Interleukin 1 Receptor Antagonist Protein: 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.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Histamine H2 Antagonists: 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.Rats, Sprague-Dawley: 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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Piperidines: A family of hexahydropyridines.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Dopamine Antagonists: 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.Interleukin-1beta: 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.Serotonin 5-HT2 Receptor Antagonists: 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.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Hormone Antagonists: 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.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Histamine H1 Antagonists: 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.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.Muscarinic Antagonists: 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.GABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Sialoglycoproteins: 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.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Histamine Antagonists: 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.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Leukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.Receptor, Endothelin A: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.Receptors, Serotonin: 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.Receptors, N-Methyl-D-Aspartate: 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.Serotonin 5-HT1 Receptor Antagonists: 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.Dizocilpine Maleate: 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.Receptors, Adrenergic, beta: 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.beta 2-Microglobulin: 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.Biphenyl CompoundsCells, Cultured: 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.Receptors, Interleukin-1: 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.Nicotinic Antagonists: 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.TetrazolesBenzazepines: Compounds with BENZENE fused to AZEPINES.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Interleukin-1: 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.Xanthines: Purine bases found in body tissues and fluids and in some plants.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Guinea Pigs: 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.Serotonin Receptor Agonists: 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, Cyclic: 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).Histamine H3 Antagonists: Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Indoles: 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.Sulfonamides: A group of compounds that contain the structure SO2NH2.Pyrazoles: 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.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.Receptors, Bradykinin: 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, Messenger: 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.Substance P: 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.Endothelin-1: 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)Azepines: Seven membered heterocyclic rings containing a NITROGEN atom.Receptors, Neurokinin-1: 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.Cimetidine: 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.Receptor, Endothelin B: A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.Binding, Competitive: 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.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Serotonin: 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.Integrin beta3: 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.Purinergic P2X Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Devazepide: 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.Receptors, Cholecystokinin: 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.Neurons: 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.Signal Transduction: 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.PyrrolidinesBehavior, Animal: The observable response an animal makes to any situation.QuinoxalinesReceptors, Vasopressin: 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.Ketanserin: 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.Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.2-Amino-5-phosphonovalerate: 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.PiperazinesReceptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.Receptors, Thromboxane: 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.Receptors, Dopamine D2: 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.Naltrexone: 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.Disease Models, Animal: 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.Bradykinin: 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.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Famotidine: A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.Injections, Intraventricular: Injections into the cerebral ventricles.Adenosine: 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.Receptors, Neurokinin-2: 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.Adrenergic alpha-Antagonists: 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.Cannabinoid Receptor Antagonists: Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Oligopeptides: Peptides composed of between two and twelve amino acids.Transforming Growth Factor beta: 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.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.QuinuclidinesHistamine: 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.BenzodiazepinonesCell Line: Established cell cultures that have the potential to propagate indefinitely.Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.Mice, Inbred C57BLAdrenergic beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.Mineralocorticoid Receptor Antagonists: Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.Angiotensin II: 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.Receptors, Histamine H3: 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)Calcium: 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.Adrenergic beta-Antagonists: 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.QuinolinesReceptors, Opioid: 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.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Receptors, Purinergic P1: 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).Receptor, Bradykinin B2: 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.Pyrilamine: 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.PhenylpropionatesEndothelins: 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.Imidazoles: 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).Peptide Fragments: Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.Synaptic Transmission: 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.Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.Receptors, Corticotropin-Releasing Hormone: 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.N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).Receptors, Dopamine D1: 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.Isoindoles: Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.Receptors, Calcitonin Gene-Related Peptide: 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.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Receptor, Angiotensin, Type 1: 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.Antihypertensive Agents: 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.Receptors, Tachykinin: 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.Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Receptors, Opioid, mu: 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.Muscle Contraction: 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.Receptors, Angiotensin: Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.Receptor, Adenosine A2A: 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.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Dopamine: 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.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Naphthalenes: 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.Ondansetron: 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.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Memantine: AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.Proglumide: 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.Receptor, Serotonin, 5-HT2A: 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.Receptors, Opioid, kappa: 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.Brain: 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.Calcium Channel Blockers: A class of drugs that act by selective inhibition of calcium influx through cellular membranes.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Kinetics: The rate dynamics in chemical or physical systems.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.CHO Cells: 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.Dioxanes: 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)Receptors, Neurotransmitter: 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.Ligands: 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)Muscle, Smooth: 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)Granisetron: A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.Receptors, Adrenergic, beta-2: 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.Mice, Knockout: 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.Receptors, Serotonin, 5-HT3: 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.Tachykinins: 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.Neurokinin A: 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.Vasoconstriction: The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)Microinjections: The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.Ritanserin: 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.Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.Rabbits: 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.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Morphine: 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.Analysis of Variance: A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Receptor, Angiotensin, Type 2: 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.Receptors, Histamine H2: 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)Patch-Clamp Techniques: 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.Receptors, Neuropeptide Y: Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.Platelet Activating Factor: 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.Receptors, GABA-A: 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.Receptor, Adenosine A1: 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.Haloperidol: 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)MorpholinesCyclic AMP: 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.Electrophysiology: 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.Thromboxane A2: 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).TriazolesBornanes8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Norepinephrine: 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.Hippocampus: 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.Integrin alpha5beta1: 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.Histamine Agonists: 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.Receptor, Bradykinin B1: 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.Prostaglandin Antagonists: Compounds that inhibit the action of prostaglandins.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.6-Cyano-7-nitroquinoxaline-2,3-dione: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
(1/33) (+/-)-Pindolol acts as a partial agonist at atypical beta-adrenoceptors in the guinea pig duodenum.

