Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.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.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.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).Adenosine 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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Receptors, 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.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.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.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.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.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.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.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.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.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.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.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.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.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)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.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.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Receptors, 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.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.Quinpirole: A dopamine D2/D3 receptor agonist.Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.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.Integrin beta3: An integrin beta subunit of approximately 85-kDa in size which has been found in INTEGRIN ALPHAIIB-containing and INTEGRIN ALPHAV-containing heterodimers. Integrin beta3 occurs as three alternatively spliced isoforms, designated beta3A-C.Piperidines: A family of hexahydropyridines.Benzazepines: Compounds with BENZENE fused to AZEPINES.8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.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.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.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.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.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.PyrrolidinesNaphthalenes: 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.Cell Line: Established cell cultures that have the potential to propagate indefinitely.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.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.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.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, Glucagon: Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.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.Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.Cholinergic Agonists: Drugs that bind to and activate cholinergic receptors.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Benzoxazines: OXAZINES with a fused BENZENE ring.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Mice, Inbred C57BLRNA, 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.Receptor, Cannabinoid, CB2: A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.Calcium: A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.Venoms: Poisonous animal secretions forming fluid mixtures of many different enzymes, toxins, and other substances. These substances are produced in specialized glands and secreted through specialized delivery systems (nematocysts, spines, fangs, etc.) for disabling prey or predator.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.Serotonin 5-HT3 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Tetrahydronaphthalenes: Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.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.Purinergic P2X Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Purinergic P2Y Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.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.Behavior, Animal: The observable response an animal makes to any situation.Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.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.Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.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.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Receptor, Serotonin, 5-HT1B: A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.Methylhistamines: Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.Benzeneacetamides: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.Xanthines: Purine bases found in body tissues and fluids and in some plants.PiperazinesMorpholinesReceptors, 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.Bicyclo Compounds, Heterocyclic: A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)Receptors, sigma: A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Enkephalins: One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.Adrenergic beta-2 Receptor Agonists: Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Receptors, Adrenergic, beta-1: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.Receptors, Prostaglandin E: Cell surface receptors which bind prostaglandins with a high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin E receptors prefer prostaglandin E2 to other endogenous prostaglandins. They are subdivided into EP1, EP2, and EP3 types based on their effects and their pharmacology.Receptor, Serotonin, 5-HT1A: A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.Receptor, Adenosine A3: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.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.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.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.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.Bicyclo CompoundsKinetics: The rate dynamics in chemical or physical systems.Receptors, GABA-B: A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.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.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.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.Oligopeptides: Peptides composed of between two and twelve amino acids.Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.Receptors, Histamine: Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.Integrin alpha5beta1: An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.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, Metabotropic Glutamate: Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.Receptors, GABA-A: Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.Receptors, Nicotinic: One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.Integrin beta4: Also known as CD104 antigen, this protein is distinguished from other beta integrins by its relatively long cytoplasmic domain (approximately 1000 amino acids vs. approximately 50). Five alternatively spliced isoforms have been described.Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.Purinergic Agonists: Compounds that bind to and activate PURINERGIC RECEPTORS.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.Integrin alpha6beta4: This intrgrin is a key component of HEMIDESMOSOMES and is required for their formation and maintenance in epithelial cells. Integrin alpha6beta4 is also found on thymocytes, fibroblasts, and Schwann cells, where it functions as a laminin receptor (RECEPTORS, LAMININ) and is involved in wound healing, cell migration, and tumor invasiveness.Dopamine Agents: Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.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.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.Hydrocarbons, FluorinatedClonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Receptors, Purinergic P2: A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.Integrin beta Chains: Integrin beta chains combine with integrin alpha chains to form heterodimeric cell surface receptors. Integrins have traditionally been classified into functional groups based on the identity of one of three beta chains present in the heterodimer. The beta chain is necessary and sufficient for integrin-dependent signaling. Its short cytoplasmic tail contains sequences critical for inside-out signaling.beta 2-Glycoprotein I: A 44-kDa highly glycosylated plasma protein that binds phospholipids including CARDIOLIPIN; APOLIPOPROTEIN E RECEPTOR; membrane phospholipids, and other anionic phospholipid-containing moieties. It plays a role in coagulation and apoptotic processes. Formerly known as apolipoprotein H, it is an autoantigen in patients with ANTIPHOSPHOLIPID ANTIBODIES.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.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.Impromidine: A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.Peptide Fragments: Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.Receptor, Serotonin, 5-HT2C: A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.Receptors, Purinergic: Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.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.Amphetamines: Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.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.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Gene Expression Regulation: Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.Receptors, Histamine H2: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Receptors, Drug: Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.Integrin alpha4beta1: Integrin alpha4beta1 is a FIBRONECTIN and VCAM-1 receptor present on LYMPHOCYTES; MONOCYTES; EOSINOPHILS; NK CELLS and thymocytes. It is involved in both cell-cell and cell- EXTRACELLULAR MATRIX adhesion and plays a role in INFLAMMATION, hematopoietic cell homing and immune function, and has been implicated in skeletal MYOGENESIS; NEURAL CREST migration and proliferation, lymphocyte maturation and morphogenesis of the PLACENTA and HEART.QuinoxalinesEstrogen Receptor beta: One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.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.Cyclohexanols: Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.Electric Stimulation: Use of electric potential or currents to elicit biological responses.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.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.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)Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.Integrin alpha2beta1: An integrin found on fibroblasts, platelets, endothelial and epithelial cells, and lymphocytes where it functions as a receptor for COLLAGEN and LAMININ. Although originally referred to as the collagen receptor, it is one of several receptors for collagen. Ligand binding to integrin alpha2beta1 triggers a cascade of intracellular signaling, including activation of p38 MAP kinase.Microinjections: The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Receptors, Serotonin, 5-HT1: A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.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.Substance P: An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.Receptors, Neurokinin-2: A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.Receptors, Neuropeptide Y: Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.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.Acetylcholine: A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.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.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.Histamine: An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.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.Dimaprit: A histamine H2 receptor agonist that is often used to study the activity of histamine and its receptors.Benzylidene Compounds: Compounds containing the PhCH= radical.Sulfonamides: A group of compounds that contain the structure SO2NH2.Receptors, Cannabinoid: A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES.Injections, Intraventricular: Injections into the cerebral ventricles.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.Phenylisopropyladenosine: N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.Membrane Potentials: The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Benzomorphans: Morphine derivatives of the methanobenzazocine family that act as potent analgesics.N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
Functional and molecular biological evidence for a possible beta3-adrenoceptor in the human detrusor muscle. (1/103)
The possible existence of a beta3-adrenergic receptor (beta3-AR) in the human detrusor muscle was investigated by in vitro functional studies and analysis of mRNA expression. Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of the human detrusor. The rank order for their relaxing potencies was isoprenaline (pD2 6.37+/-0.07) > or = noradrenaline (pD2 6.07+/-0.12) > or = adrenaline (pD2 5.88< or =0.11). Neither dobutamine (beta1- and beta2-AR agonist) nor procaterol (beta2-AR agonist) produced any significant relaxation at concentrations up to 10(-5) M. BRL37344A, CL316243 and CGP-12177A (beta3-AR agonists), relaxed the preparations significantly at concentrations higher than 10(-6) M. The pD2 values for BRL37344A, CL316243 and CGP-12177A were 6.42+/-0.25, 5.53+/-0.09 and 5.74+/-0.14, respectively. CGP-20712A (10(-7) - 10(-5) M), a beta1-AR antagonist, did not affect the isoprenaline-induced relaxation. On the other hand, ICI-118,551, a beta2-AR antagonist, produced a rightward parallel shift of the concentration-relaxation curve for isoprenaline only at the highest concentration used (10(-5) > M) and its pKB value was 5.71+/-0.19. Moreover, SR58894A (10(-7) - 10(-5) M), a beta3-AR antagonist, caused a rightward shift of the concentration-relaxation curve for isoprenaline in a concentration-dependent manner. The pA2 value and slope obtained from Schild plots were 6.24+/-0.20 and 0.68+/-0.31. The beta1-, beta2- and beta3-AR mRNAs were all positively expressed in detrusor smooth muscle preparations in a reverse transcription polymerase chain reaction assay. In conclusion, the present results provide the first evidence for the existence of the beta3-AR subtype in the human detrusor. They also suggest that the relaxation induced by adrenergic stimulation of the human detrusor is mediated mainly through beta3-AR activation. (+info)Constitutively active mutants of the beta1-adrenergic receptor. (2/103)
We provide the first evidence that point mutations can constitutively activate the beta(1)-adrenergic receptor (AR). Leucine 322 of the beta(1)-AR in the C-terminal portion of its third intracellular loop was replaced with seven amino acids (I, T, E, F, C, A and K) differing in their physico-chemical properties. The beta(1)-AR mutants expressed in HEK-293 cells displayed various levels of constitutive activity which could be partially inhibited by some beta-blockers. The results of this study might have interesting implications for future studies aiming at elucidating the activation process of the beta(1)-AR as well as the mechanism of action of beta-blockers. (+info)Dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization. (3/103)
The use of dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization was investigated in 20 men. At 2.5, 5, and 10 microg x kg(-1) x min(-1), dobutamine induced significant increases in energy expenditure, lipid oxidation, and lipolysis. The beta(1)-adrenoceptor antagonist atenolol (bolus: 42.5 microg/kg, infusion: 1.02 microg x kg(-1) x min(-1)) blocked all dobutamine-induced effects on thermogenesis and lipid utilization. All parameters remained at levels comparable to those during saline infusion. The dose of atenolol used did not inhibit beta(2)-adrenoceptor-specific changes in energy expenditure, lipid oxidation, and lipolysis during salbutamol infusion (85 ng x kg(-1) x min(-1)). This indicates that atenolol was specific for beta(1)-adrenoceptors and did not camouflage concomitant beta(2)-adrenoceptor stimulation during dobutamine infusion. Therefore, we conclude that dobutamine can be used as a selective beta(1)-adrenoceptor agonist at dosages +info)Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. (4/103)
