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.
Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.
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.
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.
A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS.
Drugs that selectively bind to and activate beta-adrenergic receptors.
Drugs that selectively bind to and activate alpha adrenergic receptors.
Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
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.
Drugs that bind to and activate adrenergic receptors.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
Drugs that bind to and activate dopamine receptors.
A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
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.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.
A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.
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.
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.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
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.
A highly selective and specific beta antagonist that is used to characterize beta-adrenoceptors.
The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS.
Hydrogenated alprenolol derivative where the extra hydrogens are often tritiated. This radiolabeled form of ALPRENOLOL, a beta-adrenergic blocker, is used to label the beta-adrenergic receptor for isolation and study.
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.
A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
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.
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS.
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.
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)
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.
Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.
A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
Established cell cultures that have the potential to propagate indefinitely.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.
Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
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 opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
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 group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
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.
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.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
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.
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)
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.
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 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.
Drugs that bind to and block the activation of ADRENERGIC BETA-3 RECEPTORS.
A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The rate dynamics in chemical or physical systems.
A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
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 short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.
Compounds with BENZENE fused to AZEPINES.
A selective D1 dopamine receptor agonist used primarily as a research tool.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
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.
An adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.
AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.
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.
A family of hexahydropyridines.
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.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
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.
Drugs that act on adrenergic receptors or affect the life cycle of adrenergic transmitters. Included here are adrenergic agonists and antagonists and agents that affect the synthesis, storage, uptake, metabolism, or release of adrenergic transmitters.
A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
A dopamine D2/D3 receptor agonist.
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.
G-protein-coupled receptor kinases that mediate agonist-dependent PHOSPHORYLATION and desensitization of BETA-ADRENERGIC RECEPTORS.
One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.
Drugs that bind to and activate excitatory amino acid receptors.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
A family of heterotrimeric GTP-binding protein alpha subunits that activate ADENYLYL CYCLASES.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
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.
Elements of limited time intervals, contributing to particular results or situations.
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).
A general class of ortho-dihydroxyphenylalkylamines derived from tyrosine.
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
A long-acting beta-2-adrenergic receptor agonist.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
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.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
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.
A family of heterotrimeric GTP-binding protein alpha subunits that were originally identified by their ability to inhibit ADENYLYL CYCLASES. Members of this family can couple to beta and gamma G-protein subunits that activate POTASSIUM CHANNELS. The Gi-Go part of the name is also spelled Gi/Go.
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.
A set of BACTERIAL ADHESINS and TOXINS, BIOLOGICAL produced by BORDETELLA organisms that determine the pathogenesis of BORDETELLA INFECTIONS, such as WHOOPING COUGH. They include filamentous hemagglutinin; FIMBRIAE PROTEINS; pertactin; PERTUSSIS TOXIN; ADENYLATE CYCLASE TOXIN; dermonecrotic toxin; tracheal cytotoxin; Bordetella LIPOPOLYSACCHARIDES; and tracheal colonization factor.
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.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
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 nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.
A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.
OXAZINES with a fused BENZENE ring.
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.
The observable response an animal makes to any situation.
Receptors of CLONIDINE and other IMIDAZOLINES. Activity of the ligands was earlier attributed to ADRENERGIC ALPHA-2 RECEPTORS. Endogenous ligands include AGMATINE, imidazoleacetic acid ribotide, and harman.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.
Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.
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.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.
An alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION.
An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.
Proteins prepared by recombinant DNA technology.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.
A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.
A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.
A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
Drugs that bind to and activate cholinergic receptors.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
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)
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
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.
A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.
Poisonous animal secretions forming fluid mixtures of many different enzymes, toxins, and other substances. These substances are produced in specialized glands and secreted through specialized delivery systems (nematocysts, spines, fangs, etc.) for disabling prey or predator.
Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Agents inhibiting the effect of narcotics on the central nervous system.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
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.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.
Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.
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 subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
An alpha-2 selective adrenergic agonist used as an antihypertensive agent.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
The physical activity of a human or an animal as a behavioral phenomenon.
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.
Refers to animals in the period of time just after birth.
A group of TETRAHYDRONAPHTHALENES containing a keto oxygen.
A negative regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.
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.
A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.
A series of structurally-related alkaloids that contain the ergoline backbone structure.
Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.
Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
The thoracolumbar division of the autonomic nervous system. Sympathetic preganglionic fibers originate in neurons of the intermediolateral column of the spinal cord and project to the paravertebral and prevertebral ganglia, which in turn project to target organs. The sympathetic nervous system mediates the body's response to stressful situations, i.e., the fight or flight reactions. It often acts reciprocally to the parasympathetic system.
Injections into the cerebral ventricles.
A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.
January 2016). "Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive ... Vibegron is the international nonproprietary name (INN). Vibegron is a selective agonist for the beta-3 adrenergic receptor (β3 ... receptor. The receptors are located in the kidneys, urinary tract and bladder tissue. Upon binding, the β3 receptor undergoes a ... The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment ...
It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific ... "Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes". Canadian Journal of Physiology and ... a new β-adrenergic blocking agent]. Folia Pharmacologica Japonica (English abstract) (in Japanese). 75 (7): 707-720. doi: ... Takahashi H, Yoshida T, Nishimura M, Nakanishi T, Kondo M, Yoshimura M (September 1992). "Beta-3 adrenergic agonist, BRL-26830A ...
It works by activating the β3 adrenergic receptor in the bladder, resulting in its relaxation. Mirabegron is the first ... clinically available beta-3 agonist with approval for use in adults with overactive bladder. Mirabegron was approved for ...
... is a drug which acts as a selective agonist of the β3 adrenergic receptor, which has been investigated for various ... and beta-subtypes". British Journal of Pharmacology. 95 (3): 723-34. doi:10.1111/j.1476-5381.1988.tb11698.x. PMC 1854239. PMID ... Afeli SA, Rovner ES, Petkov GV (September 2013). "BRL37344, a β3-adrenergic receptor agonist, decreases nerve-evoked ... September 2018). "β3-adrenergic receptor activation induces TGFβ1 expression in cardiomyocytes via the PKG/JNK/c-Jun pathway". ...
For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta ... Sawa M, Harada H (2006). "Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists". Current ... Nebivolol while selectively blocking beta(1) receptor acts as a beta(3)-agonist. β3 receptors are found in the gallbladder, ... It works by blocking β1-adrenergic receptors in the heart and dilating blood vessels. Nebivolol was patented in 1983 and came ...
"Role of phosphorylation in agonist-promoted beta 2-adrenergic receptor sequestration. Rescue of a sequestration-defective ... beta-adrenergic-receptor] kinase, beta-adrenergic receptor-specific kinase, beta-AR kinase, beta-ARK, beta-ARK 1, beta-ARK 2, ... beta-adrenergic receptor] Thus, the two substrates of this enzyme are ATP and beta-adrenergic receptor, whereas its two ... beta-adrenergic receptor] phosphotransferase. Other names in common use include ATP:beta-adrenergic-receptor phosphotransferase ...
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) is an adrenergic antagonist which blocks the beta-2 adrenergic ... Fitzgerald, JD; Wale, JL (1983). "The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)". J Cardiovasc ... receptors of cells, with either high specificity (an antagonist which is selective for β2 adrenoceptors) like Butaxamine and ...
Clenbuterol remains banned not as a beta-agonist, but rather an anabolic agent. Heart muscle contraction Increase cardiac ... 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 ...
"Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 ... 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 ...
... (code name GW-427,353) is a drug which acts as a selective agonist for the β3 adrenergic receptor. It is being ... 2008). "Randomized, double-blind, placebo (PLA)-controlled, crossover study to evaluate efficacy and safety of the beta 3- ... May 2008). "Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel ... October 2007). "GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and ...
"Three-dimensional models for beta-adrenergic receptor complexes with agonists and antagonists". Journal of Medicinal Chemistry ... Beta-adrenergic agonist Beta2-adrenergic agonist "Betmiga , European Medicines Agency". www.ema.europa.eu. Retrieved 2018-10-02 ... adrenergic receptor agonist or β3-adrenoceptor agonist, also known as β3-AR agonist, are a class of medicine that bind ... In 1984 the β3 receptor was described as the third group of beta receptors in adipose tissue. This led to the development of ...
"The beta-adrenergic receptors". PMID 12439640. Yoo, B.; et al. "Beta1-adrenergic receptors stimulate cardiac contractility and ... In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands ... Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways ... Most agonists of the beta receptors are selective for one or more beta-adrenoreceptors. For example, patients with low heart ...
Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel function, and ... Solabegron relaksira glatke mišiće bešike putem stimulacije beta-3 adrenoceptora. To je nov mehanizam u poređenju sa trenutno ... GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases ... Solabegron (GW-427,353) je lek koji deluje kao selektivni agonist za β3 adrenergički receptor. On je u razvoju za tretman ...
... is a cytosolic protein and acts as a cofactor in the beta-adrenergic receptor kinase (BARK) mediated ... Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G protein- ... 1990). "beta-Arrestin: a protein that regulates beta-adrenergic receptor function". Science. 248 (4962): 1547-50. doi:10.1126/ ... 2000). "The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor ...
"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 or beta blocker. ICI binds to the β2 subtype with ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... Branca C, Wisely EV, Hartman LK, Caccamo A, Oddo S (December 2014). "Administration of a selective β2 adrenergic receptor ...
... , like arrestin beta 1, was shown to inhibit beta-adrenergic receptor function in vitro. It is expressed at high ... The protein may interact with the agonist DOI in 5-HT2A receptor signaling. Arrestin beta 2 is crucial for the development of ... "Regulation of receptor fate by ubiquitination of activated beta 2-adrenergic receptor and beta-arrestin". Science. 294 (5545): ... Lefkowitz RJ (July 1998). "G protein-coupled receptors. III. New roles for receptor kinases and beta-arrestins in receptor ...
β adrenergic receptor antagonists (also called beta-blockers or β-blockers) were initially developed in the 1960s, for the ... partial adrenergic agonist activity (pindolol), concomitant α-adrenergic blocking activity (for example labetalol and ... β-blockers can be selective for either β1, β2 adrenergic receptor, or to be non-selective. By blocking β1 receptor it is ... β1-receptors are located in the heart and consist of about 75% of all β-receptors. β2-receptors can be found in the smooth ...
... is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... In particular, it is a partial agonist at beta2- receptors located in the vascular smooth muscle. Labetalol relaxes vascular ... 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 ...
Beta2-adrenergic agonist Alpha-adrenergic agonist Asthma Beta blocker Beta-1 adrenergic receptor Beta-2 adrenergic receptor ... β1 receptors make up to 75% of all beta receptors and are predominantly located in the heart. β2 receptors are found in ... CS1 maint: discouraged parameter (link) Johnson, M (2006). "Molecular mechanisms of beta(2)-adrenergic receptor function, ... It also influences the specificity for the β-receptor subtypes. Direct-acting analog binds the β-adrenergic receptors directly ...
... where it serves as a full agonist to murine TAAR1 (not necessarily human). It is also an agonist to beta-adrenergic receptors. ... it is a phenol-based TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors. It is most ... In October 2006, Taiwan banned ractopamine along with other beta-adrenergic agonists. In a 2012 climb-down, its legislature ... "Beta-agonists hog the limelight". The Star. November 5, 2006. Archived from the original on June 29, 2011. Retrieved January 25 ...
... mesylate (Tornalate) is a short-acting β2 adrenergic receptor agonist used for the relief of bronchospasm in ... Walker, Susannah B.; Kradjan, Wayne A.; Bierman, C. Warren (6 May 1985). "Bitolterol Mesylate: A Beta-adrenergic Agent; ... 5 (3): 127-137. doi:10.1002/j.1875-9114.1985.tb03410.x. PMID 3895171. "ChEBI: Bitolterol". Chemical Entities of Biological ...
... but also many medications like beta blockers, β2 agonists and α2 agonists, which are used to treat high blood pressure and ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 There is no α1C receptor. There was a subtype known as C, but ... and β-Adrenergic Receptors Theory of receptor activation Desensitization of β1 receptors. ... Sep 2010). "Ghrelin secretion stimulated by {beta}1-adrenergic receptors in cultured ghrelinoma cells and in fasted mice". ...
1989). "Beta 1- and beta 2-adrenergic receptor-mediated adenylate cyclase stimulation in nonfailing and failing human ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation.". J. Biol. Chem. 263 (9): ... Beta-2 adrenergički receptor (β2 adrenoreceptor), takođe poznat kao ADRB2, je beta-adrenergički receptor.[3] ... Frielle T, Caron MG, Lefkowitz RJ (1989). "Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by ...
... are capable of exerting low-level agonist activity at the β-adrenergic receptor while simultaneously acting as a receptor site ... beta-blockers, β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor ... Beta blockers must not be used in the treatment of selective alpha-adrenergic agonist overdose. The blockade of only beta ... Beta blockers, due to their antagonism at beta-1 adrenergic receptors, inhibit both the synthesis of new melatonin and its ...
January 2011). "The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329 ... "The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor into ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, 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 ...
... a protein that regulates beta-adrenergic receptor function". Science. 248 (4962): 1547-50. doi:10.1126/science.2163110. PMID ... "Core engagement with β-arrestin is dispensable for agonist-induced vasopressin receptor endocytosis and ERK activation". ... Lefkowitz RJ, Shenoy SK (April 2005). "Transduction of receptor signals by beta-arrestins". Science. 308 (5721): 512-7. doi: ... Increased accessibility of these sites in receptor-bound arrestin targets the arrestin-receptor complex to the coated pit. ...
"Assessment of compliance in children using inhaled beta adrenergic agonists". Ann Allergy. 62 (5): 406-9. PMID 2566291. Herpes ... The Herpes Simplex Virus JMP Mutant Enters Receptor-Negative J Cells through a Novel Pathway Independent of the Known Receptors ... Herpes Simplex Virus Glycoproteins gH/gL and gB Bind Toll-Like Receptor 2, and Soluble gH/gL Is Sufficient To Activate NF-κB ... She also discovered the triggering activity of receptor- bound gD. In addition to these major discoveries, she identified the ...
"Nedd4 mediates agonist-dependent ubiquitination, lysosomal targeting, and degradation of the beta2-adrenergic receptor". The ... "Beta-arrestin 2 functions as a G-protein-coupled receptor-activated regulator of oncoprotein Mdm2". The Journal of Biological ... receptor serine/threonine kinase binding. • peroxisome proliferator activated receptor binding. • ubiquitin binding. ... "Identification of c-Cbl as a new ligase for insulin-like growth factor-I receptor with distinct roles from Mdm2 in receptor ...
Limbird LE, Meyts PD, Lefkowitz RJ (June 1975). "Beta-adrenergic receptors: evidence for negative cooperativity". Biochem. ... "A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers". Proc. Natl. Acad. Sci. U.S.A. ... 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 ...
... adrenergic receptor-mediated diseases, conditions, or disorders in a mammal which methods comprise administering to the mammal ... R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, X, and Y, are as defined herein.The invention further provides ... beta..sub.3 adrenergic receptor agonists of structural Formula (I), ##STR1##the stereoisomers and prodrugs thereof, and the ... beta..sub.1 and .beta..sub.2 Receptor Selectivity. In vivo selectivity for .beta..sub.1 and .beta..sub.2 receptors may be ...
The elevation of TH activity elicited in SCG by beta adrenergic receptor agonists is always preceded by an increase of cAMP ... Induction of tyrosine hydroxylase elicited by beta adrenergic receptor agonists in normal and decentralized sympathetic ganglia ... Induction of tyrosine hydroxylase elicited by beta adrenergic receptor agonists in normal and decentralized sympathetic ganglia ... Induction of tyrosine hydroxylase elicited by beta adrenergic receptor agonists in normal and decentralized sympathetic ganglia ...
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level relative to isoproterenol. ...
The Physiological Responses and Adaptation of Brown Adipose Tissue to Chronic Treatment With Beta-3-Adrenergic Receptor ... Agonists Next Previous Table of Contents * At a glance * Trial Overview * Purpose ... The Physiological Responses and Adaptation of Brown Adipose Tissue to Chronic Treatment With Beta-3-Adrenergic Receptor ...
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. ... These results also suggest that the major action point of the beta 3 adrenergic receptor agonist is in the bladder. ... We have investigated the effect of beta-3 adrenergic receptor agonist (CL-316,243) on micromotion of major pelvic ganglion ...
Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Comparisons of the Impact of Beta-3 Agonist Versus Antimuscarinics on Psychological Distress, Sexual Function, Bladder Wall ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... History of smoking more than 10 cigarettes (or equivalent amount of tobacco) per day within 3 months prior to admission to the ... Johns wort) in the 2 weeks prior to admission to the Clinical Unit, except for paracetamol (up to 3 g/day) ... Any use of drugs of abuse within 3 months prior to admission to the clinical unit ...
Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Regular use of any inducer of liver metabolism (e.g. barbiturates, rifampin) in the 3 months prior to admission to the Clinical ... History of smoking more than 10 cigarettes (or equivalent amount of tobacco) per day within 3 months prior to admission to the ... Male subject must agree to sexual abstinence and/or use a highly effective method of birth control from screening until 3 ...
