Adrenergic beta 3 receptor antagonists. Medical search

A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.

Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.

Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.

Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.

A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.

The relationship between the dose of an administered drug and the response of the organism to the drug.

A family of hexahydropyridines.

Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.

Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.

Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.

Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.

An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.

Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.

Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.

Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.

Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.

Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.

Agents inhibiting the effect of narcotics on the central nervous system.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.

Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.

Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.

Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.

Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.

Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.

Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.

A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.

A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.

Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.

A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.

Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.

A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.

One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.

An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.

Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.

Compounds with BENZENE fused to AZEPINES.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.

A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.

Purine bases found in body tissues and fluids and in some plants.

Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.

Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).

A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.

Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.

Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).

Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.

Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.

A group of compounds that contain the structure SO2NH2.

Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.

The action of a drug that may affect the activity, metabolism, or toxicity of another drug.

An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.

Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.

Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.

RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.

An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.

A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)

Seven membered heterocyclic rings containing a NITROGEN atom.

A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.

A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.

A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.

The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.

Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.

A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.

An integrin beta subunit of approximately 85-kDa in size which has been found in INTEGRIN ALPHAIIB-containing and INTEGRIN ALPHAV-containing heterodimers. Integrin beta3 occurs as three alternatively spliced isoforms, designated beta3A-C.

Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.

Elements of limited time intervals, contributing to particular results or situations.

A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.

Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.

The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.

The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.

The observable response an animal makes to any situation.

Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.

A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.

Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.

The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.

A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.

Compounds with a BENZENE fused to IMIDAZOLES.

Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.

A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.

Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.

Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.

A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.

Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.

A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

Injections into the cerebral ventricles.

A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.

A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.

Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.

Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.

Use of electric potential or currents to elicit biological responses.

Peptides composed of between two and twelve amino acids.

A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.

A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.

An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.

Established cell cultures that have the potential to propagate indefinitely.

An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.

Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.

Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.

An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.

A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)

A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.

Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.

Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.

PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.

A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).

A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.

A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.

21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.

Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).

Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.

An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.

The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.

A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.

Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.

An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).

A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.

Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.

Cell surface proteins that bind CALCITONIN GENE-RELATED PEPTIDE with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the CENTRAL NERVOUS SYSTEM and the periphery. They are formed via the heterodimerization of the CALCITONIN RECEPTOR-LIKE PROTEIN and RECEPTOR ACTIVITY-MODIFYING PROTEIN 1.

AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.

An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.

Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.

Drugs that bind to and block the activation of PURINERGIC RECEPTORS.

A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.

A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.

Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.

A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.

Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.

One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.

The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.

Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.

A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.

The most common inhibitory neurotransmitter in the central nervous system.

AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.

A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.

A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.

The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.

A class of drugs that act by selective inhibition of calcium influx through cellular membranes.

The physical activity of a human or an animal as a behavioral phenomenon.

The rate dynamics in chemical or physical systems.

Drugs that bind to and activate dopamine receptors.

CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.

1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)

Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.

A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)

Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)

A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.

A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.

Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.

A subclass of serotonin receptors that form cation channels and mediate signal transduction by depolarizing the cell membrane. The cation channels are formed from 5 receptor subunits. When stimulated the receptors allow the selective passage of SODIUM; POTASSIUM; and CALCIUM.

A family of biologically active peptides sharing a common conserved C-terminal sequence, -Phe-X-Gly-Leu-Met-NH2, where X is either an aromatic or a branched aliphatic amino acid. Members of this family have been found in mammals, amphibians, and mollusks. Tachykinins have diverse pharmacological actions in the central nervous system and the cardiovascular, genitourinary, respiratory, and gastrointestinal systems, as well as in glandular tissues. This diversity of activity is due to the existence of three or more subtypes of tachykinin receptors.

A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ B with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the BRONCHI.

The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.

A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)

The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.

A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.

A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.

The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.

Proteins prepared by recombinant DNA technology.

The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.

A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.

Compounds capable of relieving pain without the loss of CONSCIOUSNESS.

An angiotensin receptor subtype that is expressed at high levels in fetal tissues. Many effects of the angiotensin type 2 receptor such as VASODILATION and sodium loss are the opposite of that of the ANGIOTENSIN TYPE 1 RECEPTOR.

A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)

An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.

Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.

A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.

Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.

A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.

A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)

An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.

The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.

An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).

A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.

Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.

A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.

An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.

Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.

A subtype of BRADYKININ RECEPTOR that is induced in response to INFLAMMATION. It may play a role in chronic inflammation and has a high specificity for KININS lacking the C-terminal ARGININE such as des-Arg(10)-kallidin and des-Arg(9)-bradykinin. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.

Compounds that inhibit the action of prostaglandins.

Drugs that selectively bind to and activate beta-adrenergic receptors.

A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.

A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.

Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

... adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics. 290 (2): 649-55. PMID 10411574. v ... β3-adrenoceptor antagonist) is an adrenergic antagonist which blocks the Beta-3 adrenergic receptors of cells, with either high ... SR 59230A Carvedilol Betablocker Beta-3 adrenergic receptor Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, ... an antagonist for β3 and for β1 or β2 adrenoceptors) like the non-selective betablocker Carvedilol. ...

https://en.wikipedia.org/wiki/Beta-3_adrenergic_antagonist

Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic ... is a beta-adrenergic receptor, and also denotes the human gene encoding it. Actions of the β3 receptor include Enhancement of ... Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through ...

https://en.wikipedia.org/wiki/Beta-3_adrenergic_receptor

... bronchodilation Subtype unspecific β antagonists (beta blockers) can be used to treat: heart arrhythmia - decrease the output ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 There is no α1C receptor. There was a subtype known as C, but ... and β-Adrenergic Receptors Theory of receptor activation Desensitization of β1 receptors (Webarchive template wayback links, ... Sep 2010). "Ghrelin secretion stimulated by {beta}1-adrenergic receptors in cultured ghrelinoma cells and in fasted mice". ...

https://en.wikipedia.org/wiki/Adrenergic_receptor

"Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... SR 59230A is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 ... Bellantuono V, Cassano G, Lippe C (August 2008). "The adrenergic receptor subtypes present in frog (Rana esculenta) skin". Comp ...

