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.
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.
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.
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 ...
Buy Celiprolol hydrochloride (CAS 57470-78-7), a water soluble cardioselective beta1 adrenoceptor antagonist. Join researchers using high quality Celiprolol…
The IUPHAR/BPS Guide to Pharmacology. [3H]ICI-198615 ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Save money on Adrenergic beta-1 Receptor Antagonists with free prescription coupons from RX24Drugs. We support biggest US pharmacies.
Adrenergic antagonists: Beta blockers Videos, Flashcards, High Yield Notes, & Practice Questions. Learn and reinforce your understanding of Adrenergic antagonists: Beta blockers.
This tuberculocidal, virucidal, fungicidal, and bactericidal formula kills 99.9% of germs on hard, nonporous surfaces and is effective against over 99 microorganisms including Influenza A Virus, MRSA, Norovirus, Rhinovirus, Poliovirus Type 1, Hepatitis A virus, Hepatitis B virus and HIV-1 (AIDS Virus) when used as directed. This product eliminates odors and prevents the growth of mold and mildew. Use on showers, sinks, countertops, around toilet areas, toys, telephones, garbage bins, waiting rooms and in laboratories ...
As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
Professional guide for Icatibant. Includes: pharmacology, pharmacokinetics, contraindications, interactions, adverse reactions and more.
Atipamezole HCl is a selective ??2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for ??2A, ??2B, ??2C, ??1A and ??1B receptors respectively). Has been shown to be a brain penetrant.
Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). 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). For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor,antagonists,using,CypHer5E,and,IN,Cell,Analyzer,1000,biological,advanced biology technology,biology laboratory technology,biology device technology,latest biology technology
Icatibant may cause potentially serious reactions, allergic reactions, or other problems in some people. This eMedTV Web page examines other possible side effects of icatibant and explains which problems require urgent medical attention.
AI0028 Icatibant Acetate Cas No:30308-48-4 Sequence: D-Arg-Arg-pro-Hyp-Gly-Thi-Ser-Tic-Oic-Arg-OH high quality,competitive price AI0028
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.
Also known as 1,1′-[[(1,1-dimethylethyl)imino]bis[(2-hydroxypropane1,3-diyl)oxy(3-acetyl-1,4-phenylene)]]bis(3,3-diethylurea). C36H55N5O8, 685.85 ORDER NOW or ENQUIRE about Celiprolol EP Impurity E. Comes with CoA, 1H-NMR, Mass, HPLC and MSDS. IR, 13C, 2D-NMRs, TGA, Structure Elucidation etc. also provided on request. It is used in Celiprolol impurity profiling as per limits and threshold values specified by respective drug legislations.
alpha 2C Adrenergic Receptor兔多克隆抗体(ab123368)可与人样本反应并经WB实验严格验证。所有产品均提供质保服务,中国75%以上现货。
alpha 2a Adrenergic Receptor兔多克隆抗体(ab92650)可与小鼠, 大鼠, 人样本反应并经IHC实验严格验证。所有产品均提供质保服务,中国75%以上现货。
... is a beta-adrenergic receptor antagonist. Conti P, Dallanoce C, De Amici M, De Micheli C, Klotz KN (April 1998). " ... Beta blockers, Cyclopropanes, Ketoximes, Secondary alcohols, Amines, Tert-butyl compounds, All stub articles, Cardiovascular ... "Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor ... antagonists". Bioorganic & Medicinal Chemistry. 6 (4): 401-8. doi:10.1016/s0968-0896(97)10051-7. PMID 9597184. v t e (Articles ...
Beta-adrenergic agonists, Cardiac stimulants, Catecholamines, D1-receptor agonists, D2-receptor agonists, Norepinephrine ... 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 ...
... 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 blockers, Fluoroarenes, Benzoate esters, Ureas, All stub articles, Cardiovascular system drug stubs). ...
... 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- ...
"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: ...
... 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 ...
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 ...
... 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) ... v t e (Beta blockers, All stub articles, Antihypertensive agent ...
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH antagonist, but is ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 20 (2): 375-385. doi:10.1093/schbul/20.2.375. PMID 8085139.{{cite journal}}: CS1 maint: multiple names: authors list (link) ...
... carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular ... Bronchospasms and hypoglycemia occur because at high doses, the drug can be an antagonist for β2 adrenergic receptors located ... 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". ...
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). ...
... is a beta adrenergic receptor antagonist. Allen, JD; Shanks, RG (1974). "Effects of tiprenolol, practolol and ... Beta blockers, Thioethers, N-isopropyl-phenoxypropanolamines, All stub articles, Cardiovascular system drug stubs). ... 51 (2): 179-85. doi:10.1111/j.1476-5381.1974.tb09645.x. PMC 1776753. PMID 4155971. v t e (Articles without KEGG source, Pages ...
... is a beta adrenergic receptor antagonist. Curtis-Prior, PB; Gadd, AL (1990). "Beta-adrenoceptor antagonists and human ... Beta blockers, Abandoned drugs, All stub articles, Cardiovascular system drug stubs). ... 42 (3): 220-2. doi:10.1111/j.2042-7158.1990.tb05395.x. PMID 1974626. S2CID 85573776. v t e (Articles without EBI source, ...
... beta blockers, mineralocorticoid receptor antagonists (MRA), and sodium glucose cotransporter-2 inhibitors (SGLT2 inhibitors) ... Beta-adrenergic blocking agents (beta blockers) also form part of the first line of treatment, adding to the improvement in ... Japp D, Shah A, Fisken S, Denvir M, Shenkin S, Japp A (January 2017). "Mineralocorticoid receptor antagonists in elderly ... and a mineralocorticoid receptor antagonist as it reduces the risks of cardiovascular mortality and hospitalisation for heart ...
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 ...
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. ...
... 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. ... Beta blockers, Sulfoxides, Phenols, All stub articles, Organic compound stubs, Pharmacology stubs). ... Bromination followed by condensation with 4-(4-methoxyphenyl)butan-2-amine (not PMA) gives the aminoketone 3. Successive ...
... or beta-adrenergic antagonists, may also induce bronchial constriction and block the action of other beta-receptor targeted ... In addition to corticosteroids, oral use of leukotriene receptor antagonist such as Zafirlukast may also be used as a long term ... As the FceRI receptors on mast cells capture the IgE antibodies produced by Th2 cells, they become sensitive to the specific ... Long-acting beta-agonists such as salmetrol had been used in combination with corticosteroids to control asthma symptoms. They ...
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 ...
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 blockers reduce anxiety by decreasing heart rate and preventing shaking. Beta blockers include propranolol, oxprenolol, ... Benzodiazepines bind selectively to the GABA receptor, which is the receptor protein found in the nervous system and is in ...
Beta-adrenergic agonists, Equine medications, NMDA receptor antagonists, Phenol ethers, Phenols, Phenylethanolamines, ... Falkay G, Kovács L (1986). "Affinity of tocolytic agents on human placental and myometrial beta-adrenergic receptors". Journal ... Isoxsuprine is a β2 adrenoreceptor agonist that causes direct relaxation of uterine and vascular smooth muscle via β2 receptors ... 25 (2): 81-7. doi:10.1046/j.1365-2885.2002.00386.x. PMID 12000527. Cole C, Bentz B, Maxwell L, eds. (2014). "13. Clinical ...
