Catecholamines: A general class of ortho-dihydroxyphenylalkylamines derived from tyrosine.Receptors, Adrenergic, beta-2: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.Receptors, Adrenergic: 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.Receptors, Adrenergic, beta-1: 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.Receptors, Adrenergic, alpha: 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.Epinephrine: 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.Receptors, Adrenergic, alpha-2: 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.Receptors, Adrenergic, alpha-1: 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.Norepinephrine: Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Receptors, Adrenergic, beta-3: 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.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Adrenergic beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.Adrenergic beta-2 Receptor Agonists: Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.Isoproterenol: 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.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Adrenergic alpha-Antagonists: Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Adrenal Medulla: The inner portion of the adrenal gland. Derived from ECTODERM, adrenal medulla consists mainly of CHROMAFFIN CELLS that produces and stores a number of NEUROTRANSMITTERS, mainly adrenaline (EPINEPHRINE) and NOREPINEPHRINE. The activity of the adrenal medulla is regulated by the SYMPATHETIC NERVOUS SYSTEM.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Receptors, Catecholamine: Cell surface proteins that bind catecholamines with high affinity and trigger intracellular changes which influence the behavior of cells. The catecholamine messengers epinephrine, norepinephrine, and dopamine are synthesized from tyrosine by a common biosynthetic pathway.Propranolol: 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.Adrenergic beta-Antagonists: Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.Adrenergic beta-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.Iodocyanopindolol: A highly selective and specific beta antagonist that is used to characterize beta-adrenoceptors.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.Dihydroalprenolol: 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.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Adrenergic beta-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Pindolol: 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)Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.Dioxanes: 1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)Phentolamine: 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.Dopamine beta-HydroxylaseChromaffin Cells: Cells that store epinephrine secretory vesicles. During times of stress, the nervous system signals the vesicles to secrete their hormonal content. Their name derives from their ability to stain a brownish color with chromic salts. Characteristically, they are located in the adrenal medulla and paraganglia (PARAGANGLIA, CHROMAFFIN) of the sympathetic nervous system.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 220.127.116.11.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.Arrestins: Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.Chromaffin System: The cells of the body which stain with chromium salts. They occur along the sympathetic nerves, in the adrenal gland, and in various other organs.Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.Adrenal Glands: A pair of glands located at the cranial pole of each of the two KIDNEYS. Each adrenal gland is composed of two distinct endocrine tissues with separate embryonic origins, the ADRENAL CORTEX producing STEROIDS and the ADRENAL MEDULLA producing NEUROTRANSMITTERS.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Pheochromocytoma: A usually benign, well-encapsulated, lobular, vascular tumor of chromaffin tissue of the ADRENAL MEDULLA or sympathetic paraganglia. The cardinal symptom, reflecting the increased secretion of EPINEPHRINE and NOREPINEPHRINE, is HYPERTENSION, which may be persistent or intermittent. During severe attacks, there may be HEADACHE; SWEATING, palpitation, apprehension, TREMOR; PALLOR or FLUSHING of the face, NAUSEA and VOMITING, pain in the CHEST and ABDOMEN, and paresthesias of the extremities. The incidence of malignancy is as low as 5% but the pathologic distinction between benign and malignant pheochromocytomas is not clear. (Dorland, 27th ed; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1298)Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.Tyrosine 3-Monooxygenase: An enzyme that catalyzes the conversion of L-tyrosine, tetrahydrobiopterin, and oxygen to 3,4-dihydroxy-L-phenylalanine, dihydrobiopterin, and water. EC 18.104.22.168.Normetanephrine: A methylated metabolite of norepinephrine that is excreted in the urine and found in certain tissues. It is a marker for tumors.Butoxamine: A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.Vanilmandelic AcidAlprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.Adrenergic Agents: 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.Sympathetic Nervous System: 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.GTP-Binding Proteins: 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.-.Chromaffin Granules: Organelles in CHROMAFFIN CELLS located in the adrenal glands and various other organs. These granules are the site of the synthesis, storage, metabolism, and secretion of EPINEPHRINE and NOREPINEPHRINE.Myocardium: 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.Adrenergic beta-3 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-3 RECEPTORS.Cyclic AMP-Dependent Protein Kinases: 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.Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.beta-Adrenergic Receptor Kinases: G-protein-coupled receptor kinases that mediate agonist-dependent PHOSPHORYLATION and desensitization of BETA-ADRENERGIC RECEPTORS.Adrenal Gland Neoplasms: Tumors or cancer of the ADRENAL GLANDS.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Heart Rate: The number of times the HEART VENTRICLES contract per unit of time, usually per minute.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Metanephrine: Product of epinephrine O-methylation. It is a commonly occurring, pharmacologically and physiologically inactive metabolite of epinephrine.Methoxamine: An alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION.Cells, Cultured: Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Kinetics: The rate dynamics in chemical or physical systems.Splanchnic Nerves: The major nerves supplying sympathetic innervation to the abdomen. The greater, lesser, and lowest (or smallest) splanchnic nerves are formed by preganglionic fibers from the spinal cord which pass through the paravertebral ganglia and then to the celiac ganglia and plexuses. The lumbar splanchnic nerves carry fibers which pass through the lumbar paravertebral ganglia to the mesenteric and hypogastric ganglia.Sympathomimetics: Drugs that mimic the effects of stimulating postganglionic adrenergic sympathetic nerves. Included here are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters.Oxymetazoline: A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)Ethanolamines: AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.GTP-Binding Protein alpha Subunits, Gs: A family of heterotrimeric GTP-binding protein alpha subunits that activate ADENYLYL CYCLASES.QuinoxalinesChromogranin A: A type of chromogranin which was first isolated from CHROMAFFIN CELLS of the ADRENAL MEDULLA but is also found in other tissues and in many species including human, bovine, rat, mouse, and others. It is an acidic protein with 431 to 445 amino acid residues. It contains fragments that inhibit vasoconstriction or release of hormones and neurotransmitter, while other fragments exert antimicrobial actions.Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Tyramine: An indirect sympathomimetic. Tyramine does not directly activate adrenergic receptors, but it can serve as a substrate for adrenergic uptake systems and monoamine oxidase so it prolongs the actions of adrenergic transmitters. It also provokes transmitter release from adrenergic terminals. Tyramine may be a neurotransmitter in some invertebrate nervous systems.Cattle: Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.Albuterol: 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.Molecular Sequence Data: 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.Sympatholytics: Drugs that inhibit the actions of the sympathetic nervous system by any mechanism. The most common of these are the ADRENERGIC ANTAGONISTS and drugs that deplete norepinephrine or reduce the release of transmitters from adrenergic postganglionic terminals (see ADRENERGIC AGENTS). Drugs that act in the central nervous system to reduce sympathetic activity (e.g., centrally acting alpha-2 adrenergic agonists, see ADRENERGIC ALPHA-AGONISTS) are included here.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Phenylethanolamine N-Methyltransferase: A methyltransferase that catalyzes the reaction of S-adenosyl-L-methionine and phenylethanolamine to yield S-adenosyl-L-homocysteine and N-methylphenylethanolamine. It can act on various phenylethanolamines and converts norepinephrine into epinephrine. (From Enzyme Nomenclature, 1992) EC 22.214.171.124.Catecholamine Plasma Membrane Transport Proteins: A group of membrane transport proteins that transport biogenic amine derivatives of catechol across the PLASMA MEMBRANE. Catecholamine plasma membrane transporter proteins regulate neural transmission as well as catecholamine metabolism and recycling.Dogs: 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)Dihydroxyphenylalanine: A beta-hydroxylated derivative of phenylalanine. The D-form of dihydroxyphenylalanine has less physiologic activity than the L-form and is commonly used experimentally to determine whether the pharmacological effects of LEVODOPA are stereospecific.Betaxolol: A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Calcium: A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.Methyltyrosines: A group of compounds that are methyl derivatives of the amino acid TYROSINE.Heart: The hollow, muscular organ that maintains the circulation of the blood.Pertussis Toxin: 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.Tetralones: A group of TETRAHYDRONAPHTHALENES containing a keto oxygen.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Fenoterol: An adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.Rats, Inbred Strains: 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.Procaterol: A long-acting beta-2-adrenergic receptor agonist.alpha-Methyltyrosine: An inhibitor of the enzyme TYROSINE 3-MONOOXYGENASE, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with PHEOCHROMOCYTOMA. (Martindale, The Extra Pharmacopoeia, 30th ed)RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.Chromogranins: A group of acidic proteins that are major components of SECRETORY GRANULES in the endocrine and neuroendocrine cells. They play important roles in the aggregation, packaging, sorting, and processing of secretory protein prior to secretion. They are cleaved to release biologically active peptides. There are various types of granins, usually classified by their sources.Lipolysis: The metabolic process of breaking down LIPIDS to release FREE FATTY ACIDS, the major oxidative fuel for the body. Lipolysis may involve dietary lipids in the DIGESTIVE TRACT, circulating lipids in the BLOOD, and stored lipids in the ADIPOSE TISSUE or the LIVER. A number of enzymes are involved in such lipid hydrolysis, such as LIPASE and LIPOPROTEIN LIPASE from various tissues.Amino Acid Sequence: 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.DioxolesDigitonin: A glycoside obtained from Digitalis purpurea; the aglycone is digitogenin which is bound to five sugars. Digitonin solubilizes lipids, especially in membranes and is used as a tool in cellular biochemistry, and reagent for precipitating cholesterol. It has no cardiac effects.CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.Virulence Factors, Bordetella: 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.Guanabenz: An alpha-2 selective adrenergic agonist used as an antihypertensive agent.Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.GTP-Binding Protein alpha Subunits, Gi-Go: 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.Transfection: 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.