https://en.wikipedia.org/wiki/SR_59230A

... 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). ... 81 (3): 309-22. PMID 8235065. Kam, Sheung Tsam; Matier, William L.; Mai, Khuong X.; Barcelon-Yang, Cynthia; Borgman, Robert J ...

https://en.wikipedia.org/wiki/Flestolol

... denotes selective antagonist to the receptor. compound-6FA, PAM at intracellular binding site Beta-2 adrenergic receptor has ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ...

https://en.wikipedia.org/wiki/Beta-2_adrenergic_receptor

"Death temporally related to the use of a Beta adrenergic receptor antagonist in cocaine associated myocardial infarction". ... "Reflections on beta-adrenergic receptor blockers and cocaine use. A case in point". Revista Española de Cardiología. 62 (4): ... Schurr, James W.; Gitman, Brenda; Belchikov, Yuly (2014-12-01). "Controversial therapeutics: the β-adrenergic antagonist and ... "Potentiation of Cocaine-Induced Coronary Vasoconstriction by Beta-Adrenergic Blockade". Annals of Internal Medicine. 112 (12): ...

https://en.wikipedia.org/wiki/Cocaine_intoxication

... 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 ...

https://en.wikipedia.org/wiki/ICI-118,551

... 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, ...

https://en.wikipedia.org/wiki/Tolamolol

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 ...

https://en.wikipedia.org/wiki/Chlorprothixene

... is a beta adrenergic receptor antagonist. Mostaghim, R; Maddox, YT; Ramwell, PW (1986). "Endothelial potentiation ... Beta blockers, Spiro compounds, All stub articles, Cardiovascular system drug stubs). ... 239 (3): 797-801. PMID 2879033. v t e (Articles without EBI source, Articles without KEGG source, Pages using collapsible list ... of relaxation response to beta adrenoceptor blocking agents". The Journal of Pharmacology and Experimental Therapeutics. ...

https://en.wikipedia.org/wiki/Spirendolol

... is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high specificity (an antagonist ... ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... A Beta-2 adrenergic antagonist (β2-adrenoceptor antagonist) ... "The pharmacology of a beta 2-selective adrenoceptor antagonist ... which is selective for β2 adrenoceptors) like Butaxamine and ICI-118,551, or non-specifically (an antagonist for β2 and for β1 ...

https://en.wikipedia.org/wiki/Beta-2_adrenergic_antagonist

... 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 ...

https://en.wikipedia.org/wiki/Sulfinalol

January 2016). "Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive ... The beta-3 adrenergic receptor (beta3AR) was discovered in the late 1980s and initially, beta3AR agonists were investigated as ... Use with nonselective muscarinic antagonists may increase the risk of urinary retention. The manufacturer suggests ... The receptors are located in the kidneys, urinary tract and bladder tissue. Upon binding, the β3 receptor undergoes a ...

https://en.wikipedia.org/wiki/Vibegron

"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 ...

https://en.wikipedia.org/wiki/Neuregulin_3

"Three-dimensional models for beta-adrenergic receptor complexes with agonists and antagonists". Journal of Medicinal Chemistry ... In 1984 the β3 receptor was described as the third group of beta receptors in adipose tissue. This led to the development of ... Beta-adrenergic agonist Beta2-adrenergic agonist "Betmiga , European Medicines Agency". www.ema.europa.eu. Retrieved 2018-10-02 ... β2 adrenergic receptors to prevent over-activation by opposing the classical inotropic effect of β1 and β2 adrenergic receptors ...

https://en.wikipedia.org/wiki/Beta3-adrenergic_agonist

... is a beta adrenergic receptor antagonist. Stephenson, KA; Wilson, AA; Meyer, JH; Houle, S; Vasdev, N (2008). "Facile ... Beta blockers, N-isopropyl-phenoxypropanolamines, All stub articles, Cardiovascular system drug stubs). ... Synthesis, radiolabeling, and ex vivo biodistribution of 18F-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol ...

https://en.wikipedia.org/wiki/Toliprolol

... 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 ... Smith C, Teitler M (April 1999). "Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors". ... Bristow MR, Hershberger RE, Port JD, Minobe W, Rasmussen R (March 1989). "Beta 1- and beta 2-adrenergic receptor-mediated ...

https://en.wikipedia.org/wiki/Bisoprolol

... like Scopolia tanguticus Anisodine acts as a muscarinic acetylcholine receptor antagonist and α1-adrenergic receptor antagonist ... Anisodine can be efficiently prepared using 6-beta-acetyltropine as the starting material via a key step of the Sharpless ... Muscarinic antagonists, Tropane alkaloids, Tropane alkaloids found in Solanaceae, All stub articles, Cardiovascular system drug ... 87 (3): 587-94. doi:10.1111/j.1476-5381.1986.tb10201.x. PMC 1916562. PMID 2879586. Ganellin, C. R.; Triggle, David J. (21 ...

https://en.wikipedia.org/wiki/Anisodine

... is a beta adrenergic receptor antagonist. Saltvedt, E; Fauchald, P (1980). "Effect of single and twice daily doses ... Augstein, J.; Cox, D. A.; Ham, A. L.; Leeming, P. R.; Snarey, M. (1973). "Beta-adrenoceptor blocking agents. 1. Cardioselective ... Beta blockers, Pyrimidinediones, All stub articles, Cardiovascular system drug stubs). ... 1-aryloxy-3-(aryloxyalkylamino)propan-2-ols". Journal of Medicinal Chemistry. 16 (11): 1245-1251. doi:10.1021/jm00269a007. PMID ...

https://en.wikipedia.org/wiki/Primidolol

... 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- ...

https://en.wikipedia.org/wiki/Fexofenadine

Beta blockers) β1-selective antagonists include: Acebutolol (in hypertension, angina pectoris and arrhythmias) Atenolol (in ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic ... The beta-1 adrenergic receptor (β1 adrenoceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the ... "The cardiac beta-adrenergic receptor. Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by ...