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 ...
"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 ...
Pauwels PJ (September 1997). "5-HT 1B/D receptor antagonists". Gen Pharmacol. 29 (3): 293-303. doi:10.1016/s0306-3623(96)00460- ... "Agonist activity of sumatriptan and metergoline at the human 5-HT1D beta receptor: further evidence for a role of the 5-HT1D ... and Adrenergic Receptors" (PDF). Ergot. pp. 432-462. doi:10.1201/9780203304198-21. ISBN 9780429219764. Archived from the ... Hutcheson JD, Setola V, Roth BL, Merryman WD (November 2011). "Serotonin receptors and heart valve disease--it was meant 2B". ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... Dopamine antagonists, H1 receptor antagonists, Muscarinic antagonists, Serotonin receptor antagonists, Sigma agonists, Sodium ... von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... the α1A-adrenergic, the histamine H1 and the M1-M5 muscarinic acetylcholine receptors (see the Table on the right). ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... D1 antagonists, D2 antagonists, D3 antagonists, D4 antagonists, D5 antagonists, H1 receptor antagonists, Muscarinic antagonists ... 5-HT2A antagonists, 5-HT6 antagonists, 5-HT7 antagonists, Alpha-1 blockers, Dimethylamino compounds, Antihistamines, ... von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ...
"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 ...
BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist.[1] ... 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, ...
NMDA receptor antagonists (e.g., DXM, ketamine, methoxetamine, nitrous oxide, phencyclidine, inhalants) ... Two conformers of dopamine have been identified as alpha- and beta-conformers in which the catechol ring is coplanar with the ... Adrenergic agonist (sympathomimetic). *Parasympathomimetic drug (acetylcholine agonist). *Histamine agonist. References[edit]. ... A dopamine agonist (DA) is a compound that activates dopamine receptors. There are two families of dopamine receptors, D2-like ...
Nisoli E, Tonello C, Landi M, Carruba MO (1996). „Functional studies of the first selective β3-adrenergic receptor antagonist ... Beta-3 adrenergički receptor (β3 adrenoreceptor), takođe poznat kao ADRB3, je beta-adrenergički receptor. ADRB3 je takođe ... Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes.". ... Krief S, Lönnqvist F, Raimbault S, et al. (1993). „Tissue distribution of beta 3-adrenergic receptor mRNA in man.". J. Clin. ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Robertson DW, Bloomquist W, Wong DT, Cohen ML (1992). "mCPP but not TFMPP is an antagonist at cardiac 5HT3 receptors". Life ... SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... and functions as a full agonist at all sites except the 5-HT2A receptor, where it acts as a weak partial agonist or antagonist. ...
Tolkovsky AM, Levitzki A (1978). "Mode of coupling between the beta-adrenergic receptor and adenylate cyclase in turkey ... These include receptor antagonists, neurotransmitters, neurotransmitter reuptake, G protein-coupled receptors, G proteins, ... The latter class of complexes is made up of alpha (α), beta (β) and gamma (γ) subunits.[1] In addition, the beta and gamma ... When a ligand activates the G protein-coupled receptor, it induces a conformational change in the receptor that allows the ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... LY-456220 is a potent and selective serotonin 5-HT1D receptor antagonist which has been used in research to study the function ... LY-456220 lacks significant affinity for the 5-HT1B, α1 adrenergic, and dopamine D2 receptors.[1][2] ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ...
"Rapid down regulation of beta adrenergic receptors by combining antidepressant drugs with forced swim: a model of ... Other theories for increases in strength relating to neural adaptation include: agonist-antagonist muscle decreased co- ... Antidepressant drugs, such as those that cause down regulation of β-adrenergic receptors, can cause rapid neural adaptations in ... Neural receptor cells that process and receive stimulation go through constant changes for mammals and other living organisms ...
beta β GLRB Ionotropic glutamate receptors[edit]. The ionotropic glutamate receptors bind the neurotransmitter glutamate. They ... The AMPA receptor bound to a glutamate antagonist showing the amino terminal, ligand binding, and transmembrane domain, PDB ... Adrenergic. *Adrenergic receptor agonist (α. *β (1. *2)). *Adrenergic receptor antagonist (α (1 ... The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, or quisqualate receptor) is a ...
... whereas antagonists of D2 type dopamine receptors typically slow timing;... Depletion of dopamine in healthy volunteers impairs ... 4-Hydroxyamphetamine has been shown to be metabolized into 4-hydroxynorephedrine by dopamine beta-hydroxylase (DBH) in vitro ... SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... 2)CH. 2CH. 2CH. 2CH. 2NH. 2 + 2 CH. 3SO. 3H → [PhCH. 2CH(CH. 3)NHC(O)CH(NH+. 3)CH. 2CH. 2CH. 2CH. 2NH+. 3][CH. 3SO−. 3]. 2. ...
Muscarinic antagonists (anti-cholinergics): Blocking the muscarinic acetylcholine receptors in pulmonary smooth muscle tissue ... These medications include short-acting beta agonists (SABAs) such as albuterol which typically last 4-6 hours, and long-acting ... Rau, JL (Jul 2000). "Inhaled adrenergic bronchodilators: historical development and clinical application". Respir Care. 45 (7 ... These smooth muscle cells have muscarinic M3 receptors on their membrane. The activation of these receptors by acetylcholine ...
... beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta-thromboglobulin - ... receptor (biochemistry) - receptor antagonist - receptor protein-tyrosine kinase - recombinant fusion protein - recombinant ... alpha adrenergic receptor - alpha helix - alpha-1 adrenergic receptor - alpha-2 adrenergic receptor - alpha-beta T-cell antigen ... transforming growth factor beta - transforming growth factor beta receptor - transient receptor potential - translation ( ...
"Differential distribution of beta-adrenergic receptor subtypes in blood vessels of knockout mice lacking beta(1)- or beta(2)- ... Just as with the alpha antagonists, there are selective (beta-1) and non-selective (beta-1 and beta-2) adrenoceptor antagonists ... may follow after initiating an alpha-adrenoceptor antagonist. If that is the case, a beta-adrenoceptor antagonist is then ... This complication is related to the impact that alpha and beta-adrenoceptor antagonists have on blood vessels combined with the ...
Topical beta-adrenergic receptor antagonists, such as timolol, levobunolol, and betaxolol, decrease aqueous humor production by ... Alpha2-adrenergic agonists, such as brimonidine and apraclonidine, work by a dual mechanism, decreasing aqueous humor ... Beta-blockers, such as timolol, work by decreasing aqueous formation. Carbonic anhydrase inhibitors decrease bicarbonate ... other major innovations in pharmacological glaucoma therapy were the introduction of beta blocker eye drops in the 1970s and of ...
... while the ACTH receptor and the β2 adrenergic receptor are relatively distantly-related with a sequence identity of ... Agouti-related protein and Agouti-signaling protein are antagonist peptides to MC2R. ACTH receptor is primarily found in the ... rabbits respond to alpha and beta MSH's (therefore not using the ACTH receptor), and guinea pigs responding to both ACTH and ... ACTH receptors are the shortest of the melanocortin receptor family and are the smallest known G-coupled receptors. Both human ...
