Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.Adrenergic alpha-Antagonists: Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.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 beta-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS.Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.Receptors, Adrenergic, alpha-1: A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.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.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.Receptors, Adrenergic, beta-2: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.Receptors, Adrenergic, 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.Adrenergic beta-Antagonists: Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.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.Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.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.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Receptors, Adrenergic, beta-1: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.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.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.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Receptors, Adrenergic, beta-3: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Adrenergic beta-2 Receptor Agonists: Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.Sympathetic Nervous System: The thoracolumbar division of the autonomic nervous system. Sympathetic preganglionic fibers originate in neurons of the intermediolateral column of the spinal cord and project to the paravertebral and prevertebral ganglia, which in turn project to target organs. The sympathetic nervous system mediates the body's response to stressful situations, i.e., the fight or flight reactions. It often acts reciprocally to the parasympathetic system.Piperidines: A family of hexahydropyridines.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.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).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.Serotonin 5-HT1 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.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.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.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Serotonin 5-HT2 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.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.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.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.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.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.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.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.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.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).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)Benzazepines: Compounds with BENZENE fused to AZEPINES.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.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.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Adrenergic beta-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.Hormone Antagonists: Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.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.QuinoxalinesAdenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Interleukin-1beta: An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)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.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 Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.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.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.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.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.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.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.Cell Line: Established cell cultures that have the potential to propagate indefinitely.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.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Iodocyanopindolol: A highly selective and specific beta antagonist that is used to characterize beta-adrenoceptors.Dihydroalprenolol: Hydrogenated alprenolol derivative where the extra hydrogens are often tritiated. This radiolabeled form of ALPRENOLOL, a beta-adrenergic blocker, is used to label the beta-adrenergic receptor for isolation and study.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Histamine H1 Antagonists: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.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.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).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.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.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.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.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.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.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.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.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.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.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.Xanthines: Purine bases found in body tissues and fluids and in some plants.PiperazinesCalcium: 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.PyrrolidinesCHO 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.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Behavior, Animal: The observable response an animal makes to any situation.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.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)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.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.Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.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.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Sulfonamides: A group of compounds that contain the structure SO2NH2.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).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.Arrestins: Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.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.Mice, Inbred C57BLNaphthalenes: 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.Kinetics: The rate dynamics in chemical or physical systems.8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.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.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.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.Baclofen: A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.Cyclic AMP-Dependent Protein Kinases: A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.Injections, Intraventricular: Injections into the cerebral ventricles.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.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.Nicotinic Agonists: Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.Leukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.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.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.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.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.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.Biphenyl CompoundsHistamine: 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.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)Receptors, Neurokinin-1: A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.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.Quinpirole: A dopamine D2/D3 receptor agonist.Adrenergic beta-3 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-3 RECEPTORS.MorpholinesReceptors, 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.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.Oligopeptides: Peptides composed of between two and twelve amino acids.Muscle, Smooth: Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)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.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).Transfection: The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.Azepines: Seven membered heterocyclic rings containing a NITROGEN atom.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.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.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.Mice, Knockout: Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.Tetrahydronaphthalenes: Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.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.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.Myocardium: The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.Pertussis Toxin: One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.Butoxamine: A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.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.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.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.DioxolesTetrazolesReceptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.beta 2-Microglobulin: An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.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.Benzoxazines: OXAZINES with a fused BENZENE ring.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.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.Receptors, Thromboxane: Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.Receptors, Serotonin, 5-HT4: A subtype of G-protein-coupled SEROTONIN receptors that preferentially couple to GS STIMULATORY G-PROTEINS resulting in increased intracellular CYCLIC AMP. Several isoforms of the receptor exist due to ALTERNATIVE SPLICING of its mRNA.Receptor, Cannabinoid, CB2: A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Receptor, Endothelin B: A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.Peptide Fragments: Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.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.Dogs: The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)Receptor, Adenosine A1: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.