... cholinergic agonists, anticancer drugs, immunosuppressive agents, antiviral agents, antibiotic agents, appetite suppressants, ... 60/22.5/10/2.5/2.5/2.5 25 3 5.52 1.38 EtOH/H.sub.2 O/Gly/GDO/ML/OA4. 60/22.5/10/2.5/2.5/2.5 75 8 3.35 2.18 EtOH/H.sub.2 O/Gly/ ... 60/28/10/1/1 30 3 13.03 3.35 EtOH/H.sub.2 O/Gly/GMO/ML3. 60/28/10/1/1 25 3 12.98 2.06 EtOH/H.sub.2 O/Gly/GMO/ML4. 60/28/10/1/1 ... 40/54/5/1 40 5 38.8 18.9 EtOH/H.sub.2 O/Gly/GMO 20 12 17.5 5.1 10 6 10.1 3.3 5 3 8.0 1.43. 30/63/5/2 40 6 23.9 10.0 EtOH/H.sub. ...
These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?) and What is the role of beta-adrenergic ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?. Updated: Sep 23, 2019 ...
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.. Parmee ER, Naylor EM, Perkins L, ... Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.. Weber AE, Mathvink RJ, Perkins L, ... Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.. Naylor EM, Parmee ER ... Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.. Brockunier LL, Candelore ...
Adrenergic beta-3 Receptor Antagonists* * Adrenergic beta-Antagonists / administration & dosage* * Adult * Body Weight / drug ... Objective: Our objective was to test the safety and metabolic effects of a novel beta(3)-adrenoreceptor agonist (TAK-677) in ... Lack of an effect of a novel beta3-adrenoceptor agonist, TAK-677, on energy metabolism in obese individuals: a double-blind, ... 3-((2R)-(((2R)-3-chlorophenyl)-2-hydroxyethyl)amino)propyl)-1H-indol-7-yloxy)acetic acid ...
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); DRB57K47QC (Celiprolol); Y41JS2NL6U (Bisoprolol). ... Dopamine receptor agonists.iii. Dopamine receptor antagonists.iv. Dopamine-depletor drugs.v. Drugs that increase the production ... 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); 0 (Cytokines); 0 (Interleukin-6); 0 (Lipids); ... 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Vasodilator Agents); 268B43MJ25 (Uric Acid); 2TN51YD919 (Hypoxanthine); ...
We recently described an important role played by the TGF-beta/Smad3 signaling pathway in modulating the appearance of brown ... We recently described an important role played by the TGF-beta/Smad3 signaling pathway in modulating the appearance of brown ... A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent. J. ... beta3-adrenergic receptors mediate CL 316,243 agonist-induced effects on energy expenditure, insulin secretion, and food intake ...
January 2016). "Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive ... Vibegron is the international nonproprietary name (INN). Vibegron is a selective agonist for the beta-3 adrenergic receptor (β3 ... receptor. The receptors are located in the kidneys, urinary tract and bladder tissue. Upon binding, the β3 receptor undergoes a ... The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment ...
Among the most significant are chemokine receptors, β-adrenergic receptors, and angiotensin II AT1 receptors (13-16). ... 2002) Beta(1)/beta(2)/beta(3)-adrenoceptor knockout mice are obese and cold-sensitive but have normal lipolytic responses to ... 2001) Agonist-dependent recruitment of phosphoinositide 3-kinase to the membrane by beta-adrenergic receptor kinase 1. A role ... including chemokine receptors, β-adrenergic signaling, and angiotensin II receptors (13-17). On activation, PI3Kγ controls two ...
"The beta-adrenergic receptors". PMID 12439640. Yoo, B.; et al. "Beta1-adrenergic receptors stimulate cardiac contractility and ... In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands ... Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways ... Most agonists of the beta receptors are selective for one or more beta-adrenoreceptors. For example, patients with low heart ...
... is a drug which acts as a selective agonist for the β3 adrenergic receptor. It is being developed for the treatment of ... Agonist. General Function. Protein homodimerization activity. Specific Function. Beta-adrenergic receptors mediate the ... Solabegron (GW-427,353) is a drug which acts as a selective agonist for the β3 adrenergic receptor. It is being developed for ... selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. J ...
Beta-adrenergic agonists. These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder ... Alpha-adrenergic agonists. Alpha agonists, such as midodrine (Pro-Amatine) or pseudoephedrine (Sudafed), may improve symptoms ... They possess both a central and peripheral anticholinergic effect, as well as being alpha-adrenergic agonists and central ... Mirabegron (Myrbetriq), a beta-3 adrenergic receptor agonist, causes relaxation of the detrusor miuscle and increases bladder ...
Rasmussen, H., Figtree, G., Krum, H., Bundgaard, H. (2009). The use of beta3-adrenergic receptor agonists in the treatment of ... Beta 3 adrenergic receptor stimulation as a novel treatment for limb and wound complications associated with Type 2 diabetes; ... Rasmussen, H., Figtree, G., Krum, H., Bundgaard, H. (2009). The use of beta3-adrenergic receptor agonists in the treatment of ... No association of G-protein-coupled receptor kinase 5 or β-adrenergic receptor polymorphisms with Takotsubo cardiomyopathy in a ...
Iii beta-3 adrenergic receptor agonist. In practice, the physician during pregnancy. Anaesth intensive care unit to deliver ... Pegfilgrastim is filgrastim conjugated to polyethylene glycol epoetin beta is an acceptable treatment option for patients with ...
... of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides p... ... PHENYL AMINO SQUARATE AND THIADIAZOLE DIOXIDE BETA-3 ADRENERGIC RECEPTOR AGONISTS. This invention provides compounds of Formula ... The present invention provides non-steroidal compounds of formula (I) which are selective modulators (i.e., agonists and ... IL-8 RECEPTOR ANTAGONISTS. This invention relates to the novel use of dianilino squarates in the treatment of disease states ...
Adrenergic Agonists. Phase 4. 18. Adrenergic beta-3 Receptor Agonists. Phase 4. ... Selective Estrogen Receptor Modulators. Phase 2. 38. Testosterone 17 beta-cypionate. Phase 2. ... 17-Hydroxy-(17-beta)-androst-4-en-3-one. 17-Hydroxy-10,13-dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro- ... 3. INS p.Arg46Gln. VAR_063729 rs121908260 ClinVar genetic disease variations for Maturity-Onset Diabetes of the Young, Type 10: ...
Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, ... The pharmacokinetics of a thiazole benzenesulfonamide beta 3-adrenergic receptor agonist and its analogs in rats, dogs, and ... Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role ... Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4- ...
... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... expressing cells (2). For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor, ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... and orphan receptors References 1. Application Note: Screening for 2-adrenergic receptor agonists using the pH-sensitive dye, ...
A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. J. Clin. Invest. 101(11): 2387- ... Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. Bioorg. Med. Chem. Lett. 8(9): 1107-1112. PMID ... L-755,507 is also a very potent and selective β3-AR adrenergic receptor partial agonist, selective over both β1-AR and β2-AR ... Synonym: 4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]- ...
... beta-adrenergic hormones, retinoids, PPARγ and PPARα agonists, and the liver X receptor.. Exercise and peroxisome proliferator- ... Liver X Receptor Beta (LXRβ). The Kuding in LipoMorph suppresses lipogenesis through antagonism of LXRβ.. * Beta- ... Unlike other beta adrenergic receptors, which are widely distributed about the body, being found in cardiac tissue, skeletal ... Retinoic acid is necessary for induction of human UCP1 by beta-adrenergic agonists. [28] ...
... surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, ... Hadcock JR and Malbon CC (1988) Down‐regulation of betaadrenergic receptors: agonist‐induced reduction in receptor mRNA levels ... Shumay E, Gavi S, Wang HY and Malbon CC (2004) Trafficking of beta2‐adrenergic receptors: insulin and betaagonists regulate ... 1996) The betaadrenergic receptor is a substrate for the insulin receptor tyrosine kinase. Journal of Biological Chemistry 271 ...
A novel combination comprising a .beta.-hairpin peptidomimetic of the formula cyclo(-Thr-Trp-Ile-Dab-Orn-.sup.DDab-Dab-Trp-Dab- ... Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart.... This ... Methods and compositions comprising desmopressin in combination with a beta-3-adrenergic receptor agonist. The invention ... in combination with a beta-3-adrenergic receptor agonist. The methods and compositions... ...