Black JW, Crowther AF, Shanks RG, Smith LH, Dornhorst AC (1964). "A new adrenergic betareceptor antagonist". The Lancet. 283 ( ... beta blockers (ICI Pharmaceuticals, 1964) ACE inhibitors, and angiotensin receptor blockers. ACE inhibitors reduce the risk of ... On 2 July 2012, GlaxoSmithKline pleaded guilty to criminal charges and agreed to a $3 billion settlement of the largest health- ... Wilson, Duff (2 October 2010). "Side Effects May Include Lawsuits". The New York Times. Archived from the original on 23 June ...
In contrast to dopamine, fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is ... Since fenoldopam is an intravenous agent with minimal adrenergic effects that improves renal perfusion, in theory it could be ... Concomitant use of fenoldopam with a beta-blocker should be avoided if possible, as unexpected hypotension can result from beta ... D1 receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most ...
... binds to α2-adrenergic receptor and imidazoline receptor binding sites, and blocks NMDA receptors and other cation ... Nicotinic, imidazoline I1 and I2, α2-adrenergic (no intrinsic activity-neither agonist nor antagonist), glutamate NMDAr, and ... Dale HH, Laidlaw PP (October 1911). "Further observations on the action of beta-iminazolylethylamine". The Journal of ... while agmatine binds to α2-adrenergic receptors, it exerts neither an agonistic nor antagonistic effect on these receptors, ...
It also blocks a number of other receptors, including α-adrenergic, 5-HT2C, 5-HT5A, and 5-HT6. It is of significance to note ... H1 receptor antagonists, Pyridines, Pyridoindoles, Russian drugs, Soviet inventions, Drugs in the Soviet Union, Gamma- ... Latrepirdine appears to operate through multiple mechanisms of action, both blocking the action of neurotoxic beta-amyloid ... Cerlapirdine Idalopirdine Matveeva IA (July-August 1983). "Action of dimebon on histamine receptors". Farmakologiia I ...
HIV disease-related drug reaction Hydroxyurea dermopathy Injection site reaction Iododerma Leukotriene receptor antagonist- ... Acquired C1 esterase inhibitor deficiency Acute urticaria Adrenergic urticaria Anaphylaxis Aquagenic urticaria Cholinergic ... broad beta disease, remnant removal disease) Familial hypertriglyceridemia Farber disease (fibrocytic dysmucopolysaccharidosis ... tumor necrosis factor receptor associated periodic syndrome) Chronic blistering cutaneous conditions have a prolonged course ...
Primary insights from functional genomics and effects on beta-adrenergic responsiveness". The Journal of Biological Chemistry. ... "Receptor for the pain modulatory neuropeptides FF and AF is an orphan G protein-coupled receptor". The Journal of Biological ... "Agonist and antagonist activities on human NPFF(2) receptors of the NPY ligands GR231118 and BIBP3226". British Journal of ... Two genes encoding two different receptors (NPFF1 and NPFF2) and two precursors (NPFFA and NPFFB) have been cloned in several ...
... also exhibits no anticholinergic, antidopaminergic, alpha 1-adrenergic, or beta-adrenergic receptor-blocking ... Fexofenadine is a selective peripheral H1 receptor antagonist. Blockage prevents the activation of the H1 receptors by ... H1 receptor antagonists, Peripherally selective drugs, Piperidines, Sanofi, World Health Organization essential medicines). ... 3.0.CO;2-3. PMID 9330784. Shirasaka, Y; Mori T; Murata Y; Nakanishi T; Tamai I (19 February 2014). "Substrate- and Dose- ...
... adrenergic receptors Beta, a rank in a community of social animals; See Alpha Beta carbon, in organic chemistry-the second ... an antagonist in the Walking Dead comic series Beta Hirogen, the second in command of a Hirogen hunting party, as seen in Star ... Beta (B, β) is the second letter of the Greek alphabet. Beta or BETA may also refer to: Beta (film), a 1992 Bollywood film ... "BETA" National Beta Club, a high school honor society South Texas Business Education & Technology Academy (BETA) Beta, Ohio, a ...
Angiotensin receptor blockers (ARB) and calcium channel blockers (CCB), alpha- and beta- adrenergic receptor blockers ... Prazosin has been established as an effective and safe centrally active alpha-1 adrenergic receptor antagonist. It can be used ... Drugs that act as selective antagonists at specific alpha-1 adrenergic receptor subtypes have also been developed. Benign ... Alpha-1 adrenergic receptors are present in vascular smooth muscle, the central nervous system, and other tissues. When alpha ...
... s are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The ... Cirazoline is an α1 adrenergic agonist and an α2 adrenergic antagonist". Journal of Pharmacology and Experimental Therapeutics ... mortality but there was an increased incidence of hypotension and bradycardia Alpha blocker Adrenergic agonist Beta-adrenergic ... amitraz Detomidine[citation needed] Lofexidine, an α2A adrenergic receptor agonist. Medetomidine, an α2 adrenergic agonist. ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... 5-HT2 antagonists, Abandoned drugs, Nitrogen heterocycles, Drugs with unknown mechanisms of action, H1 receptor antagonists, ... Tsai BS, Yellin TO (1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic antidepressants ... Kanba S, Richelson E (1983). "Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated brain ...
Propranolol is a nonselective beta-adrenergic receptor blocking agent. It has been found to relieve exaggerated startle ... Alpha-1 Receptor Antagonists. Class Summary. Novel pilot studies in combat veterans suggest alpha-1 antagonists have efficacy ... Beta-blockers. Class Summary. Beta-blockers such as propranolol are useful in controlling some symptoms of PTSD caused by ... Prazosin is an alpha-1 adrenergic blocker that is indicated for hypertension. Studies indicate that a nighttime dose of ...
... a new adrenergic beta receptor antagonist. Indian Journal of Medical Research. 1970 Feb; 58(2): 246-52. ... a new adrenergic beta receptor antagonist. ...
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. ...
Structural analysis of G-protein-coupled receptors (GPCRs) for hormones and neurotransmitters has been hindered by their low ... Receptors, Adrenergic, beta-2 / chemistry* * Receptors, Adrenergic, beta-2 / metabolism * Rhodopsin / chemistry ... Crystal structure of the human beta2 adrenergic G-protein-coupled receptor Nature. 2007 Nov 15;450(7168):383-7. doi: 10.1038/ ... Structural analysis of G-protein-coupled receptors (GPCRs) for hormones and neurotransmitters has been hindered by their low ...
Once-daily closed triple therapy of a Inhaled Corticosteroid/ Long-acting Muscarinic Receptor Antagonists/ Long Acting Beta- ... Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Hormones, Hormone Substitutes, and Hormone Antagonists. Adrenergic beta-2 Receptor Agonists. ... anticholinergic/muscarinic receptor antagonist, beta2-agonist, lactose/milk protein or magnesium stearate or a medical ...
Adrenergic beta-2 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Anticonvulsants. Anti- ... Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. ... Need for daily controller therapy (i.e., ICS, leukotriene modifiers, and/or long-acting beta-agonists) based on one or more of ... Current options for the second medication include a long-acting beta-agonist, a leukotriene modifier, or theophylline. It is ...