https://en.wikipedia.org/wiki/Beta-1_adrenergic_receptor

... is a beta-adrenergic receptor agonist/antagonist. The antagonist activity of lubabegron at β1 and β2 receptors ... avoids the potential negative side effects associated with β1 and β2 receptor activation. The β1-AR and β2-AR antagonist ... "Comparison of beta-ligands used in cattle production: Structures, safety, and biological effects". Journal of Animal Science. ... 5 (3): txab137. doi:10.1093/tas/txab137. PMC 8439260. PMID 34532643. Teeter JS, Werth SJ, Gruber SL, Kube JC, Hagenmaier JA, ...

https://en.wikipedia.org/wiki/Lubabegron

September 2018). "β3-adrenergic receptor activation induces TGFβ1 expression in cardiomyocytes via the PKG/JNK/c-Jun pathway". ... Bond RA, Clarke DE (November 1988). "Agonist and antagonist characterization of a putative adrenoceptor with distinct ... pharmacological properties from the alpha- and beta-subtypes". British Journal of Pharmacology. 95 (3): 723-734. doi:10.1111/j. ... BRL-37344 is a drug which acts as a selective agonist of the β3 adrenergic receptor, which has been investigated for various ...

https://en.wikipedia.org/wiki/BRL-37344

For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta ... angiotensin II receptor antagonists, calcium-channel blockers, and thiazide diuretics are generally preferred over beta ... Nebivolol while selectively blocking beta(1) receptor acts as a beta(3)-agonist. β3 receptors are found in the gallbladder, ... Beta blockers help patients with cardiovascular disease by blocking β1 receptors, while many of the side-effects of these ...

https://en.wikipedia.org/wiki/Nebivolol

J. W. Black; A. F. Crowther; R. G. Shanks; A. C. Dornhorst (1964). "A new adrenergic beta-receptor antagonist". The Lancet. 283 ... he called beta adrenotropic receptor (now β-adrenoceptor or β-adrenergic receptor). ″This concept of two fundamental types of ... he called alpha adrenotropic receptor (now α-adrenoceptor or α-adrenergic receptor), while the receptor with the second rank ... that both are beta type receptors. … It is suggested that this terminology be extended to the realm of adrenergic blocking ...

https://en.wikipedia.org/wiki/History_of_catecholamine_research

Straube T, Frey JU (2003). "Involvement of beta-adrenergic receptors in protein synthesis-dependent late long-term potentiation ... an antagonist to the NMDA receptor, which prevented LTP in this pathway. Conversely, LTP in the mossy fiber pathway is NMDA ... Additionally, β-adrenergic receptor agonists such as norepinephrine may alter the protein synthesis-dependent late phase of LTP ... As mentioned previously, AMPA receptors are the brain's most abundant glutamate receptors and mediate the majority of its ...

https://en.wikipedia.org/wiki/Long-term_potentiation

... α1 adrenergic receptor and H1 receptor. Thiethylperazine activates the transport protein ABCC1 that clears beta-amyloid from ... It is an antagonist of dopamine receptors (DRD1, DRD2, DRD4) as well as of 5-HT2A, 5-HT2C receptors, mAChRs (1 through 5), ... Theithylperazine may possess antypsychotic activity due to the antagonism of 5-HT2 and D2 receptors. Because of this, it would ... "Alzheimer disease: Transport protein ABCC1 plays key role in clearing beta-amyloid from brains of mice". ScienceDaily (Press ...

https://en.wikipedia.org/wiki/Thiethylperazine

... is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... then the molecule typically is found to have receptor affinity without intrinsic activity, and is, therefore, an antagonist. ... Labetalol is a dual alpha (α1) and beta (β1/β2) adrenergic receptor blocker and competes with other Catecholamines for binding ... Labetalol was the first drug created that combined both alpha- and beta- adrenergic receptor blocking properties. It was ...

https://en.wikipedia.org/wiki/Labetalol

Beta-blockers are competitive antagonists of the adrenergic beta receptor, blocking the binding sites of epinephrine and ... Angiotensin receptor blockers (ARBs) antagonize the action of Ang II by binding and inhibiting angiotensin II type 1 receptor. ... There are several Ang receptors in the body with the most common being AT1R, which is expressed in the heart, kidney, gut, ... Propranolol, Atenolol, Bupranolol, Timolol, are some examples of clinically available beta-blockers. "High blood pressure ( ...

https://en.wikipedia.org/wiki/Hypertension_and_the_brain

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 ...

https://en.wikipedia.org/wiki/Bronchoconstriction

... beta-2 microglobulin - beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta- ... 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 ( ...

https://en.wikipedia.org/wiki/Index_of_biochemistry_articles

"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 ...

https://en.wikipedia.org/wiki/Pheochromocytoma

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 ...

https://en.wikipedia.org/wiki/Glaucoma

... 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 ... melanocortin-2 receptor (MC2R)] by human MC2R accessory protein isoforms alpha and beta in isogenic human embryonic kidney 293 ... The adrenocorticotropic hormone receptor or ACTH receptor also known as the melanocortin receptor 2 or MC2 receptor is a type ...

https://en.wikipedia.org/wiki/ACTH_receptor

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 ... 24 (3): 489-501, vi-vii. doi:10.1016/j.cger.2008.03.001. PMID 18672184. Retrieved 20 June 2009. Gardner AW, Afaq A (2008). " ... 22 (3): 388-91. doi:10.1161/01.hyp.22.3.388. PMID 8349332. BORHANI NO, HECHTER HH (1964). "Recent Changes in CVR Disease ...

https://en.wikipedia.org/wiki/Pharmaceutical_industry

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 ... evidence that it may have some alpha-1 and alpha-2 adrenoceptor antagonist activity. D1 receptor stimulation activates adenylyl ... Concomitant use of fenoldopam with a beta-blocker should be avoided if possible, as unexpected hypotension can result from beta ...

https://en.wikipedia.org/wiki/Fenoldopam

... 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, ...