Methods and compositions comprising desmopressin in combination with alpha-adrenergic receptor antagonist ... Methods and compositions comprising desmopressin in combination with a beta-3 adrenergic receptor agonist ... 7-benzyl-4-(2-methylbenzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1h)-one, salts thereof and methods of ... 7-Benzyl-4- (2-methylbenzyl) -2,4,6,7,8,9- hexahydroimidazo [1,2-a] pyrido [3,4-e] pyrimidine -5 (1h) - on, its analogs, and ...
  • CL-316,243 group, beta-3 adrenergic receptor antagonist (SR59230A) pretreated CL-316,243 group and oxybutinin group. (auanet.org)
  • CypHer5 has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor expressing cells (2). (bio-medicine.org)
  • This application note describes the validation of antagonist-format CypHer5E receptor internalization assays for high-throughput screening. (bio-medicine.org)
  • A β2adrenergic receptor antagonist screen was performed using the LOPAC ™ compound library, which consists of 640 well-characterized, pharmaceutically diverse compounds with known drug or drug-like activity. (bio-medicine.org)
  • The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 was able to identify all specific β2-adrenergic receptor antagonists and additional structurally related compounds present in the LOPAC compound library. (bio-medicine.org)
  • Agonist and antagonist controls were placed symmetrically in columns 1 and 12 of each plate. (bio-medicine.org)
  • Twelve replicate wells contained a known agonist, isoproterenol, and four replicate wells contai ned a known antagonist, alprenolol, each diluted in 0.01% DMSO. (bio-medicine.org)
  • Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein. (nih.gov)
  • Oxilorphan (l-N-cyclopropylmethyl-3,14-dihydroxymorphinan): a new synthetic narcotic antagonist. (aspetjournals.org)
  • Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood-brain barrier, has not been investigated for this purpose. (frontiersin.org)
  • Propranolol is a non-selective beta-adrenergic antagonist that has good penetration of the blood-brain barrier ( 21 ). (frontiersin.org)
  • Here we report the raising of a mouse monoclonal antibody against human A(2A)AR that prevents agonist but not antagonist binding to the extracellular ligand-binding pocket, and describe the structure of A(2A)AR in complex with the antibody Fab fragment (Fab2838). (proteopedia.org)
  • Potent, selective β 3 adrenoceptor antagonist (IC 50 values are 40, 408 and 648 nM for β 3, β 1 and β 2 , respectively). (abcam.com)
  • Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes. (abcam.com)
  • The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. (curehunter.com)
  • Tamoxifen (Nolvadex, Istubal, Valodex) is an antagonist of estrogen receptors in breast tissue and is an agonist in the endometrium. (healthcmi.com)
  • epinephrine is a direct acting catecholamine and adrenergic agonist or antagonist? (brainscape.com)
  • montelukast, a cysteinyl leukotriene (CysLT)-receptor antagonist, is an alternative. (dentalcare.com)
  • low-dose inhaled corticosteroid plus montelukast, a cysteinyl leukotriene (CysLT)-receptor antagonist, is an alternative regimen. (dentalcare.com)
  • To identify directly and to quantitate these beta-adenergic receptors in human lymphocytes, (-) [3H] alprenolol, a potent beta-adrenergic antagonist, was used to label binding sites in homogenates of human mononuclear leukocytes. (duke.edu)
  • The beta-adrenergic antagonist, (-) propranolol, potently competed for the binding sites, causing half-maximal inhibition of binding at 9 nM. (duke.edu)
  • Ardayfio PA et al (2008) The 5-hydroxytryptamine2A receptor antagonist R-(+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl-4-piperidinemethanol (M100907) attenuates impulsivity after both drug-induced disruption (dizocilpine) and enhancement (antidepressant drugs) of differential-reinforcement-of-low-rate 72-s behavior in the rat. (springer.com)
  • The most well studied models whereby brown adipocytes appear in white fat are upon cold exposure or after stimulation of the beta(3)-adrenoceptor pathways. (frontiersin.org)
  • Upon agonist stimulation, a fluorescent signal is observed as the CypHer5E-antibody conjugate is internalized alongside the receptor into acidic endosomal vesicles. (bio-medicine.org)
  • 2004) Characterization of agonist stimulation of cAMP‐dependent protein kinase and G protein‐coupled receptor kinase phosphorylation of the beta2‐adrenergic receptor using phosphoserine‐specific antibodies. (els.net)
  • Release of norepinephrine and dopamine-beta-hydroxylase by nerve stimulation. (aspetjournals.org)
  • 2 These atypical receptors, now called β3-adrenoceptors, are found on the cell surface of both white and brown adipocytes where their stimulation promotes both lipolysis and energy expenditure in brown adipose tissue (BAT) and lipolysis in white adipose tissue (WAT). (dovepress.com)
  • Mechanism of cytokine inhibition of beta-adrenergic agonist stimulation of cyclic AMP in rat cardiac myocytes. (ahajournals.org)
  • Studies conducted in our laboratory have demonstrated that activated immune cells produce a soluble inhibitor(s) of cardiac myocyte contractile and cyclic AMP (cAMP) responses to beta-adrenergic stimulation. (ahajournals.org)
  • The proposed mechanism by which LABAs may worsen asthma control is the down-regulation of the b-adrenergic system as a result of the stimulation of b-receptors. (clinicalcorrelations.org)
  • Heart rate responsiveness to beta AR stimulation was blunted, with ED50, for isoproterenol increased 133% (p less than 0.001) after development of circulatory congestion. (ahajournals.org)
  • A range of agonists or positive allosteric modulators (PAMs) for mostly G i/o -coupled receptors, including metabotropic glutamate 2 (mGlu 2 ), adenosine A 1 , or μ-opioid receptors, suppress these effects of 5-HT 2A receptor stimulation. (springer.com)
  • The principal effects of beta-adrenergic stimulation are increased heart rate and contractility, vasodilation of the arterioles that supply the skeletal muscles, and relaxation of bronchial muscles. (thefreedictionary.com)
  • Mirabegron (Myrbetriq), a beta-3 adrenergic receptor agonist, causes relaxation of the detrusor miuscle and increases bladder capacity. (medscape.com)
  • Mirabegron is the first FDA approved selective agonist that is currently used to treat overactive bladder (OAB). (wikipedia.org)
  • Mirabegron is a beta-3 adrenergic agonist . (rxlist.com)
  • Specifically, mirabegron is a beta - 3 adrenergic agonist which specifically targets the receptors in the detrusor muscle (97 percent of beta -3 mRNA produced by the body is produced in the detrusor muscle). (verywell.com)
  • Unlike antimuscarinic drugs, mirabegron doesn't interfere with beta-1 and beta-2 receptors in other parts of the body. (verywell.com)
  • Mirabegron, a beta-3 adrenergic receptor agonist, another alternative to nonselective antimuscarinic drugs, appears to be less likely to cause dry mouth. (thedoctorweighsin.com)
  • Mirabegron is a potent and selective β(3)-adrenoceptor agonist. (unboundmedicine.com)
  • A Japanese phase 3 study showed that mirabegron has excellent efficacy and safety for treating overactive bladder. (unboundmedicine.com)
  • We next studied the clinical implications of this distribution in 12 healthy men given one-time randomized doses of placebo, the approved dose of 50 mg, and 200 mg of the β3-AR agonist mirabegron. (highwire.org)
  • Selected examples are: Arformoterol Buphenine Clenbuterol Dopexamine (β1 and β2) Epinephrine (non-selective) Fenoterol Formoterol Isoetarine Isoprenaline (INN), isoproterenol (USAN) (β1 and β2) Levosalbutamol (INN), levalbuterol (USAN) Orciprenaline (INN), metaproterenol (USAN) Pirbuterol Procaterol Ritodrine Salbutamol (INN), albuterol (USAN) Salmeterol Terbutaline These agents are also listed as agonists by MeSH. (wikipedia.org)
  • The inhibitory effect of isoproterenol, similar to that of nifedipine, was counteracted by ionomycin and also by the Ca2+ channel agonist Bay K 8644. (aspetjournals.org)
  • In first two experiments, rats received intraperitoneal injections of isoproterenol (0, 0.5, 1 and 2 mg/kg) and Nociceptin agonist 64 - 6198 (0, 1, 2 and 4 mg/kg) respectively. (zjrms.com)
  • Isoproterenol is a non-selective beta adrenergic agonist. (zjrms.com)
  • In the peripheral nervous system, as well as the brain, isoproterenol appears to have only beta-adrenergic activity. (zjrms.com)
  • Peripheral, but not central anorectic effect of isoproterenol is mediated by beta adrenergic receptors. (zjrms.com)
  • This characteristic makes it ideal for monitoring the translocation of cell surface receptors into the endosomal pathway. (bio-medicine.org)
  • Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions. (els.net)
  • G-protein-coupled receptors are the largest class of cell-surface receptors, and these membrane proteins exist in equilibrium between inactive and active states. (proteopedia.org)
  • These cell surface receptors are acted on by a wide variety of ligands, including small molecules and soluble proteins. (technologynetworks.com)
  • Comparisons of the Impact of Beta-3 Agonist Versus Antimuscarinics on Psychological Distress, Sexual Function, Bladder Wall Thickness and Blood Flow in Women With Overactive Bladder Syndrome: a Randomized Controlled Study. (clinicaltrials.gov)
  • Vibegron is a selective beta3AR agonist that is developed in Japan by Kyorin Pharmaceutical Co., Ltd and Kissei Pharmaceutical Co.,Ltd and Urovant Sciences to treat overactive bladders and pain caused by irritable bowel syndrome. (wikipedia.org)
  • MYRBETRIQ ® is a beta-3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence , urgency, and urinary frequency. (rxlist.com)
  • In three, 12-week, double-blind, placebo-controlled, safety and efficacy studies in patients with overactive bladder (Studies 1, 2, and 3), MYRBETRIQ ® was evaluated for safety in 2736 patients [see Clinical Studies ]. (rxlist.com)
  • Beta-3 adrenergic receptor agonist is a drug approved by the Federal Drug Administration of the United States and is used to treat overactive bladders, while T3 triiodothyronine is a thyroid hormone commonly used for medication for an underactive thyroid gland. (eurekalert.org)
  • Urovant Sciences, Inc (Nasdaq: UROV) announced today that the U.S. Food and Drug Administration (FDA) has approved the New Drug Application (NDA) for once-daily 75 mg GEMTESA® (vibegron), a beta-3 adrenergic receptor (β3) agonist, for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence (UUI), urgency, and urinary frequency in adults. (simonfoundation.org)
  • Urovant Sciences has submitted a New Drug Application (NDA) to the Food and Drug Administration (FDA) for vibegron, a beta-3 adrenergic agonist, for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency. (simonfoundation.org)
  • Tolterodine and oxybutynin, drugs for the treatment of overactive bladder, were cited in 4 and 3 studies, respectively. (thedoctorweighsin.com)
  • Recent studies suggest that antimuscarinics might suppress bladder afferent activity by blocking muscarinic receptors in the urothelium, myofibroblasts and detrusor, thereby improving overactive bladder symptoms. (unboundmedicine.com)
  • β3-adrenergic receptor (AR) agonists are approved to treat only overactive bladder. (highwire.org)
  • (D) They are used to stabilize the detrusor muscle, through binding and blocking muscarinic receptors. (scielo.br)
  • Beta-3 adrenergic receptor agonist is known to alleviate rodent bladder microcontractions by inhibiting afferent pathway. (auanet.org)
  • We have investigated the effect of beta-3 adrenergic receptor agonist (CL-316,243) on micromotion of major pelvic ganglion disconnected rat bladder. (auanet.org)
  • We could observe that beta-3 adrenergic receptor agonist have effect in alleviating micromotions of MPG disconnected rat bladder. (auanet.org)
  • These results also suggest that the major action point of the beta 3 adrenergic receptor agonist is in the bladder. (auanet.org)
  • These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. (medscape.com)
  • The receptors are located in the kidneys, urinary tract and bladder tissue. (wikipedia.org)
  • Tone in the bladder neck and proximal sphincter is increased by alpha adrenergic agonists and can manifest with urinary retention, particularly in men with prostatism. (auanet.org)
  • Tone in the smooth muscles of the bladder neck and proximal sphincter is decreased with alpha adrenergic antagonists. (auanet.org)
  • GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. (wikipedia.org)
  • Newer drugs, such as darifenacin and solifenacin are M3 selective receptor antagonists and may be more bladder-specific and have fewer side effects such as dry mouth. (thedoctorweighsin.com)
  • Following intravenous administration to rats, the rodent selective β3AR agonist CL316243 reduces bladder pressure and in cystomeric studies increases bladder capacity leading to prolongation of micturition interval without increasing residual urine volume. (drugapprovalsint.com)
  • β(3)-Adrenoceptors are predominantly expressed in the human bladder and mediate relaxation of detrusor muscle. (unboundmedicine.com)
  • β(3)-Adrenoceptor agonists increase bladder capacity and prolong micturition interval. (unboundmedicine.com)
  • It is assumed that β(3)-adrenoceptor agonists could exert an inhibitory effect on bladder afferent through β(3)-adrenoceptors in the urothelium and detrusor, which eventually improve the symptom of urgency. (unboundmedicine.com)
  • Gemtesa is a beta-3 adrenergic receptor agonist that activates beta-3 receptors in the bladder causing relaxation of the smooth muscle of the urinary bladder, increasing the bladder's storage capacity and helping alleviate urgency and frequency. (doctorpedia.com)
  • Dexmedetomidine is a potent alpha-2 adrenergic agonist that binds to the alpha-2 adrenergic receptor subtype A at the LC, resulting in almost complete inhibition of the LC, which has a sedative effect ( 5 , 6 ). (frontiersin.org)
  • The beta-adrenergic receptor-induced inhibition was prevented by pertussis toxin and could not be reproduced by forskolin, indicating that cAMP was not involved. (aspetjournals.org)
  • Accumulation of inositol phosphates triggered by high K+ was insensitive to the beta-adrenergic receptor inhibition. (aspetjournals.org)
  • Here we show in mammalian cells that endophilin marks and controls a fast-acting tubulovesicular endocytic pathway that is independent of AP2 and clathrin, activated upon ligand binding to cargo receptors, inhibited by inhibitors of dynamin, Rac, phosphatidylinositol-3-OH kinase, PAK1 and actin polymerization, and activated upon Cdc42 inhibition. (nature.com)
  • Signaling by 7TM receptors through G proteins leads to, for example, either inhibition (G αi ) or activation (G αs ) of adenylyl cyclase and cAMP production, activation of phospholipase C with inositol triphosphate turnover (G αq ), or activation of RhoGEF (G α 12/13 ) depending on which G protein the receptor is activating [ 3 ]. (pubmedcentralcanada.ca)
  • In fact, mutational inhibition of the sORF increased beta. (psu.edu)
  • Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. (els.net)
  • The pathophysiology of delirium is not fully understood, but several neurotransmitters are known to play an important role, including catecholamines ( 2 , 3 ). (frontiersin.org)
  • Beta adrenergic receptors are found distributed throughout the body, in both muscle and fat, and are regulated through various natural hormones (triiodothyronine or T3, thyroxine or T4, testosterone, etc…) and catecholamines (such as norepinephrine and epinephrine). (ironmagazine.com)
  • Catecholamines inhibit Ca(2+)-dependent proteolysis in rat skeletal muscle through beta(2)-adrenoceptors and cAMP. (psu.edu)
  • They also provide an experimental approach to the study of states of altered sensitivity to catecholamines at the receptor level in man. (duke.edu)
  • Adrenergic receptors (ARs) are members of the 7-transmembrane domain G-protein-coupled receptor superfamily that bind the endogenous catecholamines epinephrine and norepinephrine. (acris-antibodies.com)
  • Cheng J, Gao S, Zhu C , Liu S, Li J, Kang J, Wang Z, Wang T. Typical Stress Granule proteins interact with the 3'-UTR of Enterovirus D68 to inhibit viral replication. (academictree.org)
  • The norepinephrine provided by the LC acts at the medial septal area (MSA) and the medial preoptic area (MPOA) to activate waking-active neurons ( via alpha-1 adrenergic receptors) and inhibit sleep-active neurons ( via alpha-2 adrenergic receptors). (frontiersin.org)
  • Beta adrenergic receptors physiologically inhibit food intake in mammals. (zjrms.com)
  • CypHer5E, consequently, can be used to screen for novel antagonists of known receptors and for potential ligands of non-G-protein coupled receptors (5) and orphan receptors. (bio-medicine.org)
  • Another of our translational research projects is focused on Beta 1- adrenergic (β1-ADR) ligands as memory enhancers for cognitive disorders, and exploring the use of β1-ADR as a significant therapeutic target for AD. (stanford.edu)
  • Conformational changes induced by extracellular ligands binding to G-protein-coupled receptors result in a cellular response through the activation of G proteins. (proteopedia.org)
  • Tocrisets contain 3-5 ligands supplied as lyophilized solids or pre-dissolved in DMSO at a specified concentration. (tocris.com)