Bond RA, Clarke DE (1988) Agonist and antagonist characterization of a putative adrenoceptor with distinct pharmacological ... Adrenergic receptor beta 3 (ADRB3) gene is located on short arm of chromosome 8 and have two variants [ c.491C.T(p.Trp64Arg) ... The importance of adrenergic beta 3 receptors on gastro intestinal motility has already been documented.[2] De Ponti and co- ... ADRB2: Adrenergic receptor beta 2; ADRB3: Adrenergic receptor beta 3. Table 1b: Genotype frequencies of ADRB2 and ADRB3 ...
One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. Alprenolol is no ... Antagonist. General Function. Receptor signaling protein activity. Specific Function. Beta-adrenergic receptors mediate the ... Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO ... One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. Alprenolol is no ...
Adrenergic beta-1 Receptor Antagonists [D27.505.519.625.] Adrenergic beta-1 Receptor Antagonists ... Adrenergic beta2 Antagonists Adrenergic beta2-Antagonists Antagonists, Adrenergic beta-2 Antagonists, beta2-Adrenergic beta 2 ... Adrenergic beta2 Antagonists. Adrenergic beta2-Antagonists. Antagonists, Adrenergic beta-2. Antagonists, beta2-Adrenergic. beta ... Adrenergic beta2 Adrenergic Antagonists beta2-Adrenergic Antagonists beta2-Antagonists, Adrenergic ...
Beta-2 adrenergic receptor antagonist (disposition). Code System Preferred Concept Name. Beta-2 adrenergic receptor antagonist ...
... is a β1 receptor blocker with an IC50 of 4.5 µM. Find all the information about Nebivolol (Bystolic) for cell signaling ... Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 ... Other Adrenergic Receptor Products. * SB225002New. SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for ... Adrenergic Receptor antagonist Nebivolol hydrochloride (R-65824) Nebivolol hydrochloride (R-65824). Catalog No.S1549 Synonyms: ...
... antagonists, and inverse agonists. To discriminate the distinct efficacy profiles of the ligands, we carried out molecular ... Cannabinoid receptor 1 (CB1) is a promising therapeutic target for a variety of disorders. Distinct efficacy profiles showed ... Ligand-dependent perturbation of the conformational ensemble for the GPCR beta2 adrenergic receptor revealed by HDX. Structure ... experimentally demonstrated that the distinct conformational states of beta-2-adrenergic receptor (β2AR) were induced by the ...
... adrenergic receptor is bound to a full agonist, the G protein coupling domain exists in two distinct conformations. Moreover, ... Agonistas Adrenérgicos beta/metabolismo , Proteínas de Ligação ao GTP/metabolismo , Receptores Adrenérgicos beta 2/metabolismo ... Binding to an antagonist does not change this conformation but does reduce the flexibility of the domain. However, when the ... adrenergic receptor. Fluorescence lifetime analysis of a reporter fluorophore covalently attached to this domain revealed that ...
Beta-1 adrenergic receptor antagonist ChEMBL *Beta-1 adrenergic receptor (Homo sapiens) UniProt ... to adrenergic stimuli by competitively blocking β1-adrenergic receptors within the myocardium and β2-adrenergic receptors ... Beta-2 adrenergic receptor antagonist ChEMBL *Beta-2 adrenergic receptor (Homo sapiens) UniProt ... Sotalol has both beta-adrenoreceptor blocking and cardiac action potential duration prolongation antiarrhythmic properties. ...
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]. ...
The alpha receptor antagonists phentolamine and phenoxybenzamine, the beta-1 receptor antagonists metoprolol and practolol and ... whereas the beta-1 receptor selective agonist dobutamine was only 20% as effective. The general beta receptor antagonists ... the muscarinic receptor antagonist atropine were without effect. The histamine H2-receptor antagonist cimetidine inhibited Iso- ... The beta receptor selective agonists metaproterenol, terbutaline and zinterol stimulated AP accumulation to the same extent as ...
We discontinued diuretics and mineralocorticoid receptor antagonists for ≥6 weeks and beta-adrenergic receptor blockers for ≥2 ... Calcium channel or alpha-adrenergic receptor blockers were preferred for BP control; however, if BP was persistently elevated ... Estrogen receptor inhibits mineralocorticoid receptor transcriptional regulatory function. Endocrinology 2014;155:4461-72.. [ ... The association of estrogen receptor-β gene variation with salt-sensitive blood pressure. J Clin Endocrinol Metab 2017;102:4124 ...
Receptors, Adrenergic, beta.metabolism. Receptors, Adrenergic, beta-1.metabolism. Receptors, Adrenergic, beta-2.metabolism. ... Adrenergic beta-Agonists.metabolism. Adrenergic beta-Antagonists.metabolism.pharmacology. Animals. CHO Cells. Cricetinae. ... LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.. ... an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-selective beta- ...
Adrenergic beta-Antagonists, Angiotensin II Type 1 Receptor Blockers, Confounding Factors (Epidemiology), Diabetes Mellitus, ...
Keywords: Adrenergic beta-Antagonists, Aneurysm, Dissecting, Angiotensin Receptor Antagonists, Blood Pressure, Cardiac Surgical ... Angiotensin Receptor Blockers and Beta-Blockers in Marfan Syndrome. Sep 08, 2022 Share via: ... Angiotensin Receptor Blockers and Beta Blockers in Marfan Syndrome: An Individual Patient Data Meta-Analysis of Randomized ... YOU ARE HERE: Home , Latest in Cardiology , Angiotensin Receptor Blockers and Beta-Blockers in Marfan Syndrome ...
These stand out as particularly effective in elderly subjects, while beta adrenergic blockers and angiotensin-converting enzyme ... mainly diuretics and beta-receptor blocking agents, or the two in combination, with placebo. Two of the trials (SHEP and STOP) ... The therapy used in these studies included diuretics and calcium antagonists. ... On the basis of these trials, it is apparent that therapy with low-dose thiazides or beta-blockers, or the two in combination, ...
7.6 Beta-Adrenergic Receptor Antagonists. Beta-adrenergic receptor antagonists (beta-blockers) and formoterol may inhibit the ... receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors ... 7.6 Beta-Adrenergic Receptor Antagonists 7.7 Halogenated Hydrocarbons 8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy 8.2 Lactation ... of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the ...
... aldosterone antagonists) washout 30 days prior to the study measurements. All studies were performed after a 7 day diet ... 2022 TGF beta signaling pathway Powered by WordPress To the top ↑ Up ↑ ... PubMed] [Google Scholar] 2. Chen W, Zheng R, Zeng H, Zhang S, He J. Annual survey on position of cancers in China, 2011. Chin J ... 2) showing manifestation of Foxp3 and production of (H) IFN-, (I) TNF-, and (J) GM-CSF. Figures on plots refer to percentage in ...
Leukotriene receptor antagonist C. Mast cell stabilizer D. Beta-2 selective adrenergic agonist 16. Which of the following would ... 15) Answer- D Explanation ( These can include: Short-acting beta agonists, such as albuterol. Patient may need to use a machine ... This medication stimulates the beta cells to release more insulin into the blood stream 18. The nurse in the intensive unit is ... Exercise 2-18 (Algo) Cash versus accrual accounting (LO2-9) Stanley and Jones Lawn Service Company (S&J) maintains.... just now ...
The constriction, in turn, was reduced or reversed by phentolamine, an alpha receptor antagonist. Propranolol did not augment ... which in low doses blocks myocardial but not vascular beta receptors. The left circumflex coronary artery of dogs was perfused ... resulting from stimulation of vascular and myocardial beta receptors; the direct vascular effect predominated in this study. ... Responses of coronary vessels to adrenergic stimuli. Donald R. McRaven, Allyn L. Mark, Francois M. Abboud, and Howard E. Mayer ...