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.Myocardial Contraction: Contractile activity of the MYOCARDIUM.Colforsin: 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.Hydroxydopamines: Dopamines with a hydroxy group substituted in one or more positions.G-Protein-Coupled Receptor Kinase 5: A G-protein-coupled receptor kinase subtype that is primarily expressed in the MYOCARDIUM and may play a role in the regulation of cardiac functions.Adrenergic Uptake Inhibitors: Drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The tricyclic antidepressants (ANTIDEPRESSIVE AGENTS, TRICYCLIC) and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of these drugs also block transport of serotonin.Hypertension: Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Stimulation, Chemical: The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.G-Protein-Coupled Receptor Kinases: A family of serine-threonine kinases that are specific for G-PROTEIN-COUPLED RECEPTORS. They are regulatory proteins that play a role in G-protein-coupled receptor densensitization.G-Protein-Coupled Receptor Kinase 2: A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS. It may play an essential role in regulating myocardial contractile response.Enzyme Activation: 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.Imidazoles: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).Dihydroergotoxine: A mixture of three different hydrogenated derivatives of ERGOTAMINE: DIHYDROERGOCORNINE; DIHYDROERGOCRISTINE; and DIHYDROERGOCRYPTINE. Dihydroergotoxine has been proposed to be a neuroprotective agent and a nootropic agent. The mechanism of its therapeutic actions is not clear, but it can act as an alpha-adrenergic antagonist and a dopamine agonist. The methanesulfonate salts of this mixture of alkaloids are called ERGOLOID MESYLATES.Imidazoline Receptors: 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.COS Cells: 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).)Norepinephrine Plasma Membrane Transport Proteins: Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of noradrenergic neurons. They remove NOREPINEPHRINE from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. It regulates signal amplitude and duration at noradrenergic synapses and is the target of ADRENERGIC UPTAKE INHIBITORS.Polymorphism, Genetic: The regular and simultaneous occurrence in a single interbreeding population of two or more discontinuous genotypes. The concept includes differences in genotypes ranging in size from a single nucleotide site (POLYMORPHISM, SINGLE NUCLEOTIDE) to large nucleotide sequences visible at a chromosomal level.Adrenergic Fibers: Nerve fibers liberating catecholamines at a synapse after an impulse.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Adrenergic Neurons: Neurons whose primary neurotransmitter is EPINEPHRINE.Nadolol: A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.Hemodynamics: The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM.Protein Binding: 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.Catechols: A group of 1,2-benzenediols that contain the general formula R-C6H5O2.Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.PC12 Cells: A CELL LINE derived from a PHEOCHROMOCYTOMA of the rat ADRENAL MEDULLA. PC12 cells stop dividing and undergo terminal differentiation when treated with NERVE GROWTH FACTOR, making the line a useful model system for NERVE CELL differentiation.Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)Paraganglioma, Extra-Adrenal: A relatively rare, usually benign neoplasm originating in the chemoreceptor tissue of the CAROTID BODY; GLOMUS JUGULARE; GLOMUS TYMPANICUM; AORTIC BODIES; and the female genital tract. It consists histologically of rounded or ovoid hyperchromatic cells that tend to be grouped in an alveolus-like pattern within a scant to moderate amount of fibrous stroma and a few large thin-walled vascular channels. (From Stedman, 27th ed)Nicotine: Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.Adrenalectomy: Excision of one or both adrenal glands. (From Dorland, 28th ed)Phenoxypropanolamines: Compounds based on a propanolamine attached via an OXYGEN atom to a phenoxy ring. The side chain is one carbon longer than PHENYLETHYLAMINES.Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.Exocytosis: Cellular release of material within membrane-limited vesicles by fusion of the vesicles with the CELL MEMBRANE.Vasoconstriction: The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.Acetylcholine: A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.Stress, Physiological: The unfavorable effect of environmental factors (stressors) on the physiological functions of an organism. Prolonged unresolved physiological stress can affect HOMEOSTASIS of the organism, and may lead to damaging or pathological conditions.Veratridine: A benzoate-cevane found in VERATRUM and Schoenocaulon. It activates SODIUM CHANNELS to stay open longer than normal.Animals, Newborn: Refers to animals in the period of time just after birth.Inositol Phosphates: Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.Perfusion: Treatment process involving the injection of fluid into an organ or tissue.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Endocytosis: Cellular uptake of extracellular materials within membrane-limited vacuoles or microvesicles. ENDOSOMES play a central role in endocytosis.Adipose Tissue, Brown: A thermogenic form of adipose tissue composed of BROWN ADIPOCYTES. It is found in newborns of many species including humans, and in hibernating mammals. Brown fat is richly vascularized, innervated, and densely packed with MITOCHONDRIA which can generate heat directly from the stored lipids.Ganglionic Blockers: Agents having as their major action the interruption of neural transmission at nicotinic receptors on postganglionic autonomic neurons. Because their actions are so broad, including blocking of sympathetic and parasympathetic systems, their therapeutic use has been largely supplanted by more specific drugs. They may still be used in the control of blood pressure in patients with acute dissecting aortic aneurysm and for the induction of hypotension in surgery.Synephrine: Sympathetic alpha-adrenergic agonist with actions like PHENYLEPHRINE. It is used as a vasoconstrictor in circulatory failure, asthma, nasal congestion, and glaucoma.Receptors, Muscarinic: 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.Down-Regulation: 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.Myocytes, Cardiac: Striated muscle cells found in the heart. They are derived from cardiac myoblasts (MYOBLASTS, CARDIAC).Denervation: The resection or removal of the nerve to an organ or part. (Dorland, 28th ed)Bucladesine: A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)Cold Temperature: An absence of warmth or heat or a temperature notably below an accustomed norm.Homovanillic AcidGuanylyl Imidodiphosphate: A non-hydrolyzable analog of GTP, in which the oxygen atom bridging the beta to the gamma phosphate is replaced by a nitrogen atom. It binds tightly to G-protein in the presence of Mg2+. The nucleotide is a potent stimulator of ADENYLYL CYCLASES.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Atropine: An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.Monoamine Oxidase: An enzyme that catalyzes the oxidative deamination of naturally occurring monoamines. It is a flavin-containing enzyme that is localized in mitochondrial membranes, whether in nerve terminals, the liver, or other organs. Monoamine oxidase is important in regulating the metabolic degradation of catecholamines and serotonin in neural or target tissues. Hepatic monoamine oxidase has a crucial defensive role in inactivating circulating monoamines or those, such as tyramine, that originate in the gut and are absorbed into the portal circulation. (From Goodman and Gilman's, The Pharmacological Basis of Therapeutics, 8th ed, p415) EC 126.96.36.199.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Cats: The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801)Potassium: An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Adenylate Cyclase Toxin: One of the virulence factors produced by virulent BORDETELLA organisms. It is a bifunctional protein with both ADENYLYL CYCLASES and hemolysin components.Turkeys: Large woodland game BIRDS in the subfamily Meleagridinae, family Phasianidae, order GALLIFORMES. Formerly they were considered a distinct family, Melegrididae.Dimethylphenylpiperazinium Iodide: A selective nicotinic cholinergic agonist used as a research tool. DMPP activates nicotinic receptors in autonomic ganglia but has little effect at the neuromuscular junction.Practolol: A beta-1 adrenergic antagonist that has been used in the emergency treatment of CARDIAC ARRYTHMIAS.Serotonin: A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.Mice, Knockout: Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.Rabbits: The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.Carbazoles: Benzo-indoles similar to CARBOLINES which are pyrido-indoles. In plants, carbazoles are derived from indole and form some of the INDOLE ALKALOIDS.Neurons: The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.Heart Ventricles: The lower right and left chambers of the heart. The right ventricle pumps venous BLOOD into the LUNGS and the left ventricle pumps oxygenated blood into the systemic arterial circulation.Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.Sodium: A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.Cardiomegaly: Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.TritiumAdipose Tissue: Specialized connective tissue composed of fat cells (ADIPOCYTES). It is the site of stored FATS, usually in the form of TRIGLYCERIDES. In mammals, there are two types of adipose tissue, the WHITE FAT and the BROWN FAT. Their relative distributions vary in different species with most adipose tissue being white.Dexmedetomidine: A imidazole derivative that is an agonist of ADRENERGIC ALPHA-2 RECEPTORS. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.Recombinant Fusion Proteins: 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.Brain Chemistry: Changes in the amounts of various chemicals (neurotransmitters, receptors, enzymes, and other metabolites) specific to the area of the central nervous system contained within the head. These are monitored over time, during sensory stimulation, or under different disease states.
Outline of cardiology
Catecholamines are a set of drugs and hormones that manipulate the adrenergic receptors. The natural catecholamines are ... The adrenergic receptor is a set of receptors that are commonly manipulated. Four properties of the heart - chronotropy, ... are manipulated by adrenergic receptors. For example, the β1 receptor increases all four of these properties: chrontropy at the ... that manipulate the adrenergic receptors and have variable specificity for the receptors and are, thus, used for various ...
It works by stimulating beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... as with other catecholamines. Dopexamine may potentiate the effects of other catecholamines like noradrenaline. Effects of ... Dopexamine stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... ß2-adrenergic and dopamine receptor antagonists requires caution. The half-life of IV dopexamine is 6-7 minutes in healthy ...
Another way to inhibit adrenergic receptor signaling is by blocking the synthesis of catecholamines. Methyltyrosine, for ... inhibiting the downstream cellular signaling pathways of adrenergic receptors. However, there are exceptions: clonidine is an ... They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... adrenergic agonist at the α2 receptor; since this receptor is located presynaptically, agonism at this receptor inhibits the ...
... known as alpha and beta adrenergic receptors. Alpha receptors are divided into subtypes α1 and α2; beta receptors into subtypes ... Norepinephrine is a catecholamine and a phenethylamine. Its structure differs from that of epinephrine only in that epinephrine ... McCrink KA, Brill A, Lymperopoulos A (2015). "Adrenal G protein-coupled receptor kinase-2 in regulation of sympathetic nervous ... ISBN 1-4684-3171-4. Griffith RK (2013). "Chapter 10: Adrenergic Receptors and Drugs Affecting Adrenergic Neurotransmission". In ...
G beta-gamma complex
"Role of beta gamma subunits of G proteins in targeting the beta-adrenergic receptor kinase to membrane-bound receptors". ... failure there are sustained and elevated levels of catecholamines which result in chronic desensitization of the βAR receptor. ... Heart failure can be characterized by a loss of β adrenergic receptor (βAR) signalling in heart cells. When the βAR is ... June 1998). "Expression of a beta-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene ...
... is controlled through the balanced control of lipolytic B-adrenergic receptors and a2A-adrenergic receptor-mediated ... Release of catecholamines from sympathetic nerves results in UCP1 activation and usually occurs after extended periods of cold ... UCP1 activity is stimulated by long chain fatty acids that are produced subsequent to β-adrenergic receptor activation. UCP1 is ... Farooqi IS, O'Rahilly S (Oct 2008). "Mutations in ligands and receptors of the leptin-melanocortin pathway that lead to obesity ...