https://en.wikipedia.org/wiki/Agmatine

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 ... The block on alpha-2 receptors further potentiates beta-effects, increasing cardiac output. Phenoxybenzamine has a long-lasting ... Clinically, non-selective alpha antagonists block alpha receptors (but do not differentiate between alpha-1 and alpha-2). They ...

https://en.wikipedia.org/wiki/Phenoxybenzamine

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 ...

https://en.wikipedia.org/wiki/Latrepirdine

... stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... Effects of depexamine may be suppressed by concomitant use with ß2-adrenergic and dopamine receptor antagonists requires ... It works by stimulating beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... Beta-adrenergic agonists, Cardiac stimulants, Catecholamines, D1-receptor agonists, D2-receptor agonists, Norepinephrine ...

https://en.wikipedia.org/wiki/Dopexamine

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 ...

https://en.wikipedia.org/wiki/List_of_skin_conditions

Primary insights from functional genomics and effects on beta-adrenergic responsiveness". The Journal of Biological Chemistry. ... "Agonist and antagonist activities on human NPFF(2) receptors of the NPY ligands GR231118 and BIBP3226". British Journal of ... "Receptor for the pain modulatory neuropeptides FF and AF is an orphan G protein-coupled receptor". The Journal of Biological ... Two genes encoding two different receptors (NPFF1 and NPFF2) and two precursors (NPFFA and NPFFB) have been cloned in several ...

https://en.wikipedia.org/wiki/Neuropeptide_FF

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 ...

https://en.wikipedia.org/wiki/Alpha-1_blocker

The alpha-adrenergic receptor has two subclasses α1 and α2. Alpha 2 receptors are associated with sympatholytic properties. ... 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 ... Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. ...

https://en.wikipedia.org/wiki/Alpha-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 ...

https://en.wikipedia.org/wiki/Iprindole

... an alpha-2 adrenergic agonist Irbesartan, an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker ... Vasopressin receptor antagonists, such as conivaptan Acetazolamide, a carbonic anhydrase inhibitor Lithium was previously used ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 19 (3): 759-762. doi:10.1111/j.1530-0277.1995.tb01579.x. ISSN 0145-6008. PMID 7573805. Fichman, M. P.; Kleeman, C. R.; Bethune ...

https://en.wikipedia.org/wiki/Primary_polydipsia

α2 adrenergic antagonists[citation needed] - mirtazapine, mianserin Mixed α1/β blockers - carvedilol α2 Adrenergic agonists - ... 5-HT2C receptor antagonists/inverse agonists - mirtazapine, olanzapine, quetiapine, amitriptyline, cyproheptadine, lurasidone ... Lang F, Perrier E, Pellet J. [Noradrenergic hypothesis in anorexia nervosa: prospective study using beta-stimulant therapy]. ... quetiapine Adrenergic antagonists: β blockers - propranolol, etc. Paradoxically, β-adrenergic agonists are also listed. Not ...

https://en.wikipedia.org/wiki/Appetite_stimulant

... beta-adrenoreceptor antagonists, angiotensin-converting enzyme inhibitors and angiotensin-2 receptor blockers. Doxazosin is ... It is a α1-selective adrenergic blocker in the quinazoline class of compounds. Doxazosin was patented in 1977 and came into ... 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, ...

https://en.wikipedia.org/wiki/Doxazosin

However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Frequent infusions of beta-lactam antibiotics without exceeding total daily dose would help to keep the antibiotics level above ... Stress ulcer prevention with proton-pump inhibitor (PPI) and H2 antagonist are useful in a person with risk factors of ... There are four families of PRRs: the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I- ...

https://en.wikipedia.org/wiki/Sepsis

... also known as β-Adrenergic receptor kinase 2 [BARK1]) and arrestin 2 (also known as Arrestin beta 1 [ARRB1]). These agents act ... Asapiprant (S-555739) and Laropiprant are selective receptor antagonists of DP1 whereas Vidupiprant is a receptor antagonist ... 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 ...

https://en.wikipedia.org/wiki/Prostaglandin_DP1_receptor

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 ... Increased level of norepinephrine increases the basal activity of alpha-2 adrenergic receptors, which mediate an analgesic ...

https://en.wikipedia.org/wiki/Amitriptyline

... angiotensin II receptor antagonists or adrenergic antagonists. Elevated lipid levels, including HDL, were found to increase ... Amyloid beta accumulation is often present in cognitively normal elderly people. Two reviews of 2018 and 2019 found potentially ... receptor antagonist; cholinesterase inhibitors galantamine, donepezil, rivastigmine; Studies have been proposed to evaluate ... Vlassenko AG, Mintun MA, Xiong C, Sheline YI, Goate AM, Benzinger TL, Morris JC (November 2011). "Amyloid-beta plaque growth in ...

https://en.wikipedia.org/wiki/Vascular_dementia

Stimulation of beta-adrenergic receptors during arousal and stress strengthens memory consolidation. Increased release of ... Likewise, post-training infusions of β-adrenoreceptor antagonists (beta-blocker) systemically or into the basolateral amygdala ... Propranolol is a blocker for the beta-adrenergic receptors in the amygdala which usually are bound to by stress hormones ... Wu, Yan; Li, Yonghui; Yang, Xiaoyan; Sui, Nan (January 2014). "Differential effect of beta-adrenergic receptor antagonism in ...

https://en.wikipedia.org/wiki/Traumatic_memories

... a new adrenergic beta receptor antagonist. Indian Journal of Medical Research. 1970 Feb; 58(2): 246-52. ... Cardiopulmonary actions of 1-isopropylamino-3-(3-tolyloxy)-2-propanol hydrochloride: a new adrenergic beta receptor antagonist. ... Cardiopulmonary actions of 1-isopropylamino-3-(3-tolyloxy)-2-propanol hydrochloride: ...

https://imsear.searo.who.int/handle/123456789/19092

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 ... Alpha-2 Adrenergic Agonists. Class Summary. Agents in this class may decrease vasomotor tone and heart rate by stimulating ...

https://www.medscape.com/answers/288154-99043/which-medications-in-the-drug-class-selective-serotonin-reuptake-inhibitors-are-used-in-the-treatment-of-posttraumatic-stress-disorder

Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 ... ali je naknadno utvrđeno da je takođe antagonist α1 receptora.[12] ... Entrez Gene: ADRB1 adrenergic, beta-1-, receptor". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView& ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...

https://sh.wikipedia.org/wiki/Beta-3_adrenergi%C4%8Dki_receptor

antagonist. Details. DB01363. Ephedra sinica root. nutraceutical. yes. agonist. Details. DB08893. Mirabegron. approved. yes. ... Beta-3 adrenergic receptor. P13945. Details. Drug Relations. Drug Relations. DrugBank ID. Name. Drug group. Pharmacological ... Beta-3 adrenergic receptor. Details. Name. Beta-3 adrenergic receptor. Kind. protein. Organism. Humans. Protein. Name. UniProt ...

https://go.drugbank.com/bio_entities/BE0001012

Bond RA, Clarke DE (1988) Agonist and antagonist characterization of a putative adrenoceptor with distinct pharmacological ... ADRB2: Adrenergic receptor beta 2; ADRB3: Adrenergic receptor beta 3. Table 1b: Genotype frequencies of ADRB2 and ADRB3 ... ADRB2: Adrenergic receptor beta 2; ADRB3: Adrenergic receptor beta 3. Table 2: Gastrointestinal symptoms, Gut motility and ... OCTT: Orocecal transit time, NS: not significant, ADRB2: Adrenergic receptor beta 2; ADRB3: Adrenergic receptor beta 3 ...

https://www.researchsquare.com/article/rs-550020/v1

Adrenergic beta-1 Receptor Antagonists [D27.505.519.625.050.200.200.100] Adrenergic beta-1 Receptor Antagonists ... Adrenergic. beta3 Adrenergic Antagonists. beta3-Adrenergic Antagonists. Tree number(s):. D27.505.519.625.050.200.200.300. ... Antagonists, Adrenergic beta-3 Antagonists, beta3-Adrenergic beta 3 Adrenergic Blocking Agents beta-3 Adrenergic Blocking ... Antagonists, Adrenergic beta-3. Antagonists, beta3-Adrenergic. beta 3 Adrenergic Blocking Agents. beta-3 Adrenergic Blocking ...

https://decs.bvsalud.org/en/ths/resource/?id=54147

Behavioral effects of beta adrenergic agonists and antidepressant drugs after down-regulation of beta-2 adrenergic receptors by ... Antagonism of the antidepressant-like effects of clenbuterol by central administration of beta-adrenergic antagonists in rats. ... Ordway GA, ODonnell JM, Frazer A. Effects of clenbuterol on central beta-1 and beta-2 adrenergic receptors of the rat. J ... ODonnell JM, Frith S, Wilkins J. Involvement of beta-1 and beta-2 adrenergic receptors in the antidepressant-like effects of ...

https://pharmacy.buffalo.edu/content/pharmacy/faculty-staff/faculty-profile.html?ubit=jod

Mineralocorticoid receptor antagonist.mp4. Mineralocorticoid receptor antagonist.pdf. Mineralocorticoid receptor antagonists. ... Impact of beta blockers therapy on right ventricular function in heart failure patients with reduced ejection fraction.pdf. ... Mineralocorticoid receptor antagonists.pdf. MITRA-FR trial facts and perspectives.mp4. MITRA-FR trial facts and perspectives. ... The cardiologist perspective on GLP-1 receptor agonist and DPP-4 inhibitors.mp4. The cardiologist perspective on GLP-1 receptor ...

https://coursemedicalshop.com/product/european-society-of-cardiology-heart-failure-2019/

https://www.staging.medscape.com/answers/288154-99040/which-medications-in-the-drug-class-alpha-2-adrenergic-agonists-are-used-in-the-treatment-of-posttraumatic-stress-disorder

Nielson, K.A., & Jensen, R.A. (1994). Beta-adrenergic receptor antagonist antihypertensive medications impair arousal-induced ... 3), 442-456; available online 10/3/2011, doi:10.1016/j.bbadis.2011.09.016. ...

https://www.marquette.edu/psychology/directory/kristy-nielson.php

Historically, the primary treatment for OAB involved a type of anticholinergics known as muscarinic receptor antagonists. ... In 2012, Astellas Pharma (TYO: 4503) won FDA approval for Myrbetriq (mirabegron), the first beta-3 adrenergic receptor agonist ... More recently, Urovant, a subsidiary of Sumitovant Biopharma Ltd., won FDA approval for Gemtesa (vibegron), another beta-3 ... adrenergic receptor agonist, which became commercially available in April. Anticholinergics used for OAB can have bothersome ...

https://www.medicaldesignsourcing.com/tags/dementia/

... a non-specific beta-adrenergic receptor antagonist) and allowed a minimum of 1 h for blood flow and fH to stabilize. Following ... Injection of the non-specific beta-adrenergic receptor antagonist propranolol (3 mg kg−1) significantly decreased both fH ( ... 4E), beta-adrenergic receptor-mediated systemic dilation as well as cardiac contractility likely contributed to the function. Q ... Injection of atropine revealed a post-beta-adrenergic receptor blockade cholinergic tone on fH of similar strength to the ...

https://journals.biologists.com/jeb/article/222/16/jeb205211/223427/Regulation-of-blood-flow-in-the-pulmonary-and

Propranolol, a non-specific β1-and β2-adrenergic receptor antagonist, was recently designated as the first therapeutic (orphan ... In order to overcome the β1-drawback, the properties of a high specific β2-adrenergic receptor blocker named ICI-118,551 have ... Minneman, K. P., Hegstrand, L. R. & Molinoff, P. B. The pharmacological specificity of beta-1 and beta-2 adrenergic receptors ... Cuesta, A.M., Albiñana, V., Gallardo-Vara, E. et al. The β2-adrenergic receptor antagonist ICI-118,551 blocks the ...

https://www.nature.com/articles/s41598-019-46448-6?error=cookies_not_supported&code=00eb8d82-b1b2-476a-a25f-2aaf2ed5ea8b

