed symmetrically in columns 1 and 12 of each plate. (bio-medicine.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)
  • The objective of this study is to compare the benefits of combination long-acting beta-agonist/inhaled corticosteroid therapy to long-acting anticholinergic therapy. (clinicaltrials.gov)
  • A comparison of this structure with inactive- and active-state structures of the β 2 AR reveals the mechanism by which Cmpd-15 modulates agonist binding affinity and signalling. (rcsb.org)
  • It is used for maintenance (regular) treatment in adults whose asthma is not controlled well enough with inhaled long-acting beta-2 agonist together with a high dose of an inhaled corticosteroid. (europa.eu)
  • Indacaterol is a long-acting beta-2 adrenergic receptor agonist. (europa.eu)
  • A main study involved 3,092 patients whose asthma was not well controlled on a combination of a long-acting beta-2 agonist and a corticosteroid used by inhalation. (europa.eu)
  • In patients whose asthma is not controlled well enough on a combination of an inhaled long-acting beta-2 agonist and high-dose corticosteroid and who have had an exacerbation in the previous year, the improvement in FEV1 with Zimbus Breezhaler was modest but considered to be clinically important. (europa.eu)
  • Many G-protein coupled receptors (GPCRs) trigger, upon binding of an agonist, a transient increase in intracellular calcium concentration. (bio-medicine.org)
  • Nebivolol selective beta(1)-blocker and beta(3)-agonist. (wikipedia.org)
  • Incubation of rat cerebral cortical slices with the beta-adrenergic agonist isoproterenol causes an increase in alpha 2-adrenergic receptor binding in addition to a decrease in beta-adrenergic receptor binding. (sciencemag.org)
  • Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. (biomedsearch.com)
  • Inverse agonist activity of beta-adrenergic antagonists. (aspetjournals.org)
  • Agonist-independent properties of the human beta 2-adrenergic receptor (beta 2AR) were studied using the baculovirus expression system in Sf9 cells. (aspetjournals.org)
  • In the absence of agonist but in the presence of GTP, membranes from cells expressing the beta 2AR exhibited higher levels of cAMP production than did membranes from uninfected cells or from cells infected with wild-type baculovirus. (aspetjournals.org)
  • 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)
  • 2, 3, 9, 10 Persistent severe asthma (Step 5) is treated with high-dose inhaled corticosteroid plus inhaled long-acting selective beta 2 ‑adrenergic receptor agonist. (dentalcare.com)
  • The patient experiences prompt relief with inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol. (dentalcare.com)
  • The patient experiences prompt relief with inhaled short-acting beta 2 ‑adrenergic receptor agonist and requires routine referral for a medical evaluation. (dentalcare.com)
  • The patient experiences partial relief from frequent inhaled short-acting beta 2 ‑adrenergic receptor agonist and should be referred to an emergency room. (dentalcare.com)
  • Frequent inhaled short-acting beta 2 ‑adrenergic receptor agonist provides mild/no relief and the patient requires hospitalization. (dentalcare.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)
  • Many investigators have used dexmedetomidine and clonidine (another alpha-2 agonist) to control agitation and delirium ( 7 - 15 ). (frontiersin.org)
  • Albuterol sulfate is a beta 2 -adrenergic agonist. (rxlist.com)
  • The ability of beta 1- and beta 2ARs to form the high affinity ternary complex was assessed in agonist competition studies without guanine nucleotide. (aspetjournals.org)
  • In addition, we examined physical and functional coupling of beta 1- and beta 2ARs to Gs using the agonist epinephrine, which also has equal binding affinity for both receptor subtypes. (aspetjournals.org)
  • Thus, a greater degree of both physical and functional agonist-promoted coupling occurs between Gs and beta 2AR, compared with beta 1AR. (aspetjournals.org)
  • Beta 2-adrenergic agonist regulation of immune aggregate- and platelet-activating factor-stimulated hepatic metabolism. (wikigenes.org)
  • 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)
  • We found that several beta blockers and a beta agonist all traverse the same well-defined, dominant pathway as they bind to the β 1 - and β 2 -adrenergic receptors, initially making contact with a vestibule on each receptor's extracellular surface. (pnas.org)
  • denotes selective agonist s to the receptor. (enacademic.com)
  • Stimulation of cultured cardiac myocytes in vitro with isoproterenol (ISO), an agonist for beta(1)- and beta(2)-ARs, caused hypertrophy of myocytes along with increases in transcription of atrial natriuretic factor (ANF) and actin reorganization. (nih.gov)
  • 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 constitutive activity of these receptors may be reversed by inverse agonist binding. (chemeurope.com)
  • Partial agonists are not able to activate the receptor maximally, resulting in a partial biological response compared to a full agonist. (chemeurope.com)
  • PubChem) Pharmacology: Nadolol is a nonselective beta-adrenergic receptor antagonist with a long half-life, and is structurally similar to propranolol. (neurolex.org)
  • Clinical pharmacology studies have demonstrated beta-blocking activity by showing (1) reduction in heart rate and cardiac output at rest and on exercise, (2) reduction of systolic and diastolic blood pressure at rest and on exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia. (neurolex.org)
  • Large differences exist in the pharmacology of agents within the class, thus not all beta blockers are used for all indications listed below. (wikipedia.org)