... and β2-adrenergic receptors preventing activation of the receptors by their stimulatory ligand (catecholamines). Without the ... Sotalol is a non-selective competitive beta-adrenergic receptor blocker that also exhibits Class III antiarrhythmic properties ... Beta receptor blockade potentiates the antiarryhthmic actions of d-sotalol on re-entrant ventricular tachycardia in a canine ... As with other beta blockers, it may interact with calcium channel blockers, catecholamine-depleting drugs, insulin or ...
Alfred G. Gilman
beta-Adrenergic and PGE1 receptors in parental and hybrid cells". The Journal of Biological Chemistry. 252 (4): 1293-302. PMID ... "The crystal structure of β2-adrenergic receptor, a classic GPCR was at last revealed". Nature. 450: 355-356. doi:10.1038/ ... Sternweis, PC; Gilman, AG (1979). "Reconstitution of catecholamine-sensitive adenylate cyclase. Reconstitution of the uncoupled ... Haga, T; Haga, K; Gilman, AG (1977). "Hydrodynamic properties of the beta-adrenergic receptor and adenylate cyclase from wild ...
... adrenergic receptor blocker and competes with other Catecholamines for binding to these sites. Its action on these receptors ... Labetalol is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... Labetalol was the first drug created that combined both alpha- and beta- adrenergic receptor blocking properties. It was ... Labetalol acts by blocking alpha and beta adrenergic receptors, resulting in decreased peripheral vascular resistance without ...
Smooth muscle tissue
... muscle respond to these catecholamines producing vasodilation because the smooth muscle possess beta-adrenergic receptors. So ... The Notch receptor and cell-signaling pathway have been demonstrated to be essential to vasculogenesis and the formation of ... muscarinic receptors, adrenergic receptors), second messenger generators (adenylate cyclase, phospholipase C), G proteins (RhoA ... this response is mediated through alpha-1 adrenergic receptors). However, blood vessels within skeletal muscle and cardiac ...
... then it will favor the alpha adrenergic receptors. Direct stimulation of the α- and β-adrenergic receptors can produce ... Chemical structures of the catecholamines. Sympathomimetic drugs (also known as adrenergic drugs and adrenergic amines) are ... Also, if the amine has bulky substituents, then it will have greater beta adrenergic receptor activity, but if the substituent ... β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs ...
... is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ... When β1 receptors are activated by a catecholamine, they stimulate a coupled G protein which activates adenylyl to convert ... Like propanolol and pindolol, it is a serotonin 5-HT1A and 5-HT1B receptor antagonist; this discovery by several groups in the ... Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ...
Norepinephrine binds to the beta-1 receptor. High blood pressure medications are used to block these receptors and so reduce ... Epinephrine and norepinephrine have similar effects: binding to the beta-1 adrenergic receptors, and opening sodium and calcium ... The catecholamines, epinephrine and norepinephrine, secreted by the adrenal medulla form one component of the extended fight-or ... Among these receptors are various proprioreceptors, baroreceptors, and chemoreceptors, plus stimuli from the limbic system ...
Interest in catecholamines and their receptors dominated the Porto Department in the 1960s. Work just before Guimarães' entry ... S. Guimarães, W. Osswald (1969). "Adrenergic receptors in the veins of the dog". European Journal of Pharmacology. 5 (2): 188- ... Influence of factors which interfere with the concentrations of agonists at the receptor level". European Journal of ... alpha inhibitory and beta inhibitory adrenergic receptors in the guinea-pig stomach". Archives internationales de ...
The alpha-1 adrenergic receptor is specifically implicated. Although it has not yet been thoroughly investigated, there is ... Norepinephrine, also known as noradrenalin, is a catecholamine neurotransmitter. Administering a norepinephrine receptor ... these findings are based on the effects of other commonly prescribed drugs that happen to block noradrenergic receptors. ... agonist (a substance that initiates a cell response when it binds with a receptor) to patients promoted the recovery of memory ...
Peter J. Barnes (respiratory scientist)
... the role of endogenous catecholamines (particularly epinephrine), adrenergic receptors and the role of cholinergic neural ... "Glucocorticoid receptor recruitment of histone deacetylase 2 inhibits IL-1β-induced histone H4 acetylation on lysines 8 and 12 ... He was the first to map the distribution of receptors in the lung using radioligand autoradiography. His group investigated the ... His research initially focussed on adrenergic regulation of the airways, ...
July 2000). "The effect of polymorphisms of the beta(2)-adrenergic receptor on the response to regular use of albuterol in ... results in greater receptor downregulation by endogenous catecholamines at baseline compared to Arg-16. This results in a ... Ličko V (1985). "Drugs, Receptors and Tolerance". Pharmacokinetics and Pharmacodynamics of Psychoactive Drugs. pp. 311-322. ... Inhalation of an agonist for the beta-2 adrenergic receptor, such as Salbutamol, Albuterol (US), is the most common treatment ...
Serotonin-norepinephrine-dopamine reuptake inhibitor
... at functionally important adrenergic receptor sites in the brain. However, elation may be associated with an excess of such ... It was also supported by work demonstrating that if catecholamine levels were depleted by up to 20% but 5-HT neurotransmission ... Cocaine is a short-acting SNDRI that also exerts auxiliary pharmacological actions on other receptors. Cocaine is a relatively ... Tetrabenazine, a similar agent to reserpine, which also depletes catecholamine stores, and to a lesser degree 5-HT, was shown ...
... via the activity of β-adrenergic receptors. CREB then is able to up-regulate the transcription of many different genes. Thus, ... For example catecholamines, the class of neurotransmitters that includes dopamine and norepinephrine, have been linked with ... childhood maltreatment in rodent models and humans has been shown to alter the epigenetics of the glucocorticoid receptor gene ... through effects of canonical neurotransmitter systems such as catecholamines, social stressors are able to penetrate the ...
Premature ventricular contraction
... which can bind to beta-1 adrenergic receptor (β1 receptors) on cardiac myocytes, activating a type of guanosine nucleotide- ... This process is the underlying mechanism for arrhythmias due to excess catecholamines and some electrolyte deficiencies, ... This activation can cause a release of catecholamines such as epinephrine (adrenaline) ...
... causing excessive stimulation of adrenergic receptors, which results in peripheral vasoconstriction and cardiac stimulation. ... Schäfer SG, Kaan EC, Christen MO, Löw-Kröger A, Mest HJ, Molderings GJ (July 1995). "Why imidazoline receptor modulator in the ... ISBN 1-58562-239-7. Kassim TA, Clarke DD, Mai VQ, Clyde PW, Mohamed Shakir KM (December 2008). "Catecholamine-induced ... At high concentrations cortisol can cross-react and activate the mineralocorticoid receptor, leading to aldosterone-like ...
... of the chromaffin cells to catecholamines resulting in a decrease in production and presence of α2 adrenergic receptors on ... and downregulation of α2 adrenergic receptors is caused by the upregulation of the enzyme Adrenal G protein coupled receptor ... This causes the release of catecholamines. The chromaffin cells release catecholamines: ~80% of Adrenaline (Epinephrine) and ~ ... Chromium salts oxidise and polymerise catecholamines to form a brown color, most strongly in the cells secreting noradrenaline ...
Discovery and development of beta-blockers
β-blockers cause a competitive inhibition of the β-receptor, which counters the effects of catecholamines. β1 and β2-receptors ... 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 ... Some β-blockers partially activate the receptor while preventing catecholamines from binding to the receptor, making them ...
... because insulin release is inhibited by α2-adrenergic receptors and stimulated by β2-adrenergic receptors. The net effect of ... The effects of insulin are initiated by its binding to a receptor present in the cell membrane. The receptor molecule contains ... It appears that release of catecholamines by the sympathetic nervous system has conflicting influences on insulin release by ... Jang WG, Kim EJ, Park KG, Park YB, Choi HS, Kim HJ, Kim YD, Kim KS, Lee KU, Lee IK (January 2007). "Glucocorticoid receptor ...
... which leads to the activation of protein kinase C triggering the endocytosis of b-adrenergic receptors, which in turn leads to ... It was revealed that an increased expression of uPA and its receptor (uPAR) occurred in damaged vessel cells. This process was ... influence on the development of both cell hypersensitivity and cell tolerance to catecholamine and medication. It was revealed ... In the 90s, a group directed by V. A. Tkachuk published a number of papers on stretching receptors' involvement in specific ...
... β2 and β3 receptors. β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors are ... Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine ( ... β3-adrenergic receptors are located in fat cells. Beta receptors are found on cells of the heart muscles, smooth muscles, ... Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta ...
List of MeSH codes (D12.776.543)
... receptors, catecholamine MeSH D12.776.543.750.720.300.300.300 -- receptors, adrenergic MeSH D12.776.543.750.720.300.300.300.300 ... receptor, cannabinoid, cb2 MeSH D12.776.543.7188.8.131.520 -- receptors, adrenergic MeSH D12.776.543.7184.108.40.2060.300 -- ... receptors, catecholamine MeSH D12.776.543.750.070.300.300 -- receptors, adrenergic MeSH D12.776.543.750.070.300.300.300 -- ... receptors, adrenergic, alpha-1 MeSH D12.776.543.750.070.300.300.300.725 -- receptors, adrenergic, alpha-2 MeSH D12.776.543.750. ...
... such as a biological receptor (specifically, the adrenergic receptors). Directly acting adrenergic agonists act on adrenergic ... Inhibitors of these enzymes act as indirect agonists of adrenergic receptors as they prolong the action of catecholamines at ... All adrenergic receptors are G-protein coupled, activating signal transduction pathways. The G-protein receptor can affect the ... A great number of drugs are available which can affect adrenergic receptors. Each drug has its own receptor specificity giving ...
History of catecholamine research
... now β-adrenoceptor or β-adrenergic receptor). ″This concept of two fundamental types of receptors is directly opposed to the ... he called alpha adrenotropic receptor (now α-adrenoceptor or α-adrenergic receptor), while the receptor with the second rank ... catecholamines must pass through membranes and deliver their chemical message at membrane receptors. Catecholamines are ... that the adrenotropic inhibitory receptors and the cardiac chronotropic and inotropic adrenergic receptors are functionally ...
The adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines, ... Basic Neurochemistry: α- and β-Adrenergic Receptors Brief overview of functions of the β3 receptor Theory of receptor ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... ISBN 0-443-06911-5. Alpha receptors illustrated The Adrenergic Receptors "Adrenoceptors". IUPHAR Database of Receptors and Ion ...
Using a β2 adrenergic receptor preparation derived from transfected HEK 293 cells, Liappakis and co-workers found that in wild- ... These results led the authors to suggest that N-methylphenylethanolamine was acting on both α and β adrenergic receptors. ... J. Armstrong and R. B. Barlow (1976). "The ionization of phenolic amines, including apomorphine, dopamine and catecholamines ... Considered to be an antagonist of β1 and β2 receptors, and an agonist of β3 receptors. J.Axelrod (1962). "Purification and ...
Receptors. Varies greatly across species;. Human receptors: hTAAR1 and hTAAR2. ... FMO3 catalyzes the oxidation of catecholamine or catecholamine-releasing vasopressors, including tyramine, phenylethylamine, ... Leffler, Esther B.; Spencer, Hugh M.; Burger, Alfred (1951). "Dissociation Constants of Adrenergic Amines". Journal of the ... and PEA and p-TA have been reported to depress GABAB receptor-mediated responses in dopaminergic neurons (22,23). Although PEA ...
Posttraumatic stress disorder
Brain catecholamine levels are high, and corticotropin-releasing factor (CRF) concentrations are high. Together, ... Overactivation of norepinephrine receptors in the prefrontal cortex can be connected to the flashbacks and nightmares ... Yehuda R, Halligan SL, Grossman R, Golier JA, Wong C (September 2002). "The cortisol and glucocorticoid receptor response to ... adrenergic inhibitors, antipsychotics, and even anticonvulsants), benzodiazepines should be considered relatively ...
Red blood cell
... β-adrenergic receptors. Lipid rafts that have been implicated in cell signaling events in nonerythroid cells have been shown in ... Inhibitors of eryptosis include erythropoietin, nitric oxide, catecholamines and high concentrations of urea. ... erythroid cells to mediate β2-adregenic receptor signaling and increase cAMP levels, and thus regulating entry of malarial ... as signaling receptors, as well as other currently unknown functions. The blood types of humans are due to variations in ...
Serotonin-norepinephrine reuptake inhibitor
Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors. ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ... Throughout the 1960s and 1970s, the catecholamine hypothesis of emotion and its relation to depression was of wide interest and ... In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ...
Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... Nicotine exerts its effects through the agonism of nicotinic acetylcholine receptor, resulting in multiple downstream effects ... with its most pronounced effects targeting the catecholamine neurotransmitters norepinephrine and dopamine. At therapeutic ... on adrenergic receptors. It is most usually marketed as the hydrochloride or sulfate salt. ...
Epinephrine acts by binding to a variety of adrenergic receptors. Epinephrine is a nonselective agonist of all adrenergic ... α1 receptor-dependent vasoconstriction and to increase cardiac output via its binding to β1 receptors. The goal of reducing ... Main article: History of catecholamine research. Extracts of the adrenal gland were first obtained by Polish physiologist ... Epinephrine's binding to these receptors triggers a number of metabolic changes. Binding to α-adrenergic receptors inhibits ...
In vertebrates, melatonin secretion is regulated by activation of the beta-1 adrenergic receptor by norepinephrine. ... "Melatonin receptors , G protein-coupled receptors , IUPHAR/BPS Guide to Pharmacology". www.guidetopharmacology.org. Retrieved 7 ... the enzyme for catecholamine and serotonin biosynthesis". Biochemistry. 31 (8): 2229-38. doi:10.1021/bi00123a004. PMID 1540578. ... In humans, melatonin is a full agonist of melatonin receptor 1 (picomolar binding affinity) and melatonin receptor 2 (nanomolar ...
Examples include beta adrenergic stimulation, stimulation of the glucagon receptor and ACTH stimulation of the ACTH receptor in ... HSL is activated when the body needs to mobilize energy stores, and so responds positively to catecholamines, ACTH. It is ... which itself is provided by the activation of Gs protein-coupled receptors that promote cAMP production. ... 2002). "C3, hormone-sensitive lipase, and peroxisome proliferator-activated receptor gamma expression in adipose tissue of ...
... is controlled through the balanced control of lipolytic B-adrenergic receptors and a2A-adrenergic receptor-mediated ... BAT is robustly activated upon cold exposure by the release of catecholamines from sympathetic nerves that results in UCP1 ... β-adrenergic receptor activation. UCP1 is proposed to function as a fatty acid proton symporter, although the exact ... Several mutations of genes involving the melanocortins (used in brain signaling associated with appetite) and their receptors ...
The adrenergic substances released by the sympathetic nervous system can also bind to and influence various immunological cells ... The secretion of ACTH into systemic circulation allows it to bind to and activate Melanocortin receptor, where it stimulates ... Multiple CRH peptides have been identified, and receptors have been identified on multiple areas of the brain, including the ... During this stage, the locus coeruleus/sympathetic nervous system is activated and catecholamines such as adrenaline are being ...
... β2 and β3 receptors. β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors ... Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine ( ... β3-adrenergic receptors are located in fat cells.. Beta receptors are found on cells of the heart muscles, smooth muscles, ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, ...
The adrenergic substances released by the sympathetic nervous system can also bind to and influence various immunological cells ... The secretion of ACTH into systemic circulation allows it to bind to and activate Melanocortin receptor, where it stimulates ... Multiple CRH peptides have been identified, and receptors have been identified on multiple areas of the brain, including the ... During this stage, the locus coeruleus and sympathetic nervous system activate the production of catecholamines including ...
The potency of synephrine at adrenergic receptors of the β-class (regardless of sub-type) is much lower than at α-receptors. ... Although clearly indicating a selectivity of synephrine for α1 receptors, its potency at this receptor sub-class is still ... Biosynthetic pathways for catecholamines and trace amines in the human brain ... An adrenergic antagonist selective for α1 receptors. *^ Reversal of reserpine-induced hypothermia by a drug is a classical test ...
Main article: Thyroid hormone receptor. The thyroid hormones function via a well-studied set of nuclear receptors, termed the ... the contribution of adrenergic activity to hypermetabolism and protein breakdown". Metabolism: Clinical and Experimental. 36 (6 ... and increase the body's sensitivity to catecholamines (such as adrenaline) by permissiveness. The thyroid hormones are ... This receptor-corepressor-DNA complex can block gene transcription. When triiodothyronine (T3) binds a receptor, it induces a ...
"A β2 adrenergic receptor signaling complex assembled with the Ca2+ channel Cav1.2". Science. 293 (5527): 98-101. doi:10.1126/ ... G protein-coupled receptors (GPCRs) are a large family of integral membrane proteins that respond to a variety of extracellular ... Each GPCR binds to and is activated by a specific ligand stimulus that ranges in size from small molecule catecholamines, ... of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor trafficking through PKA phosphorylation of the Glu receptor 1 ...
Posttraumatic stress disorder
Brain catecholamine levels are high, and corticotropin-releasing factor (CRF) concentrations are high. Together, ... Overactivation of norepinephrine receptors in the prefrontal cortex can be connected to the flashbacks and nightmares ... Prazosin, an alpha-1 adrenergic antagonist, has been used in veterans with PTSD to reduce nightmares. Studies show variability ... Yehuda R, Halligan SL, Grossman R, Golier JA, Wong C (September 2002). "The cortisol and glucocorticoid receptor response to ...
In some cases, obesity in individuals is due to the overproduction of corticoids leads to the over-activation of receptor type ... Under normal conditions, adrenal hormone receptors, type I and type II, mediate the storage of carbohydrates and fats during ... In such cases, curative agents such as adrenergic agonists and antagonists are used to modify epinephrine and norepinephrine ... Glucocorticoids work to inhibit the uptake of catecholamines, like norepinephrine and epinephrine, by the nerves. The increase ...
Raymond C. Stevens
2013: Serotonin receptors 5-HT1B and 5-HT2B, the second HIV co-receptor, C-C chemokine receptor type 5 (CCR5) and the first ... The β2-adrenergic receptor work was quickly followed up 9 months later by the determination of the structure of the human A2A ... In parallel to the work on botulinum toxin, Stevens worked on the enzymes involved in the catecholamine biosynthetic pathway, ... 2016: The marijuana receptor-human Cannabinoid receptor type 1 (CB1) and the human C-C chemokine receptor type 2 (CCR2) In ...
This suggests that in schizophrenia, the alpha-2 adrenergic receptor, a presynaptic inhibitory receptor, may be less sensitive ... block reabsorption of the catecholamines dopamine and norepinephrine through monoamine transporters (including NET), thereby ... compared to normally functioning alpha-2 receptors and thus relate to elevated NE levels in the disorder. In addition to ...
FMO3 catalyzes the oxidation of catecholamine or catecholamine-releasing vasopressors, including tyramine, phenylethylamine, ... Phenethylamine has been shown to bind to two human trace amine-associated receptors, hTAAR1 and hTAAR2, as an agonist. By oral ... Pei Y, Asif-Malik A, Canales JJ (April 2016). "Trace Amines and the Trace Amine-Associated Receptor 1: Pharmacology, ... "Dissociation Constants of Adrenergic Amines". Journal of the American Chemical Society. 73 (6): 2611-3. doi:10.1021/ja01150a055 ...
Norepinephrine elevates the intracellular cAMP concentration via beta-adrenergic receptors and activates the cAMP-dependent ... 5-Methoxytryptamine 6-Hydroxymelatonin Agomelatine Health effects of sunlight exposure Melatonin receptor agonist#Drug design ... the enzyme for catecholamine and serotonin biosynthesis". Biochemistry. 31 (8): 2229-38. doi:10.1021/bi00123a004. PMID 1540578 ... "Melatonin receptors , G protein-coupled receptors , IUPHAR/BPS Guide to Pharmacology". www.guidetopharmacology.org. Retrieved ...