ICI-118,551
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InhibitionPharmacologyStimulationSelectiveDopamineCardiacPharmacologicalInhibitoryRegulationMediateCell‐surfaceSignal transductionAdrenoceptorSubtypesAlpha 1-adrenergic antagoniHigh affinityAffinityMechanismCholinergicAdrenoreceptorStimulateProteinsYohimbineMRNACalcium ChannelGPCRsPhosphorylationCharacterizationInternalizationOpiateLigandsLeukotriene B4 recepMolecularPredominantly2000ProteinPropranololMechanismsNicotinic receptorsSpecific antagonistsVascular smoothSecretionAdrenoceptorsMediatesBlockersConcentrationsAdenylate cyclaseLigand binding speEpinephrine and norepineph2001InhibitGeneAdenylyl cyclaseIsoproterenolInverse agonistBlockadeSuperfamilySpecificityRatsActivationKinaseIntracellularConfocal microscopyCannabinoid agonistsPathwaysResponses
Inhibition11
- The beta-adrenergic receptor-induced inhibition was prevented by pertussis toxin and could not be reproduced by forskolin, indicating that cAMP was not involved. (aspetjournals.org)
- Accumulation of inositol phosphates triggered by high K+ was insensitive to the beta-adrenergic receptor inhibition. (aspetjournals.org)
- We compared the effects of inhibition of angiotensin-converting enzyme or blockade of angiotensin II type 1 (AT 1 ) receptors in a model with renin-induced hypertension that is known to exhibit similar changes in sympathetic activation and β-adrenergic desensitization, as observed in heart failure. (ahajournals.org)
- Inhibition of phosphoinositide turnover by selective muscarinic antagonists in the rat striatum. (nih.gov)
- beta adrenergic response, which is inhibition of contractions. (weight-loss-tips-and-secrets.com)
- LY320135 functionally reversed anandamide-mediated adenylate cyclase inhibition in Chinese hamster ovary (CHO) cells stably expressing the CB1 receptor. (aspetjournals.org)
- Pertussis toxin treatment of CHO cells expressing the CB1 receptor attenuated the anandamide-mediated inhibition of adenylate cyclase and unmasked a stimulatory effect of anandamide on adenylate cyclase. (aspetjournals.org)
- Inhibition of ex vivo neutrophil activation by oral LY293111, a novel leukotriene B4 receptor antagonist. (nih.gov)
- This effect likely occurs through the inhibition of adrenergic stimulation found in states of hyperarousal 13 . (drugbank.ca)
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (uniprot.org)
- In the islet β-cells, catecholamines are reported to inhibit insulin release via multiple mechanisms: activation of α2-adrenoceptors coupled to pertussis toxin-sensitive Gi/Go proteins resulting in inhibition of adenylyl cyclase ( 1 ), activation of hyperpolarizing K + currents ( 2 , 3 ), inhibition of Ca 2+ currents ( 4 , 5 ), and direct inhibition of exocytosis at a distal step ( 6 - 8 ). (diabetesjournals.org)
Pharmacology3
- title=Molecular pharmacology and modeling of vasopressin receptors. (enacademic.com)
- Cannabinoid receptor pharmacology has been hampered by the availability of selective antagonists. (aspetjournals.org)
- Adrenoceptors can be divided into three main classes based on sequence similarity, receptor pharmacology and signalling mechanisms. (130.88.97)
Stimulation14
- 2004) Characterization of agonist stimulation of cAMP‐dependent protein kinase and G protein‐coupled receptor kinase phosphorylation of the beta2‐adrenergic receptor using phosphoserine‐specific antibodies. (els.net)
- These results suggest that in certain airway epithelial cell lines stimulation of β 2 ‐adrenergic receptors and the consequent production of cyclic adenosine monophosphate may upregulate cell growth, probably through activation of the mitogen-activated protein kinase cascade. (ersjournals.com)
- In addition, stimulation of cell surface receptors, linked to Gi and Gq proteins, has been shown to potently activate MAP kinase 7 , 8 , but the effect of Gs protein-coupled receptors on the enzyme activity is poorly understood. (ersjournals.com)
- Therefore, the current authors studied three human airway epithelial cell lines in vitro , in order to determine whether β 2 ‐adrenergic agonists affect the growth of airway epithelial cells and to assess a possible involvement of cAMP-mediated stimulation of the MAP kinase cascade. (ersjournals.com)
- Nylidrin hydrochloride acts mainly by beta-receptor stimulation 1 , 15 . (drugbank.ca)
- Beta stimulation with nylidrin has been studied and confirmed in a variety of isolated tissues from rabbits, guinea pigs, as well as dogs. (drugbank.ca)
- Glucose metabolism and glucagon-like peptide 1 (GLP-1) receptor stimulation both increase the activity of TRPM2 channels via cAMP signaling ( 9 ). (diabetesjournals.org)
- H2-histamine receptors mediate a wide range of physiological functions extending from stimulation of gastric acid secretion to induction of human promyelocyte differentiation. (biomedcentral.com)
- Arrestins not only target desensitized receptors to clathrin-coated pits for endocytosis but also act as scaffolding proteins that link GPCRs to the stimulation of additional signaling pathways (Shenoy and Lefkowitz, 2003). (39kf.com)
- Performing adrenergic stimulation from the topical angle is particularly advantageous to the athlete looking to avoid the central (CNS) affects manifesting from the beta agonism. (dpsnutrition.net)
- 3 . The method of claim 1 , further comprising coupling said system control unit to said stimulation site. (google.es)
- It competes with sympathomimetic neurotransmitters for binding to receptors, which inhibits sympathetic stimulation of the heart. (propranolol-abc.com)
- We recently showed that β-arrestin can also mediate β 1 AR transactivation of the EGFR, resulting in a cardioprotective effect under conditions of chronic catecholamine stimulation ( 3 ). (pnas.org)
- The appreciation that chronic stimulation of βARs likely contributes to the pathogenesis of heart failure ( 4 ) has led to the use of β-adrenergic receptor antagonists (i.e., β-blockers) to competitively inhibit the harmful effects of chronic catecholamine stimulation ( 5 ). (pnas.org)
Selective13
- ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist. (wikipedia.org)
- The alpha 2 and beta 2 adrenergic receptors, both of which are activated by epinephrine, but which can be differentiated by selective drugs, have opposite effects (inhibitory and stimulatory) on the adenylyl cyclase system. (duke.edu)
- Low concentrations of prazosin (10(-8) M) and yohimbine (10(-7) M) produced receptor subtype-selective antagonism and parallel, dextral displacement of norepinephrine curves for large arterioles and venules. (ahajournals.org)
- but prazosin had no effect at receptor subtype-selective concentrations. (ahajournals.org)
- In good agreement with the latter result, the beta 1-adrenergic receptor (beta 1-AR)-selective antagonist CGP20712A had more effect on the Iso-stimulated AC activity in pre-obese than in lean pups (2-fold decreased in IC50). (portlandpress.com)
- Effects of selective beta! (weight-loss-tips-and-secrets.com)
- denotes selective agonist s to the receptor. (enacademic.com)
- LY320135 is a selective antagonist for the brain CB1 receptor, having greater than 70-fold higher affinity for the CB1 than the peripheral CB2 receptor. (aspetjournals.org)
- LY320135 is a promising lead compound for the further development of novel, potent and selective cannabinoid antagonists of novel structure. (aspetjournals.org)
- SR141716A was found to be selective and potent at the CB1 receptor and blocked WIN 55212-2-mediated behavioral responses. (aspetjournals.org)
- Numerous drugs exert their actions via adrenoceptors: e.g., beta-2 selective agonists such as salbutamol are used in the acute treatment of asthma, while alpha agonists prolong the action of local anaesthetics, and act as nasal decongestants . (130.88.97)
- We treated isolated mouse tibialis anterior (TA) and medial gastrocnemius (MG) muscles in tissue bath with the selective dopamine 1 receptor and dopamine 5 receptor agonist SKF 81297 to determine if activation of skeletal muscle dopamine 1 and dopamine 5 receptors will increase cAMP. (biomedcentral.com)