We examined the subtype-selective binding site of the beta-adrenergic receptors (betaARs). The beta(1)/beta(2)-chimeric receptors showed the importance of the second and seventh transmembrane domains (TM2 and TM7) of the beta(2)AR for the binding of the beta(2)-selective agonists such as formoterol and procaterol. Alanine-substituted mutants of TM7 of the beta(2)AR showed that Tyr(308,) located at the top of TM7, mainly contributed to beta(2) selectivity. However, Tyr(308) interacted with formoterol and procaterol in two different ways. The results of Ala- and Phe-substituted mutants indicated that the phenyl group of Tyr(308) interacted with the phenyl group in the N-substituent of formoterol (hydrophobic interaction), and the hydroxyl group of Tyr(308) interacted with the protonated amine of procaterol (hydrophilic interaction). In contrast to beta(2)AR, TM2 is a major determinant that beta(1)-selective agonists such as denopamine and T-0509 bound the beta(1)AR with high affinity. Three amino acids (Leu(110), Thr(117), and Val(120)) in TM2 of the beta(1)AR were identified as major determinants for beta(1)-selective binding of these agonists. Three-dimensional models built on the basis of the predicted structure of rhodopsin showed that Tyr(308) of the beta(2)AR covered the binding pocket formed by TM2 and TM7 from the upper side, and Thr(117) of the beta(1)AR located in the middle of the binding pocket to provide a hydrogen bonding for the beta(1)-selective agonists. These data indicate that TM2 and TM7 of the betaAR formed the binding pocket that binds the betaAR subtype-selective agonists with high affinity. (+info)Identification of the endophilins (SH3p4/p8/p13) as novel binding partners for the beta1-adrenergic receptor. (5/103)
Several G-protein coupled receptors, such as the beta1-adrenergic receptor (beta1-AR), contain polyproline motifs within their intracellular domains. Such motifs in other proteins are known to mediate protein-protein interactions such as with Src homology (SH)3 domains. Accordingly, we used the proline-rich third intracellular loop of the beta1-AR either as a glutathione S-transferase fusion protein in biochemical "pull-down" assays or as bait in the yeast two-hybrid system to search for interacting proteins. Both approaches identified SH3p4/p8/p13 (also referred to as endophilin 1/2/3), a SH3 domain-containing protein family, as binding partners for the beta1-AR. In vitro and in human embryonic kidney (HEK) 293 cells, SH3p4 specifically binds to the third intracellular loop of the beta1-AR but not to that of the beta2-AR. Moreover, this interaction is mediated by the C-terminal SH3 domain of SH3p4. Functionally, overexpression of SH3p4 promotes agonist-induced internalization and modestly decreases the Gs coupling efficacy of beta1-ARs in HEK293 cells while having no effect on beta2-ARs. Thus, our studies demonstrate a role of the SH3p4/p8/p13 protein family in beta1-AR signaling and suggest that interaction between proline-rich motifs and SH3-containing proteins may represent a previously underappreciated aspect of G-protein coupled receptor signaling. (+info)Analysis of domain responsible for desensitization of beta1-adrenergic receptor. (6/103)
When the wild type beta1-adrenergic receptor (WT-beta1AR) was expressed in Sf9 cells, the beta1AR-stimulated adenylyl cyclase activities were desensitized by prior treatment with isoproterenol. The extent of beta1AR desensitization was not modified, and the onset was not promoted by the overexpression of G protein-coupled receptor kinase 2 (GRK2), GRK5 or GRK6. However, overexpression of the dominant negative mutant of GRK2 appeared to inhibit desensitization of the beta1AR. The change of the potential protein kinase A phosphorylation site located at the intracellular third loop did not affect beta1AR desensitization. Desensitization of the truncated mutant, in which nearly all of the serine and threonine residues from the carboxyl terminus were eliminated, was the same as that of the WT-beta1AR. A deletion mutant that lacked serine and threonine residues of the intracellular third loop was also desensitized by isoproterenol stimulation. Furthermore, the deletion of serine and threonine residues from both the intracellular third loop and carboxyl terminus did not affect desensitization of the beta1AR. These results suggested that phosphorylation by endogenous GRKs in Sf9 cells contributed to desensitization of the beta1AR and that the regions other than third intracellular loop and carboxyl terminus may be responsible for beta1AR desensitization. (+info)Regulation of beta 1- and beta 3-adrenergic agonist-stimulated lipolytic response in hyperthyroid and hypothyroid rat white adipocytes. (7/103)
1. This study examined the effects of thyroid status on the lipolytic responses of rat white adipocytes to beta-adrenoceptor (beta-AR) stimulation. The beta 1- and beta 3-AR mRNAs and proteins were measured by Northern and saturation analyses, respectively. Glycerol production and adenyl cyclase (AC) activity induced by various non-selective and selective beta 1/beta 3-AR agonists and drugs which act distal to the receptor in the signalling cascade were measured in cells from untreated, triiodothyronine (T3)-treated and thyroidectomized rats. 2. The beta 3-AR density was enhanced (72%) by T3-treatment and reduced (50%) by introduction of a hypothyroid state while beta 1-AR number remained unaffected. The beta 1- and beta 3-AR density was correlated with the specific mRNA level in all thyroid status. 3. The lipolytic responses to isoprenaline, noradrenaline (beta 1/beta 3/beta 3-AR agonists) and BRL 37344 (beta 3-AR agonist) were potentiated by 48, 58 and 48%, respectively in hyperthyroidism and reduced by about 80% in hypothyroidism. 4. T3-treatment increased the maximal lipolytic response to the partial beta 3-AR (CGP 12177) and beta 1-AR (xamoterol) agonists by 234 and 260%, respectively, increasing their efficacy (intrinsic activity: 0.95 versus 0.43 and 1.02 versus 0.42). The maximal AC response to these agonists was increased by 84 and 58%, respectively, without changing their efficacy. 5. In the hypothyroid state, the maximal lipolytic and AC responses were decreased with CGP (0.17 +/- 0.03 versus 0.41 +/- 0.08 mumol glycerol/10(6) adipocytes; 0.048 +/- 0.005 versus 0.114 +/- 0.006 pmol cyclic AMP min-1 mg-1) but not changed with xamoterol. 6. The changes in lipolytic responses to postreceptor-acting agents (forskolin, enprofylline and dibutenyl cyclic AMP, (Bu)2cAMP) suggest the modifications on receptor coupling and phosphodiesterase levels in both thyroid states. 7. Thyroid status affects lipolysis by modifying beta 3-AR density and postreceptor events without changes in the beta 1-AR functionality. (+info)Differential adrenergic regulation of the gene expression of the beta-adrenoceptor subtypes beta1, beta2 and beta3 in brown adipocytes. (8/103)
In brown adipocytes, fundamental cellular processes (cell proliferation, differentiation and apoptosis) are regulated by adrenergic stimulation, notably through beta-adrenergic receptors. The presence of all three beta-receptor subtypes has been demonstrated in brown adipose tissue. Due to the significance of the action of these receptors and indications that the subtypes govern different processes, the adrenergic regulation of the expression of the beta(1)-(,) beta(2)- and beta(3)-adrenoceptor genes was examined in murine brown-fat primary cell cultures. Moderate levels of beta(1)-receptor mRNA, absence of beta(2)-receptor mRNA and high levels of beta(3)-receptor mRNA were observed in mature brown adipocytes (day 6 in culture). Noradrenaline (norepinephrine) addition led to diametrically opposite effects on beta(1)- (markedly enhanced expression) and beta(3)-gene expression (full cessation of expression, as previously shown). beta(2)-Gene expression was induced by noradrenaline, but only transiently (<1 h). The apparent affinities (EC(50)) of noradrenaline were clearly different (7 nM for the beta(1)-gene and+info)
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ISO 3166-2:BR - Вікіпедія... is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Formerly, it was also used to prolong the ... but has little affinity for beta receptors. The drug is largely obsolete, being superseded by other hemostatics such as ... It is the ketone form of epinephrine (adrenaline). Contrary to epinephrine, adrenalone mainly acts on alpha-1 adrenergic ... 1:8) and 94% ethanol (1:45). The melting point of the hydrochloride is 243 °C (469 °F). After local application, only traces of ...
... is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. It was ... ISBN 9780071826419 Frishman, W. H., Covey, S. (1990). Penbutolol and carteolol: two new beta-adrenergic blockers with partial ... Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. ... Penbutolol acts on the β1 adrenergic receptors in both the heart and the kidney. When β1 receptors are activated by a ...
1990). "beta-Arrestin: a protein that regulates beta-adrenergic receptor function". Science. 248 (4962): 1547-50. doi:10.1126/ ... Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G protein- ... 2000). "The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor ... 1998). "Clathrin-mediated endocytosis of the beta-adrenergic receptor is regulated by phosphorylation/dephosphorylation of beta ...
"Regulation of receptor fate by ubiquitination of activated beta 2-adrenergic receptor and beta-arrestin". Science. 294 (5545): ... The protein may interact with the agonist DOI in 5-HT2A receptor signaling. Arrestin beta 2 has been shown to interact with ... Lefkowitz RJ (July 1998). "G protein-coupled receptors. III. New roles for receptor kinases and beta-arrestins in receptor ... beta-arrestin 2 (ARRB2), and beta-adrenergic receptor kinase 2 (ADRBK2) genes". Genomics. 23 (1): 286-8. doi:10.1006/geno. ...
"Role of phosphorylation in agonist-promoted beta 2-adrenergic receptor sequestration. Rescue of a sequestration-defective ... beta-adrenergic-receptor phosphotransferase, [beta-adrenergic-receptor] kinase, beta-adrenergic receptor-specific kinase, beta- ... beta-ARK 2, beta-receptor kinase, GRK2, GRK3, beta-adrenergic-receptor kinase (phosphorylating), beta2ARK, betaARK1, beta- ... beta-adrenergic receptor] Thus, the two substrates of this enzyme are ATP and beta-adrenergic receptor, whereas its two ...
ISBN 0-443-07145-4. Philipson, L. H. (December 2002). "beta-Agonists and metabolism". The Journal of Allergy and Clinical ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... Beta-2 adrenergic receptor has been shown to interact with: AKAP12, OPRD1, Grb2, SNX27 and SLC9A3R1. Other adrenergic receptors ...
Selective agonists to the beta-1 receptor are: Denopamine Dobutamine (in cardiogenic shock) Xamoterol (cardiac stimulant) (Beta ... is a beta-adrenergic receptor, and also denotes the human gene encoding it. It is a G-protein coupled receptor associated with ... "The cardiac beta-adrenergic receptor. Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by ... and beta 2-adrenergic receptors: structurally and functionally related receptors derived from distinct genes". Trends in ...
The beta-adrenergic receptor kinase specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G ... Overall, the beta adrenergic receptor kinase 2 has 85% amino acid similarity with beta adrenergic receptor kinase 1, with the ... Beta-adrenergic receptor kinase 2 (beta-ARK-2) also known as G-protein-coupled receptor kinase 3 (GRK3) is an enzyme that in ... 1991). "Cloning, expression, and chromosomal localization of beta-adrenergic receptor kinase 2. A new member of the receptor ...
... also known as Beta1-adrenergic receptor agonists, are a class of drugs that bind selectively to the beta-1 adrenergic receptor ... www.cvpharmacology.com/cardiostimulatory/beta-agonist.htm Sakuma T, Hida M, Nambu Y, et al. (February 2001). "Beta1-adrenergic ... Beta-adrenoceptors typically bind to norepinephrine release by sympathetic adrenergic nerves and to circulating epinephrine. ... September 1998). "Denopamine, a beta1-adrenergic agonist, prolongs survival in a murine model of congestive heart failure ...
Johnson, M (2006). "Molecular mechanisms of beta(2)-adrenergic receptor function, response, and regulation". J Allergy Clin ... Beta2-adrenergic agonist Alpha-adrenergic agonist Asthma Beta blocker Beta-1 adrenergic receptor Beta-2 adrenergic receptor ... β1 receptors make up to 75% of all beta receptors and are predominantly located in the heart. β2 receptors are found in ... It also influences the specificity for the β-receptor subtypes. Direct-acting analog binds the β-adrenergic receptors directly ...
Non-selective beta blockers are known to facilitate bronchospasm as well. Beta blockers bind into the β2 receptors and block ... Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ... beta blockers (used to treat hypertension), a paradoxical result of using LABA drugs (to treat COPD) and other drugs. ...
... stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... a novel agonist at peripheral dopamine receptors and beta 2-adrenoceptors". British Journal of Pharmacology. 85 (3): 599-608. ... It works by stimulating beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... It is not an α-adrenergic agonist, does not cause vasoconstriction, and is not a pressor agent. As of 2004 there was some ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 ... September 1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. doi: ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ...
Verhoeckx KC, Doornbos RP, Witkamp RF, van der Greef J, Rodenburg RJ (January 2006). "Beta-adrenergic receptor agonists induce ... Zilpaterol (zilpaterol hydrochloride; codenamed RU 42173) is a β2 adrenergic agonist. Under its trade name, Zilmax, it is used ... A. Plascencia; N. Torrentera & R.A. Zinn (1999). "Influence of the β-Agonist, Zilpaterol, on Growth Performance and Carcass ... 6 (1): 1-7. doi:10.1016/j.intimp.2005.05.013. PMID 16332507. Petersen, Melody. "As Beef Cattle Become Behemoths, Who Are Animal ...
... are capable of exerting low-level agonist activity at the β-adrenergic receptor while simultaneously acting as a receptor site ... beta-blockers, β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor ... Beta blockers must not be used in the treatment of selective alpha-adrenergic agonist overdose. The blockade of only beta ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 ...
... beta _{2}} . The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert ... receptors in the vascular smooth muscle cells). Usage of β 2 {\displaystyle \beta _{2}} receptor agonists as hypotensive agents ... beta _{2}} receptors. Agonism of β 2 {\displaystyle \beta _{2}} receptors causes vasodilation and low blood pressure (i.e. the ... See also receptor antagonist) α 2 {\displaystyle \alpha _{2}} receptors. Agonists of α 2 {\displaystyle \alpha _{2}} receptors ...
... "beta2-Adrenergic receptor regulation by GIT1, a G protein-coupled receptor kinase-associated ADP ribosylation factor GTPase- ... "Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro". FEBS ... Hu LA, Chen W, Premont RT, Cong M, Lefkowitz RJ (Jan 2002). "G protein-coupled receptor kinase 5 regulates beta 1-adrenergic ... "Identification of the G protein-coupled receptor kinase phosphorylation sites in the human beta2-adrenergic receptor". The ...
... beta-2 microglobulin - beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta- ... adrenergic receptor - adrenodoxin - aequorin - aerobic respiration - agonist - alanine - albumin - alcohol - alcoholic ... alpha-2 adrenergic receptor - alpha-beta T-cell antigen receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - ... transforming growth factor beta - transforming growth factor beta receptor - transient receptor potential - translation ( ...
