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-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: 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.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.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 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.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 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.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic 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.Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Interleukin 1 Receptor Antagonist Protein: A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.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 Agonists: Drugs that bind to and activate adrenergic receptors.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.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.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.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.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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Adrenergic beta-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 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 beta-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS.Iodocyanopindolol: A highly selective and specific beta antagonist that is used to characterize beta-adrenoceptors.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.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).Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 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.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)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)Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.Arrestins: Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.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.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.Piperidines: A family of hexahydropyridines.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.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.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.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Histamine H2 Antagonists: Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.QuinoxalinesSerotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.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.Butoxamine: A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Adrenergic beta-3 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-3 RECEPTORS.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.-.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Interleukin-1beta: An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.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.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.Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.Hormone Antagonists: Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.beta-Adrenergic Receptor Kinases: G-protein-coupled receptor kinases that mediate agonist-dependent PHOSPHORYLATION and desensitization of BETA-ADRENERGIC RECEPTORS.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.Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.Time Factors: Elements of limited time intervals, contributing to particular results or situations.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.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Muscarinic Antagonists: Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.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.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.Kinetics: The rate dynamics in chemical or physical systems.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Receptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.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.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Histamine H1 Antagonists: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.Catecholamines: A general class of ortho-dihydroxyphenylalkylamines derived from tyrosine.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).Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.DioxolesEthanolamines: AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.GTP-Binding Protein alpha Subunits, Gs: A family of heterotrimeric GTP-binding protein alpha subunits that activate ADENYLYL CYCLASES.Betaxolol: A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.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.Methoxamine: An alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION.Oxymetazoline: A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.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.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.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)Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.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.Indoles: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.GABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Sialoglycoproteins: Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.Fenoterol: An adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.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.Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.Histamine Antagonists: Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.Procaterol: A long-acting beta-2-adrenergic receptor agonist.Benzazepines: Compounds with BENZENE fused to AZEPINES.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.Sulfonamides: A group of compounds that contain the structure SO2NH2.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.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)PiperazinesLeukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Tetralones: A group of TETRAHYDRONAPHTHALENES containing a keto oxygen.Receptor, Endothelin A: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.Vasoconstriction: The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.Receptors, N-Methyl-D-Aspartate: A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.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.Disease Models, Animal: Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.Serotonin 5-HT1 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.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.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.Injections, Intraventricular: Injections into the cerebral ventricles.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.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.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Heart Rate: The number of times the HEART VENTRICLES contract per unit of time, usually per minute.Biphenyl CompoundsAzepines: Seven membered heterocyclic rings containing a NITROGEN atom.Behavior, Animal: The observable response an animal makes to any situation.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Mice, Inbred C57BLbeta 2-Microglobulin: An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.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.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.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).)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.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Receptors, Interleukin-1: Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.TetrazolesEnzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Nicotinic Antagonists: Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.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.Gene Expression Regulation: Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.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.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.Guanabenz: An alpha-2 selective adrenergic agonist used as an antihypertensive agent.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.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.Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Muscle, Smooth: Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)Animals, Newborn: Refers to animals in the period of time just after birth.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Interleukin-1: A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.Phenoxypropanolamines: Compounds based on a propanolamine attached via an OXYGEN atom to a phenoxy ring. The side chain is one carbon longer than PHENYLETHYLAMINES.Substance P: An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.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.Heart: The hollow, muscular organ that maintains the circulation of the blood.Xanthines: Purine bases found in body tissues and fluids and in some plants.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.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.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.Blotting, Western: Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.Peptides, Cyclic: Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).Pyrazoles: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.Analysis of Variance: A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.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.Receptors, Vasopressin: Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.Isoindoles: Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.Kidney: Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.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.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.Histamine H3 Antagonists: Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Histamine: An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.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.Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Gene Expression: The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.Cricetulus: A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Peptide Fragments: Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.Angiotensin II: An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.Synaptic Transmission: The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.Inositol Phosphates: Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.Myocardial Contraction: Contractile activity of the MYOCARDIUM.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.Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.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.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
"Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A ... SR 59230A is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 ... adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA in animal studies. Nisoli E, Tonello ... "Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Mol. Pharmacol ...
... beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, beta adrenergic receptor antagonists. ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 ... but receptor selectivity diminishes at higher doses. Beta blockade, especially of the beta-1 receptor at the macula densa, ... Beta-Adrenoceptor Antagonists (Beta-Blockers); "CV Pharmacology , Beta-Adrenoceptor Antagonists (Beta-Blockers)". Archived from ...
... is a non-selective beta blocker or β-adrenergic receptor antagonist with partial agonist activity and also possesses ... By blocking 5-HT1A autoreceptors at doses that are selective for them over postsynaptic 5-HT1A receptors, pindolol may be able ... "Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO ... "The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan ...
Ryanodine receptors are similar to the inositol trisphosphate (IP3) receptor, and stimulated to transport Ca2+ into the cytosol ... Antagonists:Ryanodine locks the RyRs at half-open state at nanomolar concentrations, yet fully closes them at micromolar ... It can block the phasic release of calcium, but at low doses may not block the tonic cumulative calcium release. The binding of ... Non-mammalian vertebrates typically express two RyR isoforms, referred to as RyR-alpha and RyR-beta. Many invertebrates, ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist. ICI binds to the β2 subtype with at least 100 ... Common systemic doses used in rodent research are 0.5 or 1 mg/kg although efficacy has been demonstrated at doses as low as ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ...