- A large body of data indicates that patients with COPD tolerate well selective beta-blockade that should not be denied to CHF patients with concomitant COPD. (onlinejacc.org)
Dopamine13
- Enzymes involved in the synthesis of nitric oxide, 1 2 dopamine, 3 4 and norepinephrine 3 4 5 exist within nonhuman mammalian cardiac ganglia. (ahajournals.org)
- 18 Recently, however, key marker enzymes in catecholaminergic neurons, including tyrosine hydroxylase and dopamine β-hydroxylase, were found in rat 3 4 and guinea pig 1 5 cardiac ganglia. (ahajournals.org)
- Several partial matches were also found, largely serotonin and dopamine receptors that match 2 motifs. (130.88.97)
- The precise mechanism of antipsychotic action is unclear, but is considered to be associated with the potent dopamine D2 receptor blocking activity of haloperidol and the resulting adaptive changes in the brain. (inchem.org)
- The symptomatic effects of drug abuse are a result of alterations in the functioning of the following neurotransmitters or their receptors: acetylcholine, dopamine, γ-aminobutyric acid, norepinephrine, opioids and serotonin. (aafp.org)
- The dopamine 1 receptor and its closely related homolog, the dopamine 5 receptor, are G-protein coupled receptors that are expressed in skeletal muscle and increase cAMP levels when activated. (biomedcentral.com)
- Thus we hypothesize that activation of the dopamine 1 and/or 5 receptor will increase skeletal muscle cAMP levels thereby modulating skeletal muscle mass and force production. (biomedcentral.com)
- We dosed wild-type mice, dopamine 1 receptor knockout mice and dopamine 5 receptor knockout mice undergoing casting-induced disuse atrophy with SKF 81297 to determine if activation of the dopamine 1 and dopamine 5 receptors results in hypertrophy of non-atrophying skeletal muscle and preservation of atrophying skeletal muscle mass and force production. (biomedcentral.com)
- In dopamine 1 receptor knockout mice, extensor digitorum longus (EDL) and soleus muscle mass and force was not preserved during casting with SKF 81297 treatment, in contrast to significant preservation of casted wild-type mouse EDL and soleus mass and EDL force with SKF 81297 treatment. (biomedcentral.com)
- Dosing dopamine 5 receptor knockout mice with SKF 81297 did not significantly preserve EDL and soleus muscle mass and force although wild-type mouse EDL mass and force was significantly preserved SKF 81297 treatment. (biomedcentral.com)
- These data demonstrate for the first time that treatment with a dopamine 1/5 receptor agonist results in (1) significant preservation of EDL, TA, MG and soleus muscle mass and EDL muscle force production during periods of atrophy and (2) hypertrophy of TA and MG muscle. (biomedcentral.com)
- These effects appear to be mainly mediated by both the dopamine 1 and dopamine 5 receptors. (biomedcentral.com)
- Dopamine mediates its action via the 5 known dopamine receptors (D1-D5). (biomedcentral.com)
Cardiac13
- It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue. (wikipedia.org)
- Actions of the β1 receptor include: stimulate viscous, amylase-filled secretions from salivary glands Increase cardiac output Increase heart rate in sinoatrial node (SA node) (chronotropic effect) Increase atrial cardiac muscle contractility. (wikipedia.org)
- 6 In addition, treatment with ACE inhibitors in hypertensive cardiac hypertrophy reduced sympathetic activity and restored β-adrenergic signal transduction defects at a dose that did not prevent cardiac hypertrophy, and the increase in blood pressure was unaffected. (ahajournals.org)
- Increases contractility and automaticity [3] of ventricular cardiac muscle. (worldheritage.org)
- Cardiac autonomic receptors: effect of long-term experimental diabetes. (nih.gov)
- Low doses of α-adrenergic agonists constrict veins and may often shift blood from the Vu to the Vs, subsequently increasing the venous return and cardiac output, whereas higher drug doses constrict arteries and usually decrease cardiac output. (springer.com)
- Brodde O-E (1987) Cardiac beta-adrenergic receptors. (springer.com)
- Other agonists linked to cardiac phospholipase C activation, including endothelin 1 (40 nM) and the muscarinic agonist carbamylcholine (1 mM), also decreased conduction velocity in fibers exposed to halothane. (asahq.org)
- 3 Hypertension puts the elderly at greater risk for developing several cardiovascular diseases (CVDs), ranging from myocardial infarction, angina, and cerebrovascular disease to peripheral artery disease and cardiac failure. (uspharmacist.com)
- Vasoactive intestinal peptide, 1 2 6 substance P, 1 2 somatostatin, 1 2 and neuropeptide Y 1 2 3 4 7 immunoreactivity also exists within cardiac ganglia. (ahajournals.org)
- Furthermore, electrophysiological studies show that neurons within cardiac ganglia respond to application of cholinergic 6 as well as adrenergic, 1 9 13 14 15 histaminergic, 16 purinergic, 1 11 12 and peptidergic 1 15 17 agonists and antagonists. (ahajournals.org)
- Circulating adrenaline also acts on cardiac tissue, and, in addition, acts both on alpha-1 adrenoceptors in arterial smooth muscle, stimulating vasoconstriction, and on beta-2 adrenoceptors in vascular beds of skeletal muscle, stimulating vasodilation . (130.88.97)
- Blockage of neurotransmitter binding to beta 1 receptors on cardiac myocytes inhibits activation of adenylate cyclase, which in turn inhibits cAMP synthesis leading to reduced PKA activation. (propranolol-abc.com)
Pharmacological4
- These compelling data confirm the clinical potential interest of ADRB3 agonists in the pharmacological management of preterm labour. (biomedcentral.com)
- We tested two cannabinoid compounds with different pharmacological properties in the inhibitory avoidance task, and evaluated whether the observed effects are mediated by cannabinoid, PPARα or TRPV1 receptor activation. (frontiersin.org)
- Our studies have important implications on the design of pharmacological agents targeted for action at physiological receptors. (biomedcentral.com)
- Furthermore, you'll be able to make use of tissues from genetically improved pets, and assess pharmacological modulation of agonist replies. (flora2world.com)
Inhibitory6
- The inhibitory effect of isoproterenol, similar to that of nifedipine, was counteracted by ionomycin and also by the Ca2+ channel agonist Bay K 8644. (aspetjournals.org)
- The inhibitory binding constants ( K i ) of astressin and urocortin are 1 to 2 nM for all receptors and are independent of which radioligand is employed. (aspetjournals.org)
- alpha Gi function, assessed by the inhibitory action of low concentrations of guanosine 5′-[beta gamma-imido]triphosphate upon 10(-4) M forskolin-stimulated AC activity, was equally low in both genotypes. (portlandpress.com)
- We found that the synthetic cannabinoid agonist WIN55,212-2 and the FAAH inhibitor URB597 both enhanced memory consolidation for inhibitory avoidance training. (frontiersin.org)
- The main restriction of the model is based on PPARG the fact that you will be documenting in the trunk from the vagus nerve, which bears all sorts of afferent nerve fibres (RAR, SAR, cough receptor and C-fibre) aswell as parasympathetic and possibly inhibitory nerves, and nerves innervating various other visceral organs like the center and gastrointestinal system. (flora2world.com)
- In addition to blockade of adrenergic receptors , propranolol has very weak inhibitory effects on the norepinephrine transporter and/or weakly stimulates norepinephrine release (i.e., the concentration of norepinephrine is increased in the synapse ). (propranolol-abc.com)
Regulation21
- Operating via heterotrimeric G proteins, adrenergic receptors constitute one of the most intensely studied classes of membrane proteins, whose expression and function are subject to regulation at many different levels, including transcriptional, posttranscriptional and posttranslational. (els.net)
- Hadcock JR and Malbon CC (1988) Down‐regulation of beta‐adrenergic receptors: agonist‐induced reduction in receptor mRNA levels. (els.net)
- Kallal L, Gagnon AW, Penn RB and Benovic JL (1998) Visualization of agonist‐induced sequestration and down‐regulation of a green fluorescent protein‐tagged beta2‐adrenergic receptor. (els.net)
- Kohout TA and Lefkowitz RJ (2003) Regulation of G protein‐coupled receptor kinases and arrestins during receptor desensitization. (els.net)
- Krupnick JG and Benovic JL (1998) The role of receptor kinases and receptors in G‐protein‐coupled receptor regulation. (els.net)
- Shenoy SK, McDonal PH, Kohout TA and Lefkowitz RJ (2001) Regulation of receptor fate by ubiquitination of activated beta2‐adrenergic receptor and beta‐arrestin. (els.net)
- Alpha7-nicotinic acetylcholine receptors affect growth regulation of human mesothelioma cells: role of mitogen-activated protein kinase pathway. (springer.com)
- Heterotrimeric G proteins, consisting of alpha, beta and gamma subunits, couple ligand-bound seven transmembrane domain receptors (GPCRs or G-protein coupled receptors) to the regulation of effector proteins and production of intracellular secondmessengers such as cAMP, cGMP, and Ca.sup.2+. (patentgenius.com)
