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).

Regulation of cardiac L-type Ca2+ channel by coexpression of G(alpha s) in Xenopus oocytes. (1/484)

Activation of G(alpha s) via beta-adrenergic receptors enhances the activity of cardiac voltage-dependent Ca2+ channels of the L-type, mainly via protein kinase A (PKA)-dependent phosphorylation. Contribution of a PKA-independent effect of G(alpha s) has been proposed but remains controversial. We demonstrate that, in Xenopus oocytes, antisense knockdown of endogenous G(alpha s) reduced, whereas coexpression of G(alpha s) enhanced, currents via expressed cardiac L-type channels, independently of the presence of the auxiliary subunits alpha2/delta or beta2A. Coexpression of G(alpha s) did not increase the amount of alpha1C protein in whole oocytes or in the plasma membrane (measured immunochemically). Activation of coexpressed beta2 adrenergic receptors did not cause a detectable enhancement of channel activity; rather, a small cAMP-dependent decrease was observed. We conclude that coexpression of G(alpha s), but not its acute activation via beta-adrenergic receptors, enhances the activity of the cardiac L-type Ca2+ channel via a PKA-independent effect on the alpha1C subunit.  (+info)

Examining the efficiency of receptor/G-protein coupling with a cleavable beta2-adrenoceptor-gsalpha fusion protein. (2/484)

Reconstitution of high-affinity agonist binding at the beta2-adrenoceptor (beta2AR) expressed in Sf9 insect cells requires a large excess of the stimulatory G-protein of adenylyl cyclase, Gsalpha, relative to receptor [R. Seifert, T. W. Lee, V. T. Lam & B. K. Kobilka, (1998) Eur. J. Biochem. 255, 369-382]. In a fusion protein of the beta2AR and Gsalpha (beta2AR-Gsalpha), which has only a 1 : 1 stoichiometry of receptor and G-protein, high-affinity agonist binding and agonist-stimulated GTP hydrolysis, guanosine 5'-O-(3-thiotriphosphate) (GTP[S]) binding and adenylyl cyclase (AC) activation are more efficient than in the nonfused coexpression system. In order to analyze the stability of the receptor/G-protein interaction, we constructed a fusion protein with a thrombin-cleavage site between beta2AR and Gsalpha (beta2AR-TS-Gsalpha). beta2AR-TS-Gsalpha efficiently reconstituted high-affinity agonist binding, agonist-stimulated GTP hydrolysis, GTP[S] binding and AC activation. Thrombin cleaves approximately 70% of beta2AR-TS-Gsalpha molecules in Sf9 membranes. Thrombin cleavage did not impair high-affinity agonist binding and GTP[S] binding but strongly reduced ligand-regulated GTPase activity and AC activity. We conclude that fusion of the beta2AR to Gsalpha promotes tight physical association of the two partners and that this association remains stable for a single activation/deactivation cycle even after cleavage of the link between the receptor and G-protein. Dilution of Gsalpha in the membrane and release of activated Gsalpha into the cytosol can both prevent cleaved beta2AR-TS-Gsalpha from undergoing multiple activation/deactivation cycles.  (+info)

Functional and molecular biological evidence for a possible beta3-adrenoceptor in the human detrusor muscle. (3/484)

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)

Inotropic and sympathetic responses to the intracoronary infusion of a beta2-receptor agonist: a human in vivo study. (4/484)

BACKGROUND: On the basis of the presence of beta2-receptors within the sympathetic nervous system, beta2-stimulation may increase cardiac sympathetic outflow. We addressed the hypothesis that sympathoexcitatory beta2-receptors are present in the human left ventricle. METHODS AND RESULTS: The beta2-agonist salbutamol was infused into the left coronary artery in 3 groups of patients: group 1 (n=9, no beta-blocker therapy), group 2 (n=7, beta1-selective blockade with atenolol), and group 3 (n=6, nonselective beta-blockade with nadolol). Left ventricular +dP/dt in response to increasing concentrations of salbutamol was measured in all groups, and cardiac norepinephrine spillover was measured in group 1. There were no systemic hemodynamic changes in any group. Salbutamol resulted in a 44+/-6% increase in +dP/dt in group 1, a 25+/-6% increase in group 2 (P<0.05 versus group 1), and no increase in group 3. Salbutamol also resulted in a 124+/-37% increase in cardiac norepinephrine spillover in group 1 (P<0.05). CONCLUSIONS: Evidence that salbutamol increased norepinephrine release from cardiac sympathetic nerves was provided by the observations that atenolol suppressed the salbutamol inotropic response, demonstrating that this response was mediated in part by beta1-receptors and that salbutamol also resulted in an increase in cardiac norepinephrine spillover. This result provides in vivo evidence, in humans, for the role of sympathoexcitatory cardiac beta2-receptors.  (+info)

G(i) protein-mediated functional compartmentalization of cardiac beta(2)-adrenergic signaling. (5/484)