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)

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

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)

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

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)

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

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)

(5/33) 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.

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)

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

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)

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

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)

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

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)

*  Beta-3 adrenergic receptor
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 ...
*  Beta-3 adrenergic antagonist
... adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics. 290 (2): 649-55. PMID 10411574. ... β3-adrenoceptor antagonist) is an adrenergic antagonist which blocks the Beta-3 adrenergic receptors of cells, with either high ... SR 59230A Carvedilol Betablocker Beta-3 adrenergic receptor Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, ... an antagonist for β3 and for β1 or β2 adrenoceptors) like the non-selective betablocker Carvedilol. ...
*  Adrenergic receptor
Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... Antagonists may be used primarily in hypertension, anxiety disorder, and panic attacks. The α2 receptor couples to the Gi/o ... Basic Neurochemistry: α- and β-Adrenergic Receptors Brief overview of functions of the β3 receptor Theory of receptor ... ISBN 0-443-06911-5. Alpha receptors illustrated The Adrenergic Receptors "Adrenoceptors". IUPHAR Database of Receptors and Ion ...
*  SR 59230A
"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 ...
*  Flestolol
... is a short-acting beta adrenergic receptor antagonist. Acylation of glycidol (2) with the acid chloride 1 produces ... 1. Novel .beta.-blockers with ultrashort duration of action". Journal of Medicinal Chemistry. 27 (8): 1007. doi:10.1021/ ... 81 (3): 309-22. PMID 8235065. Kam, Sheung Tsam; Matier, William L.; Mai, Khuong X.; Barcelon-Yang, Cynthia; Borgman, Robert J ... the ester 3. Reaction of that intermediate with amine 4, obtained by reaction of 1,1-dimethylethylenediamine with urea, gives ...
*  ICI-118,551
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist. ICI binds to the β2 subtype with at least 100 ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... as few other specific antagonists for this receptor are known. When dissolved in saline, the compound crosses the blood-brain ...
*  Beta-2 adrenergic receptor
... denotes selective antagonist to the receptor. Beta-2 adrenergic receptor has been shown to interact with: AKAP12, OPRD1, Grb2, ... 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 ...
*  Cocaine intoxication
"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): ...
*  Tolamolol
... is a beta adrenergic receptor antagonist. Curtis-Prior, PB; Gadd, AL (1990). "Beta-adrenoceptor antagonists and human ... 42 (3): 220-2. doi:10.1111/j.2042-7158.1990.tb05395.x. PMID 1974626. ...
*  Chlorprothixene
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Chlorprothixene is an antagonist of the following receptors: 5-HT2: antipsychotic effects, anxiolysis, weight gain D1, D2, D3: ... I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes". Methods Find ...
*  Beta-1 adrenergic receptor
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 adrenoreceptor), 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 ...
*  Spirendolol
... is a beta adrenergic receptor antagonist. Mostaghim, R; Maddox, YT; Ramwell, PW (1986). "Endothelial potentiation ... of relaxation response to beta adrenoceptor blocking agents". The Journal of Pharmacology and Experimental Therapeutics. 239 (3 ...