J. W. Black; A. F. Crowther; R. G. Shanks; A. C. Dornhorst (1964). "A new adrenergic beta-receptor antagonist". The Lancet. 283 ... that both are beta type receptors. … It is suggested that this terminology be extended to the realm of adrenergic blocking ... since Peter Holtz and his group in 1942 had found that small doses of dopamine lowered the blood pressure of rabbits and guinea ... he called beta adrenotropic receptor (now β-adrenoceptor or β-adrenergic receptor). ″This concept of two fundamental types of ...
Inactivation of receptors normally results in a depression of the maximal response of agonist dose-response curves and a right ... Phenoxybenzamine is an example of an irreversible alpha blocker-it permanently binds to α adrenergic receptors, preventing ... They are sometimes called blockers; examples include alpha blockers, beta blockers, and calcium channel blockers. In ... A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and ...
... acts on the β1 adrenergic receptors in both the heart and the kidney. When β1 receptors are activated by a ... Like propanolol and pindolol, it is a serotonin 5-HT1A and 5-HT1B receptor antagonist; this discovery by several groups in the ... ISBN 9780071826419 Frishman, W. H., Covey, S. (1990). Penbutolol and carteolol: two new beta-adrenergic blockers with partial ... 1977). Plasma level studies of penbutolol after oral dose in man. Journal of Clinical Pharmacology, 17(4):231-23 PMID 14976 ...
Long-acting β adrenoceptor agonists (LABAs, more specifically, long-acting β2 adrenergic receptor agonists) are usually ... lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to ... Umeclidinium bromide is a long-acting muscarinic antagonist. This combination was approved by the FDA on December 18, 2013 for ... allowing for once-daily dosing. They are considered to be ultra-long-acting β adrenoreceptor agonists (ultra-LABAs) and are now ...
"Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Molecular ... Although α receptors are less sensitive to epinephrine, when activated at pharmacologic doses, they override the vasodilation ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... Basic Neurochemistry: α- and β-Adrenergic Receptors Brief overview of functions of the β3 receptor Theory of receptor ...
ACE inhibitors, Adrenergic neurone blockers, Angiotensin II receptor antagonists, Beta blockers, Calcium channel blockers, ... The higher the dose and the longer the drug is taken, the greater the risk of experiencing unpleasant withdrawal symptoms. ... Benzodiazepines impair learning and memory via their action on benzodiazepine receptors, which causes a dysfunction in the ... If chlordiazepoxide is used during pregnancy the risks can be reduced via using the lowest effective dose and for the shortest ...
For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta ... However, the drug's receptor selectivity in humans is more complex and depends on the drug dose and the genetic profile of the ... Agabiti Rosei E, Rizzoni D (2007). "Metabolic profile of nebivolol, a beta-adrenoceptor antagonist with unique characteristics ... In addition, at doses above 10 mg, nebivolol loses its cardioselectivity and blocks both β1 and β2 receptors. (While the ...
As a non-selective alpha receptor antagonist, it will also affect both the postsynaptic alpha 1 and presynaptic alpha 2 ... Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of ... The block on alpha-2 receptors further potentiates beta-effects, increasing cardiac output. Phenoxybenzamine has a long-lasting ... its irreversible antagonism and the resultant depression in the maximum of the agonist dose-response curve are desirable in a ...
... such as pseudoephedrine can stimulate both alpha and beta adrenergic receptors directly and indirectly by releasing ... Adrenergic Agonists and Antagonists, McGraw-Hill, New York. Passali D, Salerni L, Passali G, Passali F, Bellussi L (2006) Nasal ... allowing the vasodilation due to beta-receptor stimulation to emerge. 2-Imidazoline derivatives, such as oxymetazoline, may ... Patients often try increasing both the dose and the frequency of nasal sprays upon the onset of RM, worsening the condition. ...
Beta blocker Adrenergic antagonists Katzung, Bertram; Masters, Susan (2013). Basic and Clinical Pharmacology. Lange. ISBN 978-0 ... angiotensin-II receptor blockers, calcium channel blockers, or thazide diuretics (in full dose or in combinations) have not ... are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha- ... Non-selective α-adrenergic receptor antagonists include: Phenoxybenzamine Phentolamine Tolazoline Trazodon Selective α1- ...
... ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic receptors. ... Schmid CL, Raehal KM, Bohn LM (January 2008). "Agonist-directed signaling of the serotonin 2A receptor depends on beta-arrestin ... Animal studies with this compound showed it to be free of hallucinogenic effects at doses up to 30 mg/kg, although several of ... However, ritanserin, like most other 5-HT2A receptor antagonists, also potently inhibits 5-HT2C receptors. Nefazodone operates ...
... is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... then the molecule typically is found to have receptor affinity without intrinsic activity, and is, therefore, an antagonist. ... Its dose and use is limited by its main side effect-postural hypotension, where there is a substantial drop in blood pressure ... Labetalol is a dual alpha (α1) and beta (β1/β2) adrenergic receptor blocker and competes with other Catecholamines for binding ...