  • title=Molecular pharmacology and modeling of vasopressin receptors. (enacademic.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)
  • A Beta-2 adrenergic antagonist (β2-adrenoceptor antagonist) is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high specificity (an antagonist which is selective for β2 adrenoceptors) like Butaxamine and ICI-118,551, or non-specifically (an antagonist for β2 and for β1 or β3 adrenoceptors) like the non-selective betablocker Propranolol. (wikipedia.org)
  • The intracellular cAMP content of Sf9 cells cultured in serum-free medium was also increased by the expression of beta 2AR, and that increase was reversed by timolol and propranolol, consistent with observations in membrane preparations. (aspetjournals.org)
  • Like propranolol and timolol, nadolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. (neurolex.org)
  • This increase was inhibited by the beta-adrenergic antagonist propranolol. (stanford.edu)
  • Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood-brain barrier, has not been investigated for this purpose. (frontiersin.org)
  • The administration of propranolol was associated with significant reductions in fentanyl equivalents (65%, p = 0.009), midazolam equivalents (57%, p = 0.048), propofol (16%, p = 0.009), and haloperidol (44%, p = 0.024) on day 2 after starting propranolol compared with baseline. (frontiersin.org)
  • Propranolol is a non-selective beta-adrenergic antagonist that has good penetration of the blood-brain barrier ( 21 ). (frontiersin.org)
  • The majority of the available literature on beta receptor antagonists and infantile hemangiomas pertains to propranolol. (jddonline.com)
  • Propranolol is a racemic mixture of 2 enantiomers where the S - -enantiomer has approximately times the binding affinity for beta adrenergic receptors. (ginzakazuya.com)
  • Propranolol is a beta-adrenergic receptor antagonist used to treat hypertension 8, 9. (ginzakazuya.com)
  • Propranolol is a beta-adrenergic blocking agent that is used for treating high blood pressure, heart pain angina, abnormal rhythms of the heart, and some neurologic conditions. (ginzakazuya.com)
  • And some of the drugs exert additional properties independent of beta-receptors, for example, carvedilol causes vasodilation via inhibition of sympathetic alpha-receptors, nebivolol causes NO-derived vasodilation, sotalol shows antiarrhythmic class III effects, and propranolol inhibits the conversion of thyroxine to triiodothyronine. (escardio.org)
  • should be used only in patients with particular additional indications such as hyperthyrosis or portal hypertension (propranolol) or special arrhythmias (sotalol) where these two substances have been shown to be particularly effective due to their additional effects on top of beta-blockade. (escardio.org)
  • Pretreatment with the 5-hydroxytryptamine3 (5-HT3) receptor antagonist, MDL-72222, the 5-HT1A/5-HT2 antagonist, spiperone, and the mixed beta adrenergic/5-HT1B antagonists, l-propranolol and CGP361A, did not attenuate clonidine-induced increases in growth hormone levels. (aspetjournals.org)
  • Allosteric ligands may bind to less-conserved regions of these receptors and therefore are more likely to be selective. (rcsb.org)
  • 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)
  • 2009), The selective antagonist EPPTB reveals TAAR1-me. (xenbase.org)
  • The selective antagonist EPPTB reveals TAAR1 -mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. (xenbase.org)
  • Here we report a selective TAAR1 antagonist, EPPTB, and characterize its physiological effects at dopamine (DA) neurons of the ventral tegmental area (VTA). (xenbase.org)
  • A non-selective beta-adrenergic antagonist … A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. (neurolex.org)
  • Selective prostanoid FP-receptor (sensitive to prostaglandin F) agonists became generally available as eyedrops for the treatment of glaucoma in 1996. (emedicinehealth.com)
  • [3] [4] Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β 1 , β 2 and β 3 receptors. (wikipedia.org)
  • The effect of both stereoisomers on the LPS-induced TNFα release could almost completely be antagonized by preincubation with the selective β2-AR-antagonist ICI-118551. (tudelft.nl)
  • Beta 1- and beta 2-adrenergic receptors display subtype-selective coupling to Gs. (aspetjournals.org)
  • We conclude that coupling to Gs by beta 1- and beta 2ARs is subtype selective and is a potentially important distinguishing feature among these members of the beta AR family. (aspetjournals.org)
  • The subtype-selective antagonists betaxolol (beta 1), practolol (beta 1), and zinterol (beta 2) compete for [125I]iodocyanopindolol-binding sites on intact myocytes in monophasic manners with dissociation constants of 46, 845, and 923 nM, respectively. (ahajournals.org)
  • Adrenergic receptors in Alzheimer's disease brain: Selective increases in the cerebella of aggressive patients. (thefreedictionary.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)
  • beta-Adrenergic receptor subtypes were localized and differentiated in rat kidney slices by in vitro autoradiography using the nonselective beta-antagonist [125I]iodocyanopindolol in the presence of the selective agents betaxolol (beta 1) and zinterol (beta 2). (ahajournals.org)
  • non-selective adrenergic antagonists are used to treat what? (studystack.com)
  • There are actually "three generations of beta-blockers" with the non-selective, the beta1-selective ("cardioselective"), and the beta-blockers with additional vasodilating effects, the latter showing no adverse metabolic effects any more. (escardio.org)