- These data suggest that adrenergic regulation of large arterioles and venules in skeletal muscle uses both alpha 1- and alpha 2-adrenoceptors. (ahajournals.org)
- Differential regulation of bladder beta-adrenergic and muscarinic cholinergic receptors in experimental diabetes. (nih.gov)
- The reciprocal regulation exerted by insulin and the adrenergic system has been well documented through a large number of studies ( 11 - 13 ). (diabetesjournals.org)
- Minneman KP, Pittman RN, Molinoff PB (1981) β -Adrenergic receptor subtypes: properties, distribution and regulation. (springer.com)
- Stiles GL, Caron MG, Lefkowitz RJ (1984) β- Adrenergic receptors: biochemical mechanisms of physiological regulation. (springer.com)
- Lefkowitz RJ (1978) Identification and regulation of alpha- and beta-adrenergic receptors. (springer.com)
- Hoffman BB, Lefkowitz RJ (1980) Radioligand binding studies of adrenergic receptors: new insights into molecular and physiological regulation. (springer.com)
- Here we report a novel role for epinephrine and cyclic adenosine monophosphate (cAMP) in the regulation of human SS RBC adhesiveness via the laminin receptor, basal cell adhesion molecule/Lutheran (BCAM/Lu). (bloodjournal.org)
- Thus, these studies demonstrate a novel, rapid regulation of SS RBC adhesion by a cAMP-dependent pathway and suggest that components of this pathway, particularly PKA, the β2-adrenergic receptor, and BCAM/Lu, should be further explored as potential therapeutic targets to inhibit SS RBC adhesion. (bloodjournal.org)
- The regulation of CD11b integrin levels on human blood leukocytes and leukotriene B4-stimulated skin by a specific leukotriene B4 receptor antagonist (LY293111). (nih.gov)
- Alpha-adrenergic receptors are essential for the regulation of blood pressure in humans. (drugbank.ca)
- Expression of -arrestin in R126N-CCR5-expressing cells resulted in receptor down-regulation, thereby suggesting that R126N-CCR5 spontaneously interacts with -arrestins. (39kf.com)
- 17 beta-estradiol regulation of human endothelial cell basal nitric oxide release, independent of cytosolic Ca2+ mobilization. (pharmaceuticalintelligence.com)
Mediate3
- Both cysteinyl-leukotrienes and extracellular nucleotides mediate inflammatory responses via specific G-protein-coupled receptors, the CysLT and the P2Y receptors, respectively. (biologists.org)
- The CB2 receptor may mediate some of the peripheral effects of THC, such as immunosuppression ( Martin, 1986 ). (aspetjournals.org)
- Endothelial {beta}3-Adrenoreceptors Mediate Nitric Oxide-Dependent Vasorelaxation of Coronary Microvessels in Response to the Third-Generation {beta}-Blocker Nebivolol. (pharmaceuticalintelligence.com)
Cell‐surface2
- Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions. (els.net)
- CRF exerts its actions by binding to specific cell surface receptors on target tissues. (aspetjournals.org)
Signal transduction4
- By this second component of the mechanism, the same stimulus directly acts on the carbonic anhydrase I isozyme (that might be functionally coupled with adrenergic receptors), so that its activation ensures an adequate pH for stimulus-receptor coupling for signal transduction into the cell, resulting in vasoconstriction. (scielo.br)
- 14 15 16 Although TG(m REN 2)27 rats are not in heart failure and might not represent all pathobiochemical alterations observed in this condition, it can be taken as valuable model to study drug effects on β-adrenergic signal transduction. (ahajournals.org)
- They are frequently referred to as G-protein-coupled receptors because they accomplish signal transduction to the interior of the cell by interactions with guanine nucleotide regulatory binding proteins . (drugbank.ca)
- 3. BIRNBAUMER, L. G proteins in signal transduction. (130.88.97)
Adrenoceptor13
- ICI binds to the β 2 subtype with at least 100 times greater affinity than β 1 or β 3 , the two other known subtypes of the beta adrenoceptor. (wikipedia.org)
- Rauwolscine is known as an Alpha-2 adrenoceptor antagonist (Alpha-2-adrenoceptor blocker). (anabolicminds.com)
- The drug ephedrine is an adrenoceptor agonist and likely has activity across several family members. (guidetopharmacology.org)
- title=Genetic variation of the beta(2)-adrenoceptor: its functional and clinical importance in bronchial asthma. (enacademic.com)
- In Purkinje fibers one pharmacologically distinguishable alpha 1-adrenoceptor subtype (alpha 1B) sensitive to the noncompetitive antagonist chloroethylcholinidine mediates decreases in automaticity. (asahq.org)
- On the other hand, some studies have reported that alpha-adrenoceptor agonists stimulate human airway smooth muscle contraction, [ 5-7 ] that alpha-adrenoceptors play a role in exercise-induced bronchoconstriction, [ 8 ] and that plasma norepinephrine (NE) increases in normal and asthmatic subjects during exercise. (asahq.org)
- Inhaled β 2 ‐adrenoceptor agonists have been widely used in the treatment of chronic obstructive pulmonary disease and asthma, and it is likely that airway epithelial cells are frequently exposed to these drugs in high concentrations. (ersjournals.com)
- Our work reported in this review focuses on a potential new target for tocolytic drugs, the β 3 -adrenoceptor (ADRB3). (biomedcentral.com)
- Among these treatments, β 2 -adrenoceptor (ADRB2) agonists are becoming less used worldwide as tocolytic agents because of important maternal and fetal side effects. (biomedcentral.com)
- Nonselective beta-blockers block both beta receptors, whereas cardioselective beta-blockers bind to the beta-adrenoceptor and partially activate the receptor while preventing other receptor agonists from binding. (uspharmacist.com)
- Administration of yohimbine, an α2-adrenoceptor antagonist, failed to affect glucose tolerance in TRPM2-KO mice, in contrast to an improved glucose tolerance in wild-type mice receiving the antagonist. (diabetesjournals.org)
- by contrast, relatively small differences in agonist and antagonist affinities are demonstrated, especially within the alpha-1 and alpha-2 adrenoceptor subtypes . (130.88.97)
- Therefore, it can be looked upon as a weak indirect α 1 -adrenoceptor agonist in addition to potent β-adrenoceptor antagonist. (propranolol-abc.com)
Subtypes2
- title=Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. (enacademic.com)
- Antagonists of alpha7 and non-alpha7 subtypes of the nicotinic receptors methyllycaconitine and mecamylamine in single IP injections selectively influenced the resistance to hypoxia of the low-resistant rats and were ineffective against the high-resistant and intact rats. (omicsonline.org)
Alpha 1-adrenergic antagoni1
- The stimulatory effect of EPI and PHE was lowered, respectively blocked, by low concentrations of the potent alpha 1-adrenergic antagonist prazosin. (kuleuven.be)
High affinity7
- The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. (curehunter.com)
- 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)
- The characteristics of a high-affinity antagonist radioligand are compared with those a high-affinity agonist in binding to the cloned corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2) and to the native receptors that exist in rat cerebellum and brain stem. (aspetjournals.org)
- Astressin binds with high affinity to the native cerebellar/brain stem receptor and relative potencies of selected CRF analogs determined with Ast* on the native receptor are similar to those obtained for the cloned CRF-R1. (aspetjournals.org)
- Because it is a high-affinity, specific CRF antagonist, astressin is eminently suitable as a ligand for detection and characterization of both endogenous and cloned CRF receptors. (aspetjournals.org)
- At the high-affinity site (mainly beta 1) these two agonists were more potent in fa/fa than in Fa/fa rats (Kact. (portlandpress.com)
- Phosphorylation and activation of Ca(2+)-sensitive cytosolic phospholipase A2 in MCII mast cells mediated by high-affinity Fc receptor for IgE. (nih.gov)
Affinity6
- Receptors that are coupled to G proteins are characterized by agonist states of high and low affinity, which interconvert via GDP/GTP exchange on the G protein ( Conklin and Bourne, 1993 ). (aspetjournals.org)
- The apparent affinity of an agonist depends on the degree of coupling of the receptor to the G protein, whereas the affinity of an antagonist is independent of such coupling. (aspetjournals.org)
- iii) noradrenaline and isoprenaline (Iso), at the low-affinity site (beta 3-AR), were less potent in fa/fa than in Fa/fa pups (Kact. (portlandpress.com)
- Kent RS, DeLean A, Lefkowitz RJ (1980) A quantitative analysis of beta-adrenergic receptor interactions: resolution of high and low affinity states of the receptor by computer modeling of ligand binding data. (springer.com)
- Among the different factors involved, of particular interest is the binding affinity of endocannabinoids, and their analogs, for other receptor families beyond cannabinoid receptors, such as the peroxisome proliferator-activated receptors (PPARs), and the transient receptor potential cation channel subfamily V member 1 (TRPV1). (frontiersin.org)