Labetalol - an alpha- and beta-adrenergic blocker, given as an intravenous bolus or infusion. Bolus followed by infusion. ... converting enzyme inhibitor or angiotensin II receptor blocker, which can interfere with renal autoregulation and produce acute ... J Chronic Dis 1: 33-42. Strandgaard S, Paulson OB (1989) Cerebral blood flow and its pathophysiology in hypertension. Am J ... Neurol Clin 1: 3-16. Moyer JH, Miller SI, Tashner AB, Snyder H, Bowman RO(1953) Malignant hypertension and hypertensive ...
"Assessment of compliance in children using inhaled beta adrenergic agonists". Ann Allergy. 62 (5): 406-9. PMID 2566291. Herpes ... The Herpes Simplex Virus JMP Mutant Enters Receptor-Negative J Cells through a Novel Pathway Independent of the Known Receptors ... Herpes Simplex Virus Glycoproteins gH/gL and gB Bind Toll-Like Receptor 2, and Soluble gH/gL Is Sufficient To Activate NF-κB ... Through her research, she also discovered the triggering activity of receptor- bound gD. In addition to these major discoveries ...
... beta-receptor agonists, follicle stimulating hormone, luteinising hormone, LHRH gamolenic acid, gonadotropin release inhibitor ... adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, parasympathomimetics, ... Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ... β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, nitrate, ...
The human beta-2 adrenergic receptor in complex with the partial inverse agonist carazolol.[1] ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... Crystal structure of activated beta-2 adrenergic receptor in complex with Gs(PDB entry 3SN6). The receptor is colored red, Gα ... "The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor into ...
... is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... In particular, it is a partial agonist at beta2- receptors located in the vascular smooth muscle. Labetalol relaxes vascular ... Labetalol is a dual alpha (α1) and beta (β1/β2) adrenergic receptor blocker and competes with other Catecholamines for binding ... Labetalol was the first drug created that combined both alpha- and beta- adrenergic receptor blocking properties. It was ...
"Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... Beta-3 adrenergic receptor has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... "Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes". ...
The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group ... This is because adrenergic stimulation by agonists, results in normal calcium channel regulation. If these adrenergic receptors ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... Alpha blocker Beta blocker Adrenergic Receptor Antagonist Sympathetic nervous system Propanolol Beta-blockers and the treatment ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... Alfa-2 (α2) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. ... Khan ZP, Ferguson CN, Jones RM (1999). "alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role". ...
Effects of the Beta-blocker Nebivolol (Bystolic) on Subjects With High Normal Blood Pressure and/or a Family History of...Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Adrenergic Antagonists. Antihypertensive Agents. Vasodilator Agents. Adrenergic beta-1 Receptor Agonists. ... Effects of the Novel Beta-adrenergic Antagonist Nebivolol (Bystolic) on Prehypertensive Subjects at Genetic Risk of ... or allergy to any beta blocker therapy or may have contraindications to beta blocker therapy such as asthma, bradycardia, etc. ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Beta-stiffness index was calculated as: Beta = ln(P1/P0)/((D1-D0)/D0), where D0 represents the minimal diameter recorded during ... Beta-stiffness Index [ Time Frame: 12 weeks ]. Longitudinal B-mode images of the left common carotid artery diameter (1-2 cm ... In contrast, there is limited evidence to suggest that nebivolol, a third generation beta-blocker that augments release of ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Physiological Effects of Drugs. ... Angiotensin Receptor Antagonists. Molecular Mechanisms of Pharmacological Action. Vasodilator Agents. Adrenergic beta-1 ... Τhe effectiveness of newer angiotensin-II receptor blockers and cardioselective beta-adrenergic blockers in treatment of ... We intend to study the effects of telmisartan, a newer angiotensin-II receptor blocker and nebivolol, a cardioselective beta- ...
Adrb1 - Beta-1 adrenergic receptor - Mus musculus (Mouse) - Adrb1 gene & proteinThis receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)- ... Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. ... Agonist or antagonistBy similarity. 1. ,p>The ,a href="http://www.geneontology.org/">Gene Ontology (GO),/a> project provides a ... alpha-2A adrenergic receptor binding Source: MGI. *beta1-adrenergic receptor activity Source: MGI ,p>Inferred from Direct Assay ...
Beta-1 adrenergic receptor - DrugBankagonist. Details. DB08347. 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile. experimental. unknown. ... Beta-1 adrenergic receptor. P08588. Details. Drug Relations. Drug Relations. DrugBank ID. Name. Drug group. Pharmacological ... Beta-1 adrenergic receptor. Details. Name. Beta-1 adrenergic receptor. Kind. protein. Organism. Human. Polypeptides. Name. ... agonist. Details. DB01407. Clenbuterol. approved, investigational, vet_approved. unknown. ...
Neuro-Drugs Flashcards by Michael Dennis | BrainscapeAlpha and Beta agonists 64 What type of receptor is used to transmit IGF-1 ... What type of receptor is used to transmit interleukin 2-10,15 ... Increased release and direct adrenergic receptor agonists 18 ...
B-Blocker Pharmacogenetics in Heart Failure - University of Florida Research Foundation, Inc.... affect tolerability to beta-blocker treatment or (2) influence responsiveness to beta-blocker treatment are disclosed. ... 2005) "Beta1-adrenergic receptor polymorphisms and left ventricular remodeling changes in response to beta-blocker therapy" ... in the third intracellular loop of the receptor and a substantial loss of agonist-mediated receptor function [Small et al. ( ... 2005) "Beta1-adrenergic receptor polymorphisms and left ventricular remodeling changes in response to beta-blocker therapy. ...
Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Formerly, it was also used to prolong the ... but has little affinity for beta receptors. The drug is largely obsolete, being superseded by other hemostatics such as ... It is the ketone form of epinephrine (adrenaline). Contrary to epinephrine, adrenalone mainly acts on alpha-1 adrenergic ... 1:8) and 94% ethanol (1:45). The melting point of the hydrochloride is 243 °C (469 °F). After local application, only traces of ...
Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( ...... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... expressing cells (2). For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor, ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... Screening for β2-adrenergic receptor agonists using the pH-sensitive dye,CypHer5, and the IN Cell Analyzer 3000. 6. A Mix-and- ...
US Patent # 7,098,196. Regulators of the hedgehog pathway, compositions and uses related thereto - Patents.com... beta.-adrenergic receptor agonists. .beta.-Adrenergic receptor agonists (sometimes referred to herein as ".beta.-adrenergic ... G.sub.i agonists, MDL 12330A, SQ 22536, GDPssS and clonidine, beta-blockers, and ligands of G-protein coupled receptors. ... beta.- and .gamma.-cyclodextrin, dimethyl-.beta. cyclodextrin and 2-hydroxypropyl-.beta.-cyclodextrin. Formulations of the ... Smo is related to the Frizzled family of Wnt receptors and more distantly to the secretin family of G protein-coupled receptors ...
Atropine is beta-adrenergic agonist at the beta-2 receptors, located primarily in lung tissue.. E. Atropine is beta-adrenergic ... Glucagon acts independent of beta-adrenergic receptors to increase activation of adenylatecyclase. ... A. Atropine is mu-receptor antagonist.. B. Atropine is an acetylcholine agonist.. C. Atropine blocks acetylcholine at the ... A, D. Management is mostly supportive; atropine is a nicotinic receptor antagonist and should be given to treat symptomatic ...
To determine whether NE can also elicit peripheral beta 1-adrenergic vasodilation, conscious dogs were studied a ... elicits alpha-adrenergic vasoconstriction and beta 1-adrenergic increases in heart rate and myocardial contractility. ... 0/Adrenergic beta-Agonists; 0/Ethanolamines; 0/Hexamethonium Compounds; 0/Receptors, Adrenergic, alpha; 0/Receptors, Adrenergic ... Receptors, Adrenergic, alpha / drug effects. Receptors, Adrenergic, beta / drug effects*, physiology. Vascular Resistance / ...
Jayakumar Rajadas | Stanford Medicine ProfilesIsoproterenol hydrochloride (ISO), a beta adrenergic agonist, is known to cause ischemic necrosis in rats. Cardiotoxicity of ... The p75 Neurotrophin Receptor Promotes Amyloid-beta(1-42)-Induced Neuritic Dystrophy In Vitro and In Vivo JOURNAL OF ... When A beta-bound red blood cells were injected, beta-amyloid is rapidly removed from these cells in vivo. Double-labeling ... Amyloid beta-protein (A beta) accumulation in brain is thought to be important in causing the neuropathology of Alzheimers ...
... beta-adrenergic receptor blocking agent without membrane stabilizing or intrinsic sympathomimetic (partial agonist) activities ... Beta-adrenergic blockade may mask certain clinical signs (eg, tachycardia) of hyperthyroidism. Abrupt withdrawal of beta ... There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenergic blocking drugs. The reported ... In addition, a variety of adverse effects not observed in clinical trials with atenolol but reported with other beta-adrenergic ...
In vitro experiments in cells expressing human beta adrenergic receptors demonstrate that xamoterol is highly selective for ... adrenergic receptor partial agonist. Moreover, an increased gene dosage of App, in the context of Down syndrome, was necessary ... We have identified Beta adrenergic system as one of key player in brain function in these disorders. Beta adrenergic modulation ... We have previously shown that acute administration of a partial agonist of the beta-1 adrenergic receptor (ADRB1), xamoterol, ...
... also known as Beta1-adrenergic receptor agonists, are a class of drugs that bind selectively to the beta-1 adrenergic receptor ... www.cvpharmacology.com/cardiostimulatory/beta-agonist.htm Sakuma T, Hida M, Nambu Y, et al. (February 2001). "Beta1-adrenergic ... Beta-adrenoceptors typically bind to norepinephrine release by sympathetic adrenergic nerves and to circulating epinephrine. ... September 1998). "Denopamine, a beta1-adrenergic agonist, prolongs survival in a murine model of congestive heart failure ...
Magiran | Iranian Journal of Fisheries Sciences، Volume:18 Issue:4, 2019... increased by all beta adrenergic agonists. The present study showed that various beta1 and beta2 adrenergic receptor agonists ... Effects of three beta adrenergic receptor agonists on growth performance, blood biochemical parameters, fatty acids composition ... The serum concentrations of phosphorus and albumin were also significantly increased by all beta adrenergic agonists and ... The fatty acids level of fish filet was significantly increased by the dietary supplement of various beta adrenergic agonists ( ...
DailyMed - ATENOLOL tablet
ATENOLOL- atenolol tablet... beta-adrenergic receptor blocking agent without membrane stabilizing or intrinsic sympathomimetic (partial agonist) activities ... Atenolol, like other beta-blockers, is a competitive inhibitor of beta-receptor agonists and its effects on the heart can be ... Beta-adrenergic blockade may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Abrupt withdrawal of beta ... There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenergic blocking drugs. The reported ...
... beta-adrenergic receptor blocking agent without membrane stabilizing or intrinsic sympathomimetic (partial agonist) activities ... Beta-adrenergic blockade may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Abrupt withdrawal of beta- ... Miscellaneous: There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenergic blocking drugs ... In addition, a variety of adverse effects have been reported with other beta-adrenergic blocking agents, and may be considered ...
Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. ... The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer- ... Receptors, Adrenergic, alpha-2 / agonists, antagonists & inhibitors, physiology*. Yohimbine / pharmacology. beta-Endorphin / ... 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/Neuropeptide Y; 0/Neurotransmitter Agents; 0/Receptors, ...
Unilateral Glaucoma Medication: Beta-adrenergic blockers, Alpha 2-adrenergic agonists, Carbonic anhydrase inhibitors,...Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral outflow. Used to treat open-angle ... Levobunolol 0.25% or 0.5% (AK Beta, Betagan). Nonselective beta-adrenergic blocking agent that lowers IOP by reducing aqueous ... Beta-adrenergic blockers. Class Summary. Decrease IOP by reducing aqueous production. Reduce elevated and normal IOP, with or ... Alpha 2-adrenergic agonists. Class Summary. Act to decrease aqueous humor formation. ...
... mutant with inverse agonist. Meleagris gallopavo (5a8e) Beta-2 adrenergic receptor, active state, complex with antibody. Homo ... Beta-2 adrenergic receptor, inactive state, dimer. 2rh1. Homo sapiens. Eukaryo. plasma. 2. 14. 31.8 ± 0.9. 0 ± 1. -143.2. ... Beta-2 adrenergic receptor, active state, complex with antibody. 3p0g. Homo sapiens. Eukaryo. plasma. 1. 7. 30.1 ± 1.4. 9 ± 1. ... Beta-2 adrenergic receptor, active state, complex with G-protein. 3sn6. Homo sapiens. Eukaryo. plasma. 1. 7. 31.0 ± 1.6. 8 ± 1 ...