Thus, beta blockers reduce the toxic effect of adrenergic excess by inhibiting the chronotropic and inotropic effect of ... Likewise, mineralocorticoid receptor antagonists impede the RAAS by directly inhibiting the effect of aldosterone in the kidney ... mineralocorticoid receptor antagonists should be considered, to further improve prognosis [20,21,22,23]. Following initiation ... Beta-blockers in heart failure with preserved ejection fraction: a meta-analysis. Heart Fail Rev. 2015;20(2):193-201. ...
Case Study 3: Beta-Adrenergic Antagonists. 1570 Words , 7 Pages. Alteration of the response to the Valsalva maneuver and amyl ... and vasodilator responses caused by beta-adrenergic receptor agonists. i. The ... Agonist is often referred to as a drug that stimulates natural processes in the body and beta-2 to a cell receptor. They are ... Benzodiazepines work by slowing down activity of the central nervous system by acting as a ligand for GABA(a) receptors ...
Beta-1 (β1) receptors are mainly in the heart, and increase heart rate and contractility. Beta-1 antagonists therefore slow and ... which binds with all of the primary adrenergic receptor sites (alpha-1, beta-1, and beta-2), and selective agonists like ... atenolol, labetalol) are beta blockers, which have a sedative effect, usually localized to the heart via beta-1 antagonism. ... receptors are mainly in the lungs, and cause bronchodilation. Beta-2 antagonists therefore cause bronchoconstriction. (Mnemonic ...
Beta adrenergic receptors facilitate norepinephrine release from rat hypothalamic and hippocampal slices. Res Commun Mol Pathol ... Antagonism of the antidepressant-like effects of clenbuterol by central administration of beta-adrenergic antagonists in rats. ... ODonnell JM, Wolfe BB, Frazer A. Agonist interactions with beta adrenergic receptors in rat brain. J Pharmacol Exp Ther. 1984 ... ODonnell JM, Frazer A. Effects of clenbuterol and antidepressant drugs on beta adrenergic receptor/N-protein coupling in the ...
Through in silico and in vitro analyses, we identified 24 agonists and 1 antagonist for this receptor. We detected that agonist ... Through in silico and in vitro analyses, we identified 24 agonists and 1 antagonist for this receptor. We detected that agonist ... These findings reveal a new role for OR51E2 and establish this G-protein coupled receptor as a novel therapeutic target in the ... These findings reveal a new role for OR51E2 and establish this G-protein coupled receptor as a novel therapeutic target in the ...
  • Distinct efficacy profiles showed different therapeutic effects on CB1 dependent on three classes of ligands: agonists, antagonists, and inverse agonists. (nature.com)
  • The beta receptor selective agonists metaproterenol, terbutaline and zinterol stimulated AP accumulation to the same extent as Iso, whereas the beta-1 receptor selective agonist dobutamine was only 20% as effective. (aspetjournals.org)
  • 15) Answer- D Explanation ( These can include: Short-acting beta agonists, such as albuterol. (techwhiff.com)
  • Timolol decreases the positive chronotropic, positive inotropic, bronchodilator, and vasodilator responses caused by beta-adrenergic receptor agonists. (antiessays.com)
  • Through in silico and in vitro analyses, we identified 24 agonists and 1 antagonist for this receptor. (frontiersin.org)
  • The pharmacophore model was composed of key features shared by all five inactive states of beta(2)-AR in complex with inverse agonists and antagonists. (khas.edu.tr)
  • the pharmacological manipulation of the sympathetic-immune interface is reviewed with focus on new therapeutic strategies using selective ?2- and ?2-adrenoreceptor agonists and antagonists and inhibitors of phosphodiesterase type IV in the treatment of experimental models of autoimmune diseases, fibromyalgia, and chronic fatigue syndrome. (poiscenter.com)
  • Long-acting beta 2 -adrenergic agonists (LABA) increase the risk of asthma-related death. (rxlist.com)
  • Adenosine A2A and beta-2 adrenergic receptor agonists: novel selective and synergistic multiple myeloma targets discovered through systematic combination screening. (cell.com)
  • Are SGLT-2 Inhibitors the Future of Heart Failure Treatment? (springer.com)
  • Previous cardiovascular outcome trials for sodium-glucose co-transporter-2 (SGLT-2) inhibitors have demonstrated significant favourable outcomes for cardiovascular disease, heart failure hospitalisation and all-cause mortality. (springer.com)
  • The trials will add substantially to our understanding of SGLT-2 inhibitors in the treatment of HFrEF and may have major implications for the treatment of people with HFpEF. (springer.com)
  • In this article we discuss the rationale for using SGLT-2 inhibitors in people with heart failure and explore the potential findings and importance of the ongoing EMPEROR-preserved and EMPEROR-reduced trials. (springer.com)
  • Cardiovascular outcome trials have shown considerable improvement in heart failure hospitalisation and other cardiovascular outcomes in people using sodium-glucose co-transporter-2 (SGLT-2) inhibitors. (springer.com)
  • The EMPEROR trials will considerably add to our understanding of the future role for SGLT-2 inhibitors in people with heart failure, particularly HFpEF. (springer.com)
  • Use of diuretics, angiotensin converting enzyme (ACE) inhibitors, beta adrenergic receptor antagonists (beta blockers), alpha adrenergic receptor antagonists (alpha blockers), calcium channel blockers (CCBs) etc. are not efficient enough to cure hypertension. (scirp.org)
  • Until now, there are different antihypertensive therapies available, such as: ACE (classified as EC3.4.15.1) inhibitors, angiotensin receptor blocker (ARB), beta blockers, diuretics, and also CCBs [7] [8]. (scirp.org)
  • Treatment of heart failure follows the same treatment regimen regardless of the underlying cause (ie, inhibitors, beta-adrenergic blockers). (medscape.com)
  • According to the 2022 AHA/American College of Cardiology/Heart Failure Society of America guidelines for the management of HF, GDMT consists of four core medication classes: renin-angiotensin system (RAS) inhibitors, sodium-glucose cotransporter-2 (SGLT2) inhibitors, beta blockers, and mineralocorticoid receptor antagonists (MRAs). (medscape.com)
  • Current options for the second medication include a long-acting beta-agonist, a leukotriene modifier, or theophylline. (clinicaltrials.gov)
  • This study will also examine whether the addition of tiotropium bromide to low dose ICS is as effective as the addition of a long-acting beta-agonist at maintaining asthma control. (clinicaltrials.gov)
  • Isoprenaline HCl (NCI-c55630,Isoproterenol hydrochloride) is a non-selective beta-adrenergic receptor agonist, used for the treatment of bradycardia and heart block. (selleckchem.com)
  • and (2) the active conformation bound to the agonist AM11542 or AM841 28 . (nature.com)
  • Use with additional long-acting beta 2 -agonist: Do not use in combination because of risk of overdose. (nih.gov)
  • A patient is experiencing an acute asthmatic attack Which agent would be most effective A Inhaled steroid B. Leukotriene receptor antagonist C. Mast cell stabilizer D. Beta-2 selective adrenergic agonist 16. (techwhiff.com)
  • A brand name for bumetanide is Bumex Anastrozole, brand name Arimidex, is a type of anti-estrogen used in treatment of breast cancer but is also used by bodybuilders to combat the estrogenic side effects associated with using anabolic steroids Beta-2 agonist is a drug that opens the bronchial airways and often helps build muscle. (antiessays.com)