  • A subcutaneous injection of an oil suspension of l-epinephrine (270 mumol/kg), dopamine (270 mumol/kg) or l-norepinephrine (270 mumol/kg), when administered with phenoxybenzamine (32 mumol/kg i.p.) to blocl alpha adrenergic effects, increases the cyclic 3', 5'-adenosine monophosphate (cAMP) content in superior cervical ganglia (SCG) of rats. (aspetjournals.org)
  • Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, in rats: identification of a novel isethionic acid conjugate. (nih.gov)
  • The pharmacokinetics of a thiazole benzenesulfonamide beta 3-adrenergic receptor agonist and its analogs in rats, dogs, and monkeys: improving oral bioavailability. (nih.gov)
  • The objective of this experiment was to study the effect of CL 316,243 (CL) (a highly selective ß3-adrenergic receptor agonist) on cellular changes occurring in retroperitoneal white adipose tissue (RWAT) of lean and obese rats. (dovepress.com)
  • Portal hypertension and liver cirrhosis in rats: effect of the ß3-adrenoceptor agonist SR58611A. (abcam.com)
  • Hajinezhad M R, Shohreh B. Possible Involvement of Beta-Adrenergic Receptors on Nociceptin/Orphanin FQ Induced Food Consumption in Male Rats, Zahedan J Res Med Sci. (zjrms.com)
  • The aim of this study was to determine the possible interaction between beta adrenergic and N/OFQ receptors on food consumption in male rats. (zjrms.com)
  • The results obtained from previous studies have shown that beta-receptor antagonists stimulate food consumption in rats [ 3 ]. (zjrms.com)
  • High dosages of beta adrenergic receptor agonists induce cardiomyocyte necrosis and interstitial fibrosis in rats [ 5 ]. (zjrms.com)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (els.net)
  • Direct sympathomimetics stimulate adrenergic and dopaminergic receptors directly. (amboss.com)
  • Beta-1 adrenergic receptor may also stimulate Rap guanine nucleotide exchange factor (GEF) 2 ( PDZ-GEF1 ) directly and/or via cAMP. (bio-rad.com)
  • It is a selective beta-2 agonist, meaning it will stimulate your beta-2 adrenergic receptors. (ironmagazine.com)
  • It is an agonist at alpha and beta adrenergic receptors which causes the release of endogenous norepinephrine (noradrenaline). (healthcmi.com)
  • Interestingly, among the viral receptors there is a greater diversity in the DRY-motif compared to their endogenous receptor homologous. (pubmedcentralcanada.ca)
  • In this review we will focus on these two structural motifs and discuss their role in viral 7TM receptor signaling compared to their endogenous counterparts. (pubmedcentralcanada.ca)
  • Despite the structural diversity in the repertoire of the endogenous 7TM receptor agonists, the conformational changes that occur upon receptor activation are believed to be overall identical. (pubmedcentralcanada.ca)
  • The nociceptin/orphanin FQ (N/OFQ) peptide is the endogenous ligand for the N/OFQ peptide (NOP) receptor. (zjrms.com)
  • Dopamine receptor agonists.iii. (bireme.br)
  • Dopamine receptor antagonists.iv. (bireme.br)
  • The A(2A) adenosine receptor (A(2A)AR) is responsible for regulating blood flow to the cardiac muscle and is important in the regulation of glutamate and dopamine release in the brain. (proteopedia.org)
  • Structurally related compounds devoid of beta-adrenergic activity such as dopamine, dihydroxymandelic acid, normetanephrine, pyrocatechol, and phentolamine did not effectively compete for the binding sites. (duke.edu)
  • L-755,507 is also a very potent and selective β3-AR adrenergic receptor partial agonist, selective over both β1-AR and β2-AR adrenoceptor binding. (scbt.com)
  • Thus, interference with agonist-occupied beta-adrenergic receptor coupling to adenylate cyclase to produce cAMP and subsequent contractile responses is induced by a factor(s) elaborated by activated immune cells. (ahajournals.org)
  • Our objective was to test the safety and metabolic effects of a novel beta(3)-adrenoreceptor agonist (TAK-677) in humans. (nih.gov)
  • PI3Kγ is selectively recruited to G protein-coupled receptors implicated in inflammation and metabolic homeostasis, including chemokine receptors, β-adrenergic signaling, and angiotensin II receptors ( 13 - 17 ). (pnas.org)
  • One of the mediators of the positive metabolic effects of endurance exercise is peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α). (anabolicminds.com)
  • A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. (scbt.com)
  • The lab also is working to determine the precise role of the "metabolic" beta-3 adrenergic receptor (ß3AR) in the heart and define the extent of its protective effect in obesity and in heart failure, including its role in maintaining nitric oxide synthase (NOS) coupling. (hopkinsmedicine.org)
  • Studies have shown that 3,3′-T2 may be more effective in raising resting metabolic rate when hypothyroid subjects are treated with T3, than when normal (euthyroid) subjects are given T3. (mindandmuscle.net)
  • (Department of Pharmacology and Toxicology, University of Lausanne, Switzerland) Working with Professor Kaethi Geering and Dr Stephanie Bibert to identify the candidate cysteine residue on the beta 1 subunit of Na+-K+ pump subunit that mediates its oxidative regulation. (edu.au)
  • Operating via heterotrimeric G proteins, adrenergic receptors constitute one of the most intensely studied classes of membrane proteins, whose expression and function are subject to regulation at many different levels, including transcriptional, posttranscriptional and posttranslational. (els.net)
  • Hadcock JR and Malbon CC (1988) Down‐regulation of beta‐adrenergic receptors: agonist‐induced reduction in receptor mRNA levels. (els.net)
  • Kallal L, Gagnon AW, Penn RB and Benovic JL (1998) Visualization of agonist‐induced sequestration and down‐regulation of a green fluorescent protein‐tagged beta2‐adrenergic receptor. (els.net)
  • Kohout TA and Lefkowitz RJ (2003) Regulation of G protein‐coupled receptor kinases and arrestins during receptor desensitization. (els.net)
  • Krupnick JG and Benovic JL (1998) The role of receptor kinases and receptors in G‐protein‐coupled receptor regulation. (els.net)
  • Shenoy SK, McDonal PH, Kohout TA and Lefkowitz RJ (2001) Regulation of receptor fate by ubiquitination of activated beta2‐adrenergic receptor and beta‐arrestin. (els.net)
  • Beta-adrenergic receptors and their regulation. (springermedizin.de)
  • Furthermore, we show that the regulation of NMII takes place downstream of guidance receptor signalling and is critical to ensure efficient collective migration. (visionsxrwabbitt36.cf)
  • Beta adrenergic receptors and N/OFQ are involved in the regulation of food intake through central and peripheral mechanisms. (zjrms.com)
  • Vibegron is a selective agonist for the beta-3 adrenergic receptor (β3-AR) receptor. (wikipedia.org)
  • Solabegron (GW-427,353) is a drug which acts as a selective agonist for the β3 adrenergic receptor. (drugbank.ca)
  • norepinephrine is a direct acting catecholamine that works through which receptors in the CNS? (brainscape.com)
  • For example, patients with low heart rate are given beta agonist treatments that are more "cardio-selective" such as dobutamine, which increases the force of contraction of the heart muscle. (wikipedia.org)
  • Beta-2 adrenergic receptor activation also appears to be important in the MSA and MPOA, resulting in dose-dependent increases in time spent awake ( 4 ). (frontiersin.org)
  • Removal of extracellular Ca2+ or addition of the Ca2+ channel antagonists nifedipine and verapamil almost totally abolished stimulations elicited by high K+ and partially attenuated receptor- and fluoroaluminate-mediated increases in inositol phosphates. (aspetjournals.org)
  • One focus has been on activating the β3-adrenergic receptor (AR), which in rodent models increases energy expenditure and improves glucose tolerance ( 1 ). (highwire.org)
  • Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs) (4). (bio-medicine.org)
  • G protein-coupled receptors (GPCRs), one of the most commonly used and successful targets for drugs, are a large family of multi-transmembrane proteins and an important class of receptors. (technologynetworks.com)
  • hence, the name is G protein coupled receptors (GPCRs). (pubmedcentralcanada.ca)
  • In this review we will use the term 7TM receptors instead of GPCRs as these receptors also signal trough non-G protein-dependent pathways, like β -arrestin-mediated signaling [ 2 ]. (pubmedcentralcanada.ca)
  • These effects on 5-HT 2A receptors and related GPCRs appear to play a major role in the behavioral effects of serotonergic hallucinogens, such as head twitches in rodents and higher order behaviors such as rodent lever pressing on the differential-reinforcement-of-low rate 72-s (DRL 72-s) schedule. (springer.com)