Effect of fluorine substitution on the adrenergic properties of 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol. -...Adrenergic beta-Agonists. *Propanolamines. *Receptors, Adrenergic, beta. *2-fluoro-3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy ... adrenergic agonists and phenylethanolamine adrenergic agonists bind in similar fashion to the adrenergic receptor, and that if ... The 2- and 6-fluoro derivatives of the potent beta-adrenergic agonist 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol ... beta-adrenergic activity (simulation of cyclic AMP formation in C6 glioma cells), 2-F = parent much greater than 6-F; beta 1- ...
Beta(2)-adrenoceptor stimulation enhances latent transforming growth factor-beta-binding protein-1 and transforming growth...Receptors, Adrenergic, beta-2 / metabolism* * Transforming Growth Factor beta / analysis * Transforming Growth Factor beta / ... adrenoceptor agonist, caused an increase in TGF-beta1 expression in non-ischemic rats and further enhanced TGF-beta1 protein ... Beta(2)-adrenoceptor stimulation enhances latent transforming growth factor-beta-binding protein-1 and transforming growth ... In saline-treated rats latent TGF-beta-binding protein-1 (LTBP-1) immunoreactivity was moderately elevated 3 and 6 h after ...
Helping you find trustworthy answers on Alpha Adrenergic Antagonist , Latest evidence made easy ... Find all the evidence you need on Alpha Adrenergic Antagonist via the Trip Database. ... A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to ... Tartrate Antihypertensive Agents Adrenergic alpha-2 Receptor Agonists Adrenergic alpha-Agonists Adrenergic Agonists Adrenergic ...
AntagonistSelectiveAntagonistsStimulationNorepinephrineDobutaminePharmacologyIsoproterenolDopamineSubtypesAdrenoceptorCardiacMyocardialAdrb1BlockadeSympathomimeticGPCRsHuman beta 3 adrenePhosphorylationAdenylateMediatePartialOrganization of adrenergic receptor genesAdenylyl cyclasePotent beta-adrenergic agonistBeta2BlockersSympathetic nervouProtein-coupledInhibitIntracellularMechanismKinaseBlockerSkeletal muscleMyocardiumSubtypePhysiological effectsPhenylephrineIsoprenalineGeneCatecholaminesAlbuterolVentricularIncreasesNoradrenalineSignal transductionProteinsEndogenousBeta1MuscarinicGPCRStimulateAffinityAlphaAdipose tissueNeuronsMediatesAssaySpecificityVascularNicotinicDesensitizationInternalizationPharmacologicalAtenololGenes
- Effects of the Novel Beta-adrenergic Antagonist Nebivolol (Bystolic) on Prehypertensive Subjects at Genetic Risk of Hypertension: Implications for Inflammation, Endothelial Dysfunction, and Oxidative Stress. (clinicaltrials.gov)
- CypHer5 has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor expressing cells (2). (bio-medicine.org)
- This application note describes the validation of antagonist-format CypHer5E receptor internalization assays for high-throughput screening. (bio-medicine.org)
- A β2adrenergic receptor antagonist screen was performed using the LOPAC ™ compound library, which consists of 640 well-characterized, pharmaceutically diverse compounds with known drug or drug-like activity. (bio-medicine.org)
- The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 was able to identify all specific β2-adrenergic receptor antagonists and additional structurally related compounds present in the LOPAC compound library. (bio-medicine.org)
- Agonist and antagonist controls were placed symmetrically in columns 1 and 12 of each plate. (bio-medicine.org)
- Twelve replicate wells contained a known agonist, isoproterenol, and four replicate wells contai ned a known antagonist, alprenolol, each diluted in 0.01% DMSO. (bio-medicine.org)
- atropine is a nicotinic receptor antagonist and should be given to treat symptomatic bradycardia. (brainscape.com)
- Importance of Alpha - adrenergic Receptor Subtypes in Regulating of Airways Tonus at Patients with Bronchial Asthma In this work, effect of Tamsulosin hydrochloride as antagonist of alpha1A and alpha1B- adrenergic receptor and effect of Salbutamol as agonist of beta2- adrenergic receptor in patients with bronchial asthma and increased bronchial reactibility was studied.Parameters of the lung function are determined by Body plethysmography. (tripdatabase.com)
- Interestingly, β2- adrenergic receptor (β2-AR) antagonist ICI 118551 attenuated ischemia-induced BBB damage by regulating HIF-1α expression. (tripdatabase.com)
- This effect was blocked by co-injection of the alpha-2-receptor antagonist, yohimbine, demonstrating that the alpha-2-receptor is related to stimulation of feeding in layer-type chicks. (biomedsearch.com)
- Andringa G, Drukarch B, Leysen JE, Cools AR, Stoof JC (1999) The alleged dopamine D1 receptor agonist SKF 83959 is a dopamine D1 receptor antagonist in primate cells and interacts with other receptors. (springer.com)
- montelukast, a cysteinyl leukotriene (CysLT)-receptor antagonist, is an alternative. (dentalcare.com)
- low-dose inhaled corticosteroid plus montelukast, a cysteinyl leukotriene (CysLT)-receptor antagonist, is an alternative regimen. (dentalcare.com)
- Ardayfio PA et al (2008) The 5-hydroxytryptamine2A receptor antagonist R-(+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl-4-piperidinemethanol (M100907) attenuates impulsivity after both drug-induced disruption (dizocilpine) and enhancement (antidepressant drugs) of differential-reinforcement-of-low-rate 72-s behavior in the rat. (springer.com)
- The 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)
- All of these ISO-mediated myocyte responses in vitro were inhibited by a beta(1)-AR antagonist, betaxolol, but not by a beta(2)-AR antagonist, ICI 118551. (nih.gov)
- Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood-brain barrier, has not been investigated for this purpose. (frontiersin.org)
- Propranolol is a non-selective beta-adrenergic antagonist that has good penetration of the blood-brain barrier ( 21 ). (frontiersin.org)
- By using [3H]rauwolscine, a selective alpha 2-adrenergic receptor antagonist, we have identified for the first time alpha 2-adrenergic receptor sites in a mammalian pineal gland. (aspetjournals.org)
- Highly selective and potent β 1 -adrenoceptor antagonist (IC 50 = 0.7 nM). (tocris.com)
- 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)
- 3: The method of claim 1, wherein the agents comprise at least two of a Gi-coupled dopamine D2 receptor agonist, a Gs-coupled .beta.1 adrenergic receptor antagonist, or a Gq-coupled .alpha.1 adrenergic receptor blocker. (patents.com)
- Amlodipine/telmisartan, where telmisartan is how an angiotensin II receptor antagonist. (farmwars.info)
- The invention features polymeric hydrogel contact lenses containing an anti-glaucoma medication, such as a beta adrenergic receptor antagonist, e.g., timolol maleate, or an alpha adrenergic receptor agonist, e.g., brimonidine tartrate, and methods of fabrication and uses thereof. (google.co.uk)
- 1 . A drug delivery system comprising a polymeric hydrogel contact lens comprising a beta adrenergic receptor antagonist, or a pharmaceutically acceptable salt thereof, at a concentration of between about 0.25% and 0.000005% by weight absorbed in said contact lens, wherein said beta adrenergic receptor antagonist is capable of being delivered into ocular fluid. (google.co.uk)
- 5 . The drug delivery system of claim 1 , wherein said beta adrenergic receptor antagonist is capable of being transferred into said ocular fluid under ambient conditions. (google.co.uk)
- 8 . The drug delivery system of claim 1 , wherein said beta adrenergic receptor antagonist is selected from the group consisting of timolol, levobunalol, carteolol, metipranolol, betaxolol, or a pharmaceutically acceptable salt thereof, or combinations thereof. (google.co.uk)
- Phenylephrine (100microM), an alpha(1)-adrenoceptor agonist, also increased firing rate, which was inhibited by 100microM prazosin, an alpha1-adrenoceptor antagonist. (nih.gov)
- It combines the antihypertensive activity of two agents: a beta 1 -selective (cardioselective) hydrophilic blocking agent (atenolol, TENORMIN ® ) and a monosulfonamyl diuretic (chlorthalidone). (drugs.com)
- Atenolol is a beta 1 -selective (cardioselective) beta-adrenergic receptor blocking agent without membrane stabilizing or intrinsic sympathomimetic (partial agonist) activities. (drugs.com)
- Selective alpha 2-receptor that reduces aqueous humor formation and increases uveoscleral outflow. (medscape.com)
- A relatively selective alpha-adrenergic agonist that does not have significant local anesthetic activity. (medscape.com)
- Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral outflow. (medscape.com)
- Denopamine (beta1-selective adrenergic receptor agonist) and isoproterenol (non-selective beta-adrenergic receptor agonist) equally increase heart rate and myocardial oxygen consumption in dog heart. (nii.ac.jp)
- 2, 3, 9, 10 Persistent severe asthma (Step 5) is treated with high-dose inhaled corticosteroid plus inhaled long-acting selective beta 2 ‑adrenergic receptor agonist. (dentalcare.com)
- L-755,507 is also a very potent and selective β3-AR adrenergic receptor partial agonist, selective over both β1-AR and β2-AR adrenoceptor binding. (scbt.com)
- A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. (scbt.com)
- Benneyworth MA et al (2007) A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. (springer.com)
- In isolated nuclei, the non-selective βAR agonist isoproterenol (ISO) and the β3AR-selective ligand BRL37344, but not the β1AR-selective xamoterol, stimulated transcription initiation in a pertussis toxin (PTX)-sensitive manner. (umontreal.ca)
- 19 Recently, we found that modest augmentation of cardiac α1A signaling with a subpressor dose of an α1A-selective agonist can prevent doxorubicin-induced cardiomyopathy in mice. (pubmedcentralcanada.ca)
- Downregulation was selective for beta 1-receptors, and remaining receptors in the right and left ventricles showed low-affinity agonist binding, suggesting an uncoupling from Gs. (ahajournals.org)
- AUVI-Q contains epinephrine, a non-selective alpha and beta-adrenergic receptor agonist, indicated in the emergency treatment of allergic reactions (type 1) including anaphylaxis. (mdedge.com)
- Arformoterol is a selective beta 2 - adrenergic bronchodilator. (rxlist.com)
- Beta-blockers that are selective for the Beta-1 receptors. (clinicaladvisor.com)
- The three beta-blockers shown to benefit survival in heart failure are either beta-1 selective (metoprolol, bisoprolol) or block both beta and alpha receptors (carvedilol). (clinicaladvisor.com)
- Purpose: We investigated the presence of functional ß1, ß2 and ß3-adrenoceptor in urothelium and detrusor muscle of human bladder through in vitro pharmacology of selective ß3 adrenoceptor agonist solabegron. (bvsalud.org)
- Conclusions: Selective ß3-adrenoceptor agonist may be a potential new treatment for the overactive bladder OAB syndrome. (bvsalud.org)
- 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)
- Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β 1 , β 2 and β 3 receptors. (wikipedia.org)
- It is a selective beta-2 agonist, meaning it will stimulate your beta-2 adrenergic receptors. (ironmagazine.com)
- Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( Introduction. (bio-medicine.org)
- CypHer5E, consequently, can be used to screen for novel antagonists of known receptors and for potential ligands of non-G-protein coupled receptors (5) and orphan receptors. (bio-medicine.org)
- Competition studies carried out with various adrenergic antagonists supported the conclusion that [3H]rauwolscine binding sites were alpha 2-adrenergic receptors. (aspetjournals.org)
- We previously reported that Asn312 of the beta 2-adrenergic receptor and Asn385 in the homologous position in the 5-hydroxytryptamine1A receptor are important for binding to a class of beta-adrenergic receptor antagonists including propranolol and alprenolol. (aspetjournals.org)
- This structure, followed by other co-crystals of β 2 AR ( Hanson and others 2008b ) and β 1 AR ( Warne and others 2008 ) with the antagonists (-)-timolol (PDB code 3D4S) and (-)-cyanopindolol (PDB code 2VT4) respectively, represents a leap forward in the understanding of the inactive state of adrenergic GPCRs. (pubmedcentralcanada.ca)
- 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)
- What we found in our laboratory is that the longer growth factor 1 and insulin), to enhance fat and water loss (diuretics, thyroid hormones, beta-2-adrenergic receptor agonists and amphetamines), to counteract negative side-effects of AAS (aromatase inhibitors and estrogen receptor antagonists) and to reactivate endogenous testosterone production at the end of a cycle (gonadotropins). (afionline.org)
- Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors , of the sympathetic nervous system , which mediates the fight-or-flight response . (wikipedia.org)