- However, no binding affinity data is available for these ligands at this receptor. (guidetopharmacology.org)
Mechanism9
- We believe that adrenergic agonists may have a dual mechanism of action: the first one consists of a catecholamine action on its receptor with the formation of a stimulus-receptor complex. (scielo.br)
- In the present investigation we studied the relationship between alpha- and beta-adrenergic agonists and CA activity in vasoconstriction mechanism. (scielo.br)
- The present data show that the natural beta-agonist epinephrine (EPI) stimulates GH release through an additional alpha-adrenergic mechanism. (kuleuven.be)
- Insights into agonist binding and the corresponding conformational changes triggering GPCR activation mechanism are of special interest. (pubmedcentralcanada.ca)
- So remember, alpha-2 adrenoceptors are blocked, so fat storage mechanism is decreased, and now allows the beta-adrenergic pathways to burn more fat in the midsection. (anabolicminds.com)
- an-d beta2-adrenoreceptor agonist ansd antagonists on intraocular pressure fects on ocular tension by action at beta-adrenergic receptors, a cholinergic mechanism may be involved as well. (weight-loss-tips-and-secrets.com)
- The assembly of the signaling complex provides a mechanism that ensures specific and rapid signaling by this G protein-coupled receptor. (enacademic.com)
- Another alpha 1 subtype (alpha 1A), sensitive to the competitive antagonist WB4101, increases spontaneous rate and action potential duration by a mechanism thought to involve hydrolysis of membrane phosphoinositides by phospholipase C. This study examined the dose-response relation and receptor-effector mechanisms underlying depression of conduction in canine Purkinje fibers by epinephrine with halothane. (asahq.org)
- Recently, we reported that α 2 adrenoceptors in the spinal cord 1 were necessary to transduce the acute antinociceptive response to N 2 O. A mechanism of action for N 2 O also has been proposed in which opiate receptors are activated through the release of endogenous opiate ligands. (asahq.org)
Cholinergic3
- Receptor characterization studies suggest not only cholinergic but also β-adrenergic, 1 8 9 serotonergic, 10 and purinergic 1 11 12 receptors on ganglionic neurons. (ahajournals.org)
- 2) In the low-resistant rats, cholinergic C-fibres into the nucleus tractus solitary of the medulla oblongata and influences of unidentified cholinergic neurons through the alpha7 nicotinic receptors in the caudal brainstem areas outside the nucleus tractus solitary. (omicsonline.org)
- 3) In intact rats, cortical cholinergic interneurons and unidentified cholinergic neurons of the brainstem structures. (omicsonline.org)
Adrenoreceptor1
- The beta-1 adrenergic receptor (β1 adrenoreceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the human gene encoding it. (wikipedia.org)
Stimulate8
- Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (els.net)
- It has been previously shown that beta-adrenergic agonists stimulate growth hormone (GH) release from perifused rat anterior pituitary cell aggregates cultured in serum-free defined medium for 5-6 days. (kuleuven.be)
- β‐adrenergic receptors are Gs protein-coupled receptors and stimulate the synthesis of intracellular cyclic adenosine monophosphate (cAMP). (ersjournals.com)
- Recent studies have shown that beta-adrenergic agents stimulate steroidogenesis and cyclic AMP formation in mouse Leydig cells in culture. (meta.org)
- Psychedelic drugs stimulate serotonin release, and sedative-hypnotic drugs potentiate the γ-aminobutyric acid receptor. (aafp.org)
- To determine whether β-adrenergic ligands that do not activate G protein signaling (i.e., β-blockers) can stabilize the β 1 AR in a signaling conformation, we screened 20 β-blockers for their ability to stimulate β-arrestin-mediated EGFR transactivation. (pnas.org)
- Our findings demonstrate that Alp and Car are ligands that not only act as classical receptor antagonists, but can also stimulate signaling pathways in a G protein-independent, β-arrestin-dependent fashion. (pnas.org)
- Beta-adrenergic receptors (βARs) are members of the seven transmembrane receptor (7TMR) family that become activated upon catecholamine binding to stimulate G protein-dependent signaling. (pnas.org)
Proteins13
- Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs share many similarities in receptor phosphorylation, use of accessory proteins and sequestration of the receptors. (els.net)
- Other studies have proved that binding of agonists to these receptors occurs when the catecholamine molecule is in the protonated state (6), all of these receptors being coupled with G proteins. (scielo.br)
- The two receptors are homologous with each other, rhodopsin, and other receptors coupled to guanine nucleotide regulatory proteins and they contain seven hydrophobic domains, which may represent transmembrane spanning segments. (duke.edu)
- The CRF receptors belong to the 7-transmembrane domain receptor family that is coupled to adenylate cyclase via GTP-binding proteins (G proteins). (aspetjournals.org)
- CysLT 1 and CysLT 2 receptors can couple to distinct types of G proteins. (biologists.org)
- This drug is classified as a beta receptor agonist 7 .The β2-adrenergic receptor belongs to the widely expressed 7-transmembrane receptors superfamily , which signals through heterotrimeric G-proteins . (drugbank.ca)
- The rhodopsin-like GPCRs themselves represent a widespread protein family that includes hormone, neurotransmitter and light receptors, all of which transduce extracellular signals through interaction with guanine nucleotide-binding (G) proteins. (130.88.97)
- Here, we show that CCR5 displayed agonist-independent coupling to G proteins. (39kf.com)
- Changing Arg-126 by the neutral residue Asn (R126N-CCR5 mutant) abolished CCR5-mediated activation of G proteins, either constitutively or in response to agonists. (39kf.com)
- Overall, these data indicate that structural requirements for CCR5-mediated activation of G proteins, albeit not involved in receptor desensitization and internalization, are needed for -arrestin-mediated chemotaxis. (39kf.com)
- Transduction of signals by GPCRs depends on the interaction of the receptors with distinct families of proteins, including heterotrimeric G proteins, G protein-coupled receptor kinases (GRKs), second messenger-dependent protein kinases, and -arrestins. (39kf.com)
- After agonist binding, GPCRs adopt an active conformation that interacts with G proteins (Seifert and Wenzel-Seifert, 2003). (39kf.com)
- Activation of GPCRs by agonists involves conformational changes that permit intracellular sequences to interact with G proteins. (39kf.com)
Yohimbine3
- Concentration-response (diameter change) curves were obtained for bath-added agonists norepinephrine (mixed alpha 1/alpha 2), phenylephrine (alpha 1), and B-HT 933 (alpha 2) in the absence or presence of antagonists prazosin (alpha 1) and yohimbine (alpha 2). (ahajournals.org)
- Higher concentrations of prazosin (10(-7) and 3 X 10(-7) M) and yohimbine (10(-6) M) produced further dextral but nonparallel displacement of norepinephrine curves. (ahajournals.org)
- Our knowledge of the adrenergic system tells us this is easily achievable by coupling alpha-2 antagonism (yohimbine) and beta-receptor activation (synephrine). (dpsnutrition.net)
MRNA2
- Bmax values for the two sites were not affected by the genotype, although the beta 3-AR mRNA concentration in BAT (quantitative reverse-transcriptase PCR) was 3-fold lower in fa/fa rats than in Fa/fa pups. (portlandpress.com)
- These signaling pathways were totally inhibited by different specific CysLT 1 -receptor antagonists, and no CysLT 2 receptor mRNA was detected, which indicates that in U937 cells LTD 4 -induced responses can be totally ascribed to a CysLT 1 receptor. (biologists.org)
Calcium Channel2
- Compared with placebo, the probability of delivery being delayed by 48 hours was highest with prostaglandin inhibitors (odds ratio 5.39, 95% credible interval 2.14 to 12.34) followed by magnesium sulfate (2.76, 1.58 to 4.94), calcium channel blockers (2.71, 1.17 to 5.91), beta mimetics (2.41, 1.27 to 4.55), and the oxytocin receptor blocker atosiban (2.02, 1.10 to 3.80). (bmj.com)
- Compared with placebo, side effects requiring a change of medication were significantly higher for beta mimetics (22.68, 7.51 to 73.67), magnesium sulfate (8.15, 2.47 to 27.70), and calcium channel blockers (3.80, 1.02 to 16.92). (bmj.com)
GPCRs8
- 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)
- sub.q protein variants that functionally couple to sensory cell receptors such as taste GPCRs (TRs) and olfactory GPCRs (ORs) in an overly promiscuous manner. (patentgenius.com)
- Although other G-protein-coupled receptors (GPCRs) recognize biogenic ligands mainly with ionic or hydrogen bonding interactions, ORs recognize odorants mostly via hydrophobic and van der Waals interactions. (jneurosci.org)