  • We detected that agonist 19-hydroxyandrostenedione, a product of the aromatase reaction, is endogenously produced upon receptor activation. (frontiersin.org)
  • Data from a large placebo-controlled US study that compared the safety of another longacting beta 2 -adrenergic agonist (salmeterol) or placebo added to usual asthma therapy showed an increase in asthma-related deaths in patients receiving salmeterol. (rxlist.com)
  • The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice. (wikipedia.org)
  • Alprenolol is a non-selective beta-blocker used in the treatment of hypertension, edema, ventricular tachycardias, and atrial fibrillation. (drugbank.com)
  • SB-334867 is a selective orexin-1 (OX1) receptor antagonist. (selleckchem.com)
  • Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 of 12 nM. (selleckchem.com)
  • LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors. (austin.org.au)
  • LK 204-545 ((+/-)-1-(2-(3-(2-cyano-4-(2-cyclopropyl-methoxy-ethoxy)phenoxy)-2-hydro xy-propyl-amino)-ethyl)-3-(4-hydrxy-phenyl) urea), an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-selective beta-adrenoceptor antagonists were examined to compare their radioligand binding affinities for human beta1-, beta2- and beta3-adrenoceptors transfected into CHO cells. (austin.org.au)
  • LK 204-545 and CGP 20712A displayed the highest beta1-/beta2- (approximately 1800 and approximately 650, respectively) and beta1-/beta3-selectivity (approximately 17000 and approximately 2200, respectively) at human beta-adrenoceptors with LK 204-545 being approximately 2.75-fold more beta1-/beta2-selective and approximately 8-fold beta1-/beta3-selective than CGP 20712A. (austin.org.au)
  • Non-selective alpha blockers work on both alpha-1 and alpha-2 adrenergic receptors and include phenoxybenzamine and phentolamine . (osmosis.org)
  • Albuterol is a sympathomimetic that is selective for beta-2 adrenergic receptors. (drugstodaypdf.com)
  • The memory-modulating effects of glucocorticoids appear to involve the selective activation of the low-affinity glucocorticoid receptor. (scholarpedia.org)
  • Role of non-selective adenosine receptor blockade and phosphodiesterase inhibition in cisplatin-induced nephrogonadal toxicity in rats. (shengsci.com)
  • Beta-blockers such as propranolol are useful in controlling some symptoms of PTSD caused by hyperarousal. (medscape.com)
  • Angiotensin Receptor Blockers and Beta Blockers in Marfan Syndrome: An Individual Patient Data Meta-Analysis of Randomized Trials. (acc.org)
  • Angiotensin receptor blockers slowed aortic root growth rate significantly as compared to control therapy in patients with Marfan syndrome. (acc.org)
  • Patients with Marfan syndrome showed similar aortic growth rate when treated with angiotensin receptor blockers and beta-blockers. (acc.org)
  • Patients with Marfan syndrome may benefit from combination therapy with angiotensin receptor blockers and beta-blockers. (acc.org)
  • What is the effect of angiotensin receptor blockers (ARBs) and beta-blockers (BBs) for patients with Marfan syndrome? (acc.org)
  • Alpha blocker and beta blockers are two types of postsynaptic anti-adrenergic medications that prevent their respective receptors from being stimulated by catecholamines, like norepinephrine and epinephrine . (osmosis.org)
  • And based on the type of receptors they block, they are divided into two main categories - alpha blockers, and beta blockers. (osmosis.org)
  • Beta-blockers are widely used for the treatment of arrhythmia, hypertension, and congestive heart failure. (jmedscindmc.com)
  • Although beta-blockers may induce negative compensatory sympathetic responses to hemorrhagic shock, the effects of beta-blocker use before major trauma on posttrauma outcomes are controversial. (jmedscindmc.com)
  • We examined the association between the use of beta-blockers before major trauma and posttrauma outcomes using a nationwide population-based database. (jmedscindmc.com)
  • Our study included 2245 patients who used beta-blockers before major trauma. (jmedscindmc.com)
  • Individuals who used beta-blockers did not have a significantly higher cumulative risk of mortality than individuals who did not use beta-blockers (beta-blockers users: 17.19%, nonbeta-blockers users: 16.70%, P = 0.662). (jmedscindmc.com)
  • Beta-blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine and norepinephrine on adrenergic beta receptors of the sympathetic nervous system. (jmedscindmc.com)
  • Beta-blockers are generally used to treat arrhythmia. (jmedscindmc.com)
  • Beta blockers may antagonize albuterol. (drugstodaypdf.com)
  • Alpha blockers, such as prazosin, are medications that work as alpha-adrenergic receptor antagonists. (digglicious.com)
  • What is difference between alpha and beta-blockers? (digglicious.com)
  • Beta blockers may be cardioprotective but in contrast to alpha-1 antagonists tend to have adverse effects on plasma lipids. (digglicious.com)
  • Beta-blockers are typically not used as first-line treatment of hypertension, but they are suitable alternatives when ischemic heart disease or another compelling cardiac indication, such as heart failure or diabetes, is present. (medscape.com)
  • Use caution when administering beta-blockers in patients with asthma or severe chronic obstructive pulmonary disease, regardless of beta-selectivity profile. (medscape.com)
  • nondihydropyridines may be a more effective class of medication for Black patients, but beta-blockers have no such recommendation. (medscape.com)
  • Learn more about beta-blockers. (medscape.com)
  • Angiotensin receptor-neprilysin inhibitor/ angiotensin-converting enzyme inhibitor/angiotensin receptor blockers inhibit the RAS and are recommended for all patients with new-onset stage C HFrEF to reduce morbidity and mortality . (medscape.com)
  • A broad group of drugs can cause dry mouth and are cited by the literature, i.e.: anticholinergics, tricyclicant idepressants, antihistamines, benzodiazepines and beta-blockers. (bvsalud.org)
  • Propranolol is a nonselective beta-adrenergic receptor blocking agent. (medscape.com)
  • The general beta receptor antagonists oxprenolol and dl-propranolol and the beta-2 receptor antagonist H35/25 inhibited Iso-stimulated AP accumulation. (aspetjournals.org)
  • Receptor stereoselectivity was shown by the approximately 100-fold difference in potency of the I- and d-isomers of propranolol. (aspetjournals.org)
  • In burned children, exercise training increases maximal oxygen consumption (VO 2 max) and can be combined with the nonspecific beta-blocker propranolol to decrease cardiac work. (cdc.gov)
  • We compared measured and estimated VO 2 max in severely burned children treated with or without propranolol to determine the suitability of commonly used formulas in these populations. (cdc.gov)
  • Measured VO 2 max was higher in the propranolol group (25.5±6.0 mL/min/kg vs. 22.0±4.7 mL/min/kg,p=0.002) and was generally lower than estimated values. (cdc.gov)
  • The VO 2 max formula reported here is suitable for propranolol-treated children and the Porro formula for non-propranolol–treated children. (cdc.gov)
  • Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes. (selleckchem.com)
  • The alpha receptor antagonists phentolamine and phenoxybenzamine, the beta-1 receptor antagonists metoprolol and practolol and the muscarinic receptor antagonist atropine were without effect. (aspetjournals.org)