- Upon agonist stimulation, a fluorescent signal is observed as the CypHer5E-antibody conjugate is internalized alongside the receptor into acidic endosomal vesicles. (bio-medicine.org)
- Stimulation of food intake caused by neuropeptide Y and beta-endorphin was attenuated by co-injection with yohimbine. (biomedsearch.com)
- The corresponding increased TGF-beta1 mRNA levels after ischemia were not further enhanced by clenbuterol, suggesting post-transcriptional regulation of TGF-beta1 protein after beta(2)-adrenoceptor stimulation. (nih.gov)
- Our data demonstrate a concomitant increase in LTBP-1 and TGF-beta1 expression in the ischemic hippocampus after stimulation of beta(2)-adrenoceptors. (nih.gov)
- Functionally active targeting domain of the beta-adrenergic receptor kinase: an inhibitor of G beta gamma-mediated stimulation of type II adenylyl cyclase. (duke.edu)
- Direct evidence that Gi-coupled receptor stimulation of mitogen-activated protein kinase is mediated by G beta gamma activation of p21ras. (duke.edu)
- Stimulation of Gi-coupled receptors leads to the activation of mitogen-activated protein kinases (MAP kinases). (duke.edu)
- The most well studied models whereby brown adipocytes appear in white fat are upon cold exposure or after stimulation of the beta(3)-adrenoceptor pathways. (frontiersin.org)
- A range of agonists or positive allosteric modulators (PAMs) for mostly G i/o -coupled receptors, including metabotropic glutamate 2 (mGlu 2 ), adenosine A 1 , or μ-opioid receptors, suppress these effects of 5-HT 2A receptor stimulation. (springer.com)
- a site in a sympathetic effector cell that reacts to adrenergic stimulation. (thefreedictionary.com)
- In general, stimulation of alpha receptors is excitatory of the function of the host organ or tissue, and stimulation of the beta receptors is inhibitory. (thefreedictionary.com)
- Stimulation of cultured cardiac myocytes in vitro with isoproterenol (ISO), an agonist for beta(1)- and beta(2)-ARs, caused hypertrophy of myocytes along with increases in transcription of atrial natriuretic factor (ANF) and actin reorganization. (nih.gov)
- Nous avons ensuite pu mettre en évidence par qPCR que la stimulation par l'ISO entrainait une augmentation du niveau d'ARNr 18S ainsi qu'une diminution de l'expression d'ARNm de NFκB. (umontreal.ca)
- Sucharov et al (2011) β-Adrenergic receptor stimulation and activation of protein kinase A protect against α1-adrenergic-mediated phosphorylation of protein kinase D and histone deacetylase 5. (tocris.com)
- Bbeta-adrenergic receptor kinase-1 levels in catecholamine-induced myocardial hypertrophy: regulation by beta- but not alpha1-adrenergic stimulation. (duke.edu)
- We have shown that healthy humans who are homozygous for the ADRB2 Arg16 variant react with lesser increment in plasma glucose levels to adrenaline infusion, suggesting a reduced EGP resulting from receptor stimulation in these persons (19). (deepdyve.com)
- Heart rate responsiveness to beta AR stimulation was blunted, with ED50, for isoproterenol increased 133% (p less than 0.001) after development of circulatory congestion. (ahajournals.org)
- Release of norepinephrine and dopamine-beta-hydroxylase by nerve stimulation. (aspetjournals.org)
- Effects of beta-adrenergic stimulation with dobutamine on isovolumic relaxation in the normal and failing human left ventricle. (semanticscholar.org)
- They therefore provide some beta adrenergic stimulation but prevent the full stimulation provided by the sympathetic nervous system and endogenous catecholamines. (clinicaladvisor.com)
- Sympathetic stimulation is necessary in supporting circulatory function in congestive heart failure, and beta blockade carries the potential hazard of further depressing myocardial contractility and precipitating more severe failure. (osel.info)
- This receptor binds epinephrine and norepinephrine with approximately equal affinity. (uniprot.org)
- Norepinephrine-induced beta 1-adrenergic peripheral vasodilation in conscious dogs. (biomedsearch.com)
- Norepinephrine (NE) elicits alpha-adrenergic vasoconstriction and beta 1-adrenergic increases in heart rate and myocardial contractility. (biomedsearch.com)
- Adrenergic receptors (ARs) are members of the 7-transmembrane domain G-protein-coupled receptor superfamily that bind the endogenous catecholamines epinephrine and norepinephrine. (acris-antibodies.com)
- Beta-adrenoceptors typically bind to norepinephrine release by sympathetic adrenergic nerves and to circulating epinephrine. (wikipedia.org)
- The norepinephrine provided by the LC acts at the medial septal area (MSA) and the medial preoptic area (MPOA) to activate waking-active neurons ( via alpha-1 adrenergic receptors) and inhibit sleep-active neurons ( via alpha-2 adrenergic receptors). (frontiersin.org)
- synthetic adrenergic agent derived from norepinephrine, having powerful bronchodilator and cardiac stimulant action. (fpnotebook.com)
- Myocardial β-ARs are studied extensively, and blocking β-ARs in heart failure (HF), when the AR agonist norepinephrine (NE) is elevated, is now a cornerstone of therapy. (pubmedcentralcanada.ca)
- Adrenergic Fibers: Nerve fibers that synthesize and release norepinephrine. (cram.com)
- Beta adrenergic receptors are found distributed throughout the body, in both muscle and fat, and are regulated through various natural hormones (triiodothyronine or T3, thyroxine or T4, testosterone, etc…) and catecholamines (such as norepinephrine and epinephrine). (ironmagazine.com)
- We have previously demonstrated the ability of dobutamine (DOB), primarily a beta1AR agonist, to inhibit reductions in cancellous bone formation and mitigate disuse-induced loss of bone mass. (iupui.edu)
- Dobutamine is a β 1 adrenergic receptor agonists that specifically acts on cardiac muscle increasing both rate and force of contraction. (egpat.com)
- Onset of action is within 1 to 2 minutes plasma half-life of Dobutamine - 2 minutes. (slideplayer.com)
- Pharmacology of combined alpha-beta-blockade. (biomedsearch.com)
- Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands. (guidetopharmacology.org)
- Large differences exist in the pharmacology of agents within the class, thus not all beta blockers are used for all indications listed below. (wikipedia.org)
- In standard animal or human pharmacological tests, beta-adrenoreceptor blocking activity of atenolol has been demonstrated by: (1) reduction in resting and exercise heart rates and cardiac output, (2) reduction of systolic and diastolic blood pressure at rest and on exercise, (3) inhibition of isoproterenol induced tachycardia and (4) reduction in reflex orthostatic tachycardia. (drugs.com)
- In normal subjects, the beta 1 -selectivity of atenolol has been shown by its reduced ability to reverse the beta 2 -mediated vasodilating effect of isoproterenol as compared to equivalent beta-blocking doses of propranolol. (drugs.com)
- In a placebo controlled comparison of approximately equipotent oral doses of several beta blockers, atenolol produced a significantly smaller decrease of FEV 1 than nonselective beta blockers, such as propranolol and unlike those agents did not inhibit bronchodilation in response to isoproterenol. (drugs.com)
- beta 1-Adrenergic blockade with atenolol reversed the vasodilation induced by NE completely, while at this time isoproterenol was still able to reduce peripheral resistance further, by 67 +/- 7%, indicating that beta 2-adrenergic receptors were not blocked. (biomedsearch.com)
- Isoproterenol exerts its effect on the beta-1 adrenergic receptors in the myocardium, thereby increasing heart rate and cardiac output. (fpnotebook.com)
- In addition, isoproterenol acts on beta-2 adrenergic receptors in bronchiolar and vascular smooth muscle, thereby causing smooth muscle relaxation. (fpnotebook.com)
- Co-application of the beta-adrenergic receptor agonist isoproterenol (10 mu M) largely increased S845 (but not S831) phosphorylation. (rug.nl)
- However, combined administration of corticosterone and 1 mu M isoproterenol - which by itself was ineffective - enhanced surface expression. (rug.nl)
- Finally, in hippocampal primary cultures, the inter-event interval of miniature excitatory postsynaptic currents (mEPSCs) was decreased by the combination of 1 mu M isoproterenol and corticosterone (which were ineffective by themselves) while the same combination did not affect the amplitude. (rug.nl)
- 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)
- In an in vitro functional bladder assay, Solabegron and other agonists for ß-adrenoceptors such as procaterol and isoproterenol evoked potent concentration-dependent relaxation of isolated human bladder strips with pD2 values of 8.73 ± 0.19, 5.08 ± 0.48 and 6.28 ± 0.54, respectively. (bvsalud.org)
- In agreement with previous reports, bath application of 100microM isoproterenol, a beta-adrenoceptor agonist, increased firing frequency in response to a long intracellular depolarizing current injection. (nih.gov)
- Bergson C, Mrzljak L, Smiley J, Pappy M, Levenson R, Goldman-Rakic P (1995) Regional, cellular, and subcellular variations in the distribution of D1 and D5 dopamine receptors in primate brain. (springer.com)
- Nine receptor subtypes have been identified thus far including three alpha-1 AR subtypes (1A/D, 1B, and 1C), three alpha-2 ARs (2A, 2B, and 2C), and three beta AR subtypes (1, 2, and 3). (acris-antibodies.com)
- There are three families of adrenergic receptors, alpha 1 , alpha 2 and beta, and each family contains three distinct subtypes. (thefreedictionary.com)
- Myocardial beta-adrenergic receptors (beta -ARs) consist of beta(1)- and beta(2)-subtypes, which mediate distinct signaling mechanisms. (nih.gov)
- As such, we sought to determine if the β-adrenergic receptor (βAR) subtypes and their associated signalling machinery are functionally localized to nuclear membranes. (umontreal.ca)
- The bovine pineal alpha 2-adrenergic receptor appears to represent a pharmacological subtype distinct from the three currently proposed subtypes, i.e., alpha 2A found in a human colonic adenocarcinoma cell line (HT29 cell), alpha 2B found in rat lung, and alpha 2C found in an opossum kidney cell line (OK cell). (aspetjournals.org)
- 1 KO of the two main myocardial α1-AR subtypes, the α1A and α1B, impairs normal post-natal cardiac growth, and causes severe dilated cardiomyopathy and death after pressure overload. (pubmedcentralcanada.ca)
- Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by photoaffinity labeling. (enacademic.com)
- ICI binds to the β 2 subtype with at least 100 times greater affinity than β 1 or β 3 , the two other known subtypes of the beta adrenoceptor. (wikipedia.org)
- In the present study, we demonstrated that intraperitoneal administration of clenbuterol, a lipophilic beta(2)-adrenoceptor agonist, caused an increase in TGF-beta1 expression in non-ischemic rats and further enhanced TGF-beta1 protein levels in rat CA1 pyramidal neurones after transient forebrain ischemia. (nih.gov)
- 1. Molecular biology and adrenoceptor subclassification. (tocris.com)
- beta-Arrestin-mediated PDE4 cAMP phosphodiesterase recruitment regulates beta-adrenoceptor switching from Gs to Gi. (duke.edu)
- Of the common adrenoceptor β-2 receptor gene (ADRB2) polymorphisms, the Arg16 allele is associated with receptor downregulation and reduced agonist-mediated endogenous glucose production. (deepdyve.com)
- A potential candidate gene to consider is the adrenoceptor β-2 receptor gene (ADRB2), in which several common variants are described (14). (deepdyve.com)
- adrenoceptor" 1 "β. (worldheritage.org)
- Although activation of beta-adrenoceptors increases firing frequency similarly to noradrenaline, it is still controversial whether alpha(1)-adrenoceptor activation influences repetitive firing. (nih.gov)
- In the present study, we examined the effects of adrenoceptor agonists on firing properties and the intracellular mechanism for alpha(1)-adrenoceptor-dependent modulation of firing in pyramidal neurons of rat cerebral cortex. (nih.gov)
- To determine whether NE can also elicit peripheral beta 1-adrenergic vasodilation, conscious dogs were studied after recovery from instrumentation for the measurement of cardiac output, arterial pressure, and left ventricular (LV) pressure and calculations of LV dP/dt and total peripheral resistance (TPR). (biomedsearch.com)
- NE, after pretreatment with hexamethonium and phentolamine, reduced mean arterial pressure 40 +/- 5% from 117 +/- 9 mmHg and TPR 60 +/- 5% from 0.058 +/- 0.007 mmHg X ml-1 X min and increased cardiac output 55 +/- 11% from 2,159 +/- 188 ml/min. (biomedsearch.com)
- Overexpression of the cardiac beta(2)-adrenergic receptor and expression of a beta-adrenergic receptor kinase-1 (betaARK1) inhibitor both increase myocardial contractility but have differential effects on susceptibility to ischemic injury. (duke.edu)
- Cardiac beta(2)-adrenergic receptor (beta(2)AR) overexpression is a potential contractile therapy for heart failure. (duke.edu)
