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.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 beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.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.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 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.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.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.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Butoxamine: A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.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.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 beta-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS.Timolol: A beta-adrenergic antagonist similar in action to PROPRANOLOL. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor.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.Medetomidine: An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE.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.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.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.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.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic 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.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.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.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).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.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.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.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.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.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.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.Muscarinic Antagonists: Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.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.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Piperidines: A family of hexahydropyridines.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.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.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Leukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.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.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.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).Receptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.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.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.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.Calcium Channel Blockers: A class of drugs that act by selective inhibition of calcium influx through cellular membranes.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.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.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.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.Benzazepines: Compounds with BENZENE fused to AZEPINES.Biphenyl CompoundsEstrogen Antagonists: Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.PiperazinesSulfonamides: A group of compounds that contain the structure SO2NH2.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.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.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.Xanthines: Purine bases found in body tissues and fluids and in some plants.Purinergic P2X Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.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.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).Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Indoles: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.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.Azepines: Seven membered heterocyclic rings containing a NITROGEN atom.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.Cannabinoid Receptor Antagonists: Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.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.PyrrolidinesTetrazolesProstaglandin Antagonists: Compounds that inhibit the action of prostaglandins.Electric Stimulation: Use of electric potential or currents to elicit biological responses.QuinoxalinesReceptors, Neurokinin-1: A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.Neurons: The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Behavior, Animal: The observable response an animal makes to any situation.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.GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.Mineralocorticoid Receptor Antagonists: Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.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.Oligopeptides: Peptides composed of between two and twelve amino acids.Time Factors: Elements of limited time intervals, contributing to particular results or situations.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.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.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.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)Muscle Contraction: A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.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.Receptors, Cholecystokinin: Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Receptor, Endothelin B: A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.BenzodiazepinonesInjections, Intraventricular: Injections into the cerebral ventricles.N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Receptors, Bradykinin: Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.Bradykinin: A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.Receptors, Neurokinin-2: A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.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.Cholinergic Antagonists: Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.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.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.Gonadotropin-Releasing Hormone: A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.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.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.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.Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.QuinuclidinesDevazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.QuinolinesMuscle, 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)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.Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.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.Receptors, Histamine H3: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)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.Isoindoles: Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.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.Receptors, Neurotransmitter: Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.Receptors, Corticotropin-Releasing Hormone: Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.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.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 D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Receptors, Metabotropic Glutamate: Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Mice, Inbred C57BLReceptors, Thromboxane: Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.TriazolesReceptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.Morphine: The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.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.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.Atropine: An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Naphthalenes: Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.Peptide Fragments: Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.Pirenzepine: An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.Endothelins: 21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.Histamine Agonists: Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.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.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.Vasoconstriction: The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.Tachykinins: A family of biologically active peptides sharing a common conserved C-terminal sequence, -Phe-X-Gly-Leu-Met-NH2, where X is either an aromatic or a branched aliphatic amino acid. Members of this family have been found in mammals, amphibians, and mollusks. Tachykinins have diverse pharmacological actions in the central nervous system and the cardiovascular, genitourinary, respiratory, and gastrointestinal systems, as well as in glandular tissues. This diversity of activity is due to the existence of three or more subtypes of tachykinin receptors.Hippocampus: A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.Receptor, Bradykinin B2: A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Receptors, Angiotensin: Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.Electrophysiology: The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Kinetics: The rate dynamics in chemical or physical systems.Receptor, Serotonin, 5-HT2A: A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.Patch-Clamp Techniques: An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.Receptors, Tachykinin: Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.Parasympatholytics: Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
Metabotropic glutamate receptor 1
... as mGluR1 antagonists block adrenergic receptor activation in neurons. Mice lacking functional glutamate receptor 1 were ... selective allosteric antagonist YM-298,198 and [3H]-analog: selective non-competitive antagonist FTIDC: highly potent and ... A respectable number of potent and specific allosteric ligands - predominantly antagonists/inhibitors - has been developed in ... selective allosteric antagonist/inverse agonist A-841,720: potent non-competitive antagonist; minor hmGluR5 binding VU-71: ...
Optimal Agonist/Antagonist Combinations Maintain Receptor Response by Preventing Rapid β-adrenergic Receptor Desensitization , ... BIO BALANCE Molecular dynamics of a biophysical model for b2-adrenergic and G protein-coupled receptor activation , BIO BALANCE ... Whereas antagonists have no preference in their affinity for a receptor state. The fact that receptor conformation (state) ... The del Castillo-Katz mechanism divorces the binding step (that can be made by agonists as well as antagonists) from the ...
... drugs such as the α2 adrenergic receptor antagonist atipamezole and the CB1 cannabinoid antagonist SR141716A (rimonabant) with ... It is believed that activation of biochemical receptors on the surfaces of neurons is involved in epileptogenesis; these ... activation of the mammalian target of rapamycin (mTOR) by drugs such as rapamycin; the hormone erythropoietin; and, ...
In such cases, curative agents such as adrenergic agonists and antagonists are used to modify epinephrine and norepinephrine ... In some cases, obesity in individuals is due to the overproduction of corticoids leads to the over-activation of receptor type ... The activation of the system is assisted by norepinephrine, acetylcholine, and epinephrine. Hypoglycemia unawareness can occur ... The sympathoadrenal system works to return the body to homeostasis through the activation or inactivation of the adrenal gland ...
... is an allosteric agonist and modulator of the 5-HT3 receptor and an antagonist of the α2A-adrenergic receptor. It has ... Michaelson SD, Paulsen IM, Kozuska JL, Martin IL, Dunn SM (2013). "Importance of recognition loops B and D in the activation of ... mCPP Bufotenidine (5-HTQ) Miles TF, Lester HA, Dougherty DA (2015). "Allosteric activation of the 5-HT3AB receptor by mCPBG". ...
A larger controlled Phase II "Clinical Trial of the Adrenergic Alpha-1 Antagonist Prazosin for Alcohol Dependence" is currently ... Its activity occurred via a PKCδ‐dependent inhibition of the AKT pathway, which resulted in caspase‐3 activation. So, prazosin ... "A pilot trial of the alpha-1 adrenergic antagonist, prazosin, for alcohol dependence". Alcoholism: Clinical and Experimental ... Day, H. E.; Campeau, S.; Watson Jr, S. J.; Akil, H. (1997). "Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic ...
... is a partial agonist/antagonist on serotonergic, dopaminergic and alpha-adrenergic receptors. Its specific ... binding and activation pattern on these receptors leads to a highly, if not completely, specific contraction of smooth uterus ... dopaminergic and adrenergic receptors". In Vladimír Křen,Ladislav Cvak. Ergot: the genus Claviceps. CRC Press. pp. 411-440. ...
The sympatholytic antihypertensive drug urapidil is an α1-adrenergic receptor antagonist and 5-HT1A receptor agonist, and it ... 5-HT1A receptor activation has been shown to increase dopamine release in the medial prefrontal cortex, striatum, and ... Activation of 5-HT1A receptors has been demonstrated to impair certain aspects of memory (affecting declarative and non- ... Activation of central 5-HT1A receptors triggers the release or inhibition of norepinephrine depending on species, presumably ...
They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... preventing postsynaptic adrenergic receptor activation and downstream signaling. Another way to inhibit adrenergic receptor ... ICI-118,551 Highly selective β2-adrenergic receptor antagonist - No known clinical applications, but used in experiments due to ... ganglion type receptor antagonist) Peripherally acting Guanethidine (Magnesium-ATPase inhibitor) Indoramin (α1 antagonist) ...
For example, if the natural activation of the α1-adrenergic receptor leads to vasoconstriction, an α1-adrenergic antagonist ... The α-adrenergic antagonists have different effects from the β-adrenergic antagonists. Adrenergic ligands are endogenous ... While a only a few α-adrenergic antagonists are competitive, all β-adrenergic antagonists are competitive antagonists. ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ...
... is an α1 adrenergic agonist and an α2 adrenergic antagonist". Journal of Pharmacology and Experimental Therapeutics ... Cirazoline has also been shown to decrease food intake in rats, purportedly through activation of α1 adrenoceptors in the ... a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α2 adrenergic receptor. It ... Cirazoline is a full agonist at the α1A adrenergic receptor, ...
Alpha-1D adrenergic receptor
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. They ... adrenergic receptor activity. • protein binding. • alpha1-adrenergic receptor activity. Cellular component. • integral ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ...
... α1-adrenergic receptors are members of the Gq protein-coupled receptor superfamily. Upon activation, a heterotrimeric G protein ... "Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Molecular ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... and β-Adrenergic Receptors Brief overview of functions of the β3 receptor Theory of receptor activation Desensitization of β1 ...
... is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker . ICI binds to the β2 ... with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic beta2-adrenoceptor activation". ... "Administration of a selective β2 adrenergic receptor antagonist exacerbates neuropathology and cognitive deficits in a mouse ... and characterization of beta-adrenergic binding sites on human fat cell membranes with highly selective beta-1 antagonists". ...
Alpha-1B adrenergic receptor
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. They ... The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... 2004). "Cell surface expression of alpha1D-adrenergic receptors is controlled by heterodimerization with alpha1B-adrenergic ...