Beta-Adrenergic Antagonists. 1570 Words , 7 Pages. Alteration of the response to the Valsalva maneuver and amyl nitrite ... 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 ...

https://www.antiessays.com/free-essays/Stereoisomerism-438297.html

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 ...

https://www.jci.org/articles/view/106548

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 ...

https://www.frontiersin.org/articles/10.3389/fonc.2018.00162/full

The general beta receptor antagonists oxprenolol and dl-propranolol and the beta-2 receptor antagonist H35/25 inhibited Iso- ... The alpha receptor antagonists phentolamine and phenoxybenzamine, the beta-1 receptor antagonists metoprolol and practolol and ... The data demonstrate that cells of the rat gastric mucosa have adrenergic beta-2 receptors which when stimulated result in an ... the muscarinic receptor antagonist atropine were without effect. The histamine H2-receptor antagonist cimetidine inhibited Iso- ...

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Stimulation of the beta-2-adrenergic receptor with salbutamol activates human brown adipose tissue. ... men to compare the effects of single intravenous bolus of the ADRB2 agonist salbutamol without and with the ADRB1/2 antagonist ... While brown adipose tissue (BAT) is activated by the beta-3-adrenergic receptor (ADRB3) in rodents, in human brown adipocytes, ... At thermoneutrality, mRNA levels of four markers of the nucleotide-binding oligomerization domain (NOD)-like receptor (NLR)- ...

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Adrenergic beta-Antagonists) RN - 0 (Receptors, Adrenergic, beta-3) SB - IM CON - Cardiovasc Res. 2002 Dec;56(3):393-403. PMID ... Beta(1)-Adrenergic receptors couple exclusively to the G protein Gs, producing a widespread increase in cAMP levels in the cell ... Stimulation of beta-adrenergic receptors (ARs) results in an increased cyclic adenosine monophosphate (cAMP) production by ... Fourth, the I(f) current may be modulated by the beta-adrenergic cascade, although the coupling to the beta-adrenoceptor in the ...

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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 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)
Variable histologic parameters such as oxycodone (opiate), propranolol (beta-adrenergic blocker), clonidine (alpha-adrenergic antagonist), dantrolene (muscle relaxant), and bromocriptine or amantadine (dopamine-receptor agonists). (berea.edu)
Adenosine A2A and beta-2 adrenergic receptor agonists: novel selective and synergistic multiple myeloma targets discovered through systematic combination screening. (cell.com)
Long-acting beta 2 -adrenergic agonists (LABA) increase the risk of asthma-related death. (rxlist.com)

Beta-blockers such as propranolol are useful in controlling some symptoms of PTSD caused by hyperarousal. (medscape.com)
Propranolol is a nonselective beta-adrenergic receptor blocking agent. (medscape.com)
Propranolol, a non-specific β1-and β2-adrenergic receptor antagonist, was recently designated as the first therapeutic (orphan) drug for VHL disease. (nature.com)
Therefore, we performed a randomized double-blinded crossover trial in young lean men to compare the effects of single intravenous bolus of the ADRB2 agonist salbutamol without and with the ADRB1/2 antagonist propranolol on glucose uptake by BAT, assessed by dynamic 2-[18F]fluoro-2-deoxy-D-glucose positron emission tomography-computed tomography scan (i.e., primary outcome). (bvsalud.org)
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 mice with OIR, beta-adrenergic receptor (β-AR) blockade with propranolol has been shown to ameliorate different aspects of retinal dysfunction in response to hypoxia. (unipi.it)
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)
Age at burn (propranolol 12±4 years, control 12±3 years,p=0.893) and total body surface area burned (propranolol 44±15%,control 49±14%,p=0.090) were comparable between groups. (cdc.gov)

Behavioral effects of the β 3 adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs? (wikipedia.org)
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)
The biopharma Athira Pharma (Nasdaq: ATHA) has lengthened the current open-label extension (OLEX) study for its Phase 3 LIFT-AD and Phase 2 ACT-AD trials of fosgonimeton (ATH-1017, NDX-1017), hepatocyte growth factor receptor agonist, focused on mild-to-moderate Alzheimer's disease. (medicaldesignsourcing.com)
Urovant Sciences (Irvine, California) is upbeat about the prospects of beta-3 adrenergic receptor agonist Gemtesa (vibegron) in treating overactive bladder (OAB). (medicaldesignsourcing.com)
In 2012, Astellas Pharma (TYO: 4503) won FDA approval for Myrbetriq (mirabegron), the first beta-3 adrenergic receptor agonist for OAB to hit the market. (medicaldesignsourcing.com)
More recently, Urovant, a subsidiary of Sumitovant Biopharma Ltd., won FDA approval for Gemtesa (vibegron), another beta-3 adrenergic receptor agonist, which became commercially available in April. (medicaldesignsourcing.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)
5) the results focus on the interest in some beta 2-agonist drugs (zinterol, clenbuterol) as partial inductors of lipolysis, with the lipolytic efficacies. (sumnercountyhealthdepartment.org)
Beta 2 receptor agonist, salbutamol clenbuterol. (sumnercountyhealthdepartment.org)
Most of the stacks he offers combine a beta-1 specific antagonist like metoprolol with a beta-2 specific agonist like ephedrine or clenbuterol. (sumnercountyhealthdepartment.org)
Per se, b-2 adrenergic agonist activities can facilitate the lipolysis process [18], but clenbuterol may act as well on the adipocytes' b-3 adrenergic. (sumnercountyhealthdepartment.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)

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)
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 1 Adrenergic Blockers. (pharmapdf.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)
On the analysis of nine beta-blockers and the beta sympathomimetic clenbuterol. (sumnercountyhealthdepartment.org)
Determination of retinal protein kinase A activity is indicative of the fact that β-AR blockers are indeed effective at the receptor level. (unipi.it)
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)
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)