- Restoration of beta-adrenergic signaling in failing cardiac ventricular myocytes via adenoviral-mediated gene transfer. (duke.edu)
- Transgenic mice were generated with cardiac-specific overexpression of the G protein-coupled receptor kinase-5 (GRK5), a serine/threonine kinase most abundantly expressed in the heart compared with other tissues. (duke.edu)
- Beta-adrenergic cardiac hypertrophy is mediated primarily by the beta(1)-subtype in the rat heart. (nih.gov)
- We examined which beta-AR subtype mediates cardiac hypertrophy. (nih.gov)
- A synthetic catechol compound and potent beta adrenergic agonist with peripheral vasodilator, bronchodilator, and cardiac stimulating properties. (fpnotebook.com)
- Catecholamines, cardiac beta-adrenergic receptors, and heart failure. (duke.edu)
- [1] It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue. (worldheritage.org)
- First it is not specific for β 1 receptors, second it increases cardiac work and oxygen consumption which are deleterious effects in heart failure. (egpat.com)
- It is a potent stimulator of the sympathetic nervous system ( adrenergic receptors ), and a powerful vasopressor , increasing blood pressure, stimulating the heart muscle, accelerating the heart rate, and increasing cardiac output. (thefreedictionary.com)
- α1-AR gain-of-function in cardiac transgenic models generally supports the KO results, although phenotypes vary greatly with receptor level, promoter, and absence or presence of an activating mutation. (pubmedcentralcanada.ca)
- title=The cardiac beta-adrenergic receptor. (enacademic.com)
- Although beta blockers were once contraindicated in congestive heart failure , as they have the potential to worsen the condition due to their effect of decreasing cardiac contractility, studies in the late 1990s showed their efficacy at reducing morbidity and mortality. (wikipedia.org)
- Atenolol is devoid of membrane stabilizing activity, and increasing the dose well beyond that producing beta blockade does not further depress myocardial contractility. (drugs.com)
- Expression of a beta-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice. (duke.edu)
- Myocardial beta-adrenergic receptor expression and signal transduction after chronic volume-overload hypertrophy and circulatory congestion. (ahajournals.org)
- Thus, changes in beta-adrenergic receptor (beta AR) expression should reflect more directly the influence of neurohumoral adrenergic tone, clarifying the manner in which peripheral (neurohumoral) versus primary myocardial factors are operative in decreased beta AR-dependent signal transduction. (ahajournals.org)
- Thus, a primary defect in intrinsic contractile function is not a necessary component for abnormalities of the myocardial beta AR-responsive adenylyl cyclase pathway. (ahajournals.org)
- Taken together, activation of the adrenergic nervous system early in the course of volume overload contributes to increased production of reactive inflammatory species (RIS) and that one mechanism underlying the salutary effects of ß-blockade may relate to attenuation of myocardial formation of RIS with subsequent beneficial effects on MMP activation and ECM and LV remodeling and function. (bioportfolio.com)
- Catecholamines increase myocardial inotropy and chronotropy by binding to beta-1-adrenergic receptors and increasing adenylate cyclase activity in myocytes. (renalandurologynews.com)
- Beta blockers ( beta-blockers , β-blockers , etc.) are a class of medications that are predominantly used to manage abnormal heart rhythms , and to protect the heart from a second heart attack ( myocardial infarction ) after a first heart attack (secondary prevention). (wikipedia.org)
- ADRB1 is an beta-adrenergic receptor. (acris-antibodies.com)
- WB Suggested Anti-ADRB1 Antibody Titration: 0.2-1 ug/ml. (acris-antibodies.com)
- Recommended dilution: 1/25-100 The image on the left is immunohistochemistry of paraffin-embedded Human tonsil tissues using ADRB1 antibody at dilution 1/25, on the right is immunohistochemistry of paraffin-embedded Human cervical cancer tissues using ADRB1 antibody at dilution 1/25. (acris-antibodies.com)
- The beta-1 adrenergic receptor (β 1 adrenoreceptor), also known as ADRB1 , is a beta-adrenergic receptor , and also denotes the human gene encoding it. (worldheritage.org)
- Auf www.antikoerper-online.de finden Sie aktuell 48 Adrenergic, beta-1-, Receptor (ADRB1) Antikörper von 16 unterschiedlichen Herstellern. (antikoerper-online.de)
- This assay has high sensitivity and excellent specificity for detection of Adrenergic Receptor Beta 1 (ADRb1). (mybiosource.com)
- No significant cross-reactivity or interference between Adrenergic Receptor Beta 1 (ADRb1) and analogues was observed. (mybiosource.com)
- 3 samples with low, middle and high level Adrenergic Receptor Beta 1 (ADRb1) were tested 20 times on one plate, respectively. (mybiosource.com)
- 3 samples with low, middle and high level Adrenergic Receptor Beta 1 (ADRb1) were tested on 3 different plates, 8 replicates in each plate. (mybiosource.com)
- MBS2019231 is a ready-to-use microwell, strip plate Double-antibody Sandwich ELISA (enzyme-linked immunosorbent assay) Kit for analyzing the presence of the Adrenergic Receptor Beta 1 (ADRb1) ELISA Kit target analytes in biological samples. (mybiosource.com)
- The microtiter plate provided in this kit has been pre-coated with an antibody specific to Adrenergic Receptor Beta 1 (ADRb1). (mybiosource.com)
- Standards or samples are then added to the appropriate microtiter plate wells with a biotin-conjugated antibody specific to Adrenergic Receptor Beta 1 (ADRb1). (mybiosource.com)
- After TMB substrate solution is added, only those wells that contain Adrenergic Receptor Beta 1 (ADRb1), biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. (mybiosource.com)
- 4. A method of treating an individual, comprising providing, on the basis of β 1 adrenergic receptor (β 1 AR) genotype, an appropriate degree of monitoring during initiation of beta-blockade, wherein individuals having a Gly49 carrier genotype or an Arg 389 homozygous genotype are monitored less closely and wherein patients having a Ser49 homozygous genotype or Gly389 carrier genotype are monitored more closely. (freepatentsonline.com)
- Consistent with its negative chronotropic effect due to beta blockade of the SA node, atenolol increases sinus cycle length and sinus node recovery time. (drugs.com)
- Thus, in the presence of alpha-adrenergic receptor blockade, either administration of NE or release of endogenous NE elicits potent peripheral vasodilation, which appears to involve a beta 1-adrenergic receptor mechanism. (biomedsearch.com)
- Observational Study in Patients Suffering From Benign Prostatic Hyperplasia Treated With Alpha - adrenergic Blockade Observational Study in Patients Suffering From Benign Prostatic Hyperplasia Treated With Alpha - adrenergic Blockade - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. (tripdatabase.com)
- Cheng et al (2012) Cytoskeletal role in protection of the failing heart by β-adrenergic blockade. (tocris.com)
- Reduced heart rate resulting from beta blockade may increase diastolic filling times, which can lower diastolic filling pressure and alleviate pulmonary congestion. (clinicaladvisor.com)
- The sustained delivery of beta blockade may account for the superior benefit of extended release metoprolol. (clinicaladvisor.com)
- 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)
- Beta-adrenergic blocker that has little or no intrinsic sympathomimetic effects and membrane-stabilizing activity. (medscape.com)
- Blocks beta 1- and beta 2-receptors and has mild intrinsic sympathomimetic effects. (medscape.com)
- alpha-adrenergic, which act in response to sympathomimetic stimuli, and beta-adrenergic, which block sympathomimetic activity. (thefreedictionary.com)
- Beta-blockers that also have "intrinsic sympathomimetic" action, meaning that they have weak beta agonist action as well as beta blocking effects. (clinicaladvisor.com)
- Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs) (4). (bio-medicine.org)
- The G protein-coupled receptor (GPCR) kinases (GRKs) phosphorylate and desensitize agonist-occupied GPCRs. (duke.edu)
- These effects on 5-HT 2A receptors and related GPCRs appear to play a major role in the behavioral effects of serotonergic hallucinogens, such as head twitches in rodents and higher order behaviors such as rodent lever pressing on the differential-reinforcement-of-low rate 72-s (DRL 72-s) schedule. (springer.com)
- Recently several G protein-coupled receptors (GPCRs) have been shown to localize to intracellular membranes, in particular the nuclear membrane. (umontreal.ca)
- Serving as an adaptor or scaffold molecule, beta Arrestin 1 is essential for mitogenic signaling and mediates agonist-dependent desensitization and internalization of Gprotein-coupled receptors (GPCRs, e.g., beta 2-adrenergic receptor). (thermofisher.com)
- After binding to their ligand and interacting with heterotrimeric G proteins, GPCRs are phosphorylated by G-protein receptor kinases (GRKs) on serine residues. (thermofisher.com)
- Class A G protein-coupled receptor (GPCRs) transduce extracellular signals across the cell membrane by activating cytoplasmic-bound heterotrimeric GTP binding proteins (G proteins), which, in turn, modulate the activity of downstream effector proteins. (psi.ch)
- Despite the physiological and pharmacological relevance of GPCRs, the structural basis of ligand efficacy and receptor activation, and how these elements translate into cytoplasmic trafficking and cellular response still remain elusive. (psi.ch)
- Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. (scbt.com)
- GRK2-mediated receptor phosphorylation is preceded by the agonist-dependent membrane association of this enzyme. (duke.edu)
- Since both noradrenaline and corticosterone are known to quickly affect properties of AMPA-type glutamate receptors (AMPAR), we here examined - in hippocampal neurons - three parameters which give insight in the functionality of AMPARs: phosphorylation, surface expression and spontaneous synaptic transmission. (rug.nl)
- We conclude that AMPAR phosphorylation, surface expression and mEPSC inter-event interval respond most strongly to a combination of corticosterone and beta-adrenergic receptors. (rug.nl)
- Phosphorylation of GTP-binding-regulatory (G)-protein-coupled receptors by specific G-protein-coupled receptor kinases (GRKs) is a major mechanism responsible for agonist-mediated desensitization of signal transduction processes. (duke.edu)
- Agonist-promoted desensitization of adenylate cyclase is intimately associated with phosphorylation of the beta-adrenergic receptor in mammalian, avian, and amphibian cells. (duke.edu)
- PKA-cat phosphorylation of Beta-2 adrenergic receptor leads to its activation switch from G-protein alpha-i family to G-protein alpha-s . (bio-rad.com)
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. (uniprot.org)
- Beta receptors are divided into beta1, beta2, beta3, which are linked to Gs, and adenylate cyclase, increasing cAMP, which in turn drives cAMP-dependent protein kinase that mediates intracellular events. (thefreedictionary.com)
- Beta-agonist- and prostaglandin E1-induced translocation of the beta-adrenergic receptor kinase: evidence that the kinase may act on multiple adenylate cyclase-coupled receptors. (duke.edu)
- 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)
- Beta-adrenergic receptor number and adenylate cyclase function in denervated transplanted and cardiomyopathic human hearts. (semanticscholar.org)
- For example, Beta-2 adrenergic receptor activate GNAS complex locus ( G-protein alpha-s )/ Adenylate cyclases, which leads to Adenosine 3',5'-cyclic phosphate ( cAMP ) production. (bio-rad.com)
- It is therefore likely that brain adrenergic alpha-2-receptors mediate the orexigenic effects of neuropeptide Y and beta-endorphin in layer-type chicks. (biomedsearch.com)
- Jane-Wit et al (2007) β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis. (tocris.com)
- The patient experiences partial relief from frequent inhaled short-acting beta 2 ‑adrenergic receptor agonist and should be referred to an emergency room. (dentalcare.com)
- Tilting of TM-Ve towards the receptor axis provides a more complete description of polar receptor/ligand interactions for full and partial agonists, by enabling optimal engagement of agonists with two experimentally identified anchor sites, formed by Asp113/Asn312 and Ser203/Ser204/Ser207 side chains. (pubmedcentralcanada.ca)
- 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)
- Effects of cholinergic and anticholinergic drugs and a partial cholinergic agonist on the development and expression of physical dependence on morphine in rat. (aspetjournals.org)