  • Indications of administration for β agonists include: Bradycardia (slow heart rate) Asthma Chronic obstructive pulmonary disease (COPD) Heart failure Allergic reactions Hyperkalemia Beta blocker poisoning Premature labor (this is an off-label use and could be detrimental) Although minor compared to those of epinephrine, beta agonists usually have mild to moderate adverse effects, which include anxiety, hypertension, increased heart rate, and insomnia. (wikipedia.org)
  • beta-adrenergic blocking agent ( beta-blocker ) any of a group of drugs that block the action of epinephrine at beta-adrenergic receptors on cells of effector organs. (thefreedictionary.com)
  • Activation of β2 receptors induces smooth muscle relaxation in the lungs, gastrointestinal tract, uterus, and various blood vessels. (wikipedia.org)
  • Agonism of the beta(2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles. (drugbank.ca)
  • No differences in the extent or potency of β3AR agonist mediated relaxation were observed, consistent with the concept that the β3AR activation is an effective way of relaxing the detrusor in normal and pathogenic states. (drugapprovalsint.com)
  • 6 It has been reported that a chronic administration of the β3-adrenergic agonists can induce the ectopic expression of UCP in white fat and skeletal muscle. (dovepress.com)
  • Recordings made from layer V (L5) pyramidal cells of the prefrontal cortex (PFC) and neocortex in rodent slice preparations have shown that serotonin (5-hydroxytryptamine, 5-HT) and serotonergic hallucinogens induce an increase in the frequency of spontaneous excitatory postsynaptic currents (EPSCs) in the apical dendritic field by activating 5-HT 2A receptors. (springer.com)
  • α 1 -adrenergic, and mGlu 5 receptors) similarly induce glutamate (Glu) release onto L5 pyramidal cells. (springer.com)
  • Thus, changes in beta-adrenergic receptor (beta AR) expression should reflect more directly the influence of neurohumoral adrenergic tone, clarifying the manner in which peripheral (neurohumoral) versus primary myocardial factors are operative in decreased beta AR-dependent signal transduction. (ahajournals.org)
  • A guideline from the American Urological Association recommends beta-3-adrenergic receptor agonists as second-line therapy in patients with an inadequate response to behavioral therapy. (medscape.com)
  • ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β 2 adrenergic receptor, as few other specific antagonists for this receptor are known. (wikipedia.org)
  • xpression of beta-2 AR in humans is diversified by regulatory polymorphisms in the promotersregion of ADRB2, contributing to inter-individualsvariation in responsiveness to beta-2 agonist-basedsdrugs =-=(13)-=- and possibly to obesity risk (14).sSimilar to human ADRB2, mRNA expression ofsthe porcine homologue is modulated by multiplespolymorphisms in the highly polymorphic 5´ flankingsregion, as evidenced b. (psu.edu)
  • Vasoconstriction of the isolated rabbit ear artery caused by nicotinic agonists acting on adrenergic neurons. (aspetjournals.org)
  • Desensitization of the adrenergic neurons of the isolated rabbit ear artery to nicotinic agonists. (aspetjournals.org)
  • Evidence implicates a number of brain regions in mediating these effects of serotonergic hallucinogens and G q/11 -coupled receptors including the midline and intralaminar thalamic nuclei, claustrum, and neurons in deep PFC. (springer.com)
  • 1987) Ligand binding to the beta‐adrenergic receptor involves its rhodopsin‐like core. (els.net)
  • This pathway mediates the ligand-triggered uptake of several G-protein-coupled receptors such as α 2a - and β 1 -adrenergic, dopaminergic D3 and D4 receptors and muscarinic acetylcholine receptor 4, the receptor tyrosine kinases EGFR, HGFR, VEGFR, PDGFR, NGFR and IGF1R, as well as interleukin-2 receptor. (nature.com)
  • 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)
  • Other studies have proved that binding of agonists to these receptors occurs when the catecholamine molecule is in the protonated state (6), all of these receptors being coupled with G proteins. (scielo.br)
  • The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. (proteopedia.org)
  • Seven transmembrane (7TM) receptors constitute the largest superfamily of membrane proteins and function as important mediators of extracellular signals to intracellular responses. (pubmedcentralcanada.ca)
  • Beta receptors are coupled to Gs proteins, which in turn are linked to adenylyl cyclase. (acris-antibodies.com)
  • The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment for obesity and diabetes. (wikipedia.org)
  • Ultimately, this work will enable the exploration of a possible therapeutic role of ß3AR agonists and re-coupling of NOS in preventing adverse ventricular remodeling in obesity and in heart failure. (hopkinsmedicine.org)
  • This physiology should be considered in the development of more selective β3-AR agonists to treat obesity-related complications. (highwire.org)
  • Several pharmaceutical companies developed β3-AR agonists for the treatment of obesity, but none progressed past phase 2 clinical trials. (highwire.org)
  • Several herpes- and poxviruses have captured chemokine receptors from their hosts and modified these to their own benefit. (pubmedcentralcanada.ca)
  • The human and viral chemokine receptors belong to class A 7 transmembrane (TM) receptors which are characterized by several structural motifs like the DRY-motif in TM3 and the C-terminal tail. (pubmedcentralcanada.ca)
  • Patients taking drugs that raise blood pressure and heart contractility should use caution if taking alpha-agonists such as pseudoephedrine (Sudafed). (healthcmi.com)
  • We believe that adrenergic agonists may have a dual mechanism of action: the first one consists of a catecholamine action on its receptor with the formation of a stimulus-receptor complex. (scielo.br)
  • On activation, PI3Kγ controls two major second messengers: phosphatidylinositol(3,4,5)-tris-phosphate (PIP 3 ) through direct phosphorylation of phosphatidylinositol 4,5 bisphosphate and cAMP by a kinase-independent mechanism ( 18 ). (pnas.org)
  • 1996) The beta‐adrenergic receptor is a substrate for the insulin receptor tyrosine kinase. (els.net)
  • Tao J, Wang HY and Malbon CC (2003) Protein kinase A regulates AKAP250 (gravin) scaffold binding to the beta2‐adrenergic receptor. (els.net)
  • G-protein alpha-i family activation releases complex of G-protein beta/gamma , which activates c-src tyrosine kinase ( c-Src ) [ 12 ]. (bio-rad.com)
  • Furthermore, the G βγ subunit is also involved in signaling and the 7TM receptors also signal via G protein-independent pathways like MAP-kinase activation-mediated by β -arrestins [ 4 ]. (pubmedcentralcanada.ca)
  • For the combined Studies 1, 2, and 3, 432 patients received MYRBETRIQ ® 25 mg, 1375 received MYRBETRIQ ® 50 mg, and 929 received MYRBETRIQ ® 100 mg once daily. (rxlist.com)
  • The beta-3 agonist class of medication has numerous advantages over the anti-cholinergic class (Detrol, Ditropan, VESIcare, Enablex, Sanctura, Toviaz) and Gemtesa affords some advantages over Myrbetriq including simple dosing, ability to crush, no worries about blood pressure and less drug-drug interactions, but has not yet been approved for pediatric indications as has Myrbetriq. (doctorpedia.com)
  • Arbutamine Befunolol Bromoacetylalprenololmenthane Broxaterol Cimaterol Cirazoline Etilefrine Hexoprenaline Higenamine Isoxsuprine Mabuterol Methoxyphenamine Oxyfedrine Ractopamine Reproterol Rimiterol Tretoquinol Tulobuterol Zilpaterol Zinterol Alpha-adrenergic agonist "WHAT ARE BETA-AGONISTS? (wikipedia.org)
  • Hypoglycemia was also reported due to increased secretion of insulin in the body from activation of β2 receptors. (wikipedia.org)
  • An optical section of the fluorescent receptors is obtained by epifluorescence confocal microscopy from insulin‐treated (a), untreated (b) and β‐adrenergic agonist‐treated (c) cells. (els.net)
  • Shumay E, Gavi S, Wang HY and Malbon CC (2004) Trafficking of beta2‐adrenergic receptors: insulin and beta‐agonists regulate internalisation by distinct cytoskeletal pathways. (els.net)
  • The hormone and ending with the saphenous opening and drain into the changed one month before the response are extensor and flexor pollicis longus, thenar muscles, the index finger may be biased by the external auditory canal insulin are rapid onset and prolonged contact can enhance all types of opioid agonists, it is excellent and similar compounds prevent the emergence of homo a man] homunculus. (dsaj.org)
  • 7 Certain polymorphisms of the human b 2 -adrenergic receptor gene have also been implicated. (clinicalcorrelations.org)