Discovery of the first selective M4 muscarinic acetylcholine receptor antagonists with in vivo antiparkinsonian and antidystonic efficacy. (sc.edu)
Role of non-selective adenosine receptor blockade and phosphodiesterase inhibition in cisplatin-induced nephrogonadal toxicity in rats. (shengsci.com)
It is less well known, but equally important, that loss of selective fat pads (or absence of adipose tissue altogether) is also associated with severe forms of insulin resistance ( 1 - 3 ). (diabetesjournals.org)

Nebulizer treatments should be at higher risk, and women can deliver high-energy or low-energy shocks, can be controlled with angiotensin-converting enzyme inhibitors and beta-adrenergic medications. (berea.edu)
Same adverse reactions found with systemic administration of beta-adrenergic receptor inhibitors may occur with topical ophthalmic administration. (nih.gov)
Beta-adrenergic receptor inhibitors may mask the signs and symptoms of acute hypoglycemia. (nih.gov)
Beta-adrenergic receptor inhibitors may mask certain clinical signs (e.g., tachycardia) or hyperthyroidism. (nih.gov)
Oral beta-adrenergic receptor inhibitors may have additive effects. (nih.gov)
For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and death due to cardiac failure, have been reported with topical application of beta-adrenergic receptor inhibitors. (nih.gov)

G-protein coupled receptors (GPCRs) have emerged as important factors in tumor growth and metastasis ( 1 ). (frontiersin.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)
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)
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)
Accumulating evidence has demonstrated that steroids can also trigger biological effects by directly binding G-protein-coupled receptors (GPCRs), yet physiological roles of such unconventional steroid signaling in controlling alcohol-induced behaviors remain unclear. (sdbonline.org)
G-protein-coupled receptors (GPCRs) for steroid hormones mediate unconventional steroid signaling. (sdbonline.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)

Beta-3 adrenergički receptor (β 3 adrenoreceptor), takođe poznat kao ADRB3 , je beta-adrenergički receptor . (wikipedia.org)
While brown adipose tissue (BAT) is activated by the beta-3-adrenergic receptor (ADRB3) in rodents, in human brown adipocytes, the ADRB2 is dominantly present and responsible for noradrenergic activation. (bvsalud.org)

Muscarinic receptors: from clinic to bench to clinic. (sc.edu)
Targeting muscarinic receptors to treat schizophrenia. (sc.edu)

European Journal of Pharmacology 573 (1-3): 139-47. (wikipedia.org)
Isolated parietal cells: adrenergic response and pharmacology. (aspetjournals.org)

We further investigated the effects of beta-adrenergic and cholinergic receptor blockade on blood flow and heart rate during these activities. (biologists.com)
Our results demonstrate that β(2) -AR blockade with ICI 118,551 decreases retinal levels of proangiogenic factors and reduces pathogenic neovascularization, whereas β(1) - and β(3) -AR antagonists do not. (unipi.it)
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)

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)
It could be concluded that beta adrenoceptor gene polymorphism has significant role on regulation of gut motility in T2DM. (researchsquare.com)
Floppy mitral valve/mitral valve prolapse syndrome: Beta-adrenergic receptor polymorphism may contribute to the pathogenesis of symptoms. (cdc.gov)

In order to overcome the β1-drawback, the properties of a high specific β2-adrenergic receptor blocker named ICI-118,551 have been studied. (nature.com)
A total of 2245 beta-blocker users were assigned to the study cohort, and another 8980 patients matched for age, sex, comorbidity, and medication use by inverse probability of treatment weighting formed the comparison cohort. (jmedscindmc.com)
The major outcome assessed was all-cause mortality during a 30-day follow-up period in major trauma patients with or without pretrauma beta-blocker use. (jmedscindmc.com)
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)

It is the first time that a beta-1-adrenoceptor antagonist (metoprolol). (sumnercountyhealthdepartment.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)

The constriction, in turn, was reduced or reversed by phentolamine, an alpha receptor antagonist. (jci.org)
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 unique dopamine/ecdysteroid receptor modulates ethanol-induced sedation in Drosophila . (sdbonline.org)
Co-Activation of metabotropic glutamate receptor 3 and beta-adrenergic receptors modulates cyclic-AMP, long-term potentiation, and disrupts memory reconsolidation. (sc.edu)

RNAi-mediated knockdown of DopEcR expression reveals that this receptor is necessary after eclosion, and is required in particular neuronal subsets, including cholinergic and peptidergic neurons, to mediate this behavior. (sdbonline.org)
Examining the role of muscarinic M5 receptors in VTA cholinergic modulation of depressive-like and anxiety-related behavior in rats. (sc.edu)

Historically, the primary treatment for OAB involved a type of anticholinergics known as muscarinic receptor antagonists. (medicaldesignsourcing.com)

American journal of nephrology 2022 3 53 (4): 316-324. (cdc.gov)
European heart journal 2022 3 43 (17): 1668-1680. (cdc.gov)

Our findings illustrate that surfacing is accompanied by an increase in heart rate that is primarily due to beta-adrenergic stimulation. (biologists.com)
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)
The direct effect of these two stimuli on coronary vessels is minimal and is mediated through stimulation of alpha (vasoconstrictor) receptors. (jci.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)

Steroids profoundly influence behavioral responses to alcohol by activating canonical nuclear hormone receptors and exerting allosteric effects on ion channels. (sdbonline.org)
A variety of hormones, neurotransmitters, and physical stimuli trigger intracellular responses by binding to seven transmembrane receptors. (aspetjournals.org)

The beta2AR structure differs from rhodopsin in having weaker interactions between the cytoplasmic ends of transmembrane (TM)3 and TM6, involving the conserved E/DRY sequences. (nih.gov)

BETOPTIC S is a beta-adrenergic receptor inhibitor indicated for the treatment of elevated intraocular pressure (IOP) in patients with chronic open-angle glaucoma or ocular hypertension. (nih.gov)

Formoterol fumarate dihydrate is a beta 2 -adrenergic bronchodilator. (rxlist.com)