  • The constriction, in turn, was reduced or reversed by phentolamine, an alpha receptor antagonist. (jci.org)
  • But what sets these two apart is that phenoxybenzamine is an irreversible, noncompetitive antagonist, while phentolamine is a reversible, competitive antagonist . (osmosis.org)
  • Novel high affinity compounds for human beta(2)-adrenergic receptor (beta(2)-AR) were searched among the clean drug-like subset of ZINC database consisting of 9928465 molecules that satisfy the Lipinski's rule of five. (khas.edu.tr)
  • Mutual information and entropy transfer analysis employed on two inactive states of human beta-2 adrenergic receptor (beta(2)-AR) unraveled distinct communication pathways. (khas.edu.tr)
  • Endocrinology and Metabolism 2022;37(2):369-382. (e-enm.org)
  • We characterized the effects of receptor activation on metabolism using a prostate cancer cell line and demonstrated decreased intracellular anabolic signals and cell viability, induction of cell cycle arrest, and increased expression of neuronal markers. (frontiersin.org)
  • Beta adrenergic receptors are thought to be involved in the control of appetite and fat metabolism and the ability of Clenbuterol to be a potent and effective inhibitor of these receptors (as well as to stimulate fatty acid synthesis from non-esterified fatty acids) is one of its main advantages in weight loss management. (destinyandspirit.com)
  • The evidence syntheses were discussed and recommendations formulated by a multidisciplinary Task Force of COPD experts.After considering the balance of desirable (benefits) and undesirable consequences (burden in the form of adverse effects and cost), quality of evidence, feasibility, and acceptability of various interventions, the Task Force made recommendations for mucolytic, long-acting muscarinic antagonist, phosphodiesterase-4 inhibitor (roflumilast) and macrolide therapy, as well as a conditional recommendation against fluoroquinolone therapy. (bvsalud.org)
  • Several GPCRs, such as the 5HT1c serotonin receptor ( 2 ), the M1, M3, and M5 muscarinic receptors ( 3 ), and the α1B-ADR adrenergic receptor ( 4 ), can function as oncogenes when persistently activated. (frontiersin.org)
  • 2004). Further, in non-habituated rats administration of a \(\beta\)-adrenoceptor antagonist immediately after the object recognition training blocked the corticosterone-induced memory enhancement (Roozendaal et al. (scholarpedia.org)
  • beta-Endorphin administered intrathecally (i.t.) in rats produced a dose-dependent elevation in tail-flick latency. (omeka.net)
  • Increased cardiac sympathetic drive and reduced vagal modulation following endothelin receptor antagonism in healthy conscious rats. (shengsci.com)
  • 1. The present study evaluated changes in autonomic control of the cardiovascular system in conscious rats following blockade of endothelin (ET) receptors with bosentan. (shengsci.com)
  • 2. Rats were treated with bosentan or vehicle (5% gum arabic) for 7 days by gavage. (shengsci.com)
  • Alprenolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. (drugbank.com)
  • Glucocorticoids alter the sensitivity of epinephrine in influencing memory consolidation and, conversely, adrenergic activation induced by emotional arousal appears to be essential in enabling glucocorticoid modulation of memory consolidation. (scholarpedia.org)
  • Formoterol fumarate dihydrate is a beta 2 -adrenergic bronchodilator. (rxlist.com)
  • Sotalol inhibits response to adrenergic stimuli by competitively blocking β1-adrenergic receptors within the myocardium and β2-adrenergic receptors within bronchial and vascular smooth muscle. (liu.edu)
  • It relaxes smooth muscles of the bronchial tree and peripheral vasculature by stimulating adrenergic receptors of the sympathetic nervous system. (drugstodaypdf.com)
  • Glucocorticoids are highly lipophilic and, thus, readily enter the brain and bind directly to mineralocorticoid receptors and glucocorticoid receptors. (scholarpedia.org)
  • Glucocorticoids act through intracellular and intranuclear receptors and can affect gene transcription by direct binding of receptor homodimers to DNA . (scholarpedia.org)
  • However, glucocorticoids may also act more rapidly by interacting with membrane receptors and/or potentiating the efficacy of the norepinephrine-signal cascade via an interaction with G-protein-mediated actions. (scholarpedia.org)
  • These results indicate that the coronary vasodilator action of norepinephrine and sympathetic nerve stimulation is indirect and caused by stimulation of myocardial beta receptors. (jci.org)
  • These two catecholamines activate the adrenergic receptors on the many different organs, which allow the sympathetic nervous system to trigger the fight or flight response that increases the heart rate and blood pressure , as well as slowing digestion. (osmosis.org)
  • Th1 cells express more beta 2 adrenergic receptors than Th2 cells, indicating a greater influence of sympathetic activity on Th1 response. (poiscenter.com)
  • Beta adrenergic receptors have also been shown to be involved in the regulation of the sympathetic nervous system, i, side effects of stopping anabolic steroids.e, side effects of stopping anabolic steroids. (destinyandspirit.com)
  • By blocking alpha-1 receptors , they cause vasodilation and lower blood pressure . (osmosis.org)
  • They act by blocking alpha-1 receptors in the brain which is thought to lead to better, deeper sleep. (digglicious.com)
  • These ligands-glial cell line-derived neurotrophic factor (GDNF), neurturin, persephin, and artemin-also interact with one of four coreceptors in the GDNF-family receptor-alpha family. (medscape.com)
  • So, phenoxybenzamine binds irreversibly, to a different site on the receptor from catecholamines, and changes the shape of the receptor so it can no longer bind to catecholamines. (osmosis.org)
  • Cannabinoid receptor 1 (CB1) is a promising therapeutic target for a variety of disorders. (nature.com)
  • These findings reveal a new role for OR51E2 and establish this G-protein coupled receptor as a novel therapeutic target in the treatment of prostate cancer. (frontiersin.org)
  • The histamine H2-receptor antagonist cimetidine inhibited Iso-stimulated AP accumulation an average of 40% at a concentration which inhibits completely histamine-stimulated AP accumulation. (aspetjournals.org)
  • Histamine 2 Antagonists. (pearsonitcertification.com)
  • Structural analysis of G-protein-coupled receptors (GPCRs) for hormones and neurotransmitters has been hindered by their low natural abundance, inherent structural flexibility, and instability in detergent solutions. (nih.gov)
  • G-protein coupled receptors (GPCRs) have emerged as important factors in tumor growth and metastasis ( 1 ). (frontiersin.org)
  • Olfactory receptors (ORs) are the largest family of GPCRs present in the olfactory epithelium but are also found in various ectopic or non-olfactory locations such as prostate, heart, placenta, embryo, erythroid cells, spleen, kidney, gut, tongue, and carotid body ( 7 ). (frontiersin.org)
  • These receptors link to downstream signaling pathways by activating heterotrimeric G proteins and, as such, are designated G protein-coupled receptors (GPCRs). (aspetjournals.org)
  • Coronary responses to adrenergic stimuli were determined in the intact beating heart before and after administration of practolol, 4-(2-hydroxy-3-isopropylaminoproproxy) acetanilide, which in low doses blocks myocardial but not vascular beta receptors. (jci.org)