Adrenergic receptor antagonistsEdit. Propranolol, the first beta-blocker to be successfully developed ... Alpha-2 adrenergic receptor agonistsEdit. Central alpha agonists lower blood pressure by stimulating alpha-receptors in the ... or angiotensin II receptor antagonists.[7] There are fixed-dose combination drugs, such as ACE inhibitor and thiazide ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... Kanba S, Richelson E (1983). "Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated brain ... A single oral dose of 60 mg iprindole to healthy volunteers has been found to achieve mean peak plasma concentrations of 67.1 ... Tsai BS, Yellin TO (1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic antidepressants ...
"Death temporally related to the use of a Beta adrenergic receptor antagonist in cocaine associated myocardial infarction". ... Multiple and escalating dose of benzodiazepines may be necessary to achieve effect, which increases risk of over-sedation and ... Narayanan, Sanju; Mesangeau, Christophe; Poupaert, Jacques H.; McCurdy, Christopher R. (2011-01-01). "Sigma receptors and ... "Reflections on beta-adrenergic receptor blockers and cocaine use. A case in point". Revista Española De Cardiología. 62 (4): ...
Optimal Agonist/Antagonist Combinations Maintain Receptor Response by Preventing Rapid β-adrenergic Receptor Desensitization , ... competitive antagonist as determined on a dose response curve used to determine the affinity of an antagonist for its receptor ... antagonist combinations on the desensitization of receptors. This is also demonstrated by receptors that are activated by ... Quirke V (2006). "Putting theory into practice: James Black, receptor theory and the development of the beta-blockers at ICI, ...
Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... The alpha1 antagonist prazosin could be effective for PTSD The Alpha2 adrenergic agonists Clonidine and guanfacine have ... Like barbiturates, therapeutic doses produce sedation and significant overdoses may be fatal. In the US, meprobamate has ... The anxiolytic effects of solvents act as positive modulators of GABAA receptors (Bowen and colleagues 2006). Psychotherapeutic ...
It is also a strong antagonist of the H1 receptor, a moderate antagonist of the 5-HT2 and α1-adrenergic receptors, and a weak ... Reproduction studies have been performed in female laboratory rabbits, mice, and rats at doses up to 1.3, 7, and 9 times the ... Additionally, increased blood-levels of Maprotiline are possible, if certain beta-blocking agents (e.g. Propranolol) are given ... Maprotiline has also more recently been identified as a potent antagonist of the 5-HT7 receptor, with this action potentially ...
... considered to be a selective β3-antagonist). Using a β2 adrenergic receptor preparation derived from transfected HEK 293 cells ... Considered to be an antagonist of β1 and β2 receptors, and an agonist of β3 receptors. Wainscott DB, Little SP, Yin T, Tu Y, ... a dose of 10 or 17.5 mg/kg decreased heart rate, but a 30 mg/kg dose caused it to increase. Other effects that were noted ... H. E. Shannon and C. M. Degregorio (1982). "Self-administration of the endogenous trace amines beta-phenylethylamine, N-methyl ...
It doesn't do anything for beta-adrenoceptors because it lacks beta-hydroxyl group and therefor can not block beta-receptors. ... Taylor, Fletcher; Raskind, Murray A. (February 2002). "The alpha1-adrenergic antagonist prazosin improves sleep and nightmares ... Additionally, the risk of first dose phenomenon may be reduced by starting at a low dose and titrating upwards as needed. ... Silodosin shows high affinity and selectivity for alpha-1a adrenergic receptors found in the prostate which ensures that it ...
There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. They activate mitogenic responses and regulate growth and proliferation of many cells. ...
The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic receptor family. The human gene encoding this receptor has the symbol ADRA2B. ADRA2B orthologs have been identified in several mammals. α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. This gene encodes the α2B subtype, which was observed to associate with eIF-2B, a guanine nucleotide exchange protein that functions in regulation of ...
3.0.CO;2-3. PMID 9359081. Hoehe MR, Berrettini WH, Schwinn DA, Hsieh WT (1993). "A two-allele PstI RFLP for the alpha-1C adrenergic receptor gene (ADRA1C)". Hum. Mol. Genet. 1 (5): 349. doi:10.1093/hmg/1.5.349-a. PMID 1363873. Schwinn DA, Lomasney JW, Lorenz W, et al. (1990). "Molecular cloning and expression of the cDNA for a novel alpha 1-adrenergic receptor subtype". J. Biol. Chem. 265 (14): 8183-9. PMID 1970822. Hirasawa A, Shibata K, Horie K, et al. (1995). "Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants". FEBS Lett. 363 (3): 256-60. doi:10.1016/0014-5793(95)00330-C. PMID 7737411. Diehl NL, Shreeve SM (1995). "Identification of the alpha 1c-adrenoceptor in rabbit arteries and the human saphenous vein using the polymerase chain reaction". Eur. J. Pharmacol. 268 (3): 393-8. doi:10.1016/0922-4106(94)90064-7. PMID ...
The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the human gene encoding it. α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Studies in mice revealed that both the α2A and α2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the α2A subtype inhibited transmitter ...