Prazosin has been established as an effective and safe, brain active alpha-1 adrenergic receptor antagonist. It can be used ... It happens because alpha 1 blockers inhibit the activation of post-synaptic alpha-1 receptors by releasing catecholamines and/ ... Alpha-1 blocker lowers the blood pressure by blocking alpha-1 receptors so norepinephrine can't bind the receptor and it causes ... Silodosin shows high affinity and selectivity for alpha-1a adrenergic receptors found in the prostate which ensures that it ...
... adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and ... nadolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Like ... PubChem) Pharmacology: Nadolol is a nonselective beta-adrenergic receptor antagonist with a long half-life, and is structurally ... It also blocks beta-2 adrenergic receptors located in bronchiole smooth muscle, causing vasoconstriction. By binding beta-2 ...
Ronald T. Borchardt | School of Pharmacy
3. E. E. Smissman and R. T. Borchardt, "A Conformational Study of Catecholamine Receptor Sites. V. The Synthesis of dl-3-Amino- ... Conformationally Defined Adrenergic Agents 5", Mol. Pharmacol., 20, 377-381 (1981).. 87. L. E. Eiden, R. T. Borchardt and C. O ... R. G. Rosenfeld, H. Pham, B. Keller, R. T. Borchardt and W. M. Pardridge, "Structural Comparison of Receptors for Insulin, ... 4. E. E. Smissman and R. T. Borchardt, "A Conformational Study of Catecholamine Receptor Sites. VI. The Synthesis of dl-3-Amino ...
Catecholamines, Cardiac β-Adrenergic Receptors, and Heart Failure | Circulation
Assessment of the β-adrenergic receptor pathway on the intact failing human heart: progressive receptor down regulation and ... Catecholamines, Cardiac β-Adrenergic Receptors, and Heart Failure. Robert J. Lefkowitz, Howard A. Rockman, Walter J. Koch ... Reciprocal in vivo regulation of myocardial G protein-coupled receptor kinase expression by β-adrenergic receptor stimulation ... The β2-adrenergic receptor interacts with the Na+/H+-exchanger regulatory factor to control Na+/H+ exchange. Nature. 1998;392: ...
β-Adrenergic Receptor Kinase-1 Levels in Catecholamine-Induced Myocardial Hypertrophy
... which phosphorylates and desensitizes β-adrenergic receptors. In this study, we examined whether increased β-adrenergic ... β-adrenergic receptor kinase-1 protein levels, whereas 24 hours of phenylephrine treatment did not alter β-adrenergic receptor ... 1999). "β-Adrenergic Receptor Kinase-1 Levels in Catecholamine-Induced Myocardial Hypertrophy." Hypertension 33(1): 396-401. ... receptor signaling due to increased levels of the β-adrenergic receptor kinase-1, ...
Endocrine Effects on Bone
Leptin induces catecholamine secretion from the hypothalamus. n Osteoblasts express beta-adrenergic receptors. n Isoproterenol ... Hormone deficiency and/or receptor malfunction. n Ovariectomy. n Menopause. n Excessive exercise. n Poor nutrition. n Low ... Similar levels of estrogen and androgen receptors in bone cells of males and females, some possibility that the receptors are ... B-ad receptor agonist) reduces bone mass in ob/ob and normal mice. n Propranolol (B-ad receptor antagonist) increased bone mass ...
Cardiac-Specific Ablation of G-Protein Receptor Kinase 2 Redefines Its Roles in Heart Development and β-Adrenergic Signaling |...
G-protein receptor kinase 2 (GRK2) is 1 of 7 mammalian GRKs that phosphorylate ligand-bound 7-transmembrane receptors, causing ... Cardiomyocyte GRK2 Protects Against Catecholamine Cardiomyopathy. Unrestrained β-AR stimulation, as with forced receptor ... Physiological induction of a beta-adrenergic receptor kinase inhibitor transgene preserves beta-adrenergic responsiveness in ... Cardiac-Specific Ablation of G-Protein Receptor Kinase 2 Redefines Its Roles in Heart Development and β-Adrenergic Signaling. ...
Methylphenidate and atomoxetine enhance prefrontal function through α2-adrenergic and dopamine D1 receptors. - PubMed - NCBI
... receptor stimulation. (E) A working model of catecholamine influences on prefrontal cortical network connectivity. Under ... Methylphenidate and atomoxetine enhance prefrontal function through α2-adrenergic and dopamine D1 receptors.. Gamo NJ1, Wang M ... Methylphenidate and Atomoxetine Enhance Prefrontal Function Through α2-Adrenergic and Dopamine D1 Receptors ... Methylphenidate and Atomoxetine Enhance Prefrontal Function Through α2-Adrenergic and Dopamine D1 Receptors ...
Blockade of catecholamine-induced growth by adrenergic and dopaminergic receptor antagonists in Escherichia coli O157:H7,...
NE and Epi bind to adrenergic-type receptors while Dop binds to dopaminergic-type receptors. The adrenergic receptors are ... adrenergic receptors. This differential ability to stimulate one or other adrenergic receptor subtype ultimately determines the ... suggesting that the QseC and QseE receptors have catecholamine binding sites with dual α and β adrenergic catecholamine ... CatecholaminePrazosinAdrenergic ReceptorLabetalolEnteric Nervous System. Background. During the past decade, there has been ...
The effect of dilevalol on cardiac autonomic neural discharge, plasma catecholamines, and myocardial beta receptor density...
0/Adrenergic beta-Antagonists; 0/Catecholamines; 0/Receptors, Adrenergic, beta; 36894-69-6/Labetalol; 51-41-2/Norepinephrine; ... The effect of dilevalol on cardiac autonomic neural discharge, plasma catecholamines, and myocardial beta receptor density ... Catecholamines / blood*. Cats. Coronary Vessels / physiology. Electrophysiology. Epinephrine / blood. Heart Rate / drug effects ... Adrenergic beta-Antagonists / pharmacology*. Animals. Autonomic Nervous System / drug effects*. Blood Pressure / drug effects. ...
Upregulation of phagocyte-derived catecholamines augments the acute inflammatory response.
... are newly discovered sources of catecholamines, we now show that both epinephrine and norepinephrine directly activate NFkappaB ... Following interaction with adrenergic receptors, the physiological actions of catecholamines can be terminated by cellular ... suggesting that it is adrenergic receptor engagement rather than cortical mineralocorticoid or glucocorticoid receptor ... As shown in Figure 8, blockade of the α2-adrenergic receptor significantly reduced by 70% (p,0.01) the intensity of the albumin ...
Atypical Reactions Associated With Heroin Use --- Five States, January--April 2005
Catecholamines, sympathomimetic drugs, and adrenergic receptor antagonists. In: Gilman AG, Hardman JG, Limbird LE, eds. Goodman ... b2 adrenergic receptors and clinical manifestations, including hypokalemia, hyperglycemia, hyperlactemia, agitation, ... Clenbuterol is a b2 adrenergic receptor agonist with a rapid onset and long duration of action approved for limited veterinary ... a b2 adrenergic receptor agonist, was reported. Information regarding the atypical reactions to heroin use was disseminated by ...
Anaesthesia and Intensive Care A-Z | ElsevierAsia - English
kidney). Stimulates both a- and b-adrenergic receptors; displays a-Adrenergic receptor antagonists (a-Blockers). Usu- ... b2-adrenergic receptors. Dopamine and dobutamine act Adrenaline (Epinephrine). Catecholamine, acting as a hor- mainly at b1- ... Celiprolol Methoxamine and phenylephrine are synthetic a1-receptor has b1-receptor antagonist and b2-receptor agonist prop- ... and a2-adrenergic receptors. but all will block b2-receptors at high doses. ...
Catecholamine-induced vasoconstriction is sensitive to carbonic anhydrase I activation
... the first consists of adrenergic agonists acting on their specific receptors with subsequent formation of a stimulus-receptor ... 1. Hoffman BB & Lefkowitz RJ (1996). Catecholamines, sympathomimetic drugs, and adrenergic receptor antagonists. In: Molinoff ... the first one consists of a catecholamine action on its receptor with the formation of a stimulus-receptor complex. The second ... 5. Kobilka BK (1987). Cloning, sequencing and expression of the gene coding for the human platelet alpha1-adrenergic receptor. ...
Outline of cardiology - Wikipedia
Catecholamines are a set of drugs and hormones that manipulate the adrenergic receptors. The natural catecholamines are ... The adrenergic receptor is a set of receptors that are commonly manipulated. Four properties of the heart - chronotropy, ... are manipulated by adrenergic receptors. For example, the β1 receptor increases all four of these properties: chrontropy at the ... that manipulate the adrenergic receptors and have variable specificity for the receptors and are, thus, used for various ...
Uncoupling between beta-adrenoceptors and adenylate cyclase in dog ischemic myocardium | SpringerLink
... β-adrenergic receptors. Internalized receptors reconstitute catecholamine stimulated adenylate cyclase activity. J Biol Chem ... β-adrenergic receptor and in the actions of catecholamines and cholera toxin on adenylate cyclase in turkey erythrocyte ... β-adrenergic receptor complex is an intermediate for catecholamine stimulation of adenylate cyclase in turkey and frog ... Mukherjee A, Bush LR, Mc Coy KE, Duke RJ, Hagler H, Buja LM, Willerson JT (1982) Relationship between beta-adrenergic receptor ...
The Campus Coffee Shop: Caffeine Conundrums by Zion Walker on Prezi
Antagonist Receptor. An antagonist is a drug that occupied receptors but do not activate them. Antagonists block receptors ... Catecholamines are hormones made by the adrenal glands. A common type being epinephrine, it acts by binding to adrenergic ... G-protein coupled receptors. -integral plasma membrane proteins that convert signals from extra cellular ligands to signal ... Caffeine, when acting as an antagonist, is doing the oppsite of activation of adenosine receptors.. Where Caffeine Acts. ...
The Role of Testosterone in the Etiology and Treatment of Obesity, the Metabolic Syndrome, and Diabetes Mellitus Type 2
Hormones affect the catecholamine receptors of the adipocytes. Testosterone stimulates the -adrenergic receptor while estrogens ... Catecholamines stimulate lipolysis via the -adrenergic receptor while 2-adrenoreceptors inhibit lipolysis. ... It is now known that estrogen receptors, progesterone receptors, and androgen receptors exist in adipose tissues, so their ... Androgen receptor CAG repeat polymorphism appears associated with serum testosterone levels, obesity, and serum leptin in men ...