Alpha-2A adrenergic receptor
"Gi-mediated activation of the p21ras-mitogen-activated protein kinase pathway by alpha 2-adrenergic receptors expressed in ... seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in ...
... and was instead found to act as a potent and selective 5-HT2A and α1-adrenergic receptor antagonist (Ki = 75 nM and 86 nM, ... and instead exerts a behavioral profile indicative of serotonergic activation. Trazodone J. Elks (14 November 2014). The ... but it does have some affinity for the α2-adrenergic receptor (Ki = 730 nM), likely acting as an antagonist there as well. ... respectively). It possesses low or no affinity for the 5-HT1A, 5-HT2B, D2, and β-adrenergic, as well as at SERT and VMAT (Ki = ...
... effects appear to be mediated via prevention of activation of serotonin 5-HT2A receptors and postsynaptic α2-adrenergic ... Rhynchophylline is a non-competitive NMDA antagonist found in kratom. Mitragynine is metabolized in humans via phase I and ... and these may be responsible for the molecules observed in the serotonin and adrenergic systems. Mitragynine is structurally ...
... while adrenaline raises arterial pressure through vasoconstriction mediated by alpha-adrenergic receptor activation. Our ... Uncompetitive antagonists differ from non-competitive antagonists in that they require receptor activation by an agonist before ... As for non-competitive antagonists and irreversible antagonists in functional assays with irreversible competitive antagonist ... The bound antagonists may prevent conformational changes in the receptor required for receptor activation after the agonist ...
Alpha-1 adrenergic receptor
α1-Adrenergic receptors are members of the G protein-coupled receptor superfamily. Upon activation, a heterotrimeric G protein ... Various heterocyclic antidepressants and antipsychotics are α1-adrenergic receptor antagonists as well. This action is ... In particular, norepinephrine decreases glutamatergic excitatory postsynaptic potentials by the activation of α1-adrenergic ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ...
Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ... Alpha-2 adrenergic receptor agonistsEdit. Central alpha agonists lower blood pressure by stimulating alpha-receptors in the ... Aldosterone receptor antagonists are not recommended as first-line agents for blood pressure, but spironolactone and ... However, ACE inhibitors (and angiotensin II receptor antagonists) should not be a first-line treatment for black hypertensives ...
Alpha-2 adrenergic receptor
α2C selective blockers include JP-1302 and spiroxatrine, the latter also being a serotonin 5-HT1A antagonist. Adrenergic ... In particular, phosphorylase kinase is responsible for the phosphorylation and activation of glycogen phosphorylase, an enzyme ... "Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... where it sits alongside the more plentiful α1-adrenergic receptor. The α2-adrenergic receptor binds both norepinephrine ...
Beta-3 adrenergic receptor
Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ...
... in human failing heart and antagonists of 5-HT2B receptors were uncovered to prevent both angiotensin II or beta-adrenergic ... activation of phospholipase C activity. • protein kinase C signaling. • cGMP biosynthetic process. • cellular response to ... AntagonistsEdit. *Agomelatine - primarily a melatonin Mt1/Mt2 receptor agonist, with a less potent antagonism of 5-HT2B and 5- ... Lisuride: a dopamine agonist of the ergoline class, that is also a 5-HT2B antagonist and a dual 5-HT2A/C agonist ...
... in human failing heart and antagonists of 5-HT2B receptors were uncovered to prevent both angiotensin II or beta-adrenergic ... Surprisingly however 5-HT2B receptor activation appears to be protective against the development of serotonin syndrome ... Metadoxine: a 5ht2b antagonist and GABA-activity modulator SDZ SER-082: a mixed 5-HT2B/C antagonist EGIS-7625: high selectivity ... that is also a 5-HT2B antagonist and a dual 5-HT2A/C agonist Tegaserod: primarily a 5-HT4 agonist, but also a 5-HT2B antagonist ...
Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta ... Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, ... β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors are located mainly in the ... β3-adrenergic receptors are located in fat cells. Beta receptors are found on cells of the heart muscles, smooth muscles, ...
... related to ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic ... activation of phospholipase D, Rho/Rho kinase, and ERK pathway activation initiated by agonist stimulation of the receptor.[ ... Other antagonists are MDL-100,907 (prototype of another new series of 5-HT2A antagonists) and cyproheptadine. Pizotifen is a ... Trazodone is a potent 5-HT2A antagonist, as well as an antagonist on other serotonin receptors. Mirtazapine is a 5-HT2A, 5-HT2C ...
The drug appears to work by increasing levels of serotonin and norepinephrine and by blocking certain serotonin, adrenergic, ... imipramine is an antagonist of the histamine H1 receptors. BDNF: BDNF is implicated in neurogenesis in the hippocampus, and ... which is associated with transcriptional activation and decondensed chromatin) at the hippocampal BDNF promotor, and also ... Epinephrine: imipramine antagonizes adrenergic receptors, thus sometimes causing orthostatic hypotension. Sigma receptor: ...
Dopamine receptor antagonists have sedative and antiemetic properties. Previously, they were used in parallel with opioids to ... This drug-elicted channel activation has been shown to be dependent upon specific amino-acids within certain K2P channels (i.e ... Administration of the alpha2 adrenergic receptor agonist dexmedetomidine leads to sedation that resembles non-REM sleep. It is ... It is postulated that general anaesthetics exert their action by the activation of inhibitory central nervous system (CNS) ...
... by drugs known as neurokinin type 1 antagonists (also termed: SP antagonists, or tachykinin antagonists.) One such drug is ... Their activation stimulates the vomiting reflex. Different emetic pathways exist, and substance P/NK1R appears to be within the ... administered through the non-adrenergic, non-cholinergic nervous system (branch of the vagal system). ... Muñoz M, Rosso M, Coveñas R (2010). "A new frontier in the treatment of cancer: NK-1 receptor antagonists". Current Medicinal ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... GnRH antagonists (e.g., cetrorelix). *Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone ... Researchers also examined how mild exercise affected androgen synthesis which in turn causes AHN activation of N-methyl-D- ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ...
However, they were able to prevent the amnesia induced by the AMPA receptor antagonist NBQX in the passive avoidance test, ... They specifically did not bind to the glutamate, GABA, serotonin, dopamine, adrenergic, histamine, acetylcholine, or opioid ... suggesting that indirect/downstream AMPA receptor activation may be involved in their memory-enhancing effects. Sunifiram, as ...
Agonists and antagonists. Specific antagonists include istradefylline (KW-6002) and SCH-58261, while specific agonists ... Mediero A, Frenkel SR, Wilder T, HeW MA, Cronstein BN (2012). "Adenosine A2A receptor activation prevents wearparticle-induced ... Specific antagonists include MRS1191, MRS1523 and MRE3008F20, while specific agonists include Cl-IB-MECA and MRS3558. ... Adenosine antagonists are widely used in neonatal medicine; A reduction in A1 expression appears to prevent hypoxia-induced ...
In addition to its activation, ALOX5 must gain access to its polyunsaturated fatty acid (PUFA) substrates, which commonly are ... Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... As a second drug added to corticosteroids, leukotriene inhibitors appear inferior to Beta2-adrenergic agonist drugs in the ... Wykle RL, Wijkander J, Nixon AB, Daniel LW, O'Flaherty JT (1996). "Activation of 85 kDa PLA2 by eicosanoids in human ...
Serotonin-norepinephrine reuptake inhibitor
This results in activation of α2 adrenergic receptors, as discussed previously. ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors. ... In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ...
Mu opioid; NMDA antagonist; SNRI.. PO, IM, IV, SC.. Protein binding = 40%; extensive first-pass metabolism; half-life = 12- ... "Combining opioid and adrenergic mechanisms for chronic pain". Postgraduate Medicine. 126 (4): 98-114. doi:10.3810/pgm.2014.07. ... "Flupirtine shows functional NMDA receptor antagonism by enhancing Mg2+ block via activation of voltage independent potassium ... Mixed opioid agonist-antagonist.. IM, IV.. Volume of distribution = 9-12 L/kg; half-life = 2.2-2.7 hours.. Moderate-severe pain ...
Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... but other drugs such as CB1 receptor antagonists exist in this class too. Drugs used to treat sleep disorders such as ... through activation of a trace amine receptor, increases biogenic amine and excitatory neurotransmitter activity in the brain, ... on adrenergic receptors. It is most usually marketed as the hydrochloride or sulfate salt. ...
5-HT4受體 - 维基百科，自由的百科全书
α1（英语：Alpha-1 adrenergic receptor） (A, B, D) · α2（英语：Alpha-2 adrenergic receptor） (A, B, C) · β1 · β2 · β3 ... Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) and 5-HT7(a). The Journal of Biological ... GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. British Journal of Pharmacology. January 1994 ...
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... and activation of ATP-sensitive potassium channels. In those with severe sepsis and septic shock, this sequence of events ... and H2 antagonist are useful in a person with risk factors of developing upper gastrointestinal bleeding (UGIB) such as on ...