- Data are presented that indicate that Iso represents a novel type of alpha1A -AR partial agonist with signaling bias toward MAPK/ERK (zeige MAPK1 ELISA Kits ) signaling cascade that is likely independent of coupling to Galphaq (zeige GNAQ ELISA Kits ). (antikoerper-online.de)
- The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor. (psi.ch)
- Chromosomal organization of adrenergic receptor genes. (duke.edu)
- Beta receptors are coupled to Gs proteins, which in turn are linked to adenylyl cyclase. (acris-antibodies.com)
- The beta-adrenergic receptor kinase (beta ARK) phosphorylates the agonist-occupied beta-adrenergic receptor to promote rapid receptor uncoupling from Gs, thereby attenuating adenylyl cyclase activity. (duke.edu)
- METHODS AND RESULTS We examined the beta-adrenergic receptor-responsive adenylyl cyclase pathway in hearts from pigs subjected to volume-overload hypertrophy with circulatory congestion. (ahajournals.org)
- Biochemical analyses of the beta AR-responsive adenylyl cyclase pathway showed uniform decreases in beta AR number in right atrium, right ventricle, and left ventricle (36-41% decreases, p less than 0.005). (ahajournals.org)
- The 2- and 6-fluoro derivatives of the potent beta-adrenergic agonist 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol were prepared and their adrenergic properties examined. (nih.gov)
- The present study showed that various beta1 and beta2 adrenergic receptor agonists had same physiological effects on rainbow trout but it seems ractopamine, as a beta1 adrenergic receptor, had more potential on fatty acid metabolism and growth response of rainbow trout. (magiran.com)
- However, the results of several studies suggest that beta-blockers may actually increase arterial stiffness. (clinicaltrials.gov)
- Τhe effectiveness of newer angiotensin-II receptor blockers and cardioselective beta-adrenergic blockers in treatment of arterial hypertension and in improvement of arterial stiffness has been established in previous studies among the hypertensive population. (clinicaltrials.gov)
- Medications used to decrease aqueous production include beta-blockers (topical), carbonic anhydrase inhibitors (topical and/or oral), and alpha 2-agonists. (medscape.com)
- Beta-blocking agents have been less well studied for ICU delirium, although beta-blockers are known to have beneficial effects on anxiety, posttraumatic Stress Disorder (PTSD) and aggressive behavior in a variety of populations ( 16 - 20 ). (frontiersin.org)
- According to previous reports, treatment with nonspecific β-blockers with effect on the β2-receptor is associated with reduced EGP to epinephrine infusion (11) and impaired recovery from hypoglycemia (12, 13). (deepdyve.com)
- Drugs blocking beta adrenergic receptors (beta-blockers) have become central to the management of cardiovascular diseases. (clinicaladvisor.com)
- This chapter focuses on the use of beta-blockers in patients with left ventricular systolic dysfunction. (clinicaladvisor.com)
- Selected beta-blockers are indicated for the chronic management of patients with congestive heart failure symptoms and reduced ventricular systolic function due to ischemic heart disease, nonischemic cardiomyopathy, and regurgitant valvular lesions. (clinicaladvisor.com)
- The negative effect of beta-blockers on ventricular contractility may alleviate outflow obstruction and may improve diastolic performance (see below). (clinicaladvisor.com)
- Nonselective beta-blockers that block both beta-1 and beta-2 adrenergic receptors. (clinicaladvisor.com)
- Pindolol is representative of this class of beta-blockers. (clinicaladvisor.com)
- Although many beta-blockers are available and supported by different drug formularies, it is not certain that the benefit of beta-blockers in heart failure is a "class effect" that extends to all agents. (clinicaladvisor.com)
- Even if the benefits of beta-blockers are a class effect, the appropriate dosing of a given beta-blocker to ensure improved symptoms and survival must be demonstrated in large clinical trials. (clinicaladvisor.com)
- Although the demonstration of efficacy of Tenormin is based entirely on data from the first seven postinfarction days, data from other beta blocker trials suggest that treatment with beta blockers that are effective in the postinfarction setting may be continued for one to three years if there are no contraindications. (osel.info)
- Beta blockers interfere with the binding to the receptor of epinephrine and other stress hormones, and weaken the effects of stress hormones. (wikipedia.org)
- For the treatment of primary hypertension, meta-analyses of studies which mostly used atenolol have shown that although beta blockers are more effective than placebo in preventing stroke and total cardiovascular events, they are not as effective as diuretics , medications inhibiting the renin-angiotensin system (e.g. (wikipedia.org)
- in cases of acute decompensated heart failure, beta blockers will cause a further decrease in ejection fraction, worsening the patient's current symptoms. (wikipedia.org)
- Beta blockers are known primarily for their reductive effect on heart rate, although this is not the only mechanism of action of importance in congestive heart failure. (wikipedia.org)
- The Theory is Out There: The Use of ALPHA-2 Agonists in Treatment of Septic Shock Ferreira, Jason 2018-04-01 00:00:00 ABSTRACTThe sympathetic nervous system plays an important role in the initial response to sepsis. (deepdyve.com)
- Beta receptors are found on cells of the heart muscles, smooth muscles , airways , arteries , kidneys , and other tissues that are part of the sympathetic nervous system and lead to stress responses, especially when they are stimulated by epinephrine (adrenaline). (wikipedia.org)
- Monoclonal antibodies reveal receptor specificity among G-protein-coupled receptor kinases. (duke.edu)
- The G-protein-coupled receptor kinases beta ARK1 and beta ARK2 are widely distributed at synapses in rat brain. (duke.edu)
- Receptor and G betagamma isoform-specific interactions with G protein-coupled receptor kinases. (duke.edu)
- Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice. (duke.edu)
- Trace amines: identification of a family of mammalian G protein-coupled receptors. (guidetopharmacology.org)
- An approach to the study of G-protein-coupled receptor kinases: an in vitro-purified membrane assay reveals differential receptor specificity and regulation by G beta gamma subunits. (duke.edu)
- A method of treating an ocular disorder in a subject includes administering to the subject subtherapeutic amounts of two or more agents that inhibit and/or blocks the activation of Gs- or Gq-protein coupled receptors or Gs- or Gq-signaling cascade in ocular cells of the subject, and/or activates Gi-protein coupled receptors, which is induced or triggered by light induced all-trans-retinal generation. (patents.com)
- The synthesis of melatonin in mammalian pineal glands is stimulated by beta 1-adrenergic receptor agonists and is potentiated by alpha 1-adrenergic receptor agonists, whereas in the avian pineal gland alpha 2-adrenergic receptor agonists inhibit its synthesis. (aspetjournals.org)
- Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. (acris-antibodies.com)
- In addition, we plan to compare the profile of activated signaling molecules with their dynamic intracellular localization pattern to learn how receptor activation translates into specific pathways of cellular signaling. (psi.ch)
- Beique J-C et al (2007) Mechanism of the 5-hydroxytryptamine 2A receptor-mediated facilitation of synaptic activity in prefrontal cortex. (springer.com)
- These results suggest that beta -AR stimulated hypertrophy is mediated by the beta(1)-subtype and by a pertussis toxin-insensitive mechanism. (nih.gov)
- Insights into agonist binding and the corresponding conformational changes triggering GPCR activation mechanism are of special interest. (pubmedcentralcanada.ca)
- Beta Arrestin 1 in the cytosol is phosphorylated by ERK1 and 2 on serine412 in a negative feedback mechanism and binds to the phosphorylated receptors at the plasma membrane. (thermofisher.com)
- The beta-adrenergic receptor kinase (beta ARK) phosphorylates its membrane-associated receptor substrates, such as the beta-adrenergic receptor, triggering events leading to receptor desensitization. (duke.edu)
- A beta-adrenergic receptor kinase-like enzyme is involved in olfactory signal termination. (duke.edu)
- Beta-adrenergic receptor kinase: identification of a novel protein kinase that phosphorylates the agonist-occupied form of the receptor. (duke.edu)
- beta-Adrenergic receptor kinase (beta-AR kinase) is a cytosolic enzyme that phosphorylates the beta-adrenergic receptor only when it is occupied by an agonist [Benovic, J. Strasser, R. H., Caron, M. G. & Lefkowitz, R. J. (duke.edu)
- PKA-cat activates RAP1A member of RAS oncogene family ( RAP-1A )/ v-raf murine sarcoma viral oncogene homolog B1 ( B-Raf )/ Mitogen-activated protein kinase kinase 2 and 1 ( MEK2(MAP2K2) and MEK1(MAP2K1) )/ Erk [ 6 ]. (bio-rad.com)
- G-protein alpha-i family activation releases complex of G-protein beta/gamma , which activates c-src tyrosine kinase ( c-Src ) [ 12 ]. (bio-rad.com)
- The investigators plan to investigate whether these subjects have the same markers (such as microscopic protein in the urine or C-reactive protein in the blood) in the blood and urine that people with high blood pressure have, and whether they are improved before and after taking the beta-blocker nebivolol. (clinicaltrials.gov)
- Subjects may not have previous intolerance, hypersensitivity, or allergy to any beta blocker therapy or may have contraindications to beta blocker therapy such as asthma, bradycardia, etc. (clinicaltrials.gov)
- In contrast, there is limited evidence to suggest that nebivolol, a third generation beta-blocker that augments release of vascular nitric oxide, reduces central arterial stiffness in hypertensive individuals. (clinicaltrials.gov)
- We intend to study the effects of telmisartan, a newer angiotensin-II receptor blocker and nebivolol, a cardioselective beta-adrenergic blocker on the 24-h ambulatory blood pressure values of subjects with stage I arterial hypertension in a total time period of 12 months. (clinicaltrials.gov)
- Polymorphisms in the beta-1 adrenergic receptor that (1) affect tolerability to beta-blocker treatment or (2) influence responsiveness to beta-blocker treatment are disclosed. (freepatentsonline.com)
- and c) administering a β-blocker medication to said individual if the genotype of the β 1 AR gene of said at least one individual is Arg389Arg and the genotype of the ADRA2C gene is DEL. (freepatentsonline.com)
- The purpose of this study tests whether a beta-blocker drug will benefit patients with chronic mitral regurgitation. (bioportfolio.com)
- Not only the class but the formulation of the beta-blocker is of clinical significance. (clinicaladvisor.com)
- Tremor is a repeated contraction skeletal muscle which is increased by β2 agonists as hey increase blood flow thereby enhance twitch response of skeletal muscle. (egpat.com)
- β 2 -adrenergic receptors are located mainly in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle, and skeletal muscle. (wikipedia.org)
- The myocardium contains adrenergic receptors (ARs) of two main classes, β and α1. (pubmedcentralcanada.ca)
- This study examined the characteristics and distribution of sarcolemmal and light vesicular beta-adrenergic receptors (BAR) in left ventricular myocardium from 15 adults (aged 17 to 58 years) without left ventricular dysfunction or coronary artery disease and 29 patients (aged 14 to 53 years) with end-stage congestive heart failure (CHF). (semanticscholar.org)
- Dexmedetomidine is a potent alpha-2 adrenergic agonist that binds to the alpha-2 adrenergic receptor subtype A at the LC, resulting in almost complete inhibition of the LC, which has a sedative effect ( 5 , 6 ). (frontiersin.org)
- We suggest that the bovine pineal receptor may represent a fourth pharmacological subtype, which would be designated as alpha 2D. (aspetjournals.org)
- Further, receptor models incorporating a flexible TM-V backbone allow reliable prediction of binding affinities for a set of diverse ligands, suggesting potential utility of this approach to design of effective and subtype-specific agonists for adrenergic receptors. (pubmedcentralcanada.ca)
- In the mouse bleomycin model of right ventricular failure, the alpha1A -adrenergic receptor subtype agonist A61603 prevents right ventricular failure. (antikoerper-online.de)
- Different beta 1 and 2 adrenergic receptors agonists might have various biological and physiological effects on fish species. (magiran.com)
- A phenylephrine-related beta-1 adrenergic and alpha adrenergic agonist used as a cardiotonic and antihypotensive agent. (nih.gov)
- Isoprenaline has higher affinity for β 1 than adrenaline , which, in turn, binds with higher affinity than noradrenaline at physiologic concentrations. (worldheritage.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)