Popular Ergogenic Drugs and Supplements in Young Athletes | American Academy of Pediatrics
Catecholamines, sympathomimetic drugs and adrenergic receptor antagonists. In: Hardman JG, Limbird LE, eds. Goodman and ... Binding androgen receptors promotes a positive nitrogen balance in muscle, which produces an anabolic state.22 However, in the ... It possesses α and β adrenergic agonistic effects, enhances the release of norepinephrine, and stimulates the central nervous ... 20 Steroids bind to androgen receptors within the cell cytoplasm. They then are transported into the nucleus before binding DNA ...
Norepinephrine - Trip Database
Beta1-adrenergic receptor blockade attenuates angiotensin II-mediated catecholamine release into the cardiac interstitium in ... response to norepinephrine in septic patients has directed our interest to the regulation of alpha1-adrenergic receptors in ... Beta1-adrenergic receptor blockade attenuates angiotensin II-mediated catecholamine release into the cardiac interstitium in ... Cytokines down-regulate alpha1-adrenergic receptor expression during endotoxemia. (Abstract). Cytokines down-regulate alpha1- ...
Dopexamine - Wikipedia
It works by stimulating beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... as with other catecholamines. Dopexamine may potentiate the effects of other catecholamines like noradrenaline. Effects of ... Dopexamine stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... ß2-adrenergic and dopamine receptor antagonists requires caution. The half-life of IV dopexamine is 6-7 minutes in healthy ...
MEDLINE - Resultado p gina 1
0 (Adrenergic Antagonists); 0 (Catecholamines); 0 (Receptors, Adrenergic); 0 (TRPV Cation Channels); 0 (Trpv1 protein, rat); ... with TRPV1 receptor as an important downstream effector. It is already known that adrenergic sensitization of TRPV1 receptors ... Receptors, Adrenergic); 0 (Receptors, Dopamine); 0 (Receptors, Serotonin); 0 (SCH 23390); 0 (Serotonin Antagonists); 0 ( ... 0 (Adrenergic Antagonists); 0 (Carbazoles); 0 (Piperazines); 0 (Receptors, Adrenergic, alpha-1); 0P2197HHHN (carbazole). ...
β-Blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation | PNAS
Beta-adrenergic receptors (βARs) are members of the seven transmembrane receptor (7TMR) family that become activated upon ... 2000) Catecholamines, cardiac beta-adrenergic receptors, and heart failure. Circulation 101:1634-1637. ... 2004) Comparative pharmacology of human beta-adrenergic receptor subtypes-characterization of stably transfected receptors in ... 2003) Protein kinase A and G protein-coupled receptor kinase phosphorylation mediates beta-1 adrenergic receptor endocytosis ...
Metformin Hydrochloride Monograph for Professionals - Drugs.com
Catecholamines, sympoathomimetic drugs, and adrenergic receptor antagonists. In: Hardman JG, Limbird LE, Molinoff PB et al, eds ... Comparison of the in vitro effect of biguanides and sulfonylureas on insulin binding to its receptors in target cells. J Clin ... If concomitant therapy necessary, a β1-selective adrenergic blocking agent or β-adrenergic blocking agents with intrinsic ... β-Adrenergic blocking agents. May impair glucose tolerance; 73 143 152 153 159 may increase frequency or severity of ...
JCI - Death begets failure in the heart
Catecholamines, cardiac beta-adrenergic receptors, and heart failure. Circulation. 2000. 101:1634-1637. View this article via: ... Beta-adrenergic signaling in the heart: dual coupling of the beta2- adrenergic receptor to G(s) and G(i) proteins. Sci. STKE. ... Several receptor/enzyme pathways influence survival in cardiomyocytes. In fact, β-adrenergic receptor antagonists and ... The beta(2)-adrenergic receptor delivers an antiapoptotic signal to cardiac myocytes through G(i)-dependent coupling to ...
PSL301: Cardio 2 Flashcards by Airi - | Brainscape
Patent US4532331 - 1-Benzyl-2-aminomethyl imidazole derivatives - Google Patents
55, 39 (1980), reviews compounds which inhibit catecholamine activity by interfering with adrenergic receptors. Alternatively, ... Angiotensin II receptor blocking imidazoles. US5153197 *. Nov 13, 1989. Oct 6, 1992. E. I. Du Pont De Nemours And Company. ... Inhibition of catecholamine activity has been found to decrease hypertension. See, for example, Matta et al., Clin. Pharm. ... In the catecholamine biosynthetic pathway, tyrosine is converted in three steps to norephinephrine (NE). Intermediates are ...
Familial Dysautonomia Medication: Benzodiazepines, H2 receptor antagonists, Alpha-adrenergic agonists, Corticosteroids
H2 receptor antagonists. Class Summary. These agents are reversible competitive blockers of histamine at the H2 receptors, ... Pattern of plasma levels of catecholamines in familial dysautonomia. Clin Auton Res. 1996 Aug. 6(4):205-9. [Medline]. ... Alpha-adrenergic agonists. Class Summary. These agents stimulate alpha-adrenoreceptors in brain stem, activating an inhibitory ... A central alpha-adrenergic agonist that suppresses peripheral release of norepinephrine, resulting in lower blood pressure; ...
Receptors, Adrenergic, beta-2 | Harvard Catalyst Profiles | Harvard Catalyst
The Sympathetic Nervous System Mitigates CNS Autoimmunity via ß2-Adrenergic Receptor Signaling in Immune Cells. Cell Rep. 2019 ... Receptors, Biogenic Amine [D12.776.543.750.070]. *Receptors, Catecholamine [D12.776.543.750.070.300]. *Receptors, Adrenergic [ ... A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to ... Receptors, Adrenergic, beta [D12.776.543.750.070.300.300.340]. *Receptors, Adrenergic, beta-2 [D12.776.543.750.070.300.300.340. ...
Catecholamines, cardiac beta-adrenergic receptors, and heart failure. Koch, Walter J; Lefkowitz, Robert J; Rockman, Howard A ( ... Level of beta-adrenergic receptor kinase 1 inhibition determines degree of cardiac dysfunction after chronic pressure overload- ... When 7 transmembrane receptors are not G protein-coupled receptors. Lefkowitz, Robert J; Rajagopal, K; Rockman, Howard A (J ... Beta-arrestin-mediated beta1-adrenergic receptor transactivation of the EGFR confers cardioprotection. Barki-Harrington, L; ...
EX 2; Thyroid Gland Flashcards by Courtney Kast | Brainscape
catecholamines 42 When the thyroid hormone up regulates beta adrenergic receptors, what does this due to the sympathetic system ... This is when antibodies to TSH receptor stimulate the gland, the feedback mechanism is disrupted, and is more common in women ... Upregulation of beta adrenergic receptors by thyroid hormone increases sensitivity to what ... Where are the receptors for thyroid hormone located and what are the different forms ...
EpinephrineInhibitionCardiac beta-adrenergic receptorsMediateAdenylateProteinsInhibitBeta1-adrenergic receptorSubtypesKinasesResponsivenessDesensitizationHeterotrimericMechanismsDensityPhysiologicalInotropicContractilityBacterial adrenergicActivateCholinergic receptorsSignal transductionVentricularRegulationBeta2Vascular smoothAlpha 1‐adreDownregulationNeuronsGenePharmacologicalNeurotransmitterAffinityMyocardiumAdenylyl cyclaseMoleculePostsynapticPathwayVasoconstrictionActivationHormonesMuscarinic receptorsMacrophagesCharacterizationCytokinesEffectsRats
- Little is still known however, concerning the nature of the putative bacterial adrenergic and/or dopaminergic receptor(s) to which catecholamines (norepinephrine, epinephrine and dopamine) may bind and exert their effects, or even whether the binding properties of such a receptor are similar between different species. (beds.ac.uk)
- Following our recent report that phagocytic cells (neutrophils, PMNs, and macrophages) are newly discovered sources of catecholamines, we now show that both epinephrine and norepinephrine directly activate NFkappaB in macrophages, causing enhanced release of proinflammatory cytokines (TNFalpha, IL-1beta, IL-6). (biomedsearch.com)
- Phagocytes isolated from adrenalectomized rats displayed enhanced expression of tyrosine-hydroxylase and dopamine-beta-hydroxylase, two key enzymes for catecholamine production and exhibited higher baseline secretion of norepinephrine and epinephrine. (biomedsearch.com)
- A common type being epinephrine, it acts by binding to adrenergic receptors. (prezi.com)
- The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. (rcsb.org)
- Supporting this concept are the observations that elevated catecholamine levels preceded the development of acute infectious disease episodes ( 12 ) and that levels of epinephrine and norepinephrine (NE) were significantly higher in postoperative patients who developed severe sepsis than in those with uncomplicated recovery ( 11 ). (asm.org)
- an agent that evokes responses similar to those produced by adrenergic nerve activity (for example, epinephrine, ephedrine, isoproterenol). (thefreedictionary.com)
- Beta-blockers bind to beta-adrenoceptors, which inhibit normal sympathetic effects that act through the receptors norepinephrine and epinephrine. (uspharmacist.com)
- This receptor binds epinephrine and norepinephrine with approximately equal affinity. (uniprot.org)
- Alternatively, it may refer to something which is susceptible to epinephrine, or similar substances, such as a biological receptor (specifically, the adrenergic receptors ). (rug.nl)
- The adrenergic receptors (subtypes alpha 1, alpha 2, beta 1, and beta 2) are a prototypic family of guanine nucleotide binding regulatory protein-coupled receptors that mediate the physiological effects of the hormone epinephrine and the neurotransmitter norepinephrine. (genecards.org)
- Inhibition of catecholamine activity has been found to decrease hypertension. (google.com)
- Level of beta-adrenergic receptor kinase 1 inhibition determines degree of cardiac dysfunction after chronic pressure overload-induced heart failure. (duke.edu)
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (nih.gov)
- The balance of inhibition and maintenance of β 1 -adrenergic signaling is predicted to depend on the specific β -blocker (with greater responsiveness for metoprolol than carvedilol) and β 1 -adrenergic receptor Arg389Gly polymorphisms. (aspetjournals.org)
Cardiac beta-adrenergic receptors2
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. (rcsb.org)
- V1 vascular receptors mediate vasoconstriction and are located on vascular smooth muscle. (scribd.com)
- In general, alpha receptors mediate excitation or increased activity of the effector cells. (washington.edu)
- In general, beta receptors mediate relaxation or decreased activity of the effector cells. (washington.edu)
- Cholinergic, receptors mediate the actions of acetylcholine (ACh). (washington.edu)
- β receptors activate adenylate cyclase (via G s ), thus increasing the activity of PKA. (rug.nl)
- Cholinergic activation of cardiac muscarinic receptors reduces heart rate and contractile activity due in part to the activation of the inhibitory G protein G i , which inhibits adenylate cyclase and the subsequent production of cAMP. (aspetjournals.org)