Serotonin-norepinephrine-dopamine reuptake inhibitor
The nocaine analog JZAD-IV-22 only partly substituted for cocaine in animals, but produced none of the psychomotor activation ... Patients taking strong dopaminergic antagonists such as those used in the treatment of psychosis are more likely than the ... at functionally important adrenergic receptor sites in the brain. However, elation may be associated with an excess of such ... Although their primary mechanisms of action are as NMDA receptor antagonists, ketamine and phencyclidine are also SNDRIs and ...
Cysteinyl leukotriene receptor 2
The CysLT-induced activation of CysLTR2 induces many of the same in vitro responses of cells involved in allergic reactions as ... drugs which are selective receptor antagonists of CysLTR1 but not CysLTR2. Models of allergic reactions in ... a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma". Journal of Medicinal Chemistry. 58 (15): 6093-113. doi: ... and development asthma and that drugs targeting CYSLTR2 may work in a manner that differs from those of CYSLTR1 antagonists. ...
... activation of GPER has been found to be anxiogenic in mice, while activation of ERβ has been found to be anxiolytic. There ... CCL18 has been identified as an endogenous antagonist of the GPER. ... GPER is expressed in the breasts, and activation by estradiol produces cell proliferation in both normal and malignant breast ... negative regulation of leukocyte activation. • apoptotic chromosome condensation. • regulation of cytosolic calcium ion ...
... related to ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic ... activation of phospholipase D, Rho/Rho kinase, and ERK pathway activation initiated by agonist stimulation of the receptor.[ ... Silent antagonistsEdit. *Trazodone is a potent 5-HT2A antagonist, as well as an antagonist on other serotonin receptors. ... Other antagonists are MDL-100,907 (prototype of another new series of 5-HT2A antagonists) and cyproheptadine. ...
Pumu, kamusi elezo huru
O'Rourke ST (October 2007). "Antianginal actions of beta-adrenoceptor antagonists". Am J Pharm Educ 71 (5): 95. PMC 2064893 . ... Dalili kali hutibiwa na Beta2-adrenergic agonist ya kuvuta (kama vile salbutamol) na kotikosteroidi za mdomo. Katika visa ... Wood LG, Gibson PG (July 2009). "Masuala ya chakula husababisha innate immune activation katikia athma". Pharmacol. Ther. 123 ( ... Leukotriene antagonist (kama vile montelukast na zafirlukast) zinaweza kutumika kando na kotikosteroidi za kuvuta, pia pamoja ...
... beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, beta adrenergic receptor antagonists. ... Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta ... Beta-Adrenoceptor Antagonists (Beta-Blockers); "CV Pharmacology , Beta-Adrenoceptor Antagonists (Beta-Blockers)". Archived from ... Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, ...
An adrenergic antagonist selective for α1 receptors. *^ Reversal of reserpine-induced hypothermia by a drug is a classical test ... C. Carpéné, J. Galitzky, E. Fontana, C. Atgié, M. Lafontan, and M. Berlan (1999). "Selective activation of β3-adrenoceptors by ... β1 antagonist): 6.09 μM; ICI-118,551 (β2 antagonist): 3.58 μM; SR-5923A (β3 antagonist): 17 μM. ... a standard α1 antagonist) and ketanserin,[o] with prazosin being the more potent antagonist (pA2 = 9.38, vs pA2 = 8.23 for ...
G protein-coupled receptor
G-protein activation/deactivation cycleEdit. Cartoon depicting the Heterotrimeric G-protein activation/deactivation cycle in ... Regulation of beta2-adrenergic receptor dephosphorylation by vesicular acidification". The Journal of Biological Chemistry. 272 ... and neutral antagonists are ligands that do not affect the equilibrium. It is not yet known how exactly the active and inactive ... Crystal structure of activated beta-2 adrenergic receptor in complex with Gs(PDB entry 3SN6). The receptor is colored red, Gα ...
Dopamine receptor D4
Apomorphine - D4 selective but also D2 and D3 agonist, α-adrenergic and serotonergic weak antagonist ... activation of MAPK activity. • behavioral response to cocaine. • positive regulation of sodium:proton antiporter activity. • ... Lanig H, Utz W, Gmeiner P (April 2001). "Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[ ... an antagonist with high affinity and selectivity for the human dopamine D4 receptor". Journal of Medicinal Chemistry. 39 (10): ...
Category:Dopamine antagonists. References. *^ Girault JA, Greengard P (2004). "The neurobiology of dopamine signaling". ... Dopamine receptor activation of Ca2+/calmodulin-dependent protein kinase II can be cAMP dependent or independent. ... Beta arrestin has been shown to form complexes with MAP kinase, leading to activation of Extracellular signal-regulated kinases ... resulting in activation of mTOR. The behavioral implications are unknown. Dopamine receptors may also regulate ion channels and ...
... receptor D2 agonist bromocriptine inhibits glucose-stimulated insulin secretion by direct activation of the α2-adrenergic ... Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Antagonists: Agomelatine. *Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, ...
Prostaglandin DP2 receptor
The following compounds are selective receptor antagonists of and thereby inhibit the activation of DP2: fevipiprant, ... "Mechanisms of cell activation"). The DP2 receptor antagonist, AZD1981, is in a phase 2 clinical trial for the treatment of ... Ligand-induced activation of DP2 has similar activities in vivo it stimulates the accumulation on and activation of eosinophils ... activation of GIRK channels and activation of GRK. IP3 raises cytosolic Ca2 levels thereby regulating Ca2-sensitive signal ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Lejeune F, Millan MJ (1998). "Induction of burst firing in ventral tegmental area dopaminergic neurons by activation of ... dopamine hD2/hD3 and h alpha2A-adrenergic receptors in relation to modulation of cortical monoamine release and activity in ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ...
Postural orthostatic tachycardia syndrome
Alpha-2 adrenergic antagonist Increase blood pressure Yohimbine Prognosis. POTS has a favorable prognosis when ... Mast cell activation disorder (6-9%). Autoimmunity. There is an increasing number of studies indicating that POTS is an ... Alpha-1 adrenergic receptor agonist Constrict the peripheral blood vessels aiding venous return. Midodrine ... alpha-2 adrenergic receptor agonist Decreases blood pressure and sympathetic nerve traffic. Clonidine, Methyldopa ...
Pure β-blockers do not inhibit lid-retraction in the eyes, which is mediated by alpha adrenergic receptors. ... Agents that act as antagonists at thyroid stimulating hormone receptors are currently under investigation as a possible ... autoimmune activation of orbital fibroblasts, which in TAO express the TSH receptor, is thought to play a central role. ...
However, they were able to prevent the amnesia induced by the AMPA receptor antagonist NBQX in the passive avoidance test, ... They specifically did not bind to the glutamate, GABA, serotonin, dopamine, adrenergic, histamine, acetylcholine, or opioid ... "AMPA-receptor activation is involved in the antiamnesic effect of DM 232 (unifiram) and DM 235 (sunifiram)". Naunyn- ... suggesting that indirect/downstream AMPA receptor activation may be involved in their memory-enhancing effects. Galeotti, N.; ...
Posttraumatic stress disorder
Prazosin, an alpha-1 adrenergic antagonist, has been used in veterans with PTSD to reduce nightmares. Studies show variability ... "Behavioral Activation in the Treatment of Comorbid Posttraumatic Stress Disorder and Major Depressive Disorder". International ... adrenergic inhibitors, antipsychotics, and even anticonvulsants), benzodiazepines should be considered relatively ...
The β2-adrenergic receptor antagonist ICI-118,551 blocks the constitutively activated HIF signalling in hemangioblastomas from...
... is the constitutive activation of the HIF pathway. This activation ends up in the generation of Central Nervous System (CNS) ... Propranolol, a non-specific β1-and β2-adrenergic receptor antagonist, was recently designated as the first therapeutic (orphan ... In order to overcome the β1-drawback, the properties of a high specific β2-adrenergic receptor blocker named ICI-118,551 have ... reducing significantly the activation of HIF-target genes and halting the tumour-related angiogenic processes. In this work, we ...
PTSD Symptom Reduction by Propranolol Given After Trauma Memory Activation - Full Text View - ClinicalTrials.gov
The treatment of heart failure: the role of neurohumoral activation.
It is now known that neurohumoral activation contributes to the transition from ventricular ... Neurohumoral activation refers to increased activity of the sympathetic nervous system, renin-angiotensin system, vasopressin ... Adrenergic beta-Antagonists / therapeutic use. Angiotensin-Converting Enzyme Inhibitors / therapeutic use. Clinical Trials as ... 0/Adrenergic beta-Antagonists; 0/Angiotensin-Converting Enzyme Inhibitors; 0/Neurotransmitter Agents; 0/Receptors, Angiotensin ...
Catecholamine-induced vasoconstriction is sensitive to carbonic anhydrase I activation
... and beta-adrenergic agonists activated purified and red cell CA while adrenergic antagonists inhibited CA and reduced the ... Puscas I, Buzas G & Moldovan A (1985). Effect of beta-adrenergic agonists and antagonists on carbonic anhydrase. Revue Roumaine ... Puscas I, Pasca R, Lazoc L & Kun C (1994). Effects of alpha- and beta-adrenergic agonists and antagonists on carbonic anhydrase ... 1. Hoffman BB & Lefkowitz RJ (1996). Catecholamines, sympathomimetic drugs, and adrenergic receptor antagonists. In: Molinoff ...
Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( ...
2-adrenergic,receptor,antagonists,using,CypHer5E,and,IN,Cell,Analyzer,1000,biological,advanced biology technology,biology ... has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 ... Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs ...
Adrenergic antagonist - Wikipedia
For example, if the natural activation of the α1-adrenergic receptor leads to vasoconstriction, an α1-adrenergic antagonist ... The α-adrenergic antagonists have different effects from the β-adrenergic antagonists. Adrenergic ligands are endogenous ... While a only a few α-adrenergic antagonists are competitive, all β-adrenergic antagonists are competitive antagonists. ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ...
ANS neuropharmacology Flashcards by Tiffany Pointon | Brainscape
Name the primary modes of action of adrenergic antagonists and clinical utility ... Activation of a2 receptors: decreases sympathetic activity ... List adrenergic receptor blockers and which receptor they block ... Produce the same effect as NE and Epi at α- and β-adrenergic receptors on sympathetic end organs. Direct agonists activate ... Interference with adrenergic function in the presynaptic neuron via block of synthesis, storage or release ...
Antihypertensive question set 7
Stimulation of Phospholipase D via α1-Adrenergic Receptors in Madin-Darby Canine Kidney Cells is Independent of PKCα and -ε...
... an α-adrenergic antagonist, and propranolol, a β-adrenergic antagonist. Complete inhibition of epinephrine-induced PEt ... To investigate whether activation of PKCα or other PKC isoforms plays a similar regulatory role in α1-adrenergic stimulation of ... PLD activation is downstream of activation of PKCα. Taken together, the data thus indicate that activation of PLD, in a ... 1992) α1-Adrenergic receptor-mediated activation of phospholipase D in rat cerebral cortex. J Biol Chem 267:3679-3685. ...
Repeated Social Defeat, Neuroinflammation, and Behavior: Monocytes Carry the Signal | Neuropsychopharmacology
... β-adrenergic receptor antagonist, before stress reexposure. Therefore, sympathetic activation of NE is an early mediator in ... In support of this, daily administration of the β-adrenergic antagonist propranolol before social defeat reduced primed and GC- ... Johnson JD, Zimomra ZR, Stewart LT (2013). Beta-adrenergic receptor activation primes microglia cytokine production. J ... Social defeat also initiates brain-to-immune outflow via SNS and HPA axis activation. SNS and HPA activation shifts peripheral ...
CCK Stimulation of GLP-1 Neurons Involves α1-Adrenoceptor-Mediated Increase in Glutamatergic Synaptic Inputs | Diabetes
Its effect is occluded by either α-adrenergic receptor antagonists or non-NMDA glutamate receptor antagonists. Thus, it acts ... and this involved activation of α1-adrenergic receptors. Inhibition of adrenergic signaling abolished the excitatory action of ... The effect of epinephrine is blocked by the glutamate receptor antagonist kynurenic acid (Kyn) and by the α-adrenergic receptor ... and activation of α2-adrenoceptors causes hyperphagia (41,42). The findings that the satiety factor CCK activates adrenergic/ ...
Question of Strength 56 | T Nation
Stimulants and antagonists of the alpha-adrenergic receptors are effective, but not magic. They should be used carefully, only ... When activated they increase heart rate, CNS activation, energy mobilization (including fat) and muscle strength. These are the ... Some supplements are antagonists of the alpha adrenergic receptors. This simply means that these supplements block the alpha ... Increased Fat Mobilization Via Inhibition of the Alpha-Adrenergic Receptors. We have two main types of adrenergic (adrenaline) ...
A Category Names List - Drug Information Portal - U.S. National Library of Medicine
Adrenergic alpha-2 Receptor Antagonists (5) • Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS. MeSH ... Adrenergic Antagonists (132) • Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the ... Adrenergic beta-1 Receptor Antagonists (10) • Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS. MeSH ... Adrenergic beta-2 Receptor Antagonists (1) • Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS. MeSH ...
PRIME PubMed | Clonidine depresses LTP of C-fiber evoked field potentials in spinal dorsal horn via NO-cGMP pathway
Adrenergic alpha-2 Receptor AgonistsAdrenergic alpha-AgonistsAdrenergic alpha-AntagonistsAfferent PathwaysAnimalsClonidine ... Activation of spinal d1/d5 receptors induces late-phase LTP of C-fiber-evoked field potentials in rat spinal dorsal horn. ... 4) Pretreatment with alpha2-adrenergic receptor antagonist yohimbine completely blocked the inhibitory effect of clonidine. (5 ... 4) Pretreatment with alpha2-adrenergic receptor antagonist yohimbine completely blocked the inhibitory effect of clonidine. (5 ...
Metabotropic glutamate receptor 1 - Wikipedia
... as mGluR1 antagonists block adrenergic receptor activation in neurons. Mice lacking functional glutamate receptor 1 were ... selective allosteric antagonist YM-298,198 and [3H]-analog: selective non-competitive antagonist FTIDC: highly potent and ... A respectable number of potent and specific allosteric ligands - predominantly antagonists/inhibitors - has been developed in ... selective allosteric antagonist/inverse agonist A-841,720: potent non-competitive antagonist; minor hmGluR5 binding VU-71: ...
Adrenergic Agonists and Antagonists at University of Texas - Health Science Center at Houston - StudyBlue
Study 53 Adrenergic Agonists and Antagonists flashcards from Alex L. on StudyBlue. ... activation of alpha-receptors may be used for ________ for local anesthesia, hemorrhage, hemostasis during surgery ... reuptake into adrenergic neurons; NE feedback inhibiton on alpha2-adrenergic receptors; diffusion from site of action; ... activation of beta receptors blocks mast cell degranulation, prevents CV collapse, supports BP, prevents suffocation ...
Serotonin HTR1 Group and FOS Pathway (Homo sapiens) - WikiPathways
Identification of adenylate cyclase-coupled beta-adrenergic receptors with radiolabeled beta-adrenergic antagonists.; Biochem ... Indirect activation by Pak3 and protein kinase C.; J Biol Chem, 1997 PubMed Europe PMC Scholia*Yosimichi G, Nakanishi T, ... Silverman E, FrÃ Â¯Ã Â¿Ã Â½din M, Gammeltoft S, Maller JL; Activation of p90 Rsk1 is sufficient for differentiation of PC12 ... Mochizuki N, Ohba Y, Kobayashi S, Otsuka N, Graybiel AM, Tanaka S, Matsuda M; Crk activation of JNK via C3G and R-Ras.; J ...
Richard Burnard Rodnight, 1921-2012 - Dunkley - 2012 - Journal of Neurochemistry - Wiley Online Library
Frontiers | Involvement of gap junction channels in the pathophysiology of migraine with aura | Physiology
In the pathophysiology of migraine with aura, activation of the trigeminovascular system from the meningeal vessels mediates ... In the pathophysiology of migraine with aura, activation of the trigeminovascular system from the meningeal vessels mediates ... are also dopaminergic and adrenergic antagonists. Only two molecules are indicated in migraine attacks: ergotamine (exclusive ... The inhibition of Panx1 channel by carbenoxolone abolishes caspase 1 activation, NF-κB translocation and trigeminal activation ...
Norepinephrine Directly Activates Adult Hippocampal Precursors via β3-Adrenergic Receptors | Journal of Neuroscience
Only SR59230A (10 nm), a specific β3-adrenergic receptor antagonist, completely blocked the norepinephrine-mediated activation ... Next, to identify the subtype of β-adrenergic receptor involved, we tested selective antagonists to β1-, β2-, and β3-adrenergic ... A, Neither the α1-adrenergic receptor antagonist prazosin nor the α2-adrenergic receptor blocker yohimbine had any effect on ... The hippocampal cells were treated with specific antagonists to α1-adrenergic receptors (prazosin), α2-adrenergic receptors ( ...
β-Adrenergic Receptor Antagonism Prevents Anxiety-Like Behavior and Microglial Reactivity Induced by Repeated Social Defeat |...
... a unique pattern of c-Fos activation in the brain that was blocked by pretreatment with a β-adrenergic receptor antagonist. ... 1), it is plausible that β-adrenergic receptor activation promotes microglia/macrophage activation that contributes to the ... Because β-adrenergic receptor blockade with propranolol reduced c-Fos activation, the affect of propranolol on repeated social ... 1, 2). Although the induction of c-Fos was dependent on activation of β-adrenergic receptors, it did not depend on the presence ...
Textbook of Psychiatry/Psychopharmacology - Wikibooks, open books for an open world
It is an antagonist at alpha-2-adrenergic autoreceptors thereby increasing norepinephrine and serotonin release, and it blocks ... The reasons for this increase in suicidality are not clear, although increased agitation (e.g., akathisia) or activation as a ... Propranolol is a beta-adrenergic antagonist. Although it is primarily used medically for its effect on heart rate and blood ... Prazosin is an alpha-1-adrenergic receptor antagonist. Like clonidine, it is an antihypertensive which can decrease anxiety ...
Phosphorylation and activation of mitogen- and stress-activated protein kinase-1 in adult rat cardiac myocytes by G-protein...