Adverse drug reactions associated with the use of beta blockers include: nausea, diarrhea, bronchospasm, dyspnea, cold extremities, exacerbation of Raynaud's syndrome, bradycardia, hypotension, heart failure, heart block, fatigue, dizziness, alopecia (hair loss), abnormal vision, hallucinations, insomnia, nightmares, sexual dysfunction, erectile dysfunction and/or alteration of glucose and lipid metabolism. Mixed α1/β-antagonist therapy is also commonly associated with orthostatic hypotension. Carvedilol therapy is commonly associated with edema.[44] Due to the high penetration across the blood-brain barrier, lipophilic beta blockers, such as propranolol and metoprolol, are more likely than other less lipophilic beta blockers to cause sleep disturbances, such as insomnia, vivid dreams and nightmares.[45] Adverse effects associated with β2-adrenergic receptor antagonist activity ...
This gene encodes the α2B subtype, which was observed to associate with eIF-2B, a guanine nucleotide exchange protein that functions in regulation of translation. A polymorphic variant of the α2B subtype, which lacks 3 glutamic acids from a glutamic acid repeat element, was identified to have decreased G protein-coupled receptor kinase-mediated phosphorylation and desensitization; this polymorphic form is also associated with reduced basal metabolic rate in obese subjects and may therefore contribute to the pathogenesis of obesity. This gene contains no introns in either its coding or untranslated sequences.[5]. A deletion variant of the α2B adrenergic receptor has been shown to be related to emotional memory in Europeans and Africans.[7] This variant also predisposed people who had it to focus more on negative aspects of a situation.[8] This predisposition remained present in people with the variant gene who took a single ...
... is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor.[3][4] The compound was developed by Imperial Chemical Industries, which was acquired by AkzoNobel in 2008. ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β2 adrenergic receptor, as few other specific antagonists for this receptor are known.[5] ICI-118,551 has been used in pre-clinical studies using murine models.[6][7][8] When dissolved in saline, the compound crosses the blood-brain barrier. Common systemic doses used in rodent research are 0.5 or 1 mg/kg although ...
... (also βARKct) is a peptide composed of the last 194 amino acid residues of the carboxyl-terminus of beta adrenergic receptor kinase 1 (βARK1). It binds the βγ subunits of G proteins located in the plasma membrane of cells. It is currently an experimental gene therapy for the treatment of heart failure. During heart failure, the heart is not able to pump enough blood to the rest of the body and will begin to undergo processes in order to compensate for its decreased function. These processes will attempt to increase the heart's output; however, the heart may become overstressed and eventually dysfunctional as a result. The sympathetic nervous system increases norepinephrine release to stimulate β-adrenergic receptors (βARs) located on heart cell (cardiomyocyte) membranes to increase the heart's rate and force of ...
A sympatholytic (or sympathoplegic) drug is a medication that opposes the downstream effects of postganglionic nerve firing in effector organs innervated by the sympathetic nervous system (SNS). They are indicated for various functions; for example, they may be used as antihypertensives. They are also used to treat anxiety, such as Generalized Anxiety Disorder, Panic Disorder and PTSD. Antiadrenergic agents inhibit the signals of epinephrine and norepinephrine. They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers"), inhibiting the downstream cellular signaling pathways of adrenergic receptors. However, ...
There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. They activate mitogenic responses and regulate growth and proliferation of many cells. ...
The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic receptor family. The human gene encoding this receptor has the symbol ADRA2B. ADRA2B orthologs have been identified in several mammals. α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. This gene encodes the α2B subtype, which was observed to associate with eIF-2B, a guanine nucleotide exchange protein that functions in regulation of ...
... (Regitine) is a reversible nonselective α-adrenergic antagonist. Its primary action is vasodilation due to α1 blockade. Non-selective α-blockers can cause a much more pronounced reflex tachycardia than the selective α1 blockers. Like the selective α1 blockers, phentolamine causes a relaxation of systemic vasculature, leading to hypotension. This hypotension is sensed by the baroreceptor reflex, which results in increased sympathetic nerve firing on the heart, releasing norepinephrine. In response, the β1 adrenergic receptors on the heart increase its rate, contractility, and dromotropy, which help to offset the decrease in systemic blood pressure. Unlike the α1 selective blockers, phentolamine also inhibits the α2 receptors, which function predominantly as presynaptic negative feedback ...
Adverse drug reactions associated with the use of beta blockers include: nausea, diarrhea, bronchospasm, dyspnea, cold extremities, exacerbation of Raynaud's syndrome, bradycardia, hypotension, heart failure, heart block, fatigue, dizziness, alopecia (hair loss), abnormal vision, hallucinations, insomnia, nightmares, sexual dysfunction, erectile dysfunction and/or alteration of glucose and lipid metabolism. Mixed α1/β-antagonist therapy is also commonly associated with orthostatic hypotension. Carvedilol therapy is commonly associated with edema.[44] Due to the high penetration across the blood-brain barrier, lipophilic beta blockers, such as propranolol and metoprolol, are more likely than other less lipophilic beta blockers to cause sleep disturbances, such as insomnia, vivid dreams and nightmares.[45] Adverse effects associated with β2-adrenergic receptor antagonist activity ...
... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... beta,2-adrenergic,receptor,antagonists,using,CypHer5E,and,IN,Cell,Analyzer,1000,biological,advanced biology technology,biology ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... expressing cells (2). For live-cell receptor internalization studies a,Screening,for,potential, ...
... beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, beta adrenergic receptor antagonists. ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 ... but receptor selectivity diminishes at higher doses. Beta blockade, especially of the beta-1 receptor at the macula densa, ... Beta-Adrenoceptor Antagonists (Beta-Blockers); "CV Pharmacology , Beta-Adrenoceptor Antagonists (Beta-Blockers)". Archived from ...
"Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A ... SR 59230A is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 ... adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA in animal studies. Nisoli E, Tonello ... "Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Mol. Pharmacol ...
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 ... 08/01/2010 - "The aim of this study was to evaluate the effect of intra-operative low-dose infusion of landiolol hydrochloride ... G-Protein-Coupled Receptors: 810*Catecholamine Receptors: 32*Adrenergic Receptors: 3359*beta Adrenergic Receptors: 720*beta-1 ...
Beta-adrenergic antagonists. Attitudes towards beta-blockade in the field of human dilated cardiomyopathy have undergone ... some beta-adrenergic blockers produce an improvement in systolic function without causing any ß-receptor up-regulation. It now ... doses must be extremely low initially (often , 0.1 of target dose); and doses must be titrated upwards slowly (at 1-2 week ... It was initially believed that the mechanism was related to reversal of the down-regulation of ß-receptors that occurs with ...
The present invention provides the use of somatostatin antagonists for treating and preventing HISS-dependent insulin ... Beta-Adrenergic Blockade Does Not Prevent Hemorrhage-Induced HDIR. Identification of Blocking Dose of Isopropanol: A standard ... Propranolol was administered in order to block hepatic β-adrenergic receptors. Although hepatic β-adrenergic receptors were ... the somatostatin receptor antagonist is cyclosomatostatin. Other somatostatin receptor antagonists which may be used to prepare ...
... receptor antagonists, .beta.2 adrenergic receptor antagonists, Adenosine A.sub.2B receptor antagonists, corticotropin releasing ... Low doses of combined GPCR-targeted drugs can also prevent massive internalization of their receptors and enable prolonged ... receptor antagonists, .beta.2 adrenergic receptor antagonists, Adenosine A.sub.2B receptor antagonists, corticotropin releasing ... receptor antagonists, .beta.2 adrenergic receptor antagonists, Adenosine A.sub.2B receptor antagonists, corticotropin releasing ...
Pindolol is a non-selective beta blocker or β-adrenergic receptor antagonist with partial agonist activity and also possesses ... By blocking 5-HT1A autoreceptors at doses that are selective for them over postsynaptic 5-HT1A receptors, pindolol may be able ... "Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO ... "The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan ...
Behavioral effects of beta adrenergic agonists and antidepressant drugs after down-regulation of beta-2 adrenergic receptors by ... ODonnell JM, Frazer A. Effects of clenbuterol and antidepressant drugs on beta adrenergic receptor/N-protein coupling in the ... Antagonism of the antidepressant-like effects of clenbuterol by central administration of beta-adrenergic antagonists in rats. ... Microwave attenuation of ethanol-induced hypothermia: ethanol tolerance, time course, exposure duration, and dose response ...
TIQ binding to cortical adrenergic alpha1, alpha2 and beta receptors, striatal dopamine D1 and D2 receptors and cortical L-type ... TIQ did not displace ligands that are antagonists for several receptor sites (including D1 and D2 receptors), but displaced an ... Both compounds in high doses reduced the mouse locomotor activity, and in doses not affecting activity inhibited the motor ... Opposite genotypic differences in locomotor activity induced by NMDA receptor antagonists versus cocaine or amphetamine in ...
Beta-adrenergic receptor blockers play an important role in the management of cardiovascular disease, including hypertension, ... Bucindolol is a non-selective and lipophilic beta blocker with a higher affinity then beta receptors. Vasodilator effects seem ... causes a dose dependent nitric-oxide related renal artery dilatation and increases glomerular filtration rate, urine flow and ... 17) Greven J, Gabriels G. Effect of nebivolol, a novel B1-selective adrenoceptor antagonist with vasodilating properties, on ...
Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood brain barrier, has not been ... We recorded the sedation level and daily dose of sedatives, analgesics, and antipsychotics administered each day for 6 days ... Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood brain barrier, has not been ... We recorded the sedation level and daily dose of sedatives, analgesics, and antipsychotics administered each day for 6 days ...
Beta blockers, β-blockers , , , ... World Heritage Encyclopedia, the aggregation of the largest online encyclopedias available ... beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, or beta adrenergic receptor antagonists) are a ... β-adrenergic receptors and others are selective. Three types of beta receptors are known, designated β1, β2 and β3 receptors.[6 ... but receptor selectivity diminishes at higher doses. Beta blockade, especially of the beta-1 receptor at the macula densa, ...