*  Sulfinalol
... is a beta adrenergic receptor antagonist. The methyl group on a sulfoxide is sufficiently acidic to substitute for ... "Studies on the mechanism of the acute antihypertensive and vasodilator actions of several beta-adrenoceptor antagonists". J. ... Bromination followed by condensation with 4-(4-methoxyphenyl)butan-2-amine (not PMA) gives the aminoketone 3. Successive ...
*  Beta-2 adrenergic antagonist
... 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 ...
*  Adimolol
... and β-adrenergic receptor antagonist. Alpha blocker Beta blocker Palluk R, Hoefke W, Gaida W, Mierau J, Bechtel WD (July 1986 ... "Interactions of MEN 935 (adimolol), a long acting beta- and alpha-adrenolytic antihypertensive agent, with postsynaptic alpha- ...
*  Toliprolol
... is a beta adrenergic receptor antagonist. Stephenson, KA; Wilson, AA; Meyer, JH; Houle, S; Vasdev, N (2008). "Facile ... Synthesis, radiolabeling, and ex vivo biodistribution of 18F-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol ...
*  History of hypertension
Black JW, Crowther AF, Shanks RG, Smith LH, Dornhorst AC (May 1964). "A new adrenergic beta receptor antagonist". Lancet. 1 ( ... February 1996). "Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy". J. Med. Chem ... The first member was verapamil, a derivative of papaverine that was initially thought to be a beta blocker and used for angina ... More recently angiotensin receptor blockers and renin inhibitors have also been introduced as antihypertensive agents. Esunge ...
*  History of catecholamine research
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 ...
*  Adrenergic antagonist
Alpha blocker Beta blocker Adrenergic Receptor Antagonist Sympathetic nervous system Propanolol Beta-blockers and the treatment ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group ... The α-adrenergic antagonists have different effects from the β-adrenergic antagonists. Adrenergic ligands are endogenous ...
*  Long-term potentiation
Straube T, Frey J (2003). "Involvement of beta-adrenergic receptors in protein synthesis-dependent late long-term potentiation ... "Selective impairment of learning and blockade of long-term potentiation by an N-methyl-D-aspartate receptor antagonist, AP5". ... 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 ...
*  Beta blocker
Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, ... β2 and β3 receptors. β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors are ... β3-adrenergic receptors are located in fat cells. Beta receptors are found on cells of the heart muscles, smooth muscles, ... Beta blockers, due to their antagonism at beta-1 adrenergic receptors, inhibit both the synthesis of new melatonin and its ...
*  GPCR oligomer
Limbird LE, Meyts PD, Lefkowitz RJ (June 1975). "Beta-adrenergic receptors: evidence for negative cooperativity". Biochem. ... "Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists". Science. 330 (6007): 1066-71. doi: ... and hetero-oligomerization of β2-adrenergic receptor in receptor trafficking, signaling pathways and receptor pharmacology". ... "The size of the mammalian lung beta 2-adrenergic receptor as determined by target size analysis and immunoaffinity ...
*  G protein-coupled receptor
"The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor into ... and neutral antagonists are ligands that do not affect the equilibrium. It is not yet known how exactly the active and inactive ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... Lohse MJ, Benovic JL, Codina J, Caron MG, Lefkowitz RJ (June 1990). "beta-Arrestin: a protein that regulates beta-adrenergic ...
*  Bronchospasm
Both of these medications activate alpha-1 adrenergic receptors that result in smooth muscle constriction. Non-selective beta ... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ... Beta blockers bind into the β2 receptors and block the action of epinephrine and norepinephrine from binding to its receptors, ... Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ...