Porcine hepatic response to sepsis and its amplification by an adrenergic receptor α1 agonist and a β2 antagonist Clin Sci ( ... Maximal activation of MSK1 in adult cardiomyocytes temporally coincided with maximal p38 MAPK activation while activation of ... However, little is known regarding the physiological activation of enzymes downstream of MAPKs. We examined the activation of ... Phosphorylation and activation of mitogen- and stress-activated protein kinase-1 in adult rat cardiac myocytes by G-protein- ...
Inverse Agonist Activity at the α2A-Adrenergic Receptor | Molecular Pharmacology
1999) G-protein activation by putative antagonists at mutant Thr373Lys α2A adrenergic receptors. Br J Pharmacol 126:939-948. ... Inverse Efficacies of α2-Adrenergic Antagonists.. We next looked at the effects of antagonists on forskolin-stimulated cAMP ... 1999) Gi activator region of α2A adrenergic receptors: Distinct basic residues mediate Gi vs Gs activation. Mol Pharmacol 56: ... 1992) Constitutive activation of the a1B-adrenergic receptor by all amino acid substitutions at a single site. Evidence for a ...
Analysis of Full and Partial Agonists Binding to β2-Adrenergic Receptor Suggests a Role of Transmembrane Helix V in Agonist...
Keywords: Adrenergic, GPCR, G-protein, agonist, antagonist, activation, flexible docking, binding energy, conformational change ... Beta2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch. The Journal ... Thus, most β-adrenergic agonists and antagonists have a positively charged amine or ethanolamine groups ("tails") which has ... A critical role for Ser-2035.42 in ligand binding to and activation of the beta 2-adrenergic receptor. The Journal of ...
Locus coeruleus integrity in old age is selectively related to memories linked with salient negative events | PNAS
... memory enhancement for emotional items can be attenuated by the beta-adrenergic antagonist propanolol (16, 17). The proposed ... We used MRI neuromelanin (NM) imaging to assess LC structural integrity and pupillometry as a putative index of LC activation ... 2004) Beta-adrenergic modulation of emotional memory-evoked human amygdala and hippocampal responses. Proc Natl Acad Sci USA ... 2010) Beta-adrenergic blockade during memory retrieval in humans evokes a sustained reduction of declarative emotional memory ...
Effect of Bee Venom Acupuncture on Oxaliplatin-Induced Cold Allodynia in Rats
We further confirmed that an intrathecal (i.t.) injection of idazoxan (α2-adrenergic receptor antagonist, 50 μg), but not N/S, ... BVA has been reported to attenuate neuropathic pain symptoms induced by CCI through activation of α2-adrenergic receptors, but ... We further confirmed that an intrathecal administration of idazoxan (α2-adrenergic antagonist, 50 μg) blocked the BVA-induced ... As shown in Figure 4, phentolamine- (α-adrenergic receptor antagonist, 2 mg/kg, i.p.) pretreated group exhibited no significant ...
Left Ventricular Remodeling With Carvedilol in Patients With Congestive Heart Failure Due to Ischemic Heart Disease | JACC:...
The beta-adrenergic antagonists may provide further benefit for patients with congestive heart failure through inhibition of ... 1990) Sympathetic activation in congestive heart failure. Eur Heart J 11(Suppl A):3-11. ... Beta-adrenergic blocking drugs have been shown to improve left ventricular ejection fraction in patients with heart failure due ... 1979) Haemodynamic effects of acute beta-adrenergic receptor blockade in congestive cardiomyopathy. Br Heart J 42:311-315. ...
Alpha Adrenergic Antagonist - Trip Database
Helping you find trustworthy answers on Alpha Adrenergic Antagonist , Latest evidence made easy ... Find all the evidence you need on Alpha Adrenergic Antagonist via the Trip Database. ... on cellular effects of receptor activation, and on relative affinities and reactions to synthetic blocking or stimulating ... Antagonists Adrenergic alpha-1 Receptor Antagonists Adrenergic Antagonists Adrenergic Agents Neurotransmitter Agents Molecular ...
7. In which disorder would beta-adrenergic antagonists be used to control symptoms?. ... increased sympathetic activation, such as nervousness, sweating and increased heart rate. For this reason, beta-adrenergic ... antagonists may be used to relieve symptoms.. Graves disease can be treated by drugs that inhibit thyroid hormone synthesis. ...
Agonists And AntagonistsAgonistPropranololPrazosinPhentolamineAlpha2-adrenergicStimulationRole of the adrenergic signalNeuronsYohimbineNorepinephrineLigandsIsoproterenolReceptor agonistsCalled adrenergic receptorsDopamineMediatesPharmacologicalVasoconstrictionGPCRBeta receptorsInhibitInhibitoryMuscarinicSubtypesAdrenoreceptorPathwaysAdenylate cyclaseEpinephrineGPCRsInhibitionAlpha 1bInhibitsInhibitorSelective allostericPotentConstitutively activeCompoundsSystemicCardiovascularCyclicEffectsCardiac outputSympathetic activationMechanismsVivoCongestiveAlprenolol
Agonists And Antagonists3
- Stereoisomers of beta-adrenergic agonists and antagonists were 9- to 300-fold more potent than their corresponding (+) stereoisomers. (duke.edu)
- Most of the knowledge regarding the role of adrenoceptors in glucose homeostasis has been derived from the use of adrenergic agonists and antagonists. (diabetesjournals.org)
- We have investigated the interactions between the cAMP and inositol 1,4,5-trisphosphate (IP3)-Ca2+ signalling systems in the bovine iris sphincter by measuring the effects of beta-adrenergic and cholinergic muscarinic agonists and antagonists on cAMP formation, IP3 accumulation and muscle contraction-relaxation. (arvojournals.org)
- Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). (bio-medicine.org)
- CypHer5 has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor expressing cells (2). (bio-medicine.org)
- Agonist and antagonist controls were placed symmetrically in columns 1 and 12 of each plate. (bio-medicine.org)
- Twelve replicate wells contained a known agonist, isoproterenol, and four replicate wells contai ned a known antagonist, alprenolol, each diluted in 0.01% DMSO. (bio-medicine.org)
- A competitive antagonist will attach itself to the same binding site of the receptor that the agonist will bind to. (wikipedia.org)
- This type of binding is reversible as increasing the concentration of agonist will outcompete the concentration of antagonist, resulting in receptor activation. (wikipedia.org)
- If the non-competitive antagonist binds to the allosteric site and an agonist binds to the ligand site, the receptor will remain unactivated. (wikipedia.org)
- This means only after the agonist binds to the receptor can the antagonist block the receptor's function. (wikipedia.org)
- In the current work, we investigated PLD activation in MDCK-D1 cells triggered by the adrenergic receptor agonist epinephrine and its mechanism of activation. (aspetjournals.org)
- In the current study, we examined the activation of PLD in MDCK-D1 cells stimulated by another stimulus, the adrenergic receptor agonist epinephrine. (aspetjournals.org)
- Mimicking the neurotransmitter action (Agonist at the receptor level), Blocking the neurotransmitter action (antagonist at the receptor level), or change normal action of transmitter indirectly (ie. (brainscape.com)
- Clonidine, a specific alpha2-adrenergic receptor agonist, has been found to be effective for the treatment of neuropathic pain, the mechanism underlying the effect is, however, not well understood. (unboundmedicine.com)
- Moreover, intrahippocampal injection of a selective β 3 -adrenergic receptor agonist in vivo increases the number of proliferating cells in the SGZ. (jneurosci.org)
- Similarly, systemic injection of the β-adrenergic receptor agonist isoproterenol not only results in enhancement of proliferation in the SGZ but also leads to an increase in the percentage of nestin/glial fibrillary acidic protein double-positive neural precursors in vivo . (jneurosci.org)
- Binding of agonist stabilizes R * causing G protein coupling and activation of cellular responses. (aspetjournals.org)
- The 2.4 Å crystal structure of the β 2 -adrenergic receptor (β 2 AR) in complex with the high-affinity inverse agonist (-)-carazolol provides a detailed structural framework for the analysis of ligand recognition by adrenergic receptors. (pubmedcentralcanada.ca)
- Insights into agonist binding and the corresponding conformational changes triggering GPCR activation mechanism are of special interest. (pubmedcentralcanada.ca)
- Importance of Alpha - adrenergic Receptor Subtypes in Regulating of Airways Tonus at Patients with Bronchial Asthma In this work, effect of Tamsulosin hydrochloride as antagonist of alpha1A and alpha1B- adrenergic receptor and effect of Salbutamol as agonist of beta2- adrenergic receptor in patients with bronchial asthma and increased bronchial reactibility was studied.Parameters of the lung function are determined by Body plethysmography. (tripdatabase.com)
- Bath application of 10 to 100 μM phenylephrine, an α 1 adrenergic receptor agonist, significantly increased the frequency of spontaneous excitatory postsynaptic currents in a concentration-dependent manner. (aspetjournals.org)
- Constitutive activation of G-protein-coupled receptors is a well recognized phenomenon, and G-protein-coupled receptor antagonists have been found to possess inverse agonist activity. (aspetjournals.org)
- Binding of agonist to receptors stabilizes R* causing G-protein-coupling and activation of cellular responses whereas binding of inverse agonist stabilizes the R at the expense of R*. It has been reported that the primary structure and the expression level of receptors are major factors that govern the equilibrium and therefore determines the intrinsic basal activity of GPCRs. (aspetjournals.org)