... for a dose of 10 microgram/kg/min. This increase occurs via the specific activation of beta2-adrenergic receptor. It can be ... Mg2+ extrusion can be inhibited by the administration of non-selective beta-adrenergic receptor antagonist (propranolol or ... and beta-adrenergic receptors or distinct beta-adrenoceptor subtypes, modality, rate and duration of drug infusion are but a ... and beta2-adrenergic receptor stimulation. Circ Res 77, 973-983 (1995) 17. P B Molinoff: Alpha- and beta-adrenergic receptor ...
... down regulation of beta and alpha-2 adrenergic receptors, increased reactivity to alpha-2 antagonist Yohimbine. Alpha-1 ... 5-HT2 receptors hypersensitive. `. Treatment SAD 1st line SSRI or CBT. Pharmacotherapy x 10-12 weeks at max dose before ... decreased receptor binding, low levels of metabolites, high incidence in Parkinsons, Emergence of SAD during antipsychotic tx. ... Higher Dose SSRI may be more effective. Pediatric partial response to SSRI addition of CBT increased efficacy. SGAs may be ...
... receptor antagonist, MDL-72222, the 5-HT1A/5-HT2 antagonist, spiperone, and the mixed beta adrenergic/5-HT1B antagonists, l- ... Administration of various doses of clonidine increased plasma growth hormone levels. Pretreatment with the alpha 2 adrenergic ... Furthermore, either 5-HT1C receptors or alpha 2 adrenergic heteroreceptors or both are functionally sub-sensitive in the Fawn- ... In contrast, pretreatment with the non-selective 5-HT1/2 antagonist, metergoline, and the 5-HT1C/5-HT2-selective antagonist, ...
In addition, epinephrine is not reliable in patients who have received a beta-adrenergic receptor antagonist.77 Other subtle ... Test doses: optimal epinephrine content with and without acute beta-adrenergic blockade. Anesthesiology 1990;73:386-392. ... including the stretch receptors), practitioners must rule out an impending "high spinal" anesthetic by repetitive examinations. ... The administration of histamine (H2)-receptor antagonists, such as cimetidine and ranitidine, requires anticipation and careful ...
Beta-Blockers. Beta-adrenergic receptor antagonists (beta-blockers) and UTIBRON NEOHALER may interfere with the effect of each ... Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the ... Inhalation of high doses of beta2-adrenergic agonists may produce increases in plasma glucose. ... there are also beta2-adrenergic receptors in the human heart comprising 10% to 50% of the total adrenergic receptors. The ...
It works by blocking beta-adrenergic receptors in the heart, which leads to decreased force and rate of heart contractions. ... without causing significant intrinsic sympathomimetic or membrane stabilizing activities at recommended therapeutic doses. ... is a cardioselective beta-1 receptor blocker. It has a rapid onset but short duration of action ... Antagonist. General Function. Receptor signaling protein activity. Specific Function. Beta-adrenergic receptors mediate the ...
... beta-adrenergic receptor stimulating action of epinephrine when present. The net effect is normally a modest hypotension when ... Its most prominent actions are on the beta receptors of the heart, vascular and other smooth muscle. When given by rapid ... Neonates may be given a dose of 0.01 mg per kg of body weight; for the infant 0.05 mg is an adequate initial dose and this may ... Epinephrine relaxes the smooth muscles of the bronchi and iris and is a physiologic antagonist of histamine. The drug also ...
HETLIOZ in treating Non-24 may be reduced in subjects with concomitant administration of beta-adrenergic receptor antagonists. ... Reduced body weight in offspring was also observed at the mid-dose. The no effect dose (NOEL), (50 mg/kg/day) is approximately ... Major metabolites had 13-fold or less activity at melatonin receptors compared to tasimelteon. ... the highest dose tested is approximately 75 times the maximum recommended human dose (MRHD) of 20 mg/day, based on a mg/m2 body ...
... dosing and administering information to help phsyicans more efficiently and accurately prescribe in their practice PDRs drug ... the drug is also an antagonist at alpha-2A adrenergic receptors. Lurasidone exhibits little or no affinity for histamine-1 or ... Levodopa: (Moderate) Levodopa is a potent dopamine-receptor agonist. Dopamine-receptor antagonists, including the atypical ... Beta-adrenergic blockers: (Moderate) Due to the antagonism of lurasidone at alpha-1 adrenergic receptors, the drug may enhance ...
... beta-adrenergic receptor blockers (b blockers). 2. alpha-adrenergic receptor blockers (a blockers). 3. centrally-acting anti- ... antagonist at NMDA receptor to block excitatory effects. -not good for adults, better in kids ... Direct acting Sympathomimetic agents - interact with a or b receptors, can be receptor selective or non-selective. Include -> ... response CAN be achieved by increasing agonist dose. -NO response with increasing agonist ...
Preclinical data indicate the potential benefit of combinations of CCBs and oxytocin antagonists. However, the combinations of ... whose efficacy is superior or comparable to those of β-agonists and oxytocin antagonists. Additionally, it has a favourable ... beta-adrenergic receptors (β-ARs) and sexual hormones. In clinical practice, most experience has been gained with the use of ... Factor 2: Beta-Adrenergic Receptors. The adrenergic system plays an important role in the control of uterine contractility. ...