- Because opiate receptors like muscarinic receptors are also coupled to adenylate cyclase through the inhibitory G protein G i , a coincident parallel direct effect of morphine could add significantly to that mediated indirectly through its activation of the vagus nerve. (aspetjournals.org)
- Beta-adrenergic receptor number and adenylate cyclase function in denervated transplanted and cardiomyopathic human hearts. (semanticscholar.org)
- G-protein receptor kinase 2 (GRK2) is 1 of 7 mammalian GRKs that phosphorylate ligand-bound 7-transmembrane receptors, causing receptor uncoupling from G proteins and potentially activating non-G-protein signaling pathways. (ahajournals.org)
- 1,2 Receptor phosphorylation by any of the 7 mammalian GRKs induces recruitment and binding of β-arrestin, which displaces bound G proteins and uncouples the receptor from downstream signaling effectors in a process termed "desensitization. (ahajournals.org)
- Multiple mechanisms have been proposed, including desensitization of β-adrenergic receptor signaling ( 3 ), dysregulation of excitation-contraction coupling ( 4 , 5 ), alterations in cytoskeletal proteins ( 6 ), myosin isoform switches ( 7 ), and dysfunctional energy utilization ( 8 , 9 ), all topics covered elsewhere in this series. (jci.org)
- Brown and beige fat cells express certain transcription factors, such as early B-cell factor 2 (EBF2), PR domain zinc finger protein 16 (PRDM16), interferon regulatory factor 4 (IRF4) and zinc finger protein 516 (ZFP516), that cooperate with the general adipogenic factors peroxisome proliferator-activated receptor-γ (PPARγ) and the CCAAT/enhancer-binding proteins (C/EBPs) to drive brown adipocyte differentiation and thermogenic gene programming. (nature.com)
- In particular it is well known that: (a) levels of cathecolamines are directly correlated with mortality and functional status in heart failure, (b) β 1 -adrenergic receptor subtype is down-regulated in heart failure, (c) heart failure-dependent cardiac adrenergic responsiveness reduction is related to changes in G proteins activity. (frontiersin.org)
- Desensitization in response to GRK-mediated phosphorylation involves the binding of arrestin proteins that serve to sterically uncouple the receptor from its G protein. (scielo.br)
- These receptors are seven transmembrane-spanning proteins that respond to a wide variety of stimuli including light, odour, taste, hormones and neurotransmitters. (scielo.br)
- Activation of a GPCR results in the modulation of intracellular second messenger levels and/or ionic conductances via the coupling of receptors to a wide variety of effector systems via heterotrimeric guanine nucleotide-binding proteins (G proteins). (scielo.br)
- 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)
- 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)
- Thus, one neurotransmitter molecule can interact with quite different receptor proteins, based on its molecular flexibility. (washington.edu)
- Chemokines, a family of 8- to 10-kDa chemotactic cytokines, provide signals that guide leukocytes to their appropriate location in the body through transmembrane receptors coupled to heterotrimeric GTP-binding proteins under inflammatory or physiological conditions ( 2 , 31 ). (physiology.org)
- 55, 39 (1980), reviews compounds which inhibit catecholamine activity by interfering with adrenergic receptors. (google.com)
- These agents are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells where they inhibit acid secretion. (medscape.com)
- γ-aminobutyric acid and atrial natriuretic peptide inhibit vasopressin by α1-adrenoreceptors whereas the α2-adrenoreceptors and β-adrenergic receptors inhibit vasopressin and oxytocin release. (scribd.com)
- Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes. (nih.gov)
- Potential contributions of other AR subtypes to the mechanism(s) of catecholamine action in the heart were largely ignored in early studies. (ahajournals.org)
- Schematic of pathways activated by β-adrenergic receptor subtypes. (ahajournals.org)
- 3 βARK is one of a family of enzymes (G protein-coupled receptor kinases) that phosphorylate βARs and other G protein-coupled receptors after they have been stimulated, thus leading to their desensitization. (ahajournals.org)
- G-protein receptor kinases (GRKs) function as "off switches" for the superfamily of G-protein coupled, 7-transmembrane spanning receptors (7TMR), members of which are activated by such diverse stimuli as photons, odorants, neurotransmitters, and cardio-active hormones. (ahajournals.org)
- Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (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)
- Adrenergic responsiveness is altered with aging and the age-related changes are limited to the β-adrenergic receptor density reduction and to the β-adrenoceptor-G-protein(s)-adenylyl cyclase system abnormalities, while the type and level of abnormalities change with species and tissues. (frontiersin.org)
- Although these β 2 -AR-dependent signals may represent only a relatively minor component of catecholamine responsiveness under normal physiological conditions, β 2 -ARs assume increased importance as a mechanism for inotropic support in the failing or aged heart, where there is a selective downregulation of β 1 -ARs. (ahajournals.org)
- While some studies indicate that β -blockers are efficacious by inhibiting β -adrenergic signaling, other studies suggest that they work by maintaining β -adrenergic responsiveness. (aspetjournals.org)
- Gene ablation studies have been especially valuable in defining the essential functions of individual GRKs by generating phenotypes related to impaired desensitization of specific receptor types. (ahajournals.org)
- Accordingly, deletion of retinal GRK1 caused persistence of visual signals, 5 GRK3 ablation affected sensing of odors, 6 GRK5 ablation produced an asthma-like phenotype and behavioral supersensitivity related to persistent cholinergic signaling, 7,8 and GRK6 ablation caused hypersensitivity to cocaine and amphetamines because of impaired desensitization of central nervous system dopamine receptors. (ahajournals.org)
- β-Adrenergic desensitization is one pathophysiologically important alteration of the failing heart that contributes to contractile dysfunction and reduced exercise tolerance. (ahajournals.org)
- GPCR sequestration, the endocytosis of receptors to endosomes, not only contributes to the temporal desensitization of GPCRs, but plays a critical role in GPCR resensitization. (scielo.br)
- Receptor desensitization plays an important physiological role by preventing overstimulation of GPCR signaling cascades which in the case of constitutively active mutant receptors leads to diseases such as retinal degeneration, precocious puberty and thyroid tumors (2-4). (scielo.br)
- Moreover, receptor desensitization provides a mechanism by which GPCR-mediated signals from multiple cellular or hormonal inputs can be filtered into meaningful information. (scielo.br)
- Consequently, a firm understanding of how the processes of receptor activation, desensitization and resensitization are related to one another is critical to the development of strategies aimed at ameliorating GPCR-related diseases. (scielo.br)
- A biochemical study of receptor internalization during beta-adrenergic receptor desensitization in frog erythrocytes. (semanticscholar.org)
- High circulating catecholamine concentrations have been linked, via desensitization, to β-adrenergic receptor (βAR) dysfunction after CPB. (asahq.org)
- 4 Currently, it is widely believed that these mechanisms protect the heart from the toxic effects of inotropic β-adrenergic support. (ahajournals.org)
- This study examined the effects of the attention-deficit/hyperactivity disorder treatments, methylphenidate (MPH) and atomoxetine (ATM), on prefrontal cortex (PFC) function in monkeys and explored the receptor mechanisms underlying enhancement of PFC function at the behavioral and cellular levels. (nih.gov)
- Discrete -adrenergic mechanisms regulate early and late erythropoiesis in erythropoietin-resistant anemia. (bireme.br)
- We have shown previously that erythropoietin-dependent development is intact in burn patients and the erythropoietin-independent early commitment stage, which is regulated by 1/ 2-adrenergic mechanisms, is compromised. (bireme.br)
- CONCLUSION: The study unfolds novel 2 and 3 adrenergic mechanisms orchestrating erythropoietin resistant anemia after burn, which impedes both the early commitment stage and the late maturation stages, respectively. (bireme.br)
- In vivo studies have raised questions regarding the mechanisms involved in the adrenergic receptor alterations and the consequences of these alterations. (semanticscholar.org)
- However, there are also other mechanisms of adrenergic agonism. (rug.nl)
- Two uptake mechanisms exist for terminating the action of adrenergic catecholamines - uptake 1 and uptake 2. (rug.nl)
- Other drugs affect the uptake and storage mechanisms of adrenergic catecholamines, prolonging their action. (rug.nl)
- β -Adrenergic receptor blockers ( β -blockers) are commonly used to treat heart failure, but the biologic mechanisms governing their efficacy are still poorly understood. (aspetjournals.org)
- The variation in beta receptor density distribution may be related to functional differences. (biomedsearch.com)
- Important factors in the response of any cell or organ to sympathomimetic amines are the density and proportion of alpha- and beta-adrenergic receptors (3,4). (scielo.br)
- In turn, increased THs increase the density of beta-adrenergic receptors, thereby enhancing the effect of catecholamines. (medscape.com)
- However, in the spontaneously hypertensive rat (SHR), a polygenic model of long-term pressure overload-induced hypertrophy and failure, no decrease in β-adrenergic receptor density or affinity was found, 5 suggesting that other factors also may modulate sensitivity. (ahajournals.org)
- Isoprenaline- and guanylylimidodiphosphate-stimulated adenylyl cyclase activities and β-adrenergic receptor density were reduced, whereas the catalyst and G sα -function were unchanged. (ahajournals.org)
- Contrary to expectations, morphine increased muscarinic receptor density in the right atrium and left ventricle by 17 and 34%, respectively, with no change in the apparent affinity of the receptor ( K D ). Morphine also increased the expression of the G protein G i α by 115 and 233%, respectively, in right atrial and left ventricular sarcolemmal membranes. (aspetjournals.org)
- Measurement of intraoperative right atrial βAR density and adenylyl cyclase activity have served as good indices for gauging the effectiveness of various techniques in blunting catecholamine-mediated stress responses. (asahq.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)
- These prokaryotic sensors, or receptors, have a double function: stereospecific recognition in a complex environment and transduction of the message in order to initiate bacterial physiological modifications. (mdpi.com)