*  Receptor theory
Optimal Agonist/Antagonist Combinations Maintain Receptor Response by Preventing Rapid β-adrenergic Receptor Desensitization , ... Quirke V (2006). "Putting theory into practice: James Black, receptor theory and the development of the beta-blockers at ICI, ... Whereas antagonists have no preference in their affinity for a receptor state. The fact that receptor conformation (state) ... Receptor theory is the application of receptor models to explain drug behavior. Pharmacological receptor models preceded ...
*  Bronchoconstriction
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 ... http://www.atsjournals.org/doi/abs/10.1164/rccm.201303-0437ST Rau, JL (Jul 2000). "Inhaled adrenergic bronchodilators: ... These smooth muscle cells have muscarinic M3 receptors on their membrane. The activation of these receptors by acetylcholine ...
Drug Information Portal - U.S. National Library of Medicine - Quick Access to Quality Drug Information  Drug Information Portal - U.S. National Library of Medicine - Quick Access to Quality Drug Information
Info Adrenergic Agents. * Info Adrenergic Antagonists. * Info Adrenergic beta-3 Receptor Antagonists ... 1 result for Category equals ADRENERGIC BETA-3 RECEPTOR ANTAGONISTS. Property. Value. ... 3-(2-Ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate View Synonyms. View Structure. ...
more infohttps://druginfo.nlm.nih.gov/drugportal/category/adrenergic%20beta-3%20receptor%20antagonists
Beta-3 adrenergic receptor - Wikipedia  Beta-3 adrenergic receptor - Wikipedia
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 ...
more infohttps://en.wikipedia.org/wiki/Beta-3_adrenergic_receptor
MP38-07: The effect of beta-3 adrenergic receptor a ... r pelvic ganglion disconnected rat bladder (VM - 2018) | AUA University  MP38-07: The effect of beta-3 adrenergic receptor a ... r pelvic ganglion disconnected rat bladder (VM - 2018) | AUA University
The effect of beta-3 adrenergic receptor agonist on micromotions of major pelvic ganglion disconnected rat bladder. View Poster ... Beta-3 adrenergic receptor agonist is known to alleviate rodent bladder microcontractions by inhibiting afferent pathway. ... MP38-07: The effect of beta-3 adrenergic receptor a ... r pelvic ganglion disconnected rat bladder (VM - 2018). Open/Close ... These results also suggest that the major action point of the beta 3 adrenergic receptor agonist is in the bladder. ...
more infohttps://auau.auanet.org/content/mp38-07-effect-beta-3-adrenergic-receptor-r-pelvic-ganglion-disconnected-rat-bladder-vm-2018
MP38-07: The effect of beta-3 adrenergic receptor a ... r pelvic ganglion disconnected rat bladder (AM - 2018) | AUA University  MP38-07: The effect of beta-3 adrenergic receptor a ... r pelvic ganglion disconnected rat bladder (AM - 2018) | AUA University
The effect of beta-3 adrenergic receptor agonist on micromotions of major pelvic ganglion disconnected rat bladder. View Poster ... Beta-3 adrenergic receptor agonist is known to alleviate rodent bladder microcontractions by inhibiting afferent pathway. ... MP38-07: The effect of beta-3 adrenergic receptor a ... r pelvic ganglion disconnected rat bladder (AM - 2018). Open/Close ... These results also suggest that the major action point of the beta 3 adrenergic receptor agonist is in the bladder. ...
more infohttps://auau.auanet.org/content/mp38-07-effect-beta-3-adrenergic-receptor-r-pelvic-ganglion-disconnected-rat-bladder-am-2018
Beta-3 Adrenoceptors as New Therapeutic Targets for Cardiovascular Pathologies | SpringerLink  Beta-3 Adrenoceptors as New Therapeutic Targets for Cardiovascular Pathologies | SpringerLink