- Isoprenaline has higher affinity for β 1 than noradrenaline , which, in turn, binds with higher affinity than adrenaline . (enacademic.com)
- cAMP stimulates transcription of the beta 2-adrenergic receptor gene in response to short-term agonist exposure. (duke.edu)
- cDNA for the human beta 2-adrenergic receptor: a protein with multiple membrane-spanning domains and encoded by a gene whose chromosomal location is shared with that of the receptor for platelet-derived growth factor. (duke.edu)
- A mutation of rs2322333, located in the intronic and 3' UTR (zeige UTS2R ELISA Kits ) part of the gene ADRA1A in chromosome 8, has a probability of being deleterious the abolition of ELAV-like protein 1 (ELAVL1 (zeige ELAVL1 ELISA Kits )) binding site rs2695260. (antikoerper-online.de)
- and (ii) at least one nitric oxide enhancing compound, wherein the patient has at least one polymolphism in a beta 1 adrenergic receptor gene. (patentsencyclopedia.com)
- 2. The method of claim 1, wherein the at least one polymorphism in the beta 1 adrenergic receptor gene is an Arg389Arg polymorphism and/or a Gly389Gly polymorphism in the beta 1 adrenergic receptor gene. (patentsencyclopedia.com)
- 3. The method of claim 1, wherein the patient has at least one polymorphism in the endothelial nitric oxide synthase (NOS3) gene and/or at least one polymorphism in an aldosterone synthase promoter gene. (patentsencyclopedia.com)
- 1) Alpha receptors, which evoke an excitatory response of smooth muscle cells to catecholamines. (thefreedictionary.com)
- 2) Beta receptors, which dampen the response to catecholamines. (thefreedictionary.com)
- They are in effect weak agonists that stimulate the beta receptors to a lesser degree than endogenous catecholamines. (clinicaladvisor.com)
- 9, 10 In patients with intermittent asthma an inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol is preferred (Step 1). (dentalcare.com)
- The patient experiences prompt relief with inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol. (dentalcare.com)
- Distribution and function of human ventricular beta adrenergic receptors in congestive heart failure. (semanticscholar.org)
- Nonselective beta-adrenergic blocking agent that lowers IOP by reducing aqueous humor production and possibly increases outflow of aqueous humor. (medscape.com)
- Altogether, these data indicate that beta1AR agonist treatment during disuse mitigates negative changes in cancellous bone microarchitecture and inhibits increases in osteocyte apoptosis. (iupui.edu)
- We have shown that beta-2 adrenergic receptor (β2AR) engagement on CD40L/IL-4-primed B cells increases the level of IgE produced per cell, without affecting class switch recombination. (jimmunol.org)
- Beta-2 adrenergic receptor activation also appears to be important in the MSA and MPOA, resulting in dose-dependent increases in time spent awake ( 4 ). (frontiersin.org)
- As the chain length of alkyl group in amine increases, the duration of action of β 2 agonists increases. (egpat.com)
- Behavioural effects critically depend on noradrenaline acting via beta-adrenergic receptors, but these effects are strongly modulated by corticosterone, indicating putative interactions between the two hormones. (rug.nl)
- Backbone NMR reveals allosteric signal transduction networks in the beta 1-adrenergic receptor. (psi.ch)
- Beta Arrestin 1 is a member of a family of proteins widely expressed but especially abundant in the central nervous system. (thermofisher.com)
- An early blunting of the glucagon response is accompanied by disappearing endogenous insulin production (1, 2), rendering patients increasingly dependent upon epinephrine as their first-line protection against development of severe hypoglycemia. (deepdyve.com)
- However, in many patients, as a result of recurrent hypoglycemia and/or long duration of diabetes, the epinephrine response to hypoglycemia also becomes blunted (i.e., hypoglycemia-associated autonomic failure) (1), leading to reduced endogenous glucose production (EGP) during hypoglycemia and impaired recognition of warning symptoms (i.e., impaired hypoglycemia awareness). (deepdyve.com)
- In parallel with the up-regulation of TGF-beta1 immunoreactivity, LTBP-1 levels in the hippocampus were considerably increased by clenbuterol from 3 h to 2 days after ischemia. (nih.gov)
- Beta1-adrenergic agonists, also known as Beta1-adrenergic receptor agonists, are a class of drugs that bind selectively to the beta-1 adrenergic receptor. (wikipedia.org)
- knocking out of the beta1/2 (zeige TFAP2B Antikörper ) receptor significantly diminished the ST25 acupuncture-induced inhibition of gastric motility and jejunal motility without significantly altering the enhancement of colonic motility induced by acupuncture at ST25. (antikoerper-online.de)
- alpha1A -adrenergic receptors are stably expressed and stimulate cell migration and TGF-beta1 (zeige TGFB1 ELISA Kits ), IGF-1 (zeige IGF1 ELISA Kits ), hyaluronan and PIP (zeige PIP ELISA Kits ) production in human skin fibroblasts. (antikoerper-online.de)
- Muscarinic receptors. (cueflash.com)
- 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)
- Beta-1 adrenergic receptor may also stimulate Rap guanine nucleotide exchange factor (GEF) 2 ( PDZ-GEF1 ) directly and/or via cAMP. (bio-rad.com)
- Contrary to epinephrine, adrenalone mainly acts on alpha-1 adrenergic receptors, but has little affinity for beta receptors. (wikipedia.org)
- beta 2-activity (relaxation of guinea pig tracheal strip), 2-F greater than parent much greater than 6-F. The affinity of the 2-fluoro analogue for beta 1-adrenergic receptors (inhibition of the specific binding of [3H]dihydroalprenolol, rat cerebral cortical membranes) was 2 times greater, while the 6-fluoro analogue was 1450 times less than the parent. (nih.gov)
- 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)
- We were surprised to find that two of these substitutions led to an increase in affinity for alpha-adrenergic ligands. (aspetjournals.org)
- Substitution with glutamine and threonine at position 312 led to a 11-15-fold increase in affinity for yohimbine and enabled p-aminoclonidine to act as an agonist. (aspetjournals.org)
- The 2.4 Å crystal structure of the β 2 -adrenergic receptor (β 2 AR) in complex with the high-affinity inverse agonist (-)-carazolol provides a detailed structural framework for the analysis of ligand recognition by adrenergic receptors. (pubmedcentralcanada.ca)
- The melting point of the hydrochloride is 243 °C (469 °F). After local application, only traces of adrenalone are found in the blood, which is partly a consequence of the vasoconstriction caused by the drug via alpha-1 adrenergic receptors. (wikipedia.org)
- Role of adrenergic alpha-2-receptors on feeding behavior in layer-type chicks. (biomedsearch.com)
- The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer-type chicks. (biomedsearch.com)
- Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. (biomedsearch.com)
- 4.2 Is there a role for alpha-adrenergic receptors in Mg 2+ extrusion? (bioscience.org)
- Alpha receptors are divided into alpha1 (Gq) and alpha2 (Gi) coupled receptors. (thefreedictionary.com)
- Alpha receptor effects Vasoconstriction, reduced GI tract motility. (thefreedictionary.com)
- Recent studies have examined the effectiveness of alpha-2 adrenergic agonists for controlling delirium and agitation. (frontiersin.org)
- Many investigators have used dexmedetomidine and clonidine (another alpha-2 agonist) to control agitation and delirium ( 7 - 15 ). (frontiersin.org)
- Identification and characterization of alpha 2D-adrenergic receptors in bovine pineal gland. (aspetjournals.org)
- However, the pharmacologic profile of the pineal alpha 2 receptor resembles that found in the rat submaxillary gland. (aspetjournals.org)
- The alpha 6 beta 1 integrin is expressed on the macrophage surface in an inactive state and requires cellular activation with PMA or cytokines to function as a laminin receptor (Shaw, L. M., J. M. Messier, and A. M. Mercurio. (semanticscholar.org)
- Analysis of the role of the alpha 6A beta 1 and alpha 6B beta 1 integrin variants in laminin adhesion by cDNA expression in an alpha 6 integrin-deficient macrophage cell line. (semanticscholar.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)
- 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)
- Alpha-1-adrenergic receptors (α1-ARs) play adaptive roles in the heart and protect against the development of heart failure (HF). (pubmedcentralcanada.ca)
- Alpha and beta adrenergic agonist. (cueflash.com)
- Agents that block both beta adrenergic receptors and alpha adrenergic receptors (prototypes include labetalol, carvedilol). (clinicaladvisor.com)
- While conventional understanding of alpha 2 agonists activity is depletion of sympathetic outflow, novel evidence suggests mitigation rather than depletion. (deepdyve.com)
- The hypothesis by which alpha agonists affect the pathology of sepsis is multifactorial, but includes influence on inflammatory regulation, coagulopathy, dynamic flow, as well as vascular responsiveness and integrity. (deepdyve.com)
- 9 . The drug delivery system of claim 1 , further comprising an alpha adrenergic receptor agonist. (google.co.uk)
- 17 . The drug delivery system of claim 10 , wherein said alpha adrenergic receptor agonist is selected from the group consisting of brimonidine, apraclonidine, or a pharmaceutically acceptable salt thereof, or combinations thereof. (google.co.uk)
- Zusätzlich bieten wir Ihnen alpha 1 Adrenergic Receptor Antikörper (92) und alpha 1 Adrenergic Receptor Proteine (7) und viele weitere Produktgruppen zu diesem Protein an. (antikoerper-online.de)
- Insgesamt sind aktuell 149 alpha 1 Adrenergic Receptor Produkte verfügbar. (antikoerper-online.de)
- Patients with type-1 diabetes also undergo dysregulation of adipose tissue metabolism (lipolysis and lipogenesis) due to insulin deficiency. (hindawi.com)
- Double immunostaining showed that HIF-1α was upregulated in ischemic neurons but not in astrocytes andendothelial cells. (tripdatabase.com)
- Evidence implicates a number of brain regions in mediating these effects of serotonergic hallucinogens and G q/11 -coupled receptors including the midline and intralaminar thalamic nuclei, claustrum, and neurons in deep PFC. (springer.com)
- Vasoconstriction of the isolated rabbit ear artery caused by nicotinic agonists acting on adrenergic neurons. (aspetjournals.org)
- Desensitization of the adrenergic neurons of the isolated rabbit ear artery to nicotinic agonists. (aspetjournals.org)
- β2- Adrenergic Receptor-Mediated HIF-1α Upregulation Mediates Blood Brain Barrier Damage in Acute Cerebral Ischemia Disruption of the blood brain barrier (BBB) within the thrombolytic time window is an antecedent event to intracerebral hemorrhage in ischemic stroke. (tripdatabase.com)
- In this assay system, a CypHer5E-conjugated anti-VSV-G epitope antibody is incubated with a clonal stable HEK 293 cell line expressing N-terminally epitope tagged β2-adrenergic receptor. (bio-medicine.org)
- DMSO at ≤1% was demonstrated to have no detectable adverse effect on the cells or the assay (data not shown). (bio-medicine.org)
- 9. Add 20 µl assay medium containing agonist to a final assay concentration of 100 nM and incubate at 37 ºC for 30 min. (bio-medicine.org)
- Amino acid substitutions at position 312 in the seventh hydrophobic segment of the beta 2-adrenergic receptor modify ligand-binding specificity. (aspetjournals.org)
- Ganglionic transmission is mediated by nicotinic receptors. (cram.com)
- Of these, the single nucleotide polymorphism (SNP) Gly vs Arg at codon 16 (rs1042713) affects β2-receptor desensitization during β2-agonist treatment of asthma in a clinically important manner (15). (deepdyve.com)
- Although diverse results are reported, the Arg16 variant of polymorphism in ADRB2 is associated with increased β2-receptor desensitization during agonist therapy, resulting in reduced treatment efficiency (16-18). (deepdyve.com)
- The data are compatible with a catecholamine-driven beta AR pathway desensitization. (ahajournals.org)
- Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. (genetex.com)
- For live-cell receptor internalization studies, an enhanced version of this dye, CypHer5E, has been developed (3). (bio-medicine.org)
- Pharmacological, structural, and molecular cloning data indicate significant heterogeneity within this receptor family. (acris-antibodies.com)
- Pharmacological characterization of membrane-expressed human trace amine-associated receptor 1 (TAAR1) by a bioluminescence resonance energy transfer cAMP biosensor. (guidetopharmacology.org)
- Our goal is to link receptor structure, cellular biological data and pharmacological results to physiological function. (psi.ch)
- title=Genetic mapping of adrenergic receptor genes in humans. (enacademic.com)