- This reaction sequence was applied to the synthesis of the β 3 -adrenergic receptor agonist solabegron. (diva-portal.org)
- Cirazoline is a full agonist at the alpha-1A (α1A) adrenergic receptor, a partial agonist at both the alpha-1B (α1B) adrenergic receptor and alpha-1D (α1D) adrenergic receptor, and a nonselective antagonist to the alpha-2 adrenergic receptor. (drugbank.ca)
- The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor. (psi.ch)
- The structural basis of agonist-induced activation in constitutively active rhodopsin. (psi.ch)
- It is a prodrug of aripiprazole , which acts as a partial agonist at the D2 and 5-HT1A receptors, and as an antagonist at the 5-HT2A receptors 1 . (drugbank.ca)
- The pharmacologic effects of beta-adrenergic agonist drugs, including albuterol are at least in part attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic - 3', 5' - adenosine monophosphate (cyclic AMP). (nih.gov)
- The two treatments used in the research were a CXCR4 antagonist, used for bone marrow transplants, and a beta-3 adrenergic agonist, that is used for bladder control. (infowars.com)
- Clonidine is an α2-adrenergic receptor agonist which, at low doses, inhibits noradrenergic signaling by decreasing norepinephrine release from presynaptic noradrenergic neurons. (iupui.edu)
- Controlled clinical studies and other clinical experience have shown that inhaled albuterol, like other beta-adrenergic agonist drugs, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or ECG changes. (nih.gov)
- Propranolol, a non-specific β1-and β2-adrenergic receptor antagonist, was recently designated as the first therapeutic (orphan) drug for VHL disease. (nature.com)
- Two examples of competitive adrenergic antagonists are propranolol and phentolamine. (wikipedia.org)
- Phentolamine Propranolol Nebivilol Atenolol Oxprenolol Metoprolol Timolol Pindolol Nadolol Pindolol Esmolol Acebutolol Sotalol Talinolol Betaxolol Labetalol Carvedilol Adrenergic antagonists have inhibitory or opposing effects on the receptors in the adrenergic system. (wikipedia.org)
- The stress-dependent changes in microglia and macrophages were prevented by propranolol, a β-adrenergic receptor antagonist. (jneurosci.org)
- Of particular significance was the finding that infusion of the beta-adrenergic antagonist propranolol into the amygdala blocked the effect of peripherally administered epinephrine. (psychologicalscience.org)
- To determine whether systemic application of propranolol, a nonselective β-adrenergic receptor antagonist, with an osmotic pump will decrease the b-wave amplitude of the electroretinogram (ERG) and increase insulin-like growth factor (IGF)-1 receptor signaling. (arvojournals.org)
- Young rats at 8 weeks of age were treated with saline, phentolamine, a nonselective α-adrenergic receptor antagonist, or propranolol, a nonselective β-adrenergic receptor antagonist, delivered by osmotic pumps for 21 days. (arvojournals.org)
- The beta-adrenergic antagonist, (-) propranolol, potently competed for the binding sites, causing half-maximal inhibition of binding at 9 nM. (duke.edu)
- Maximal activation of MAPK by isoprenaline was inhibited by the beta-adrenergic antagonist, propranolol, whereas the activation by noradrenaline was inhibited by the alpha1-adrenergic antagonist, prazosin. (gla.ac.uk)
- The depression-triggered bone loss is associated with a substantial increase in bone norepinephrine levels and can be blocked by the beta-adrenergic antagonist propranolol, suggesting that the sympathetic nervous system mediates the skeletal effects of stress-induced depression. (dericbownds.net)
- All of these events were blocked by pretreatment of cells with the α 1 -adrenergic antagonist prazosin. (aspetjournals.org)
- This effect was blocked by the α 1 adrenergic receptor antagonists prazosin or corynanthine. (aspetjournals.org)
- BK-induced tachycardia was attenuated (>90%) by the beta-adrenergic receptor antagonist sotalol, and the hypertensive response was attenuated (>70%) by the alpha-adrenergic receptor antagonist prazosin, indicating that effects of python BK are mediated at least in part by activation of the extensive network of adrenergic neurons present in vascular tissues. (eurekamag.com)
- In a separate group of male P rats, clonidine (40 µg/kg BW) suppressed intake of a saccharin solution (0.04 g/L). These results are consistent with and complement our previous findings that the α1-adrenergic receptor antagonist, prazosin, decreases voluntary alcohol drinking in alcohol-preferring rats, but suggests that effects of clonidine may not be specific for alcohol. (iupui.edu)
- Phentolamine is a competative and nonselective α-adrenoreceptor antagonist. (wikipedia.org)
- MK912, whereas phentolamine and idazoxan were essentially neutral antagonists. (aspetjournals.org)
- Phentolamine ( α -adrenergic antagonist, 2 mg/kg, i.p.) partially blocked the relieving effect of BVA on allodynia, whereas naloxone (opioid antagonist, 2 mg/kg, i.p.) did not. (hindawi.com)
- Structurally related compounds devoid of beta-adrenergic activity such as dopamine, dihydroxymandelic acid, normetanephrine, pyrocatechol, and phentolamine did not effectively compete for the binding sites. (duke.edu)
- 6. The method of claim 5 wherein the stimulation pulses are infusion pulses providing at least one of an inhibitory drug, GABA, phentolamine, and a norepinephrine antagonist. (google.es)
- 4) Pretreatment with alpha2-adrenergic receptor antagonist yohimbine completely blocked the inhibitory effect of clonidine. (unboundmedicine.com)
- METHODS: In study 1, healthy subjects were examined in a placebo-controlled, double-blind paradigm using yohimbine, an alpha2-adrenergic antagonist. (uzh.ch)
- 9 In CHF, it appears to act predominantly via stimulation of sympathoinhibitory α 2 -adrenergic and/or imidazoline receptors in the central nervous system, 10 and chronic administration has been demonstrated to attenuate the systemic sympathetic activation in CHF. (ahajournals.org)
- Stimulation of α 1 adrenergic receptors in the PVN increases sympathetic outflow, but the cellular mechanisms remain unclear. (aspetjournals.org)
- In particular, the stimulation of ventricular vagal receptors would be produced by an enhancement of heart contractility due to an exaggerated cardiac sympathetic activation. (ahajournals.org)
- Activation of beta-adrenergic receptors causes stimulation of cyclic AMP, inhibition of inositol trisphosphate, and relaxation of bovine iris sphincter smooth muscle. (arvojournals.org)
Role of the adrenergic signal1
- Another satiety hormone, cholecystokinin (CCK), has also been linked to activation of brain stem neurons, suggesting that it might act partially via centrally projecting neurons from the nucleus tractus solitarius (NTS). (diabetesjournals.org)
- Both CCK and epinephrine acted to increase glutamatergic transmission to the PPG neurons, and this involved activation of α 1 -adrenergic receptors. (diabetesjournals.org)
- CONCLUSIONS CCK activates NTS-PPG cells by a circuit involving adrenergic and glutamatergic neurons. (diabetesjournals.org)
- Activation of central GLP-1 receptors seems likely to require release of GLP-1 from PPG neurons. (diabetesjournals.org)
- A possible connection has been suggested between mGluRs and neuromodulators, as mGluR1 antagonists block adrenergic receptor activation in neurons. (wikipedia.org)
- In this study, we determined the role of α 1 adrenergic receptors in the regulation of glutamatergic and GABAergic synaptic inputs to spinally projecting PVN neurons. (aspetjournals.org)
- However, phenylephrine failed to increase the firing of most labeled PVN neurons in the presence of GABA A and ionotropic glutamate receptor antagonists. (aspetjournals.org)
- Thus, these data suggest that activation of α 1 adrenergic receptors increases the excitability of PVN presympathetic neurons primarily through augmentation of glutamatergic tone and attenuation of GABAergic inputs. (aspetjournals.org)
- In rats tested for c-Fos activation after intermittent esophageal balloon distension, no colocalization with TH-IR was observed in DMV neurons. (physiology.org)
- The present experiments, part of an ongoing study designed to characterise the role norepinephrine (NE) in regulating the activity of putative nociceptive modulatory neurons in the rostral ventromedial medulla (RVM), assessed the effects of α-adrenergic receptor-selective agents on the nociceptive threshold (as measured by the tail-flick withdrawal response on noxious heat). (elsevier.com)
- Mechanistically, we provide evidence that β 3 -adrenergic receptors, which are preferentially expressed on a Hes5-expressing precursor population in the subgranular zone (SGZ), mediate this norepinephrine-dependent activation. (jneurosci.org)
- Finally, using a novel ex vivo "slice-sphere" assay that maintains an intact neurogenic niche, we demonstrate that antidepressants that selectively block the reuptake of norepinephrine, but not serotonin, robustly increase hippocampal precursor activity via β-adrenergic receptors. (jneurosci.org)
- Because thyroid hormone increases the responsiveness to epinephrine and norepinephrine, excess thyroid hormone can cause symptoms that occur due to increased sympathetic activation, such as nervousness, sweating and increased heart rate. (washington.edu)
- 3 Occurring concurrently with the increase in VEGF and IGF-1R is an increase in β-1-adrenergic receptor levels, likely because of denervation sensitivity in response to reduced norepinephrine. (arvojournals.org)