... adrenergic receptor antagonists. J Pharmacol Exp Ther. 1999;290:649-55.PubMedGoogle Scholar ... Differential distribution of beta-adrenergic receptor subtypes in blood vessels of knockout mice lacking beta(1)- or beta(2)- ... Beta3-adrenergic receptor subtype signaling in senescent heart: nitric oxide intoxication or "endogenous" beta blockade for ... Functional beta-adrenergic receptor signalling on nuclear membranes in adult rat and mouse ventricular cardiomyocytes. ...
more infohttps://link.springer.com/article/10.1007%2Fs11897-011-0064-6
Beta-3 adrenergic antagonist - Wikipedia  Beta-3 adrenergic antagonist - Wikipedia
... adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics. 290 (2): 649-55. PMID 10411574. ... 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. ...
more infohttps://en.wikipedia.org/wiki/Beta-3_adrenergic_antagonist
beta.3 adrenergic receptor agonists and uses thereof - Patent # 6706743 - PatentGenius  beta.3 adrenergic receptor agonists and uses thereof - Patent # 6706743 - PatentGenius
... adrenergic receptor-mediated diseases, conditions, or disorders in a mammal which methods comprise administering to the mammal ... beta..sub.3 adrenergic receptor agonists of structural Formula (I), ##STR1##the stereoisomers and prodrugs thereof, and the ... pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R.sub.1, R.sub.2, R.sub.3, R.sub ... a glucocorticoid receptor agonist or antagonist, an orexin receptor antagonist, a urocortin binding protein antagonist, a ...
more infohttp://www.patentgenius.com/patent/6706743.html
β<sub>2</sub>-adrenoceptor | Adrenoceptors | IUPHAR/BPS Guide to...  β<sub>2</sub>-adrenoceptor | Adrenoceptors | IUPHAR/BPS Guide to...
Dual inhibition of beta-adrenergic and angiotensin II receptors by a single antagonist: a functional role for receptor-receptor ... 2002) Beta 1/beta 2-adrenergic receptor heterodimerization regulates beta 2-adrenergic receptor internalization and ERK ... 1988) Structural basis of beta-adrenergic receptor subtype specificity studied with chimeric beta 1/beta 2-adrenergic receptors ... beta-2 adrenergic receptor , beta-2 adrenoreceptor , Adrb-2 , beta 2-AR , Gpcr7 , adrenoceptor beta 2, surface , adrenergic ...
more infohttps://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=29&familyId=4&familyType=GPCR
Vibegron ビベグロン - Drug Approvals International  Vibegron ビベグロン - Drug Approvals International
β Adrenergic receptors (βAR) are present in detrusor smooth muscle of various species, including human, rat, guinea pig, rabbit ... Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists. US20110028481 *. Apr 2, 2009. Feb 3, 2011. Richard Berger. ... Cyclic amine phenyl beta-3 adrenergic receptor agonists. US20070185136. Feb 2, 2007. Aug 9, 2007. Sanofi-Aventis. Sulphonamide ... Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists. US20120202819 *. Sep 27, 2010. Aug 9, 2012. Merck Sharp & ...
more infohttp://drugapprovalsint.com/vibegron-%E3%83%93%E3%83%99%E3%82%B0%E3%83%AD%E3%83%B3/
Pharmacologic Effect for Female Overactive Bladder Syndrome: Mirabegron Versus Solifenacin - Full Text View - ClinicalTrials.gov  Pharmacologic Effect for Female Overactive Bladder Syndrome: Mirabegron Versus Solifenacin - Full Text View - ClinicalTrials.gov
Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Muscarinic Antagonists. Cholinergic Antagonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Comparisons of the Impact of Beta-3 Agonist Versus Antimuscarinics on Psychological Distress, Sexual Function, Bladder Wall ...
more infohttps://clinicaltrials.gov/ct2/show/NCT04023253?recrs=abc&cond=Pharmacology&rank=91
A Study to Evaluate the Efficacy, Safety, and Tolerability of Mirabegron in Men With OAB Symptoms While Taking Tamsulosin...  A Study to Evaluate the Efficacy, Safety, and Tolerability of Mirabegron in Men With OAB Symptoms While Taking Tamsulosin...
Adrenergic alpha-1 Receptor Antagonists. Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. ... Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. To Top ... At Visits 2, 3, 4, and 5, subjects will complete the IPSS, EQ-5D-5L, OAB-q, PPBC, and TS-VAS. Maximum urinary flow (Qmax) will ... Change from Baseline to Week 12 (End of Treatment) in mean number of micturitions per day based on a 3-day diary [ Time Frame: ...