In contrast to beta(1)-adrenoreceptor (beta(1)-AR) signaling, beta(2)-AR stimulation in cardiomyocytes augments L-type Ca(2+) current in a cAMP-dependent protein kinase (PKA)-dependent manner but fails to phosphorylate phospholamban, indicating that the beta(2)-AR-induced cAMP/PKA signaling is highly localized. Here we show that inhibition of G(i) proteins with pertussis toxin (PTX) permits a full phospholamban phosphorylation and a de novo relaxant effect following beta(2)-AR stimulation, converting the localized beta(2)-AR signaling to a global signaling mode similar to that of beta(1)-AR. Thus, beta(2)-AR-mediated G(i) activation constricts the cAMP signaling to the sarcolemma. PTX treatment did not significantly affect the beta(2)-AR-stimulated PKA activation. Similar to G(i) inhibition, a protein phosphatase inhibitor, calyculin A (3 x 10(-8) M), selectively enhanced the beta(2)-AR but not beta(1)-AR-mediated contractile response. Furthermore, PTX and calyculin A treatment had a non-additive potentiating effect on the beta(2)-AR-mediated positive inotropic response. These results suggest that the interaction of the beta(2)-AR-coupled G(i) and G(s) signaling affects the local balance of protein kinase and phosphatase activities. Thus, the additional coupling of beta(2)-AR to G(i) proteins is a key factor causing the compartmentalization of beta(2)-AR-induced cAMP signaling.  (+info)

Constitutively active mutants of the beta1-adrenergic receptor. (6/484)

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. (7/484)

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)

Beta(2)-adrenergic receptor down-regulation. Evidence for a pathway that does not require endocytosis. (8/484)

Sustained activation of most G protein-coupled receptors causes a time-dependent reduction of receptor density in intact cells. This phenomenon, known as down-regulation, is believed to depend on a ligand-promoted change of receptor sorting from the default endosome-plasma membrane recycling pathway to the endosome-lysosome degradation pathway. This model is based on previous studies of epidermal growth factor (EGF) receptor degradation and implies that receptors need to be endocytosed to be down-regulated. In stable clones of L cells expressing beta(2)-adrenergic receptors (beta(2)ARs), sustained agonist treatment caused a time-dependant decrease in both beta(2)AR binding sites and immuno-detectable receptor. Blocking beta(2)AR endocytosis with chemical treatments or by expressing a dominant negative mutant of dynamin could not prevent this phenomenon. Specific blockers of the two main intracellular degradation pathways, lysosomal and proteasome-associated, were ineffective in preventing beta(2)AR down-regulation. Further evidence for an endocytosis-independent pathway of beta(2)AR down-regulation was provided by studies in A431 cells, a cell line expressing both endogenous beta(2)AR and EGF receptors. In these cells, inhibition of endocytosis and inactivation of the lysosomal degradation pathway did not block beta(2)AR down-regulation, whereas EGF degradation was inhibited. These data indicate that, contrary to what is currently postulated, receptor endocytosis is not a necessary prerequisite for beta(2)AR down-regulation and that the inactivation of beta(2)ARs, leading to a reduction in binding sites, may occur at the plasma membrane.  (+info)