  • The direct effect of these two stimuli on coronary vessels is minimal and is mediated through stimulation of alpha (vasoconstrictor) receptors. (jci.org)
  • A variety of hormones, neurotransmitters, and physical stimuli trigger intracellular responses by binding to seven transmembrane receptors. (aspetjournals.org)
  • It could be concluded that beta adrenoceptor gene polymorphism has significant role on regulation of gut motility in T2DM. (researchsquare.com)
  • The high potency of LK 204-545 at transfected human beta1-adrenoceptors and in functional models of rat beta1-adrenoceptors together with its high selectivity, identify it as a useful ligand for studying beta1-adrenoceptors and suggest that it may be the preferred ligand for human beta-adrenoceptor studies. (austin.org.au)
  • Spinal administration of the alpha 1-adrenoceptor antagonist WB-4101 failed to alter the analgesic effects of the opioid, whereas the alpha 2-adrenoceptor antagonist yohimbine completely blocked beta-endorphin-induced elevations in tail-flick latency. (omeka.net)
  • IMSEAR at SEARO: Cardiopulmonary actions of 1-isopropylamino-3-(3-tolyloxy)-2-propanol hydrochloride: a new adrenergic beta receptor antagonist. (who.int)
  • Treatment of asthma in patients ≥12 years: 2 inhalations twice daily of DULERA 100 mcg/5 mcg or 200 mcg/5 mcg. (nih.gov)
  • Treatment of asthma in patients aged 5 to less than 12 years: 2 inhalations twice daily of DULERA 50 mcg/5 mcg. (nih.gov)
  • So when a presynaptic nerve ending is stimulated to release noradrenaline in the synaptic cleft, some of that norepinephrine turns around and binds to alpha-2 receptors on the presynaptic membrane. (osmosis.org)
  • Sotalol has both beta-adrenoreceptor blocking and cardiac action potential duration prolongation antiarrhythmic properties. (liu.edu)
  • The cardiac beta-receptors low affinity was compensated for by an increment in their density. (curehunter.com)
  • This probably maintained cardiac function since 70% of the mice survived for more than 2 years even though anti- cruzipain titers remained high. (curehunter.com)
  • Thus, RGS3 can impair Gi- (but not Gz-) and Gq-mediated signaling in hematopoietic and other cell types by acting as a GAP for G iα and G qα subfamily members and as a potent G qα subfamily effector antagonist. (aspetjournals.org)
  • Tumor necrosis factor-alpha antagonist etanercept decreases blood pressure and protects the kidney in a mouse model of systemic lupus erythematosus. (medscape.com)
  • Angiotensin II receptor antagonists or ARBs are typically used for patients who cannot tolerate ACEIs. (medscape.com)
  • RET consists of 3 domains, including a cysteine-rich extracellular receptor domain, a hydrophobic transmembrane domain, and an intracellular tyrosine kinase catalytic domain. (medscape.com)
  • Previously, a so-called "highly" inactive state of the receptor was observed during 1.5 microsecond long molecular dynamics simulation where the largest intracellular loop (ICL3) was swiftly packed onto the G-protein binding cavity, becoming entirely inaccessible. (khas.edu.tr)
  • Activation of beta 2 -adrenergic receptors on airway smooth muscle leads to the activation of adenylcyclase, and to an increase in the intracellular concentration of cyclic-3',5'-adenosine monophosphate cyclic AMP. (privelexperiences.com)
  • Subjects will run-in on their existing COPD medications for 2 weeks and in addition will be provided with short acting albuterol/salbutamol to be used on an as-needed basis (rescue medication) throughout the study. (clinicaltrials.gov)
  • Alright, so medications that inhibit peripheral postsynaptic adrenergic neurons are called peripheral postsynaptic anti-adrenergics. (osmosis.org)
  • Pretrauma beta-blocker users did not have a higher mortality rate after a major trauma even after adjusting for several comorbidities and medications in a nationwide population database. (jmedscindmc.com)
  • Alprenolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, alprenolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action. (drugbank.com)
  • Stimulation of angiotensin II receptor 2 preserves cognitive function and is associated with an enhanced cerebral vascular density after stroke. (musc.edu)
  • 1959). The memory modulation is initiated, at least in part, by activation of peripheral \(\beta\)-adrenoceptors located on vagal afferents that project to the nucleus of the solitary tract (NTS) in the brain stem. (scholarpedia.org)
  • [2] [3] It is chiefly responsible for regulating digestive processes and contains over a hundred million neurons of over fifteen morphologies, greater than the sum of all other peripheral ganglia. (nih.gov)
  • The Δ 9 -tetrahydrocannabivarin (THCV) 21 is a CB1 antagonist that is structurally similar to THC. (nature.com)
  • Beta-3 adrenergički receptor (β 3 adrenoreceptor), takođe poznat kao ADRB3 , je beta-adrenergički receptor . (wikipedia.org)
  • However, no study has been conducted to observe whether adrenergic beta receptor (ADRB) 2 and 3 gene polymorphism could influence the gut motility in T2DM. (researchsquare.com)
  • Very few studies have reported the association between ADRB2 gene polymorphism and type 2 diabetes mellitus (T2DM) and some of them have contradictory findings. (researchsquare.com)
  • Floppy mitral valve/mitral valve prolapse syndrome: Beta-adrenergic receptor polymorphism may contribute to the pathogenesis of symptoms. (cdc.gov)
  • Let's focus on alpha receptors, which have two subtypes: alpha-1 and alpha-2. (osmosis.org)
  • Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (K i value = 0.9 nM and beta 2/beta 1 ratio = 50). (selleckchem.com)
  • Patients with cardiovascular disorders: Use with caution because of beta-adrenergic stimulation. (nih.gov)
  • Also, with a more minor effect, by binding beta-2 receptors in the juxtaglomerular apparatus, alprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively. (drugbank.com)
  • One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. (drugbank.com)
  • Question 4 Marks: 1 The physician has ordered the adrenergic drug doxazosin (Cardura), an antihypertensive drug, for a patient. (antiessays.com)
  • Aldosterone (beta-hydroxybutyrate) receptors are located along the cell membrane in the periphery of cells. (destinyandspirit.com)
  • Clenbuterol is an aldosterone (beta-hydroxybutyrate) receptor antagonist. (destinyandspirit.com)
  • Aldosterone receptor antagonist, is also known as an aldosterone-receptor blocker, side effects of stopping steroid cream. (destinyandspirit.com)
  • The risk or severity of adverse effects can be increased when Alprenolol is combined with 1,2-Benzodiazepine. (drugbank.com)
  • Mutations in RET, a transmembrane proto-oncogene, have been localized to 10q11.2 and are responsible for MEN 2. (medscape.com)
  • These receptors are responsible for the transport of hormones and a number of other substances, side effects of stopping steroids too quickly. (destinyandspirit.com)
  • Parenteral for IV injection 3 mg/ml in 2-ml flip -top vials Dosage and Administration a. 6.0 mg IV/Saline Lock bolus, rapidly , followed by a Normal Saline (0.9 NS) flush. (drugstodaypdf.com)
  • Albuterol acts as a functional antagonist to relax the airway irrespective of ventolin spasmogen involved, thus protecting against all bronchoconstrictor challenges. (privelexperiences.com)