  • However, there is still a number of marked differences between "the members of the family of beta-blockers", first of all the fact that there are actually "three generations of beta-blockers" (Table 1), with the 1st generation being non-selective , the 2nd generation being beta1-selective ("cardioselective"), and the 3rd generation showing additional vasodilating effects . (escardio.org)
  • Non-selective beta-blockers are currently used to treat several diseases and have been proven to reduce stress-induced inflammation and reduce anxiety. (bvsalud.org)
  • That's what this lesson is about, the basics surrounding cardioselective (heart-selective) and non-cardioselective beta blockers. (study.com)
  • In contrast, pretreatment with the non-selective 5-HT1/2 antagonist, metergoline, and the 5-HT1C/5-HT2-selective antagonist, mesulergine, reduced clonidine-induced increases in growth hormone levels 81 to 87% without affecting clonidine-induced decreases in locomotor activity. (aspetjournals.org)
  • Metoprolol is a selective beta1 receptor blocker used in treatment of several diseases of the cardiovascular system. (hmdb.ca)
  • A selective adrenergic beta-1-blocking agent with no stimulatory action. (hmdb.ca)
  • beta-Adrenergic receptor (beta AR) subtypes differ in their affinities for some agonists and antagonists and thus may potentially impart different cellular effects based on this ligand-binding specificity. (aspetjournals.org)
  • The adrenergic receptor specificity of these effects was determined through the use of specific adrenergic subtype-specific agonists and antagonists to be mediated by beta 2-adrenergic receptors. (wikigenes.org)
  • The effect of beta-adrenoreceptor signaling on the expression of VEGF and interleukin 6 (IL-6) was investigated in primary mouse choroidal endothelial cells, retinal pigment epithelial (RPE) cells, microglia cells, and human fetal RPE cells using specific beta-adrenoreceptor agonists and antagonists. (arvojournals.org)
  • The increase and its reversal both were independent of the possible presence of contaminating catecholamines in the culture medium and thus appear to reflect spontaneous beta 2AR activity and direct antagonist-receptor interactions, respectively. (aspetjournals.org)
  • Mechanism of action: Like other beta-adrenergic antagonists, nadolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. (neurolex.org)
  • These studies demonstrate that peripheral nerves have beta 2-adrenergic receptors that are responsive to exogenously applied catecholamines and suggest a role for these ligands in the previously described modulation of axonal conduction. (stanford.edu)
  • The effect of dilevalol on cardiac autonomic neural discharge, plasma catecholamines, and myocardial beta receptor density associated with coronary occlusion. (biomedsearch.com)
  • Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors , of the sympathetic nervous system , which mediates the fight-or-flight response . (wikipedia.org)
  • The pathophysiology of delirium is not fully understood, but several neurotransmitters are known to play an important role, including catecholamines ( 2 , 3 ). (frontiersin.org)
  • The sympathetic autonomic response is mediated by adrenergic receptors, the targets of intrinsic catecholamines. (jddonline.com)
  • The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. (uniprot.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)
  • 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). (wikipedia.org)
  • Beta blockers interfere with the binding to the receptor of epinephrine and other stress hormones, and weaken the effects of stress hormones. (wikipedia.org)
  • As with isoproterenol, epinephrine was more potent in stimulating adenylyl cyclase and promoted a higher affinity ternary complex for the beta 2AR. (aspetjournals.org)
  • 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)
  • beta2-adrenergic receptor antagonism reduces laser-induced CNV in vivo and decreases Vegf and IL-6 mRNA expression in vitro . (arvojournals.org)
  • 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)
  • The majority of GPCR crystal structures published to date were obtained with receptors bound to orthosteric antagonists, and only a few structures bound to allosteric ligands have been reported. (rcsb.org)
  • These ligands all lie buried within a deep binding pocket-the canonical "orthosteric" site that is cradled within a characteristic bundle of seven transmembrane helices-that is typically accessed from the extracellular side of the receptor. (pnas.org)
  • Ligand-induced changes in the behavior of receptor proteins result in physiological changes that constitute the biological actions of the ligands. (chemeurope.com)
  • The activation of the second messenger cascade and the final biological response is achieved only when at a certain time point a significant number of receptors are activated by bound ligands. (chemeurope.com)
  • Glycopyrronium bromide is a muscarinic receptor antagonist. (europa.eu)
  • Glycopyrronium is a muscarinic-receptor antagonist. (europa.eu)
  • Cmpd-15PA binds to a pocket formed primarily by the cytoplasmic ends of transmembrane segments 1, 2, 6 and 7 as well as intracellular loop 1 and helix 8. (rcsb.org)
  • 1. a substance that tends to nullify the action of another, as a drug that binds to a cellular receptor for a hormone, neurotransmitter, or another drug blocking the action of that substance without producing any physiologic effect itself. (thefreedictionary.com)
  • The beta-adrenergic antagonist ligand (+/-)-[125I] iodocyanopindolol binds to 2 X 10(5) receptors per purified adult rat cardiomyocyte, with a dissociation constant of 70 pM. (ahajournals.org)
  • It may be reduced to 5 alpha-dihydrotestosterone, which binds more avidly to the androgen receptor than testosterone. (taylorhooton.org)