  • Identification of novel polymorphisms within the promoter region of the human beta2 adrenergic receptor gene. (psu.edu)
  • β3 receptors are mainly located in adipose tissue. (wikipedia.org)
  • We performed tissue receptor profiling and showed that the human β3-AR mRNA is also highly expressed in gallbladder and brown adipose tissue (BAT). (highwire.org)
  • What is the role of beta-adrenergic agonists in urinary incontinence treatment? (medscape.com)
  • Treatment of Postprostatectomy Male Urinary Incontinence With the Transobturator Retroluminal Repositioning Sling Suspension: 3-Year Follow-up. (medscape.com)
  • Clenbuterol is a Beta(2) agonist similar in some structural respects to salbutamol. (drugbank.ca)
  • Aim: To evaluate the effect of the short-acting beta agonists (SABAs) salbutamol on cardiovascular response rest, exercise and recovery phase. (bvsalud.org)
  • Long-acting beta 2 -adrenergic agonists (LABA), such as salmeterol, the active ingredient in SEREVENT ® DISKUS ® , increase the risk of asthma-related death. (drugs.com)
  • Advair HFA should be used for patients not adequately controlled on a long-term asthma control medication such as an inhaled corticosteroid (ICS) or whose disease warrants initiation of treatment with both an ICS and long-acting beta 2 -adrenergic agonist (LABA). (drugs.com)
  • Wixela™ Inhub™ combines the inhaled corticosteroid (ICS) medicine fluticasone propionate and the long-acting beta 2 - adrenergic agonist (LABA) medicine salmeterol. (rxlist.com)
  • The region of i loop 3 highlighted in blue is implicated in signalling from receptor to G protein. (els.net)
  • Marchese A, Chen C, Kim YM and Benovic JL (2003) The ins and outs of G‐protein‐coupled receptor trafficking. (els.net)
  • 3 The thermogenesis function in BAT largely depends on an integral membrane protein located at the inner membrane of mitochondria that is called thermogenin or uncoupling protein one (UCP1). (dovepress.com)
  • CDR-H3 is located in a similar position to the G-protein carboxy-terminal fragment in the active opsin structure and to CDR-3 of the nanobody in the active beta(2)-adrenergic receptor structure, but locks A(2A)AR in an inactive conformation. (proteopedia.org)
  • These results suggest a new strategy to modulate the activity of G-protein-coupled receptors. (proteopedia.org)
  • G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody. (proteopedia.org)
  • For example, Beta-2 adrenergic receptor activate GNAS complex locus ( G-protein alpha-s )/ Adenylate cyclases, which leads to Adenosine 3',5'-cyclic phosphate ( cAMP ) production. (bio-rad.com)
  • PKA-cat phosphorylation of Beta-2 adrenergic receptor leads to its activation switch from G-protein alpha-i family to G-protein alpha-s . (bio-rad.com)
  • c-Src phosphorylates SHC transforming protein 1 ( Shc ) and Growth factor receptor-bound protein 2 ( GRB2 ), activating Son of sevenless homolog ( SOS )/ H-Ras / c-Raf-1 and subsequent MEK and Erk activation [ 12 ], [ 13 ]. (bio-rad.com)
  • Ringstad, N., Nemoto, Y. & De Camilli, P. The SH3p4/Sh3p8/SH3p13 protein family: binding partners for synaptojanin and dynamin via a Grb2-like Src homology 3 domain. (nature.com)
  • Binding was rapid (t1/2 less than 30 s) and rapidly reversible (t1/2 less than 3 min) at 37 degrees C. Binding was a saturable process with 75 +/- 12 fmol (-) [3H] alprenolol bound/mg protein (mean +/- SEM) at saturation, corresponding to about 2,000 sites/cell. (duke.edu)
  • The focus of work in this laboratory is on the elucidation of the molecular properties and regulatory mechanisms controlling the function of G protein-coupled receptors. (duke.edu)
  • B, β, the second letter of the Greek alphabet, used in scientific notation to denote position of a carbon atom in a molecule, a type of protein configuration, or identification of a type of activity, as beta blocker, beta particle, or beta rhythm. (thefreedictionary.com)
  • Beta adrenergic receptors (or β receptors) belong to the guanine nucleotide-binding G protein-coupled receptor (GPCR) superfamily. (zjrms.com)
  • Myocardial beta-adrenergic receptor expression and signal transduction after chronic volume-overload hypertrophy and circulatory congestion. (ahajournals.org)
  • METHODS AND RESULTS We examined the beta-adrenergic receptor-responsive adenylyl cyclase pathway in hearts from pigs subjected to volume-overload hypertrophy with circulatory congestion. (ahajournals.org)
  • acts through which 2 subtype receptors? (brainscape.com)
  • ICI binds to the β 2 subtype with at least 100 times greater affinity than β 1 or β 3 , the two other known subtypes of the beta adrenoceptor. (wikipedia.org)
  • Benneyworth MA et al (2007) A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. (springer.com)
  • Selection of 3 β-adrenoceptor agonists (Cat. (tocris.com)
  • If you know of a relevant reference for β -Adrenoceptor Agonist Tocriset™, please let us know . (tocris.com)
  • Do you know of a great paper that uses β -Adrenoceptor Agonist Tocriset™ from Tocris? (tocris.com)
  • Be the first to review β -Adrenoceptor Agonist Tocriset™ and earn rewards! (tocris.com)
  • Beta-adrenoceptor agonists and asthma-100 years of development. (psu.edu)
  • Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. (nih.gov)
  • Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. (scbt.com)
  • 1989) Molecular characterization of the human beta 3‐adrenergic receptor. (els.net)
  • The new type of skin patch contains hundreds of micro-needles, each thinner than a human hair, which are loaded with the drug Beta-3 adrenergic receptor agonist or another drug called thyroid hormone T3 triiodothyronine. (eurekalert.org)
  • The team estimates that their prototype patch had a material cost of about S$5 (US$3.50) to make, which contains beta-3 adrenergic receptor agonist combined with Hyaluronic acid, a substance naturally found in the human body and commonly used in products like skin moisturisers. (eurekalert.org)
  • 3vga is a 3 chain structure with sequence from Human and Mus musculus . (proteopedia.org)
  • AA2AR_HUMAN ] Receptor for adenosine. (proteopedia.org)
  • Also this region is more variable among virus-encoded 7TM receptors compared to human class A receptors. (pubmedcentralcanada.ca)
  • sThe CRE located at -275 to -268 in the human ADRB2sgene mediates the transcriptional enhancing activitysof cyclic AMP (7) in response to agonists that actsthrough the PKA signal transduction pathway =-=(19)-=-.sThus, both elements most likely drive basal and regulated promoter activity of ADRB2 in the pig, as well.sBasal ADRB2 promoter activity was further enhanced in all used cell lines by a GC-rich segme. (psu.edu)
  • Identification of beta-adrenergic receptors in human lymphocytes by (-) (3H) alprenolol binding. (duke.edu)
  • Human lymphocytes are known to posessess a catecholamine-responsive adenylate cyclase which has typical beta-adrenergic specificity. (duke.edu)
  • These results demonstrate the feasibility of using direct binding methods to study beta-adrenergic receptors in a human tissue. (duke.edu)
  • These observations also suggested that there were undefined, fundamental differences between rodent and human receptor physiology that needed to be addressed so that the therapeutic promise of β3-AR agonists could be achieved. (highwire.org)
  • 1988) Molecular cloning and expression of the cDNA for the hamster alpha 1‐adrenergic receptor. (els.net)
  • 9, 10 In patients with intermittent asthma an inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol is preferred (Step 1). (dentalcare.com)
  • The patient experiences prompt relief with inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol. (dentalcare.com)
  • Binding of (-) [3H] alprenolol to these sites demonstrated the kinetics, affinity, and stereospecificity expected of binding to adenylate cyclase-coupled beta-adrenergic receptors. (duke.edu)
  • The C-terminal receptor tail constitutes another regulatory region that through a number of phosphorylation sites is involved in signaling, desensitization, and internalization. (pubmedcentralcanada.ca)
  • Activation of β1 receptors induces positive inotropic, chronotropic output of the cardiac muscle, leading to increased heart rate and blood pressure, secretion of ghrelin from the stomach, and renin release from the kidneys. (wikipedia.org)
  • Activation of beta-adrenergic receptors inhibits Ca2+ entry-mediated generation of inositol phosphates in the guinea pig myometrium, a cyclic AMP-independent event. (aspetjournals.org)
  • Tamoxifen is an estrogen receptor agonist in bone and therefore inhibits osteoclasts. (healthcmi.com)
  • The data are compatible with a catecholamine-driven beta AR pathway desensitization. (ahajournals.org)