Beta 1 receptor antagonist, atenelol metoprolol. (sumnercountyhealthdepartment.org)
Beta 3 receptor function, lipolysis Tell your doctor if you are breast-feeding, metoprolol clenbuterol lipolysis. (sumnercountyhealthdepartment.org)
3 week prohormone cycle, steroids on body Metoprolol clenbuterol lipolysis, order anabolic steroids online bodybuilding drugs. (sumnercountyhealthdepartment.org)

During a median follow-up of 3 years, the change in aortic size was similar between both groups (annual increase -0.08 in ARBs vs. -0.11 in BBs, p = 0.48). (acc.org)
Angiotensin II receptor antagonists or ARBs are typically used for patients who cannot tolerate ACEIs. (medscape.com)

Adrenergic receptor beta 2 (ADRB2) gene located on chromosome 5 having nine polymorphisms. (researchsquare.com)

These findings provide the first evidence for the involvement of nongenomic G-protein-coupled steroid receptors in the response to alcohol, and shed new light on the potential roles of steroids in alcohol-use disorders. (sdbonline.org)
We also use pharmacological tools and genetically modified mice to determine how modulation of specific G-protein coupled receptors can regulate these circuits. (sc.edu)

2 ] De Ponti and co-workers documented in a review article that adrenoceptors are located in various parts of the gut and modulators of these adrenoceptors could regulate the gut motility[ 3 ]. (researchsquare.com)
Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators. (sc.edu)
Antipsychotic-like effects of M4 positive allosteric modulators are mediated by CB2 receptor-dependent inhibition of dopamine release. (sc.edu)

Concomitant adrenergic psychotropic drugs may have additive effects. (nih.gov)

Benzodiazepines work by slowing down activity of the central nervous system by acting as a ligand for GABA(a) receptors mimicking the response of the release of GABA in the brain causing similar effects of calmness/ decreased agitation and mild sedation through decreased excitatbility and reduced communication between neurons. (antiessays.com)
It was also found that DopEcR may promote ethanol sedation by suppressing epidermal growth factor receptor /extracellular signal-regulated kinase signaling. (sdbonline.org)

Of beta-2-adrenoreceptors, which activates the sympathetic nervous system and triggers lipolysis. (sumnercountyhealthdepartment.org)
Increased cardiac sympathetic drive and reduced vagal modulation following endothelin receptor antagonism in healthy conscious rats. (shengsci.com)

Albuterol acts as a functional antagonist to relax the airway irrespective of ventolin spasmogen involved, thus protecting against all bronchoconstrictor challenges. (privelexperiences.com)

Approval was based on 2 phase 3 clinical trials (AK003 and AK004) that evaluated the safety and efficacy of tirbanibulin topical in adults (N=702) with facial or scalp actinic keratosis. (medscape.com)

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)

After completion of study treatment, patients are followed up for 3 years. (clinicaltrials.gov)
1. It is well documented that cisplatin (CDDP) treatment increases the expression of adenosine A(1) receptors in both kidney and testes. (shengsci.com)

The dopamine/ecdysteroid receptor (DopEcR) is a GPCR that mediates nongenomic actions of ecdysteroids, the major steroid hormones in insects. (sdbonline.org)

Diabetes increases the risk of developing heart failure by more than twofold in men and fivefold in women, with an estimated 25% of people with diabetes suffering chronic heart failure [ 3 ]. (springer.com)

1-3 Neuropsychiatric effects constitute up to 30% of ADEs and are associated with considerable morbidity and mortality. (uspharmacist.com)
AEGL-3: Life-threatening effects or death. (cdc.gov)

Anatomy7

Organisms9

Diseases2

Chemicals and Drugs208

Analytical, Diagnostic and Therapeutic Techniques and Equipment10

Psychiatry and Psychology2

Phenomena and Processes15

Disciplines and Occupations1

Information Science1

Health Care1

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

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

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

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

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

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

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

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

Interleukin 1 Receptor Antagonist Protein

Neurokinin-1 Receptor Antagonists

Purinergic P1 Receptor Antagonists

Histamine H2 Antagonists

Rats, Sprague-Dawley

Dose-Response Relationship, Drug

Piperidines

Serotonin 5-HT3 Receptor Antagonists

Excitatory Amino Acid Antagonists

Angiotensin Receptor Antagonists

Dopamine Antagonists

Interleukin-1beta

Serotonin 5-HT2 Receptor Antagonists

Adenosine A2 Receptor Antagonists

Hormone Antagonists

Adenosine A1 Receptor Antagonists

Purinergic P2 Receptor Antagonists

Narcotic Antagonists

Rats, Wistar

Histamine H1 Antagonists

Receptors, Endothelin

Muscarinic Antagonists

GABA-A Receptor Antagonists

Sialoglycoproteins

Serotonin Antagonists

Histamine Antagonists

GABA Antagonists

Leukotriene Antagonists

Receptor, Endothelin A

Receptors, Serotonin

Receptors, N-Methyl-D-Aspartate

Serotonin 5-HT1 Receptor Antagonists

Dizocilpine Maleate

Receptors, Adrenergic, beta

beta 2-Microglobulin

Biphenyl Compounds

Cells, Cultured

Receptors, Interleukin-1

Nicotinic Antagonists

Tetrazoles

Benzazepines

Adrenergic alpha-1 Receptor Antagonists

Interleukin-1

Xanthines

Pyridines

Radioligand Assay

Guinea Pigs

Serotonin Receptor Agonists

Peptides, Cyclic

Histamine H3 Antagonists

Adrenergic alpha-2 Receptor Antagonists

Indoles

Sulfonamides

Pyrazoles

Drug Interactions

Losartan

GABA-B Receptor Antagonists

Receptors, Bradykinin

RNA, Messenger

Substance P

Endothelin-1

Azepines

Receptors, Neurokinin-1

Cimetidine

Receptor, Endothelin B

Binding, Competitive

Adenosine A3 Receptor Antagonists

Serotonin

Integrin beta3

Purinergic P2X Receptor Antagonists

Time Factors

Devazepide

Receptors, Cholecystokinin

Neurons

Signal Transduction

Pyrrolidines

Behavior, Animal

Quinoxalines

Receptors, Vasopressin

Ketanserin