  • In biochemistry , a receptor is a protein on the cell membrane or within the cytoplasm or cell nucleus that binds to a specific molecule (a ligand ), such as a neurotransmitter , hormone , or other substance, and initiates the cellular response to the ligand. (chemeurope.com)
  • Not every ligand that binds to a receptor also activates the receptor. (chemeurope.com)
  • Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline 7 . (drugbank.ca)
  • The affinity for adenosine A1, A2A and A2B receptors are reported to be all higher than 100 µM 6 . (drugbank.ca)
  • GSK233705 is a high-affinity specific muscarinic receptor (mAChR) antagonist which is being developed for once daily treatment of chronic obstructive pulmonary disease (COPD). (bioportfolio.com)
  • Similarly, hydroxyzine has greater affinity for H1 receptors than alpha-1 adrenergic receptors , while trazodone has greater affinity for alpha-1 adrenergic receptors than for H1 receptors. (thefreedictionary.com)
  • In the ensuing century, such measurements of drug efficacy and-once the molecular targets of drugs, or "receptors," were identified-of drug-receptor affinity have become de rigueur ( 1 , 2 ). (pnas.org)
  • and slow unbinding leads to long drug-receptor residence times that can dramatically enhance therapeutic efficacy at equivalent affinity ( 3 , 4 ). (pnas.org)
  • A measure of how well a certain molecule fits into a given receptor is the binding affinity which is measured as the dissociation constant K d (good fit means high affinity and a low K d ). (chemeurope.com)
  • Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. (uniprot.org)
  • Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (uniprot.org)
  • This effect was blocked by co-injection of the alpha-2-receptor antagonist, yohimbine, demonstrating that the alpha-2-receptor is related to stimulation of feeding in layer-type chicks. (biomedsearch.com)
  • Stimulation of food intake caused by neuropeptide Y and beta-endorphin was attenuated by co-injection with yohimbine. (biomedsearch.com)
  • Adrenergic receptor beta 2 (ADRB2) stimulation leads to the activation of both stimulatory and inhibitory [alpha]-subunits of the guanosine triphosphate activated protein. (thefreedictionary.com)
  • A somewhat more specialized view for the role of NE came to light when it was shown that NE and LC activation can modulate the response properties of sensory neurons following stimulation in a dose-dependent manner [1, 2, 57]. (thefreelibrary.com)
  • Their predominant mechanism of action, i.e., the inhibition of the stimulation of sympathetic beta-adrenoceptors by adrenaline and noradrenaline , is well known all around. (escardio.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)
  • These findings suggest that clonidine stimulates growth hormone secretion by activation of alpha 2 adrenergic heteroreceptors present on 5-HT nerve terminals which, in turn, enhance 5-HT activity via stimulation of postsynaptic 5-HT1C receptors to promote growth hormone releasing factor. (aspetjournals.org)
  • Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs) (4). (bio-medicine.org)
  • Doxepin sits deep in the ligand-binding pocket and directly interacts with Trp 428(6.48), a highly conserved key residue in G-protein-coupled-receptor activation. (nih.gov)
  • Aminergic G protein-coupled receptors (GPCRs) have been a major focus of pharmaceutical research for many years. (nih.gov)
  • G-protein-coupled receptors (GPCRs) pose challenges for drug discovery efforts because of the high degree of structural homology in the orthosteric pocket, particularly for GPCRs within a single subfamily, such as the nine adrenergic receptors. (rcsb.org)
  • G protein-coupled receptors enable cells to sense extracellular signals and translate them into physiological responses. (pnas.org)
  • In addition to a transmembrane domain that transduces signals into the cytoplasm, adhesion G protein-coupled receptors (aGPCRs) have large extracellular regions (ECRs) that interact with proteins in the extracellular space. (pnas.org)
  • Adhesion G protein-coupled receptors (aGPCRs) play critical roles in diverse biological processes, including neurodevelopment and cancer progression. (pnas.org)
  • Although ECRs regulate receptor function, it is not clear whether ECRs play a direct regulatory role in G-protein signaling or simply serve as a protective cap for the activating " Stachel " sequence. (pnas.org)
  • Here, we present a mechanistic analysis of ECR-mediated regulation of GPR56/ADGRG1, an aGPCR with two domains [pentraxin and laminin/neurexin/sex hormonebinding globulin-like (PLL) and G protein-coupled receptor autoproteolysis-inducing (GAIN)] in its ECR. (pnas.org)
  • The G protein-coupled receptor (GPCR) superfamily exhibits great diversity with regard to the length and complexity of the extracellular region (ECR). (pnas.org)
  • Members of the less well-studied adhesion G protein-coupled receptor (aGPCR) family are characterized by particularly diverse and large ECRs: hundreds to thousands of amino acid residues compose multiple protein domains ( 5 , 6 ). (pnas.org)
  • Cell lines expressing recombinant aequorin and a G-protein coupled receptor for functional screening ( INTRODUCTION Man. (bio-medicine.org)
  • Many G-protein coupled receptors (GPCRs) trigger upon binding of an a. (bio-medicine.org)
  • After selection with antibiotics, recombinant cells were subjected to a limit dilution, and clones expressing the G-protein coupled receptor and apoaequorin at a high level were selected. (bio-medicine.org)
  • If the G-protein coupled receptor is not naturally coupled to a calcium signalling pathway, a universal coupling effector is coexpressed in order to redirect the coupling towards intracellular calcium release. (bio-medicine.org)