- These animals still displayed markedly elevated cardiac contractility at 1 year of age and developed mild fibrosis late in life (≥1 year), 9 as would be expected from the dose-response curves for receptor expression now provided by Liggett et al. (ahajournals.org)
- Augmentation of cardiac contractility mediated by the human beta(3)-adrenergic receptor overexpressed in the hearts of transgenic mice. (duke.edu)
- Which adrenergic receptor causes increased HR and contractility? (studystack.com)
- The β 1 -adrenergic receptor pathway has a dominant role in the regulation of heart contractility ( Saucerman and McCulloch, 2006 ). (aspetjournals.org)
- Cholinergic receptors are receptive to what? (studystack.com)
- Beta adrenergic and muscarinic cholinergic receptors in canine myocardium. (semanticscholar.org)
- Autonomic receptors are broadly divided into those for ACh (cholinergic receptors) and those for catecholamines such as NE or EPI (adrenergic receptors or adrenoceptors). (washington.edu)
- Cholinergic receptors were originally divided and named on the basis of sensitivity to alkaloids that mimicked some, but not all, of the actions of ACh. (washington.edu)
- Thus, cholinergic receptors are broadly classified as muscarinic (mAChR) or nicotinic (nAChR). (washington.edu)
- By this second component of the mechanism, the same stimulus directly acts on the carbonic anhydrase I isozyme (that might be functionally coupled with adrenergic receptors), so that its activation ensures an adequate pH for stimulus-receptor coupling for signal transduction into the cell, resulting in vasoconstriction. (scielo.br)
- 14 15 16 Although TG(m REN 2)27 rats are not in heart failure and might not represent all pathobiochemical alterations observed in this condition, it can be taken as valuable model to study drug effects on β-adrenergic signal transduction. (ahajournals.org)
- Pressure overload ventricular hypertrophy is accompanied by dysfunctional β-adrenergic receptor signaling due to increased levels of the β-adrenergic receptor kinase-1, which phosphorylates and desensitizes β-adrenergic receptors. (duke.edu)
- Distribution and function of human ventricular beta adrenergic receptors in congestive heart failure. (semanticscholar.org)
- This study examined the characteristics and distribution of sarcolemmal and light vesicular beta-adrenergic receptors (BAR) in left ventricular myocardium from 15 adults (aged 17 to 58 years) without left ventricular dysfunction or coronary artery disease and 29 patients (aged 14 to 53 years) with end-stage congestive heart failure (CHF). (semanticscholar.org)
- examined 2048 consecutive brain dead donors to study almost 1500 with a focus on four known and functional genetic polymorphisms of β-adrenergic receptors and determined their association with left ventricular function during the donor management period. (wiley.com)
- GPCR down-regulation, a loss of the total cellular complement of receptors, is the consequence of both increased lysosomal degradation and decreased mRNA synthesis of GPCRs. (scielo.br)
- 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)
- Regulation of the functions of different organs depends to a greater or lesser extent on alpha or beta receptors. (washington.edu)
- Furthermore, it gives the first evidence of the presence of a local, non-neuronal production in the tendon tissue of signal substances normally seen in neurons, and a basis for these substances to affect the tenocytes as these cells also display muscarinic and adrenergic receptors. (diva-portal.org)
- 9 Strikingly, ablation of the gene for GRK2, also known as β-adrenergic receptor (β-AR) kinase 1, 10 was unique in causing intrauterine heart failure and death. (ahajournals.org)
- Moreover, repeated social defeat promotes a similar pattern of inflammation and β-adrenergic receptor-mediated-gene expression (e.g. (jneurosci.org)
- 10 11 A close relation between α- MHC and β-adrenergic receptor gene expression was found, and it has been suggested that these 2 genes may be coregulated. (ahajournals.org)
- Affinity chromatography of digitonin-solubilized membranes yielded a 20,000-fold purified receptor which had conserved essentially all the pharmacological properties of the membrane-bound binding sites. (springer.com)
- Pharmacological differentiation of alpha and beta receptors, and application of this technology to the treatment of disease, is an outstanding biomedical achievement. (washington.edu)
- Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as a hormone and neurotransmitter. (wikipedia.org)
- SNS activity maintains vascular tone, and thus blood pressure, by maintaining a tone of neurotransmitter on vascular alpha receptors. (washington.edu)
- It is suggested that HC increases the affinity of the catecholamine or possibly its p-hydroxy analog for the adrenergic receptor by modifying the interaction of the p -hydroxyl group in the molecule with the receptor. (aspetjournals.org)
- Characterization of beta-adrenergic receptors in rat brain and pituitary using a new high-affinity ligand, [125I]iodocyanopindolol. (semanticscholar.org)
- One such β-arrestin-mediated pathway uses the β 1 -adrenergic receptor (β 1 AR) to transactivate the EGFR. (pnas.org)
- In the catecholamine biosynthetic pathway, tyrosine is converted in three steps to norephinephrine (NE). (google.com)
- Alternatively, the catecholamine biosynthetic pathway can be suppressed at any of the three steps, resulting in decreased levels of NE. (google.com)
- Here, we tested whether genes encoding for key components of the β-adrenergic signaling pathway are associated with human longevity. (wiley.com)
- We extended a computational model of the β 1 -adrenergic pathway and excitation-contraction coupling to include detailed receptor interactions for 19 ligands. (aspetjournals.org)
- The complexity of the β -adrenergic receptor pathway, coupled with the influence of receptor polymorphisms, makes it difficult to intuit the effect of β -blockers on observed cardiac physiology. (aspetjournals.org)
- Which adrenergic receptor is responsible for vasoconstriction of the arterioles in the skin and viscera, and intestinal relaxation? (studystack.com)
- By selectively activating the alpha receptors in the mucosa tract of the respiratory and nasal pathways, pseudoephedrine produces vasoconstriction shrinking membranes and relieving congestion. (mindandmuscle.net)
- Last, repeated social defeat increased c-Fos activation in IL-1 receptor type-1-deficient mice, but did not promote anxiety-like behavior or microglia activation in the absence of functional IL-1 receptor type-1. (jneurosci.org)
- These findings indicate that repeated social defeat-induced anxiety-like behavior and enhanced reactivity of microglia was dependent on activation of β-adrenergic and IL-1 receptors. (jneurosci.org)
- Adrenergic receptor activation is another hypothesis. (medscape.com)
- Adrenergic receptors activation by catecholamines is the most important regulatory mechanism of cardiovascular performance. (frontiersin.org)
- The activation of one receptor signaling system can alter the effectiveness of opposing systems. (aspetjournals.org)
- Catecholamines exert physiologically important effects on the electrical properties and mechanical performance of the heart through the activation of adrenergic receptors. (ahajournals.org)
- Thus, blood vessels dilate and uterine smooth muscle relaxes in response to activation of beta receptors. (washington.edu)
- Sustained toll-like receptor 9 activation promotes systemic and cardiac inflammation, and aggravates diastolic heart failure in SERCA2a KO Mice. (uio.no)
- Muscarinic receptors are located postsynaptically at the parasympathetic neuroeffector junction. (washington.edu)
- At these junctions muscarinic receptors function either to increase or decrease the activity of the effector cells. (washington.edu)
- At this junction muscarinic receptors function to increase sweating. (washington.edu)
- Drugs that block muscarinic receptors can thus interfere with sweating. (washington.edu)
- Another important site of muscarinic receptors is on endothelial cells of blood vessels. (washington.edu)
- Although these muscarinic receptors are not innervated by cholinergic nerve fibers, they are sensitive to circulating molecules. (washington.edu)
- Ganglionic and other neural muscarinic receptors (M1) are apparently involved in CNS transmission. (washington.edu)
- The classical site of muscarinic receptors is at the postganglionic parasympathetic neuroeffector junction in smooth muscle, heart, and exocrine glands. (washington.edu)
- However, muscarinic receptors also exist on effectors cells, even in the absence of cholinergic innervation. (washington.edu)
- Collectively, these data demonstrate that catecholamines are potent inflammatory activators of macrophages, upregulating NFkappaB and further downstream cytokine production of these cells. (biomedsearch.com)
- In adrenalectomized animals, which have been used to further assess the role of catecholamines, there appears to be a compensatory increase in catecholamine generating enzymes and catecholamines in macrophages, resulting in amplification of the acute inflammatory response via engagement of alpha(2)-adrenoceptors. (biomedsearch.com)
- Alternatively activated macrophages secrete catecholamines in WAT to promote browning. (nature.com)
- 1989) Molecular characterization of the human beta 3‐adrenergic receptor. (els.net)
- Characterization of a potentially reversible increase in beta-adrenergic receptors in isolated, neonatal rat cardiac myocytes with impaired energy metabolism. (semanticscholar.org)
- Alexander, R.W., Davis, J.N., and Lefkowitz, R.J. (1975) Direct identification and characterization of 6-adrenergic receptors in rat brain. (springer.com)
- Caron, M.G. and Lefkowitz, R.J. (1976) Solubilization and characterization of the ß-adrenergic receptor binding sites of frog erythrocytes. (springer.com)
- These receptor actions likely contribute to their therapeutic effects in the treatment of attention-deficit/hyperactivity disorder. (nih.gov)
- The effects of upregulation of phagocyte-derived catecholamines were investigated in two models of acute lung injury (ALI). (biomedsearch.com)
- By binding to specific receptor-sites these agents appear to potentiate the effects of gamma-aminobutyric acid (GABA) and facilitate inhibitory GABA neurotransmission and other inhibitory transmitters. (medscape.com)
- This conclusion is supported by the observations that potentiation was obtained for both the alpha and beta adrenergic effects of catecholamines in vivo and in vitro . (aspetjournals.org)
- V2 receptors are responsible for antidiuretic effects of vasopressin. (scribd.com)
- The following headings provide some useful examples to illustrate the various ways in which drugs can enhance the effects of adrenergic receptors. (rug.nl)
- The receptor concept has been used for some time to explain the striking specificity of hormone and drug effects on tissues. (springer.com)