These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... QT and QTc interval with standard and supratherapeutic doses of darifenacin, a muscarinic M3 selective receptor antagonist for ... These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?) and What is the role of beta-adrenergic ...
  • The effect of beta-adrenoreceptor signaling on the expression of VEGF and interleukin 6 (IL-6) was investigated in primary mouse choroidal endothelial cells, retinal pigment epithelial (RPE) cells, microglia cells, and human fetal RPE cells using specific beta-adrenoreceptor agonists and antagonists. (arvojournals.org)
  • Here we tested the hypothesis that beta2-adrenergic receptors regulate CNV in vivo , investigated the role of beta2-adrenoreceptors in inflammatory signaling, and extended these results into primary human cells. (arvojournals.org)
  • Similarly, activation of beta2-adrenergic receptors during the time of amine depletion also attenuates anisomycin-induced amnesia assessed at 48 h after training. (blogspot.com)
  • In this study, we demonstrate that a soluble ectodomain of LRIG1, containing only the LRRs, inhibits ligand-independent epidermal growth factor receptor (EGFR) activation and causes growth inhibition of A431, HeLa and MDA-468 carcinoma cells. (embl-heidelberg.de)
  • Doxofylline does not demonstrate direct inhibition of any histone deacetylase (HDAC) enzymes or known PDE enzyme isoforms and did not act as an antagonist at A2 or A2 receptors. (drugbank.ca)
  • Both compounds in high doses reduced the mouse locomotor activity, and in doses not affecting activity inhibited the motor stimulation induced by amphetamine, 2 or 3 mg/kg ip, but facilitated the hyperactivity induced by 10 mg/kg of morphine. (eurekamag.com)
  • anti-hypertensive drugs dose should be titrated against the response, because rapid falls in BP can cause? (cram.com)
  • ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β 2 adrenergic receptor, as few other specific antagonists for this receptor are known. (wikipedia.org)
  • Attenuation of EGFR activity without physical downregulation of the receptor could represent a novel therapeutic approach toward malignancies in which EGFR plays a primary role in tumor growth and survival. (embl-heidelberg.de)
  • Our study provides translational insights into mechanisms underlying amyloid-beta protein toxicity, which may have strong implications for future drug design," said Qin Wang, M.D., Ph.D. "It identifies an amyloid-beta/G protein-coupled receptor interaction that represents an attractive, disease-specific therapeutic target for Alzheimer's disease. (eurekalert.org)
  • Because of their efficacy and once-daily dosing, the prostaglandin analogues are typical first-line agents, although others can also be used as a primary choice. (medscape.com)
  • Functional subsensitivity of 5-hydroxytryptamine1C or alpha 2 adrenergic heteroreceptors mediating clonidine-induced growth hormone release in the Fawn-Hooded rat strain relative to the Wistar rat strain. (aspetjournals.org)
  • Administration of various doses of clonidine increased plasma growth hormone levels. (aspetjournals.org)
  • Also, epidemiologic analysis of cases from the National Alzheimer's Coordinating Center showed that taking the drug clonidine -- an activator of alpha-2A adrenergic receptor used to lower blood pressure -- worsened cognitive function in patients with cognitive deficits. (eurekalert.org)
  • In the present study an attempt was made to further elucidate the molecular mechanisms whereby protein kinase C (PKC) modulates the beta-cell stimulus-secretion coupling. (diva-portal.org)
  • This characteristic makes it ideal for monitoring the translocation of cell surface receptors into the endosomal pathway. (bio-medicine.org)
  • The pD 2 values (-log of the dose that produces 50% of the maximal responses) for arbutamine and isoproterenol were 8.45 ± 0.15 and 8.55 ± 0.02, respectively. (elsevier.com)
  • We used uniform methodology to investigate BB dose-ADRB1 Arg389Gly polymorphism interaction with major clinical end points in BEST/bucindolol and HF-ACTION/other BB databases. (cdc.gov)
  • Subjects were genotyped for ADRB1 Arg389Gly and ADRA2C (α2C adrenergic receptor) Ins322-325Del. (cdc.gov)
  • Conclusions The enhanced HF with reduced ejection fraction efficacy of bucindolol in the ADRB1 Arg389Arg versus 389Gly carrier genotypes occurs at high dose. (cdc.gov)
  • All patients should be monitored for symptom worsening or suicidality, especially at treatment initiation or after dose changes. (pdr.net)
  • A 26-week, parallel-arm placebo-controlled study (Study 1) evaluated HETLIOZ (n=42) compared to placebo (n=42) in patients with Non-24. (rxlist.com)
  • A guideline from the American Urological Association recommends beta-3-adrenergic receptor agonists as second-line therapy in patients with an inadequate response to behavioral therapy. (medscape.com)
  • Therefore, these patients generally require high-dose immunoglobulin therapy an. (bioportfolio.com)
  • The study measured the change in patients' forced expiratory volume over 1 second (FEV1, the maximum volume of air they could breathe out in 1 second) just before their next dose was due. (europa.eu)
  • After 26 weeks of treatment, FEV1 improved by 65 ml more in patients treated with Zimbus Breezhaler than in patients using an inhaler containing equivalent doses of indacaterol and mometasone, two of the three active substances in Zimbus Breezhaler. (europa.eu)