  • 2004. Cannabinoid CB1 receptor protein expression in the rat choroid plexus: a possible involvement of cannabinoids in the regulation of cerebrospinal fluid. (springer.com)
  • 2000. Crystal structure of rhodopsin: A G protein-coupled receptor. (springer.com)
  • 2008. Crystal structure of the ligand-free G-protein-coupled receptor opsin. (springer.com)
  • Trace amine-associated receptor 1 ( TAAR1 ) is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids. (xenbase.org)
  • Trace amines: identification of a family of mammalian G protein-coupled receptors. (xenbase.org)
  • A G protein-gated K channel is activated via beta 2-adrenergic receptors and G beta gamma subunits in Xenopus oocytes. (xenbase.org)
  • Trace amine-associated receptors form structurally and functionally distinct subfamilies of novel G protein-coupled receptors. (xenbase.org)
  • The increase in cAMP production was proportional to the number of beta 2AR expressed, up to 40 pmol/mg of membrane protein, and it could be inhibited in a dose-dependent manner by beta AR antagonists. (aspetjournals.org)
  • In particular, although beta ARs stimulate adenylyl cyclase by coupling to the guanine nucleotide-binding protein Gs, no studies have directly assessed the coupling efficiencies among isolated beta AR subtypes. (aspetjournals.org)
  • We, therefore, permanently transfected the mammalian fibroblast cell line CHW-1102 with beta 1- or beta 2AR cDNAs and studied the coupling characteristics of these two receptor subtypes, each expressed at approximately 335 fmol/mg of protein. (aspetjournals.org)
  • 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)
  • Beta-adrenergic receptors are G-protein linked and mediate the adenylate cyclase cascade in targeted cells. (jddonline.com)
  • How drugs bind to their receptors-from initial association, through drug entry into the binding pocket, to adoption of the final bound conformation, or "pose"-has remained unknown, even for G-protein-coupled receptor modulators, which constitute one-third of all marketed drugs. (pnas.org)
  • We captured this pharmaceutically critical process in atomic detail using the first unbiased molecular dynamics simulations in which drug molecules spontaneously associate with G-protein-coupled receptors to achieve final poses matching those determined crystallographically. (pnas.org)
  • G-protein-coupled receptors (GCPRs) represent the largest class of drug targets, and one-third of all drugs act by binding to GCPRs. (pnas.org)
  • This receptor-channel complex also contains a G protein - G s , which activate an adenylyl cyclase , cAMP-dependent kinase , and the counterbalancing phosphatase , PP2A . (enacademic.com)
  • The assembly of the signaling complex provides a mechanism that ensures specific and rapid signaling by this G protein-coupled receptor. (enacademic.com)
  • Both proteins also inhibit ligand-dependent activation of the EGFR and extracellular signal-regulated protein kinase 1/2 signaling in a rapid and dose-dependent manner. (embl-heidelberg.de)
  • The structural analysis suggests that the virus enters human cells through the ligation of the spike protein to angiotensin-converting enzyme 2 (ACE2). (bvsalud.org)
  • Thus, at the submaximal isoproterenol concentration of 30 nM, the beta 2AR stimulated adenylyl cyclase approximately 50% more than did the beta 1AR. (aspetjournals.org)
  • This finding was not due to a difference in the affinities of isoproterenol for these receptors, which were found to be the same, as determined by competition binding studies with 125I-cyanopindolol in the presence of GTP. (aspetjournals.org)
  • 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)
  • Due partly to the lack of reliable receptor structures, drug discovery efforts have been largely ligand-based. (nih.gov)
  • The recently determined X-ray structure of the beta(2)-adrenergic receptor offers an opportunity to investigate the advantages and limitations inherent in a structure-based approach to ligand discovery against this and related GPCR targets. (nih.gov)
  • In this study, we demonstrate that a soluble ectodomain of LRIG1, containing only the LRRs, inhibits ligand-independent epidermal growth factor receptor (EGFR) activation and causes growth inhibition of A431, HeLa and MDA-468 carcinoma cells. (embl-heidelberg.de)
  • If the receptor exists in two states (see this picture [1]), then the ligand binding must account for these two receptor states. (chemeurope.com)
  • Receptors which are active in the absence of a ligand. (chemeurope.com)
  • transmembrane receptors are embedded in the phospholipid bilayer of cell membranes, that allow the activation of signal transduction pathways in response to the activation by the binding molecule, or ligand . (chemeurope.com)
  • Ionotropic receptors contain a central pore which functions as a ligand-gated ion channel. (chemeurope.com)
  • These receptors often can enter the cell nucleus and modulate gene expression in response to the activation by the ligand. (chemeurope.com)
  • Doxofylline does not demonstrate direct inhibition of any histone deacetylase (HDAC) enzymes or known PDE enzyme isoforms and did not act as an antagonist at A2 or A2 receptors. (drugbank.ca)
  • Differential inhibition of beta adrenergic receptors in human and rabbit ciliary process and heart. (aspetjournals.org)
  • Propranolol's efficacy is most probably attributable to its inhibition of vasodilation and angiogenesis-functions associated with beta-2 blockade. (jddonline.com)
  • Amit Z, Brown ZW, Levitan DE, Ogren SO (1977) Noradrenergic mediation of the positive reinforcing properties of ethanol: I. Suppression of ethanol consumption in laboratory rats following dopamine-beta-hydroxylase inhibition. (springer.com)