more infohttps://clinicaltrials.gov/ct2/show/NCT02757768?term=178-MA-1008&rank=1
researchmarkets: November 2011  researchmarkets: November 2011
Pipeline candidates fall under major therapeutic classes such as transient receptor potential vanilloid (TRPV) antagonists, ... beta 3 adrenergic receptor antagonists and others.. - Analysis of the current and future competition in the global UI ... 3. The status quo of two market segments in China: internal combustion forklifts and electric forklifts; 4. The operations, ... 3)Analysis on the operation and developments of 19 solar cell conductive paste manufacturers in the world, including Dupont, ...
more infohttp://researchinmarket.blogspot.com/2011/11/
Refine your search  Refine your search
Adrenergic receptor antagonist (1) * Cardiac fibrosis (1) * Cardiac hypertrophy (1) * Deficient mice (1) ... Acute intravenous infusion of the beta-3 adrenergic receptor antagonist APD418 improves left ventricular function in dogs with ... Acute intravenous infusion of the beta-3 adrenergic receptor antagonist APD418 improves left ventricular function in dogs with ...
more infohttp://semsearch.escardio.org/esc-en/search/theme/esc?fq%5B%5D=feed%3Aall&fq%5B%5D=original_date%3A%5BNOW-1MONTH+TO+NOW%5D&fq%5B%5D=otca_concept_Complex%3ARapid+Fire&
Adrenergic Receptors  Adrenergic Receptors
... surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, ... adrenergic receptor. Science 245: 1118-1121. Hadcock JR and Malbon CC (1988) Down‐regulation of betaadrenergic receptors: ... Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. In: Hardman JG and Limbird L (eds) ... 1996) The betaadrenergic receptor is a substrate for the insulin receptor tyrosine kinase. Journal of Biological Chemistry 271 ...
more infohttp://www.els.net/WileyCDA/ElsArticle/refId-a0000005.html
Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog. |...  Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog. |...
Alpha- or beta-adrenergic antagonists did not attenuate the initial rise in PRA. The PRA increased again after 48 hours of ... Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog.. C R Ayers ... At the end of the chronic isoproterenol infusion period, beta-adrenergic receptor refractoriness was demonstrated, as PRA did ... Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog. ...
more infohttp://hyper.ahajournals.org/content/3/5/615
Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs? | BMC Pregnancy and Childbirth | Full Text  Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs? | BMC Pregnancy and Childbirth | Full Text
Beta-adrenergic receptors in human myometrium during pregnancy: changes in the number of receptors after beta-mimetic treatment ... Romero R, Sibai BM, Sanchez-Ramos L, et al: An oxytocin receptor antagonist (atosiban) in the treatment of preterm labor: a ... Adrenergic receptors in inner and outer layers of human myometrium near term: characterization of beta-adrenergic receptor ... Tsatsaris V, Papatsonis D, Goffinet F, Dekker G, Carbonne B: Tocolysis with nifedipine or beta-adrenergic agonists: a meta- ...
more infohttps://bmcpregnancychildbirth.biomedcentral.com/articles/10.1186/1471-2393-7-S1-S14
Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( 		               ...  Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( ...
For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor,antagonists,using,CypHer5E, ... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ...
more infohttp://www.bio-medicine.org/biology-technology/Screening-for-potential-beta-2-adrenergic-receptor-antagonists-using-CypHer5E-and-IN-Cell-Analyzer-1000-1255-1/
beta-1 Adrenergic Receptors
      - beta 1 Adrenergic Receptor