- 3. _____ Drugs that block the action of norepinephrine and epinephrine on alpha receptors (alpha adrenergic antagonists or alpha-blockers) dilate most blood vessels. (coursehero.com)
- Clearly, if an adrenergic receptor mediates the action in the spinal cord, then an endogenous pathway that releases norepinephrine or epinephrine should be activated by N 2 O exposure. (asahq.org)
- Alk1 +/− mice showed a greater hypotensive response to the β-adrenergic antagonist atenolol and higher concentrations of epinephrine and norepinephrine in plasma than Alk1 +/+ mice. (biologists.org)
- 16 Therefore, the purpose of the current investigation was to examine the effect of nAChR activation on norepinephrine release, using both microdialysis perfusion in vivo , in which neuronal circuits are in place, and synaptosome release in vitro , where direct synaptic connections are lacking. (asahq.org)
- CypHer5E, consequently, can be used to screen for novel antagonists of known receptors and for potential ligands of non-G-protein coupled receptors (5) and orphan receptors. (bio-medicine.org)
- Adrenergic ligands are endogenous proteins that modulate and evoke specific cardiovascular effects. (wikipedia.org)
- Since this response, which is mostly seen as an increase in blood pressure, is produced by the release of the endogenous adrenergic ligands], administration of an adrenergic antagonist results a decrease in blood pressure, which is controlled by both heart rate and vasculature tone. (wikipedia.org)
- A respectable number of potent and specific allosteric ligands - predominantly antagonists/inhibitors - has been developed in recent years, although no orthosteric subtype-selective ligands have yet been discovered (2008). (wikipedia.org)
- Further, receptor models incorporating a flexible TM-V backbone allow reliable prediction of binding affinities for a set of diverse ligands, suggesting potential utility of this approach to design of effective and subtype-specific agonists for adrenergic receptors. (pubmedcentralcanada.ca)
- Substantial evidence indicates that PKC activation can lead to PLD activation in response to receptor agonists ( Liscovitch and Chalifa, 1994 ). (aspetjournals.org)
- These data demonstrate that MSK1 activation in adult rat cardiac myocytes by G-protein-coupled receptor agonists requires the simultaneous activation of both the ERK and p38 MAPK pathways. (portlandpress.com)
Called adrenergic receptors1
- More adrenaline production can lead to what we wrongfully refer to as "CNS fatigue" either by depleting dopamine (adrenaline is made from dopamine) or a desensitization of the adrenergic receptors due to overstimulation. (t-nation.com)
- Presynaptic 3-adrenoceptor activation causes release of dopamine receptors pargyline amoxapine phenelzine buspirone selegiline clozapine tranylcypromine droperidol haloperidol phenothiazines -adrenergic antagonists calcium channel blockers (ccbs) were first used in the developing fetus. (biointegrity.org)
- In the pathophysiology of migraine with aura, activation of the trigeminovascular system from the meningeal vessels mediates migraine pain via the brainstem and projections ascend to the thalamus and cortex. (frontiersin.org)
- Î²2- Adrenergic Receptor-Mediated HIF-1Î± Upregulation Mediates Blood Brain Barrier Damage in Acute Cerebral Ischemia Disruption of the blood brain barrier (BBB) within the thrombolytic time window is an antecedent event to intracerebral hemorrhage in ischemic stroke. (tripdatabase.com)
- This striking difference in inverse efficacy between idazoxan and RX821002 may account for in vivo pharmacological differences between these two α 2 -adrenergic antagonists. (aspetjournals.org)
- Several H3 antagonists have been shown to act as inverse agonists and such profiles of H3 antagonists have been implicated in their pharmacological functions. (aspetjournals.org)
- One alternative approach to complement the pharmacological tools and further investigate the interactions between the adrenergic system and glucose homeostasis is the suppression of the β-adrenoceptors by gene targeting disruption. (diabetesjournals.org)
- Despite the physiological and pharmacological relevance of GPCRs, the structural basis of ligand efficacy and receptor activation, and how these elements translate into cytoplasmic trafficking and cellular response still remain elusive. (psi.ch)
- CONCLUSIONS: Alpha-amylase in blood increases after pharmacological activation of the adrenergic pathways suggesting that sympathetic receptors are responsible for these changes. (uzh.ch)
- 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)
- In the present investigation we studied the relationship between alpha- and beta-adrenergic agonists and CA activity in vasoconstriction mechanism. (scielo.br)
- For example, if the natural activation of the α1-adrenergic receptor leads to vasoconstriction, an α1-adrenergic antagonist will result in vasodilation. (wikipedia.org)
- However, the continued neurohormonal activation in chronic heart failure ( ) becomes deleterious with excessive vasoconstriction, volume expansion and continued deterioration in cardiac function. (onlinejacc.org)
- 2. ____ Vascular smooth muscle cells of most blood vessels have alpha receptors, and activation of vascular smooth muscle alpha receptors causes vasoconstriction. (coursehero.com)
- Constitutive activation of G protein-coupled receptors (GPCRs) is now well recognized and many classical GPCR antagonists have been found to be inverse agonists. (aspetjournals.org)
- Despite extensive studies investigating the regulation of single GPCR signaling cascades, the effects of concomitant GPCR activation on downstream signaling and cellular function remain unclear. (ahajournals.org)
- We aimed to characterize the cellular mechanism by which GPCR crosstalk regulates mitogen-activated protein kinase (MAPK) activation. (ahajournals.org)
- We show a general mechanism in which arrestin activation by one GPCR is capable of regulating signaling originating from another GPCR. (ahajournals.org)
- 2 Despite extensive studies investigating the regulation of single GPCR signaling cascades, the effect of concomitant GPCR activation by endogenous stimuli on downstream signaling remains poorly understood. (ahajournals.org)
- 4 However, chronic activation of multiple GPCR signaling pathways during maladaptive tissue and organ remodeling suggests the potential of downstream crosstalk away from the plasma membrane. (ahajournals.org)
- Arrestins not only scaffold proteins for the activation of different MAPK families under single receptor activation, but also mediate transactivation of epidermal growth factor receptor signaling pathways 2,6 and activation of many other non-GPCR signaling cascades. (ahajournals.org)
- 7 In the case of GPCR-induced extracellular signal-regulated kinase (ERK) mitogen-activated protein kinase (MAPK) activation, both G proteins and arrestins are capable of mediating ERK activation via independent mechanisms, with each pathway leading to unique spatiotemporal consequences. (ahajournals.org)
- Because arrestins preferentially bind to some, but not all, GPCRs in a ligand-dependent manner, we envision that arrestins may play a role in GPCR crosstalk by coordinating MAPK activation in distinct subcellular compartments. (ahajournals.org)
- While the antagonists for alpha and beta receptors are usually different compounds, there has been recent drug development that effects both types of the adrenoreceptors. (wikipedia.org)
- Administration of an adrenergic antagonist that specifically targets the beta receptors, results in this decrease in blood pressure by slowing or reducing cardiac output. (wikipedia.org)
- 4. ____ Some blood vessels have beta receptors, and activation of vascular smooth muscle beta receptors causes vasodilation. (coursehero.com)
- Moderate levels of C-NE enhance working memory through alpha 2 adrenergic receptors, while higher levels of C-NE, acting on alpha 1 and beta receptors, enhance other executive network functions such as the stopping of ongoing behavior, attentional set-shifting, and sustained attention. (blogspot.com)
- D609, an inhibitor of phosphatidylcholine hydrolysis, blocked translocation of PKC α and PKC ε but did not inhibit PLD activation. (aspetjournals.org)
- Both proteins also inhibit ligand-dependent activation of the EGFR and extracellular signal-regulated protein kinase 1/2 signaling in a rapid and dose-dependent manner. (embl-heidelberg.de)
- 5) Pretreatment with muscarinic receptor antagonist atropine, nitric oxide synthesis inhibitor l-NNA or cGMP inhibitor ODQ depressed the fast phase inhibition significantly and abolished the slow phase inhibition completely. (unboundmedicine.com)
- These results suggest that clonidine may exert analgesic effect by depressing the synaptic plasticity in spinal dorsal horn, via activation of muscarinic receptor-NO-cGMP pathway. (unboundmedicine.com)
- Adrenergic antagonists reverse the natural cardiovascular effect, based on the type of adrenoreceptor being blocked. (wikipedia.org)
- The alpha-1D adrenergic receptor (α 1D adrenoreceptor), also known as ADRA1D , is an alpha-1 adrenergic receptor , and also denotes the human gene encoding it. (wikipedia.org)
- However, while 75%-90% of human diseases is related to the activation of stress system, the common pathways between stress exposure and pathophysiological processes underlying disease is still debatable. (frontiersin.org)
- Both α 1 -adrenergic receptor (α 1 ARs) and βARs are expressed in cardiac tissue and are activated by catecholamines to modulate maladaptive cardiac remodeling, including cardiac fibroblast proliferation, by activation of distinct pathways. (ahajournals.org)