- A molecular basis for the detection of odorants was provided by the discovery of the olfactory receptor (OR) superfamily, which is a large family of multigenes that encode rhodopsin-like G-protein-coupled receptors (GPCRs) ( Buck and Axel, 1991 ). (jneurosci.org)
- This dual function of an odorant as an agonist and antagonist may provide insight into the structure-function relationship of GPCRs in general. (jneurosci.org)
- G protein-coupled receptors (GPCRs) constitute a vast protein family that encompasses a wide range of functions (including various autocrine, para- crine and endocrine processes). (130.88.97)
- The currently known clan members include the rhodopsin-like GPCRs, the secretin-like GPCRs, the cAMP receptors, the fungal mating pheromone receptors, and the metabotropic glutamate receptor family. (130.88.97)
- The waning of G protein-dependent signaling (i.e., desensitization of GPCRs) rapidly takes place with the phosphorylation of agonist-occupied GPCRs, which then interact with -arrestins (Shenoy and Lefkowitz, 2003). (39kf.com)
Phosphorylation5
- Desensitization, which rapidly turns off G protein-dependent signaling, involves phosphorylation of CCR5 that promotes interaction of the receptor with -arrestins for endocytosis. (39kf.com)
- In contrast, R126N-CCR5 not only retained agonist-promoted phosphorylation and -arrestin-dependent endocytosis but also displayed a higher basal phosphorylation than wild-type CCR5. (39kf.com)
- Subcellular Targeting and Agonist-induced Site-specific Phosphorylation of Endothelial Nitric-oxide Synthase. (pharmaceuticalintelligence.com)
- By using mutants of the β 1 AR lacking G protein-coupled receptor kinase phosphorylation sites and siRNA directed against β-arrestin, we show that Alp- and Car-stimulated EGFR transactivation requires β 1 AR phosphorylation at consensus G protein-coupled receptor kinase sites and β-arrestin recruitment to the ligand-occupied receptor. (pnas.org)
- Turning off the G protein signal by a process known as desensitization occurs through G protein-coupled receptor kinase (GRK) phosphorylation of the 7TMR, and subsequent binding of β-arrestin ( 1 , 2 ). (pnas.org)
Characterization1
- 1989) Molecular characterization of the human beta 3‐adrenergic receptor. (els.net)
Internalization4
- Exposure to agonist induced a rapid homologous desensitization of the CysLT 1 receptor [as measured by the reduction in the maximal agonist-induced intracellular cytosolic Ca 2+ ([Ca 2+ ] i ) transient], followed by receptor internalization (as assessed by equilibrium binding and confocal microscopy). (biologists.org)
- Furthermore, ATP/UDP-induced CysLT 1 receptor desensitization was unable to cause receptor internalization, induced a faster recovery of CysLT 1 functionality and was dependent upon protein kinase C. By contrast, homologous desensitization, which is probably dependent upon G-protein-receptor kinase 2 activation, induced a fast receptor downregulation and, accordingly, a slower recovery of CysLT 1 functionality. (biologists.org)
- In the absence of agonist, EGFR had a uniform membrane distribution ( Fig. 1 A ). In contrast, the βAR agonists dobutamine (Dob) and isoproterenol (Iso) resulted in internalization of EGFRs as visualized by marked redistribution into cellular aggregates, similar to that seen with EGF ( Fig. 1 A Upper ). (pnas.org)
- EGFR internalization following agonists (Dob, Iso, and EGF) or β-blocker administration is visualized using confocal microscopy. (pnas.org)
Opiate6
- It is the most potent of the opiate agonists and is useful for the acute management of headache due to migraine. (medscape.com)
- A second aspect of the present invention relates to the use of the diazabicyclo[4.3.onanes as ligands for various cellular receptors, including opiate receptors. (google.com)
- Haloperidol is also a potent antagonist of opiate receptors, and has weak antagonist activity at muscarinic, histamine H1, alpha-adrenergic, and serotonin receptors (Dollery 1991). (inchem.org)
- We 7 and others 8 demonstrated that the analgesic properties of N 2 O could be blocked by the discrete introduction of opiate antagonists directly into the PAG. (asahq.org)
- Several enigmatic issues concerning N 2 O remain, including the circuitry involved between the opiate receptors in the PAG and the α 2 adrenoceptors in the spinal cord. (asahq.org)
- Does a pathway descend in the spinal cord to link N 2 O-induced activation of opiate receptors in the PAG with activation of α 2 adrenoceptors in the spinal cord? (asahq.org)
Ligands4
- 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)
- Although their activating ligands vary widely in structure and character, the amino acid sequences of the receptors are very similar and are believed to adopt a common structural framework comprising 7 transmembrane (TM) helices [3- (130.88.97)
- Recent evidence suggests that binding of different ligands promotes distinct receptor conformations leading to specific signaling events ( 9 - 12 ). (pnas.org)
- We screened β-adrenergic ligands to determine if any could lead to β 1 AR-mediated EGFR transactivation. (pnas.org)
Leukotriene B4 recep3
- Pharmacologic actions of the second generation leukotriene B4 receptor antagonist LY29311: in vivo pulmonary studies. (nih.gov)
- The discovery of LY293111, a novel, potent and orally active leukotriene B4 receptor antagonist of the biphenylphenol class. (nih.gov)
- Effect of a leukotriene B4 receptor antagonist, LY293111, on allergen induced responses in asthma. (nih.gov)
Molecular4
- 1988) Molecular cloning and expression of the cDNA for the hamster alpha 1‐adrenergic receptor. (els.net)
- However, current evidence indicates that aging may downregulate βAR signaling, β 2 AR in particular, by decreasing the expression of molecular components of the adrenergic signaling machinery ( 21 - 24 ). (diabetesjournals.org)
- We investigated the molecular basis of desensitization and trafficking of the CysLT 1 receptor constitutively and transiently expressed in the human monocyte/macrophage-like U937 or COS-7 cells in response to LTD 4 or nucleotides. (biologists.org)
- The availability of genes encoding an increasingly wide array of receptors for regulatory substances has led to insight into the molecular basis of ligand-receptor interactions. (biomedcentral.com)
Predominantly3
- The effectiveness of PHE but not clonidine, together with the high potency of the alpha 1-blocker prazosin suggest that the alpha-adrenergic receptor is predominantly of the alpha 1-subtype. (kuleuven.be)
- Precapillary arterioles, however, may be subserved predominantly by alpha 2-receptors. (ahajournals.org)
- WIN55,212-22 effects on memory consolidation were predominantly mediated by CB1 receptor activation but CB2 receptors were involved as well. (frontiersin.org)
20002
- While detailed knowledge of ligand-receptor interactions would be instrumental in design of new and improved clinical candidates, the insight into spatial structure of GPCR has been limited to ab initio models ( Goddard and Abrol 2007 ) or models based on rhodopsin crystal structure ( Palczewski and others 2000 ). (pubmedcentralcanada.ca)
- and rat I7 (octanal receptor) ( Singer, 2000 ), based on the 7.5 Å rhodopsin structure ( Schertler, 1998 ). (jneurosci.org)
Protein22
- The region of i loop 3 highlighted in blue is implicated in signalling from receptor to G protein. (els.net)
- Marchese A, Chen C, Kim YM and Benovic JL (2003) The ins and outs of G‐protein‐coupled receptor trafficking. (els.net)
- Tao J, Wang HY and Malbon CC (2003) Protein kinase A regulates AKAP250 (gravin) scaffold binding to the beta2‐adrenergic receptor. (els.net)
- Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. (springer.com)
- This invention relates to G.alpha.q protein variants and their use in the analysis and discovery of agonists and antagonsists of chemosensory receptors, such as G protein coupled receptors involved in sensing of tastants, olfactants, andpheromones. (patentgenius.com)
- subunits also contribute to the specificity of receptor-G protein coupling (Xuet al. (patentgenius.com)
- Muscarinic receptor function, density and G-protein coupling in the overactive diabetic rat bladder. (nih.gov)
- High resolution crystal structure of human β 2 -adrenergic G protein-coupled receptor. (guidetopharmacology.org)
- Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
- This receptor-channel complex also contains a G protein - G s , which activate an adenylyl cyclase , cAMP-dependent kinase , and the counterbalancing phosphatase , PP2A . (enacademic.com)
- Capra, 2004 ), both belonging to the G-protein-coupled receptor (GPCR) superfamily. (biologists.org)
- Mitogen-activated protein (MAP) is a family of 42 and 44 kDa cytosolic serine-threonine kinases 1 , 2 , and has been identified as an important regulatory component in the growth and proliferative responses of many cell types 3 . (ersjournals.com)
- have been identified, cloned and sequenced to date and are members of the superfamily of G-protein-coupled receptors. (aspetjournals.org)
- The protein product can be uncoupling protein 1 (UCP1), uncoupling protein 2 (UCP2), uncoupling protein 3 (UCP3), uncoupling protein 4 (UCP4), and uncoupling protein 5 (UCP5). (justia.com)