     Summary Report | CureHunter  beta-1 Adrenergic Receptors - beta 1 Adrenergic Receptor Summary Report | CureHunter
... beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist ... A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic ... beta-1; Adrenergic Receptor, beta-1; Receptor, Adrenergic, beta-1; Adrenergic Receptor, beta 1; Adrenergic Receptors, beta-1; ... Adrenergic beta 1 Receptors; Receptor, beta-1 Adrenergic; Receptors, Adrenergic beta-1; Receptors, beta 1 Adrenergic; beta 1 ...
more infohttp://www.curehunter.com/public/keywordSummaryD018342-beta-1-Adrenergic-Receptors-beta-1-Adrenergic-Receptor.do
Imidazoline .alpha.-adrenergic receptor antagonist compounds in combination     with nitric oxide donors, compositions and...  Imidazoline .alpha.-adrenergic receptor antagonist compounds in combination with nitric oxide donors, compositions and...
... adrenergic receptor antagonists, compositions comprising .alpha.-adrenergic receptor antagonists that are optionally ... 2-((.beta.-(4-Hydroxyphenyl) ethyl) t-butoxycarbonylaminomethyl)-1-tetralone. 2-((.beta.-(3-(4-Hydroxyphenyl) ethyl) ... adrenergic receptor antagonists: NO.sub.n -.alpha.-antagonists where n is 1 or 2. The .alpha.-adrenergic antagonists can be ... adrenergic receptor antagonists or the modifications of .alpha.-adrenergic receptor antagonists to be directly or indirectly ...
more infohttp://www.patentgenius.com/patent/6514934.html
  • Operating via heterotrimeric G proteins, adrenergic receptors constitute one of the most intensely studied classes of membrane proteins, whose expression and function are subject to regulation at many different levels, including transcriptional, posttranscriptional and posttranslational. (els.net)
  • Kohout TA and Lefkowitz RJ (2003) Regulation of G protein‐coupled receptor kinases and arrestins during receptor desensitization. (els.net)
  • Krupnick JG and Benovic JL (1998) The role of receptor kinases and receptors in G‐protein‐coupled receptor regulation. (els.net)
  • Shenoy SK, McDonal PH, Kohout TA and Lefkowitz RJ (2001) Regulation of receptor fate by ubiquitination of activated beta2‐adrenergic receptor and beta‐arrestin. (els.net)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs share many similarities in receptor phosphorylation, use of accessory proteins and sequestration of the receptors. (els.net)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (els.net)
  • 1996) The betaadrenergic receptor is a substrate for the insulin receptor tyrosine kinase. (els.net)
  • Description: Membrane radioligand displacement assay using [ 3 H]CGP12177 as tracer. (guidetopharmacology.org)
  • In this assay system, a CypHer5E-conjugated anti-VSV-G epitope antibody is incubated with a clonal stable HEK 293 cell line expressing N-terminally epitope tagged β2-adrenergic receptor. (bio-medicine.org)
  • Pindolol is a beta blocker initially synthesized by the pharmaceutical company Sandoz in the 1960s. (mentalhealthdaily.com)
  • Bupranolol is a competitive, nonselective beta-blocker similar to propanolol without intrinsic sympathomimetic activity. (drugbank.ca)
  • Among a subset of individuals with depression, it is theorized that low serotonin in the synaptic cleft leads to hypersensitivity of the postsynaptic receptor sites. (mentalhealthdaily.com)
  • Description: Measuring displacement of [ 3 H]-DHA from recombinant human β 2 adrenoceptors expressed in HEK293T cells. (guidetopharmacology.org)
  • Adding to its complex toxicity, cocaine targets muscarinic acetylcholine, N-methyl-D-aspartate (NMDA), sigma, and kappa-opioid receptors. (wikipedia.org)
  • After ß 3 -AR cloning in the late 1980s, convincing evidence for ß 3 -AR expression and function in cardiovascular tissues recently initiated a reexamination of their involvement in the pathophysiology of cardiovascular diseases. (springer.com)
  • Cocaine and its metabolites are completely eliminated from the body by 3 days. (wikipedia.org)