- In addition, we plan to compare the profile of activated signaling molecules with their dynamic intracellular localization pattern to learn how receptor activation translates into specific pathways of cellular signaling. (psi.ch)
- We conclude that alpha- and beta-adrenergic agonists can activate the MEK/MAPK pathway in the heart by different signalling pathways. (gla.ac.uk)
- Y16 specifically inhibits LARG catalyzed activation of RhoA and RhoA signaling pathways. (sigmaaldrich.com)
- These findings suggest a link among smoking, platelet 5‐ HT , catecholamine signaling, and their downstream effectors-including phospholipase C and inositol‐1,4,5‐triphosphate pathways-resulting in an increased tonic level of platelet activation in smokers. (ahajournals.org)
- Human lymphocytes are known to posessess a catecholamine-responsive adenylate cyclase which has typical beta-adrenergic specificity. (duke.edu)
- Binding of (-) [3H] alprenolol to these sites demonstrated the kinetics, affinity, and stereospecificity expected of binding to adenylate cyclase-coupled beta-adrenergic receptors. (duke.edu)
- Dissociation constants computed from binding experiments were virtually identical to those obtained from adenylate cyclase activation studies. (duke.edu)
- Marked stereospecificity was observed for both binding and activation of adenylate cyclase. (duke.edu)
- Tolkovsky AM, Levitzki A. Mode of coupling between the (3-adrenergic receptor and adenylate cyclase in turkey erythrocytes. (springer.com)
- Hanski E, Rimon G, Levitzki A. Adenylate cyclase activation by the 3-adrenergic receptor as a diffusion controlled process. (springer.com)
- Epinephrine, acting through the α 1 -adrenergic receptor subtype, promoted transient translocation of PKC α and more prolonged translocation of PKC ε to the membrane fraction, indicating activation of these two isoforms. (aspetjournals.org)
- In addition, epinephrine promoted activation of PLD, as shown by a sustained accumulation of phosphatidylethanol. (aspetjournals.org)
- However, PLD activation by epinephrine was abolished by concomitant incubation of cells with the calcium chelator EGTA. (aspetjournals.org)
- These data, together with previous results, are consistent with the hypothesis that in MDCK-D1 cells, epinephrine acting on α 1 -adrenergic receptors, promotes a rapid increase in cytosolic Ca 2+ that promotes activation of PLD through an as-yet poorly defined mechanism. (aspetjournals.org)
- we hypothesized that activation of PKC α would be required for activation of PLD by epinephrine in MDCK-D1 cells. (aspetjournals.org)
- However, we now report that, although epinephrine activates PKC α , this activation was not associated with an activation of PLD. (aspetjournals.org)
- We also find that epinephrine activates PKC ε , although this isoenzyme also does not seem to be involved in PLD activation. (aspetjournals.org)
- Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs) (4). (bio-medicine.org)
- naturally occurring point mutations that lead to constitutive activation of GPCRs have been implicated. (aspetjournals.org)
- This structure, followed by other co-crystals of β 2 AR ( Hanson and others 2008b ) and β 1 AR ( Warne and others 2008 ) with the antagonists (-)-timolol (PDB code 3D4S) and (-)-cyanopindolol (PDB code 2VT4) respectively, represents a leap forward in the understanding of the inactive state of adrenergic GPCRs. (pubmedcentralcanada.ca)
- Inhibition of adrenergic signaling abolished the excitatory action of CCK. (diabetesjournals.org)
- The beta-adrenergic antagonists may provide further benefit for patients with congestive heart failure through inhibition of sympathetic activation. (onlinejacc.org)
- 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)
- These findings suggest that the activation of neurogenic precursors and stem cells via β 3 -adrenergic receptors could be a potent mechanism to increase neuronal production, providing a putative target for the development of novel antidepressants. (jneurosci.org)
- To identify directly and to quantitate these beta-adenergic receptors in human lymphocytes, (-) [3H] alprenolol, a potent beta-adrenergic antagonist, was used to label binding sites in homogenates of human mononuclear leukocytes. (duke.edu)
- YIL-781 is a potent antagonist (Ki = 17 nM) of the growth hormone secretagogue receptor (GHS-R1). (sigmaaldrich.com)
- YM022 is a very potent, selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor. (sigmaaldrich.com)
- A β2adrenergic receptor antagonist screen was performed using the LOPAC ™ compound library, which consists of 640 well-characterized, pharmaceutically diverse compounds with known drug or drug-like activity. (bio-medicine.org)
- The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 was able to identify all specific β2-adrenergic receptor antagonists and additional structurally related compounds present in the LOPAC compound library. (bio-medicine.org)
- Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS. (nih.gov)
- 1 Neurohormonal activation is initially beneficial, helping to maintain systemic blood pressure and perfusion to vital organs, but is maladaptive in the long-term, contributing to worsening of CHF and sudden cardiac death. (ahajournals.org)
- Systemic application of β-adrenergic receptor antagonists may have detrimental effects on the retina. (arvojournals.org)
- Patients with chronic congestive heart failure have a sequential and incessant activation of those neurohormonal systems, which control body fluids, cardiac output and systemic blood pressure. (nih.gov)
- Adrenergic antagonists are mostly used for cardiovascular disease. (wikipedia.org)
- There are few non-cardiovascular uses for adrenergic antagonists. (wikipedia.org)
- While these adrenergic antagonists are used for treating cardiovascular disease, mainly hypertension, they can evoke harmful cardiac events. (wikipedia.org)
- Beta blockers, also called beta- adrenergic blocking agents, b-blockers or beta antagonists, are medications used for a variety of cardiovascular conditions. (wisegeek.com)
- A role for cyclic AMP in activation of the MAPK pathway was eliminated when other agonists that elevate cyclic AMP in the cardiac myocyte did not activate MAPK. (gla.ac.uk)
- Elevation of intracellular Ca2+ rather than cyclic AMP appears important in the activation of MAPK by isoprenaline in the cardiac myocyte. (gla.ac.uk)
- The primary action of beta-adrenergic drugs, including albuterol, is to stimulate adenyl cyclase, the enzyme which catalyzes the formation of cyclic-3',5'-adenosine monophosphate (cyclic AMP) from adenosine triphosphate (ATP) in beta-adrenergic cells. (nih.gov)
- The α-adrenergic antagonists have different effects from the β-adrenergic antagonists. (wikipedia.org)
- In contrast, neutral antagonists bind equally well to R and R *, have no effect on basal receptor activity, but block the effects of both agonists and inverse agonists. (aspetjournals.org)
- Notably, however, URB597 elicits profound anxiolytic-like effects in rats, which are prevented by the CB 1 antagonist rimonabant ( 16 ). (pnas.org)
- Because the β2-ARs are also expressed on dermal fibroblasts, a study was initiated to determine the effects of β-adrenergic agonists on dermal fibroblast-mediated collagen gel contraction. (elsevier.com)
- 2) Timolol, a beta-adrenergic antagonist, inhibited the ISO effects in a dose-dependent manner, with IC50 values for cAMP formation, IP3 accumulation and muscle relaxation of 1.8 X 10(-5) M, 3.2 X 10(-5) M and 2.2 X 10(-5) M, respectively. (arvojournals.org)
- The chronic activation of the arousal part of our autonomic nervous system (the sympathetic nervous system) that can occur during stress has been shown to cause an array of degenerative effects. (dericbownds.net)
- However, the effects of nAChR activation in the spinal cord need not be identical to that in the brain, and the only study of direct relevance to the spinal cord was performed in cultured fetal cells, which may differ in important ways from the adult. (asahq.org)
- In addition, microdialysis and slice perfusion studies cannot distinguish between direct effects of nAChR activation on noradrenergic terminals from indirect effects. (asahq.org)
- The acute effects of cigarette smoking produce central nervous system-mediated activation of the sympathetic nervous system. (ahajournals.org)
- Metoprolol antagonizes beta 1-adrenergic receptors in the myocardium, thereby reducing the rate and force of myocardial contraction leading to a reduction in cardiac output. (fpnotebook.com)
- Metoprolol tartrate antagonizes beta 1-adrenergic receptors in the myocardium, thereby reducing the rate and force of myocardial contraction, and consequently a diminished cardiac output. (fpnotebook.com)
- Although the ultimate stimulus responsible for the activation of these neurohormonal systems is unknown, a decreased cardiac output and diminished effective blood volume have been proposed as the responsible mechanisms. (nih.gov)
- Sympathetic activation leads to the local release of catecholamines by the sympathetic nerve terminals and to an increase in circulating catecholamines by the activation of the adrenal medulla. (diabetesjournals.org)
- INTRODUCTION: Sympathetic activation is present in patients having chronic mitral valve regurgitation even in asymptomatic ones. (usp.br)
- However, the effect of beta- blockers and a physical training program to modulate this sympathetic activation during this valve disease is unknown. (usp.br)