  • Nadolol has no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, nadolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action. (neurolex.org)
  • Coronary occlusion and saline or dilevalol did not modify the myocardial beta receptor density regional distribution. (biomedsearch.com)
  • Beta blockers ( beta-blockers , β-blockers , etc.) are a class of medications that are predominantly used to manage abnormal heart rhythms , and to protect the heart from a second heart attack ( myocardial infarction ) after a first heart attack (secondary prevention). (wikipedia.org)
  • Myocardial beta-adrenergic receptors (beta -ARs) consist of beta(1)- and beta(2)-subtypes, which mediate distinct signaling mechanisms. (nih.gov)
  • 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. (wikipedia.org)
  • Landmark mechanistic and functional studies of GPCRs to date have almost exclusively focused on receptors without prominent extracellular domains, particularly those from the rhodopsin family ( 1 ⇓ - 3 ). (pnas.org)
  • We report that peripheral nerves have a functional adenylate cyclase-coupled beta-adrenergic receptor. (stanford.edu)
  • The present experiments evaluate a number of beta adrenergic antagonists, including several recently developed drugs, for their ability to block rabbit and human ciliary process and heart beta adrenergic receptors activating adenylate cyclase. (aspetjournals.org)
  • Our study sheds light on the molecular basis of H(1)R antagonist specificity against H(1)R. (nih.gov)
  • The pharmacological specificity of this receptor is shown to be of the beta 2 subtype. (stanford.edu)
  • Which adrenergic receptor causes vasodilation of skeletal muscle and liver, intestinal relaxation, bronchodilation, and increased metabolic rate? (studystack.com)
  • 4. ____ Some blood vessels have beta receptors, and activation of vascular smooth muscle beta receptors causes vasodilation. (coursehero.com)
  • [4] β 2 -adrenergic receptors are located mainly in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle, and skeletal muscle. (wikipedia.org)
  • By binding beta-2 receptors in the juxtaglomerular apparatus, nadolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. (neurolex.org)
  • This results in a receptor blockade that inhibits the binding of agonists. (chemeurope.com)
  • Additional physiological studies of cardiac chronotropic response revealed that, compared with nonselective beta blockers, compounds with biochemical oculoselectivity demonstrate decreased physiological effects on cardiac function. (aspetjournals.org)
  • A nonselective beta-adrenoceptor antagonist used in the treatment of glaucoma. (drugbank.com)
  • As the drug is a nonselective β-adrenergic blocking agent, it can produce both systemic pulmonary and cardiovascular effects following topical application to the eye. (drugbank.com)
  • 2006. Cannabinoid receptors as therapeutic targets for obesity and metabolic diseases. (springer.com)
  • 2007. Cannabinoid-1 receptor blockade in cardiometabolic risk reduction: Safety, tolerability, and therapeutic potential. (springer.com)
  • The therapeutic potential of drugs that target cannabinoid receptors or modulate the tissue levels or actions of endocannabinoids. (springer.com)
  • 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)
  • Attenuation of EGFR activity without physical downregulation of the receptor could represent a novel therapeutic approach toward malignancies in which EGFR plays a primary role in tumor growth and survival. (embl-heidelberg.de)
  • Bi-directional effects of GABA(B) receptor agonists on the mesolimbic dopamine system. (xenbase.org)
  • Psychostimulants act as inverse agonists at dopamine receptors . (chemeurope.com)
  • Compound 15 (Cmpd-15) is an allosteric modulator of the β 2 adrenergic receptor (β 2 AR) that was recently isolated from a DNA-encoded small-molecule library. (rcsb.org)
  • Orthosteric β-adrenergic receptor antagonists, known as beta-blockers, are amongst the most prescribed drugs in the world and Cmpd-15 is the first allosteric beta-blocker. (rcsb.org)
  • To reduce blood pressure, beta blocker antihypertensive drugs are intended to inhibit specific, cardioselective, beta-1 adrenergic receptors in the heart and vascular walls. (thefreedictionary.com)
  • Levobunolol is an ophthalmic beta-blocker, equally effective at β(1)- and β(2)-receptor sites. (drugbank.com)
  • A beta blocker sounds about right. (study.com)
  • Hence the name beta blocker, beta antagonist, or beta-adrenergic antagonist. (study.com)
  • Pretreatment with the alpha 2 adrenergic antagonists, yohimbine and 1-(2-pyrimidyl)piperazine, completely blocked clonidine's effect on growth hormone levels. (aspetjournals.org)
  • What we found in our laboratory is that the longer 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). (afionline.org)
  • 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)
  • 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)
  • At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy. (drugbank.ca)
  • This receptor is directly associated with one of its ultimate effectors, the class C L-type calcium channel Ca V 1.2. (enacademic.com)
  • For the treatment of primary hypertension, meta-analyses of studies which mostly used atenolol have shown that although beta blockers are more effective than placebo in preventing stroke and total cardiovascular events, they are not as effective as diuretics , medications inhibiting the renin-angiotensin system (e.g. (wikipedia.org)
  • Levobunolol is a beta-adrenergic antagonist used for the reduction of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. (drugbank.com)
  • Beta-blockers are well known to be effective in the treatment of arterial hypertension, coronary artery disease, tachyarrhythmias arterial hypertension and heart failure. (escardio.org)