  • For renal-impaired or elderly patients, a lower dose of 25 mg once a day may be used if they have a creatinine clearance of under 15 ml/min or a maximum dose of 50 mg a day if the creatinine clearance is 15 to 35 ml/min. (statpearls.com)
  • When discontinuing long-term therapy, particularly in patients with ischemic heart disease, reduce dosage gradually over 1 to 2 weeks and monitor patient carefully. (thefreedictionary.com)
  • In both studies, the main measure of effectiveness was how Ultibro Breezhaler improved patients' forced expiratory volumes (FEV 1 , the maximum volume of air a person can breathe out in one second) after 26 weeks of treatment. (europa.eu)
  • Benson MK, Berrill WT, Cruickshank JM, Sterling GS (1978) A comparison of four β-adrenoceptor antagonists in patients with asthma. (springer.com)
  • Dorow P, Tönnesmann U (1984) Dose-response relationship for the β-adrenoceptor antagonist bisoprolol in patients with coronary heart disease and chronic obstructive bronchitis. (springer.com)
  • For example, it is recommended that the insulin dose be decreased by 10% to 25% when fasting plasma glucose concentrations decrease to less than 120 mg/dL in patients receiving concomitant insulin and metformin. (pdr.net)
  • This theory suggests why multiple clinical trials to reduce levels of amyloid-beta oligomers in Alzheimer's disease patients have failed -- they cannot reduce the amyloid levels to such low concentrations. (eurekalert.org)
  • The researchers found that alpha-2A adrenergic receptor from the postmortem prefrontal cortexes of Alzheimer's disease patients had a significant increase in alpha-2A adrenergic receptor activity, compared with non-demented, low-pathology controls. (eurekalert.org)
  • 6,906 patients) of soluble urokinase-type plasminogen activator receptor (suPAR, at or within 24 h of admission) as a biomarker for sepsis and confirmed elevated suPAR levels had moderate sensitivity/specificity in differentiating sepsis from systemic inflammatory response syndrome (SIRS) and for mortality prediction. (lww.com)
  • In some patients with sexual relief from symptoms, an toned dose of 60 mg once again may increase efficacy. (chuyenmach.com)
  • Pungent endarterectomy and prevention of reproductive ischemia in healthy carotid stenosis The proportion of patients down rescue medication usage within the first 24 hours of dosing was Arcoxia 90 mg 90 tabl. (chuyenmach.com)
  • β 1 -adrenergic receptors are located mainly in the heart and in the kidneys. (wikipedia.org)
  • It works by blocking beta-adrenergic receptors in the heart, which leads to decreased force and rate of heart contractions. (drugbank.ca)
  • Systolic and diastolic blood pressures (SBP, DBP), heart rate (HR) as well as airway resistance (AWR, and less frequently forced expiratory volume in 1 s (FEV 1 ) and intrathoracic gas volume (ITGV) were measured in the sitting position before and at various times up to 24 h after drug intake. (springer.com)
  • In dog studies, doxofylline decreased airway responsiveness at a dose that did not affect heart rate and respiratory rate 6 . (drugbank.ca)
  • In clinical practice, most experience has been gained with the use of nifedipine, whose efficacy is superior or comparable to those of β-agonists and oxytocin antagonists. (mdpi.com)
  • Common systemic doses used in rodent research are 0.5 or 1 mg/kg although efficacy has been demonstrated at doses as low as 0.0001 mg/kg in rhesus monkeys . (wikipedia.org)
  • Other BBs taken at low dose have reduced efficacy for Arg389Arg genotype subjects compared with 389Gly carriers, suggesting a greater relative treatment effect at high dose. (cdc.gov)
  • In arcoxia 20mg xr, low doses are found to strongly activate NE and DA neurotransmission within the os cortex which is an area of the most thought to play a prominent side in ADHD pathophysiology, thereby improving clinical efficacy and vomiting side effects. (chuyenmach.com)
  • In checker, low doses are found to considerably activate NE and DE neurotransmission within the greasy cortex which is an option of the brain thought to enchain a prominent role in ADHD pathophysiology, thereby necessitating clinical efficacy and preventing side effects. (chuyenmach.com)
  • The most common side effects with Zimbus Breezhaler (which may affect more than 1 in 10 people) are worsening of asthma and nasopharyngitis (inflammation in the nose and throat). (europa.eu)
  • Other common side effects (which may affect up to 1 in 100 people) include upper respiratory tract infection (nose and throat infections) and headache. (europa.eu)
  • The duration of action is dose-related - following administration of a dose, the effects are apparent within an hour and are maximal at 2 to 4 hours, persisting for at least 24 hours. (statpearls.com)
  • In certain cancers, TNF is infused locally to promote tumor regression, but dose-limiting inflammatory effects limit broader utility. (duke.edu)
  • The most common side effects with Ultibro Breezhaler (which may affect more than 1 in 10 people) are upper-respiratory-tract infections (colds). (europa.eu)
  • Day one I felt negative side effects after taking the second dose. (chuyenmach.com)
  • In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors and lacks stimulating effects. (drugbank.ca)