- 1. ATTWOOD, T.K. AND FINDLAY, J.B.C. Fingerprinting G protein-coupled receptors. (130.88.97)
- 2. ATTWOOD, T.K. AND FINDLAY, J.B.C. G protein-coupled receptor fingerprints. (130.88.97)
- 4. CASEY, P.J. AND GILMAN, A.G. G protein involvement in receptor-effector coupling. (130.88.97)
- 5. ATTWOOD, T.K. AND FINDLAY, J.B.C. Design of a discriminating fingerprint for G protein-coupled receptors. (130.88.97)
- the role of the Fragile X mental retardation protein in the formation of neural circuits, an array tomographic study on the influence of synaptic plasticity on the number of synapses made in neural microcircuits, and on the localization of AMPA receptor subunits in different states of plasticity. (stanford.edu)
- CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor that governs migration of leukocytes and serves as a coreceptor for the R5 tropic strains of human immunodeficiency virus (HIV). (39kf.com)
- CCR5 is a G protein-coupled heptahelical receptor (GPCR) that initiates intracellular signaling in response to CC chemokines, including CCL3/MIP-1, CCL4/MIP-1, CCL5/RANTES, and CCL8/monocyte chemoattractant protein 2. (39kf.com)
- Recent evidence suggests that binding of agonist to its cognate receptor initiates not only classical G protein-mediated signaling, but also β-arrestin-dependent signaling. (pnas.org)
Propranolol8
- The cremaster skeletal muscle of anesthetized rats was acutely denervated and suspended in a Krebs bath containing cocaine, normetanephrine, and propranolol to block uptake1, uptake2, and beta-receptors, respectively. (ahajournals.org)
- The growth-promoting effect of salbutamol in 16-HBE cells was equipotent to 10% foetal bovine serum and was inhibited by propranolol and a cyclic adenosine monophosphate (cAMP) antagonist, Rp-adenosine 3′,5′-cyclic monophosphorothioate triethylammonium salt (Rp-cAMPS). (ersjournals.com)
- Hepa cells transfected with the Ala 186 -Ser 187 mutant H2 receptor demonstrated a biphasic rise in cAMP in response to epinephrine with an early phase (ED 50 ≈10 −11 M) that could be inhibited by both propranolol and cimetidine. (biomedcentral.com)
- L cells transfected with the Ala 186 -Ser 187 mutant H2 receptor also responded to epinephrine in a cimetidine and propranolol inhibitable manner. (biomedcentral.com)
- Propranolol is classified as a competitive non-cardioselective sympatholytic beta blocker that crosses the blood-brain barrier . (propranolol-abc.com)
- In addition to its effects on the adrenergic system, there is evidence that indicates that propranolol may act as a weak antagonist of certain serotonin receptors , namely the 5-HT 1A , 5-HT 1B , and 5-HT 2B receptors . (propranolol-abc.com)
- Propranolol is a competitive antagonist of beta-1-adrenergic receptors in the heart. (propranolol-abc.com)
- Propranolol is rapidly and completely absorbed, with peak plasma levels achieved about 1-3 hours after ingestion. (propranolol-abc.com)
Mechanisms4
- To address the question of whether AT 1 receptor antagonists or ACE inhibitors exhibit differential alterations of β-adrenergic neuroeffector mechanisms, TG(m REN 2)27 rats were treated with the ACE inhibitor captopril or the AT 1 receptor antagonist Bay 10-6734. (ahajournals.org)
- Our findings drive beyond the classical hypothesis centered on the unique role of CB1 receptor activation for cannabinoid effects on memory, and reveal new insights in the neural mechanisms of memory consolidation. (frontiersin.org)
- Nevertheless, the significance of these signaling pathways for physiological adrenergic functions in β-cells is largely unknown, because pharmacologically higher concentrations (µmol/L order) of catecholamines have been used for the analysis of these signaling mechanisms. (diabetesjournals.org)
- Though the mechanisms are still under research, data suggest that beta alanine can contribute to gains in lean muscle mass3. (priceplow.com)
Nicotinic receptors2
- Gotti C, Clementi F. Neuronal nicotinic receptors: from structure to pathology. (springer.com)
- Leonard S, Bertrand D. Neuronal nicotinic receptors: from structure to function. (springer.com)
Specific antagonists2
- ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β 2 adrenergic receptor, as few other specific antagonists for this receptor are known. (wikipedia.org)
- The actions of CRF are inhibited by specific antagonists. (aspetjournals.org)
Vascular smooth1
- The purpose of this study was to determine whether both alpha 1- and alpha 2-adrenergic receptors exist on vascular smooth muscle of microvessels and whether adrenergic constriction of anatomically distinct microvascular segments is differentially subserved by either receptor subtype. (ahajournals.org)
Secretion3
- In this study, we investigated the significance of β 2 -adrenergic receptor (β 2 AR) in age-related impaired insulin secretion and glucose homeostasis. (diabetesjournals.org)
- Studies with β 2 AR agonists further suggest that the β 2 AR may play an important role in regulating insulin secretion ( 15 ). (diabetesjournals.org)
- We previously reported that the transient receptor potential melastatin 2 (TRPM2) channel, a type of NSCC, in β-cells plays an essential role in glucose-induced and incretin-potentiated insulin secretion ( 9 ). (diabetesjournals.org)
Adrenoceptors4
- Description: Measuring displacement of [ 3 H]-DHA from recombinant human β 2 adrenoceptors expressed in HEK293T cells. (guidetopharmacology.org)
- Furchgott RF (1972) The classification of adrenoceptors (adrenergic receptors). (springer.com)
- BOTH muscarinic receptors and alpha-adrenoceptors have been shown to exist in airway smooth muscle. (asahq.org)
- Beta-blockers bind to beta-adrenoceptors, which inhibit normal sympathetic effects that act through the receptors norepinephrine and epinephrine. (uspharmacist.com)
Mediates2
- The aim of this study was to investigate which receptor subtype mediates cannabinoid effects on memory consolidation for emotionally arousing experiences. (frontiersin.org)
- 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)
Blockers7
- The role of beta-blockers, calcium antagonists, and ACE-inhibitors. (springer.com)
- The enantiomers of some of these drugs possess other effects, codynamics of beta-blockers. (weight-loss-tips-and-secrets.com)
- Although the available treatments (beta-blockers, BBs) improve the evolution of the disease, they do not protect MFS patients from progression of ARD and dissection. (clinicaltrials.gov)
- A key molecule that negatively influences cell growth, differentiation, survival and death in MFS is TGFb which is antagonised by existing drugs employed in the clinical practice, the Angiotensin II receptor blockers (ARB). (clinicaltrials.gov)
- Beta blockers or angiotensin-converting-enzyme inhibitor/angiotensin receptor blocker: what should be first? (meta.org)
- Cells stably expressing WT β 1 ARs were transfected with GFP-tagged EGFR (EGFR-GFP) and stimulated with several agonists or 20 different β-blockers. (pnas.org)
- oxytocin receptor blockers (for example, atosiban), and others. (bmj.com)
Concentrations3
- After administration of an oral dose, peak plasma concentrations are attained at approximately 3 hours Label . (drugbank.ca)
- Peak plasma concentrations occur within 3-9 days, then decrease slowly (Beresford & Ward 1987). (inchem.org)
- Nowadays, nitrous oxide is still used in combination with various anaesthetic agents such as isoflurane and ketamine for anaesthetic sparing, to allow lower concentrations of volatile or non-gaseous anaesthetics to be used [ 3 , 4 ]. (mdpi.com)
Adenylate cyclase1
- This study was undertaken to determine whether receptor and non-receptor components of the adenylate cyclase (AC) cascade were altered in brown adipose tissue (BAT) of 14-day-old pre-obese (fa/fa) rats, before endocrine status is strongly modified by fa gene expression. (portlandpress.com)
Ligand binding spe2
- Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity. (duke.edu)
- Major determinants of alpha 2- and beta 2-adrenergic receptor agonist and antagonist ligand binding specificity are contained within the seventh membrane spanning domain. (duke.edu)
Epinephrine and norepineph1
- Through blood vessel constriction by adrenergic receptor activation, epinephrine and norepinephrine normally act to increase blood pressure 10 . (drugbank.ca)
20012
- Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. (els.net)
- Nicotine Tob Res, 2001, 3: 203-223. (springer.com)
Inhibit3
- 3 . The lacrimal implant of claim 1 , wherein the implant body is configured to partially or completely inhibit fluid flow into and through the lacrimal canaliculus. (google.es)
- We demonstrated that ADRB3 agonists are able to inhibit in-vitro spontaneous contractions of myometrial strips, via a cyclic AMP-mediated pathway. (biomedcentral.com)
- Results: NK1 receptor antagonist was found to inhibit substance P induced histamine release in samples from stressed female rats but not in samples from control animals. (bmj.com)
Gene3
- Treatment with captopril (100 mg/kg of feed) or the AT 1 -antagonist Bay 10-6734 (100 mg/kg of feed) was performed in transgenic rats harboring the mouse renin 2 d gene [TG(m REN 2) (ahajournals.org)