  • Unfortunately, most outcome studies in arterial hypertension showing other antihypertensives being "better" than beta-blockers used atenolol as a reference drug. (escardio.org)
  • Due to their additional vasodilating effects Beta-blockers of the 3rd generation are particularly useful in patients with arterial hypertension and/or heart failure. (escardio.org)
  • However, beta-blockers have been questioned in the treatment of arterial hypertension since they may cause metabolic side effects, whereas this obviously does not hold true for the 3rd generation. (escardio.org)
  • Accordingly, the 2007 Guidelines for the management of arterial hypertension of the European Society of Hypertension and the European Society of, Cardiology4,5 emphasise that "this may not apply, however, to vasodilator beta-blockers, such as carvedilol and nebivolol, which have less or no metabolic action, as well as a reduced incidence of new onset diabetes compared with classical beta-blockers. (escardio.org)
  • In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors and lacks stimulating effects. (drugbank.ca)
  • Role of adrenergic alpha-2-receptors on feeding behavior in layer-type chicks. (biomedsearch.com)
  • The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer-type chicks. (biomedsearch.com)
  • It is therefore likely that brain adrenergic alpha-2-receptors mediate the orexigenic effects of neuropeptide Y and beta-endorphin in layer-type chicks. (biomedsearch.com)
  • Direct analysis of beta-adrenergic receptor subtypes on intact adult ventricular myocytes of the rat. (ahajournals.org)
  • These results indicate that beta 1- and beta 2-adrenergic receptor subtypes are differentially distributed within the kidney: beta 1, predominantly contained in juxtaglomerular granule cells and glomeruli, and beta 2, predominantly in medullary tubules. (ahajournals.org)
  • title=Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. (enacademic.com)
  • 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)
  • Association of arg16gly and gln27glu, [beta]2-adrenergic receptor gene polymorphism with asthma. (thefreedictionary.com)
  • Substitution of a mutant alpha-2A adrenergic receptor via "hit and run" gene targeting reveals the role of this subtype in sedative, analgesic, and anesthetic- sparing responses in vivo. (thefreedictionary.com)
  • Different polymorphic forms, point mutation s, and/or downregulation of this gene are associated with nocturnal asthma , obesity and type 2 diabetes . (enacademic.com)
  • Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor. (xenbase.org)
  • The released neurotransmitters attach to receptors on other cells and induce changes within the receptor-containing cells. (ginzakazuya.com)
  • On the other hand, it is capable of inhibiting serotonin and norepinephrine reuptake and can bind to [alpha]2 adrenergic receptors as well as potentiating the neuronal release of serotonin (8, 16, 17). (thefreedictionary.com)
  • In stark contrast, essentially nothing is known about the process by which drugs bind to their receptors. (pnas.org)
  • AAS that are more anabolic bind more weakly to the androgen receptor, but all AAS are virilising if used for long enough at high enough doses. (taylorhooton.org)
  • Antagonists bind to the receptor but do not activate it. (chemeurope.com)
  • Alprenolol is a nonspecific beta-adrenergic inhibitor with additional antagonist effects on serotonin 5HT-1a receptors. (jddonline.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)
  • Although beta blockers were once contraindicated in congestive heart failure , as they have the potential to worsen the condition due to their effect of decreasing cardiac contractility, studies in the late 1990s showed their efficacy at reducing morbidity and mortality. (wikipedia.org)
  • in cases of acute decompensated heart failure, beta blockers will cause a further decrease in ejection fraction, worsening the patient's current symptoms. (wikipedia.org)
  • Beta-blocking agents have been less well studied for ICU delirium, although beta-blockers are known to have beneficial effects on anxiety, posttraumatic Stress Disorder (PTSD) and aggressive behavior in a variety of populations ( 16 - 20 ). (frontiersin.org)
  • These findings, identifying relatively specific blockers of rabbit and human ciliary process beta adrenergic receptors, have implications for the development of ocular hypotensive agents with fewer systemic side effects on tissues enriched in beta-1 adrenergic receptors. (aspetjournals.org)
  • Beta-blockers: May decrease effectiveness of Albuterol sulfate inhalation aerosol and produce severe bronchospasm. (nih.gov)
  • Patients with asthma should not normally be treated with beta-blockers. (nih.gov)
  • Beta-blockers: May block bronchodilatory effects of beta-agonists and produce severe bronchospasm. (nih.gov)
  • Recent studies have reported the successful use of beta- adrenergic blockers in treating infantile hemangiomas. (jddonline.com)
  • 5 Individual beta-blockers have varying affinities for the receptor subclasses, leading to diverse physiologic effects. (jddonline.com)
  • The majority of the beta-blockers with reported use in treating infantile hemangioma are nonspecific beta antagonists, with activity on both beta-1 and beta-2 receptor sites. (jddonline.com)
  • What is the suffix for beta blockers? (studystack.com)
  • Pentoxifylline: Moderate Pentoxifylline has been used concurrently with antihypertensive drugs beta blockers, the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures. (ginzakazuya.com)
  • A dose reduction of some beta-blockers may be needed when a hyperthyroid patient treated with methimazole becomes euthyroid. (ginzakazuya.com)