- We have previously cloned the H2-histamine receptor gene and noted that only three amino acids on the receptor were sufficient to define its specificity and selectivity. (biomedcentral.com)
- The canine H2 receptor gene was mutated at Asp 186 and Gly 187 (Asp 186 to Ala 186 and Gly 187 to Ser 187 ) by oligonuceotide directed mutagenesis. (biomedcentral.com)
Adenylyl cyclase2
- Neuropeptide Y and angiotensin II levels, adenylyl cyclase activity, β-adrenergic receptors, G sα , and G iα were investigated. (ahajournals.org)
- Isoprenaline- and guanylylimidodiphosphate-stimulated adenylyl cyclase activities and β-adrenergic receptor density were reduced, whereas the catalyst and G sα -function were unchanged. (ahajournals.org)
Isoproterenol3
- Here we show that while the carazolol pocket captured in the β 2 AR crystal structure accommodates (-)-isoproterenol and other agonists without steric clashes, a finite movement of the flexible extracellular part of TM-V helix (TM-Ve) obtained by receptor optimization in the presence of docked ligand can further improve the calculated binding affinities for agonist compounds. (pubmedcentralcanada.ca)
- Lands AM, Luduena FP, Buzzo HJ (1967) Differentiation of receptors responsive to isoproterenol. (springer.com)
- The order of potency of a series of agonists competing for [125I]cyanopindolol binding is consistent with the interaction of a beta 2-subtype receptor: zinterol greater than (-) isoproterenol greater than (-) epinephrine = salbutamol much greater than (-) norepinephrine. (meta.org)
Inverse agonist1
- Rosenbaum and others 2007 ) revealing in atomic detail the binding interactions for an inverse agonist (-)-carazolol (PDB code 2RH1). (pubmedcentralcanada.ca)
Blockade5
- Chronic obstructive pulmonary disease (COPD) may delay the diagnosis of chronic heart failure (CHF), and promote nonadherence to therapeutic guidelines, especially beta-blockade. (onlinejacc.org)
- Beta-blockade is safe in stable COPD. (onlinejacc.org)
- Beta -blockade should be attempted in all CHF patients with coexistent CHF and COPD. (onlinejacc.org)
- The presence of COPD impacts on the treatment of CHF, as COPD is still viewed as a contraindication to beta-blockade. (onlinejacc.org)
- Among the comorbid conditions commonly associated with CHF, COPD is the one that most delays the diagnosis of CHF and is most often advocated for nonadherence to therapeutic guidelines, especially beta-blockade (BB) ( 3 ). (onlinejacc.org)
Superfamily1
- The olfactory receptor (OR) superfamily provides a basis for the remarkable ability to recognize and discriminate a large number of odorants. (jneurosci.org)
Specificity3
- Furthermore, we succeeded in rational receptor design, inserting point mutations in the odorant-binding site that resulted in predicted changes in ligand specificity and antagonist activity. (jneurosci.org)
- We hypothesized that, if the specificity and selectivity of both receptors are invested in just three amino acids, it should be possible to convert one of the receptors into one that recognizes the ligand of the other by simple mutations at only one or two sites. (biomedcentral.com)
- These results support the hypothesis that ligand specificity is determined by only a few key points on a receptor regardless of the structure of the remainder of the molecule. (biomedcentral.com)
Rats11
- ii) BRL37344 and CGP12177 (beta 3 agonists) were less potent in fa/fa than in Fa/fa rats (Kact. (portlandpress.com)
- Binding experiments with [3H]CGP12177 show that in BAT of suckling rats, beta 3-ARs represent 80% of the total beta-ARs. (portlandpress.com)
- In conclusion, these results provide evidence for alterations in beta 1- and beta 3-AR signalling in BAT of 14-day-old suckling pre-obese Zucker rats with a decreased activity of alpha Gs. (portlandpress.com)
- Biochemical and functional characteristics of bladder muscarinic receptors and effects of experimental diabetes in rats]. (nih.gov)
- Changes in muscarinic responsiveness, muscarinic receptor density and Ca2+ mobilization of the urinary bladder in streptozotocin-induced diabetic rats. (nih.gov)
- Effects of ONO-2235, an aldose reductase inhibitor, on muscarinic receptors and contractile response of the urinary bladder in rats with streptozotocin-induced diabetes. (nih.gov)
- EFFECT OF ADRENERGIC RECEPTOR-BLOCKING DRUGS IN indicate that the sympatheticalphaand beta receptors in the rat uterus do not appear to play any significantpart in Effect ofan intra-uterine silk thread suture on the fertility of female rats. (weight-loss-tips-and-secrets.com)
- Dial /8-adrenergic receptors in female Fischer 344 rats of 3, 12, and 24 months of age. (weight-loss-tips-and-secrets.com)
- In T3-treated rats (50 jag0 T3/kg-day for 3 days), adrenergic receptors may explain these changes associ-ated with aging, since plasma catecholamine levels in-crease with age (8). (weight-loss-tips-and-secrets.com)
- Therefore, we investigated the influence of stress on NK1 receptor activation at the colonic level in female rats. (bmj.com)
- 3, 4 Thus experimental models have been developed to evaluate the effect of stress on lower gut function in rats. (bmj.com)
Activation6
- Activation of beta-adrenergic receptors inhibits Ca2+ entry-mediated generation of inositol phosphates in the guinea pig myometrium, a cyclic AMP-independent event. (aspetjournals.org)
- Activation of P2Y receptors with ATP or UDP induced heterologous desensitization of the CysLT 1 receptor. (biologists.org)
- Conversely, LTD 4 -induced CysLT 1 receptor activation had no effect on P2Y receptor responses, which suggests that the latter have a hierarchy in producing desensitizing signals. (biologists.org)
- The URB597-induced memory enhancement was dependent on the activation not only of CB1 and CB2 receptors but, notwithstanding, PPAR-α and TRPV1 receptors were involved as well. (frontiersin.org)
- Epinephrine also induced IP3 generation in the same cells, a biological response that is characteristic of activation of the wild-type H2 but not of the β -adrenergic receptor. (biomedcentral.com)
- Conclusions: Stress induces NK1 receptor activation in the colon, and ovarian steroids are involved in this response. (bmj.com)
Kinase1
- 1996) The beta‐adrenergic receptor is a substrate for the insulin receptor tyrosine kinase. (els.net)
Intracellular2
- Agonist-bound sensory receptors catalyze theexchange of GTP for GDP on the surface of the G.alpha.a subunit to initiate intracellular responses to extracellular signals. (patentgenius.com)
- Exposure to salbutamol in serum-free medium increased 3‐(4,5-dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium-bromide reduction and intracellular deoxyribonucleic acid (DNA) contents in 16-human bronchial epithelium (16-HBE) cells and NCI-H292 cells, but not in A549 cells. (ersjournals.com)
Confocal microscopy1
- An optical section of the fluorescent receptors is obtained by epifluorescence confocal microscopy from insulin‐treated (a), untreated (b) and β‐adrenergic agonist‐treated (c) cells. (els.net)
Cannabinoid agonists1
- and the well known behavioral effects of cannabinoid agonists ( Mechoulam, 1986 ), it is likely that this receptor regulates short-term memory, coordination of movement and emotions. (aspetjournals.org)
Pathways5
- Shumay E, Gavi S, Wang HY and Malbon CC (2004) Trafficking of beta2‐adrenergic receptors: insulin and beta‐agonists regulate internalisation by distinct cytoskeletal pathways. (els.net)
- 1-3 Maintenance of electroneutrality across the alveolar epithelium requires that Cl − exit the airspace via trans- and paracellular pathways. (ahajournals.org)
- The beta-adrenergic pathway is one of the strongest fat burning pathways in the body. (anabolicminds.com)
- Instead of stuffing Alpha-T2 full of stimulants that give nasty jitters and crash in an attempt to indirectly activate beta-adrenergic pathway, PES took these biochemical pathways a step further. (anabolicminds.com)
- However, the significance of these signaling pathways for physiological adrenergic functions in β-cells is largely unknown. (diabetesjournals.org)
Responses5
- When tested on days 1, 3, 6 and 8 in culture, both alpha- and beta-adrenergic responses appeared to be higher in the presence of the glucocorticoid dexamethasone compared to the responses in the absence of dexamethasone. (kuleuven.be)
- Systematic differences in capacity of partial, full and inverse agonists to induce TM-V helix tilt in the β 2 AR model suggest potential role of TM-V as a conformational "rheostat" involved in the whole spectrum of β 2 AR responses to small molecule signals. (pubmedcentralcanada.ca)
- Since these mediators accumulate at sites of inflammation, and inflammatory cells express both classes of receptors, their responses are likely to be crossregulated. (biologists.org)
- These results have implications for how distinct biological responses of CCR5 might rely on a different set of receptor conformations. (39kf.com)
- 3) and treatment responses for IBS occur earlier than the antidepressant effect. (bmj.com)