  • Examples of other beta-adrenergic blockers include metoprolol Lopressor, atenolol Tenormin, and timolol Blocadren. (ginzakazuya.com)
  • Therefore, beta-blockers should be recognised as individual substances with their own qualities and used according to the individual features, needs and demands of every single patient. (escardio.org)
  • and the significant benefits from beta-blockers in reducing cardiovascular end-points result from beta1-blockade.1 Since intrinsic sympathomimetic activity (ISA) detracts from efficacy, beta-blockers with ISA (particularly pindolol, xamoterol and bucindolol) have performed poorly in reducing morbidity and mortality.1 Therefore, beta-blockers with ISA cannot be recommended per se, and this article refers to beta-blockers without ISA. (escardio.org)
  • other beta-blockers of the 2nd generation, especiallly metoprolol and bisoprolol, still remain indicated particularly in the treatment of coronary artery disease, tachyarrhythmias and heart failure since they never were shown to share these disadvantages with atenolol. (escardio.org)
  • In this lesson, you'll learn a bit about the adrenergic system and how it relates to the names and functions of various cardioselective and non-cardioselective beta blockers. (study.com)
  • Now that you've got that down pat, let's move on to the blocking part of beta-blockers. (study.com)
  • Beta blockers are used to treat a wide variety of conditions, including high blood pressure and all sorts of heart problems like heart failure or arrhythmias. (study.com)
  • Structure-activity studies suggested that, among antagonists of the aryloxymethyl type, methylation of the side-chain alpha-carbon or the aromatic ring may enhance oculoselectivity primarily by decreasing potency at cardiac beta adrenergic receptors. (aspetjournals.org)
  • Beta-1 adrenergic receptors have an important role in cardiac function. (jddonline.com)
  • Beta-adrenergic cardiac hypertrophy is mediated primarily by the beta(1)-subtype in the rat heart. (nih.gov)
  • We examined which beta-AR subtype mediates cardiac hypertrophy. (nih.gov)
  • This book presents a comprehensive view of the developments in the fields of receptors and centrally acting drugs as well as in pharmacokinetics and drug metabolism. (elsevier.com)
  • Histamine H(1) receptor (H(1)R) antagonists are very effective drugs alleviating the symptoms of allergic reactions. (nih.gov)
  • 2. Drugs Recommended for Routine Use. (onlinejacc.org)
  • Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs: May potentiate effect. (nih.gov)
  • By what pathway, or pathways, do drugs enter and exit the receptor binding pocket? (pnas.org)
  • 2 Most stacks include non-steroidal drugs. (taylorhooton.org)
  • In 2010, the Advisory Council on the Misuse of Drugs recommended that anabolic steroids should continue to be controlled as class C drugs under the Misuse of Drugs Act 1971, but there is no possession offence for AAS.2 Most users obtain their AAS from the illicit market. (taylorhooton.org)
  • Advances in Pharmacological Research and Practice, Volume 2: Receptors and Centrally Acting Drugs presents the proceeding of the 4th Congress of the Hungarian Pharmacological Society, held in Budapest, Hungary in 1985. (elsevier.com)
  • 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)
  • Metabotropic receptors are coupled to G proteins and affect the cell indirectly through enzymes which control ion channels . (chemeurope.com)
  • Another major class of receptors are intracellular proteins such as those for steroid and intracrine peptide hormone receptors. (chemeurope.com)
  • Large molecules are incorporated by endocytosis and the smaller molecules are incorporated by simple diffusion or diffusion provided by receptor proteins, as appropriate. (biocellmedical.com)
  • SARS-CoV-2 infection is a new threat to global public health in the 21st century (2020), which has now rapidly spread around the globe causing severe pneumonia often linked to Acute Respiratory Distress Syndrome (ARDS) and hyperinflammatory syndrome. (bvsalud.org)
  • We additionally found that both the acute application of EPPTB and the constitutive genetic lack of TAAR1 increase the potency of DA at D2 receptors in DA neurons. (xenbase.org)
  • We hypothesize that the EPPTB-induced increase in the potency of DA at D2 receptors is part of a homeostatic feedback mechanism compensating for the lack of inhibitory TAAR1 tone. (xenbase.org)
  • p less than 0.05), resulting in an approximately 4-fold greater potency for the beta 2AR versus the beta 1AR. (aspetjournals.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)
  • Computer analysis of competition of [125I]iodocyanopindolol binding by betaxolol, practolol, and zinterol in nonmyocyte membranes demonstrates biphasic curves that comprise binding to both beta 1- and beta 2-receptors. (ahajournals.org)
  • All of these ISO-mediated myocyte responses in vitro were inhibited by a beta(1)-AR antagonist, betaxolol, but not by a beta(2)-AR antagonist, ICI 118551. (nih.gov)
  • title=Genetic variation of the beta(2)-adrenoceptor: its functional and clinical importance in bronchial asthma. (enacademic.com)
  • The interaction of doxofylline with beta-2 adrenoceptors was demonstrated by a study using nonlinear chromatography, frontal analysis and molecular docking [A31646]. (drugbank.ca)
  • Via mediating the actions of beta-2 adrenoceptors, doxofylline induces blood vessel relaxation and airway smooth muscle relaxation. (drugbank.ca)
  • Prior biochemical studies have suggested that beta adrenergic receptors in the ciliary process are mostly of the beta-2 subtype. (aspetjournals.org)
  • The rate of production is also influenced by adrenergic receptors in the ciliary epithelium. (thefreelibrary.com)