COPD is a major cause of morbidity and mortality with a rising incidence worldwide. Large RCTs and meta-analyses show that currently available pharmacotherapy may improve symptoms and perhaps even survival. Appleton and colleagues provided an in-depth systematic review of the role of LABAs in the management of stable COPD. LABAs led to small statistically significant increases in lung function (FEV1) and improvement in some measures of health status compared with placebo. These findings further support current guideline recommendations for use of LABAs in stable moderate-to-severe COPD. However, the story does not end here. In light of recent concerns and the continued debate about LABAs and increased asthma-related deaths (1), is it possible that LABAs also increase deaths in patients with COPD? The meta-analysis by Salpeter and colleagues shows the effectiveness of anticholinergics in reducing COPD exacerbations and hospitalizations. Interestingly, compared with placebo, anticholinergics ...
A Moderate Drug Interaction exists between indacaterol and olodaterol. View detailed information regarding this drug interaction.
oh loe da ter ol). Brand Name(s): Striverdi® Respimat®, Stiolto ® Respimat® (as a combination product containing olodaterol and tiotropium). WHY is this medicine prescribed?. Olodaterol oral inhalation is used to control wheezing, shortness of breath, coughing, and chest tightness caused by chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs and airways, which includes chronic bronchitis and emphysema). Olodaterol oral inhalation is in a class of medications called long-acting beta-agonists (LABAs). It works by relaxing and opening air passages in the lungs, making it easier to breathe.. Are there OTHER USES for this medicine?. This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.. HOW should this medicine be used?. Olodaterol inhalation comes as a solution to inhale by mouth using a special inhaler. It is usually used once a day. Inhale olodaterol at around the same time every day. Follow the directions on ...
Advisors to the US Food and Drug Administration has recommended approval of Boehringer Ingelheims chronic obstructive pulmonary disease drug olodaterol. - News - PharmaTimes
本次文獻回顧找到71篇相關試驗,但並非所有試驗均包含我們所關注的結果。生活品質分析 (使用聖喬治呼吸問卷測量) 納入42篇試驗,肺功能分析則納入46篇試驗。. 品質優良的相似試驗所得到的證據,支持LABA/ICS合併療法為最適當的治療策略,患者的生活品質和肺功能改善幅度最高。於6個月時,合併療法的平均療效較安慰劑高3.9個單位。於6個月時LAMA排名第二 (-2.63個單位),LABA排名第三 (-2.29 個單位),尤其是將不可靠的試驗予以排除時,但估計值的重疊度很高。. 對最低第一秒用力吐氣肺容積 (FEV11) 而言,LABA/ICS合併療法為排序最高的治療類別,相對於安慰劑,於6個月時的平均改善幅度為133.3 mL (95% 可靠區間 [CrI] 為101至164)。如同SGRQ的結果,於6個月時LAMA (平均差 [MD] 為104,95% CrI為82至125) 的排序,恰在LABA (MD為99,95% CrI為72至128) ...
This is a 4-week, multicenter, randomized, double-blind, parallel group and active controlled study.. Patients will be randomized (1 to 1 ratio) to a 4-week double-blind treatment period of either FDC (fixed-dose combination) of tiotropium + olodaterol (5/5 µg) plus placebo or the free combination of tiotropium 5 µg and olodaterol 5 µg; all administered via the Respimat® inhaler. The purpose is to show non-inferiority between the FDC and the free combination of tiotropium and olodaterol in patients with COPD. ...
A Moderate Drug Interaction exists between CPM-PSE DM Drops and olodaterol. View detailed information regarding this drug interaction.
An article in the Cochrane Library highlights five studies on cessation of LABA compared to continued use of LABA/ICS for adults with well-controlled asthma to determine whether stopping LABA treatment has an impact on asthma control, exacerbations, and other serious adverse events.
The beta-2 agonist Clenbuterol is used for treating asthma, since it is a bronchodilator, in many countries. However, it is more commonly used to burn fat
In treatment period 1, patients received indacaterol 300 μg once daily for 14 days via single-dose dry-powder inhaler (SDDPI); in treatment period 2, patients received placebo to indacaterol once daily for 14 days via SDDPI; and in treatment period 3, patients received salmeterol 50 μg twice daily for 14 days via multi-dose dry-powder inhaler (MDDPI). There was a washout period of 14 days between each treatment period. Indacaterol and placebo to indacaterol were administered double-blind; salmeterol was administered open-label. Daily inhaled corticosteroid treatment (if applicable) was to remain stable throughout the study. The short-acting β2-agonist salbutamol/albuterol was available for rescue use throughout the study ...
Comparative efficacy of inhaled medications (ICS/LABA, LAMA, LAMA/LABA and SAMA) for COPD: a systematic review and network meta-analysis Mohamed Ismail Abdul Aziz,1,* Ling Eng Tan,1,* David Bin-Chia Wu,1 Fiona Pearce,1 Gerald Seng Wee Chua,2 Liang Lin,1 Ping-Tee Tan,1 Kwong Ng1 1Agency for Care Effectiveness, Ministry of Health, Singapore; 2Division of Medicine, Ng Teng Fong General Hospital, Singapore *These authors contributed equally to this work Purpose: To assess the comparative efficacy of short-acting muscarinic antagonists (SAMAs), long-acting muscarinic antagonists (LAMAs), LAMA in combination with long-acting beta-agonists (LABAs; LAMA/LABAs) and inhaled corticosteroids (ICS) in combination with LABA (ICS/LABAs) for the maintenance treatment of COPD.Materials and methods: We systematically reviewed 74 randomized controlled trials (74,832 participants) published up to 15 November 2017, which compared any of the interventions (SAMA [ipratropium], LAMA [aclidinium, glycopyrronium, tiotropium,
The principal mechanism by which bronchodilator β-adrenoceptor agonists act is to relax airways smooth muscle although they may also be anti-inflammatory. However, the extent of anti-inflammatory activity and the cell types affected by these agonists are uncertain. The purpose of this study was to evaluate whether β-adrenoceptor agonists prevent pro-inflammatory cytokine generation from activated human lung macrophages. Macrophages were isolated and purified from human lung. The cells were pre-treated with both short-acting (isoprenaline, salbutamol, terbutaline) and long-acting (formoterol, salmeterol, indacaterol) β-agonists before activation with lipopolysaccharide (LPS) to induce cytokine (TNFα, IL-6, IL-8 and IL-10) generation. The experiments showed that short-acting β-agonists were poor inhibitors of cytokine generation. Of the long-acting β-agonists studied, formoterol was also a weak inhibitor of cytokine generation whereas only indacaterol and salmeterol showed moderate ...
Long-acting bronchodilators (LABD) are similar in structure to short-acting selective beta2-adrenoceptor agonists, but have much longer side chains resulting in a 12-hour effect, and are used to give a smoothed symptomatic relief (used morning and night). While patients report improved symptom control, these drugs do not replace the need for routine preventers, and their slow onset means the short-acting dilators may still be required. In November 2005, the American FDA released a health advisory alerting the public to findings that show the use of long-acting β2-agonists could lead to a worsening of symptoms, and in some cases death. Currently available long-acting beta2-adrenoceptor agonists include salmeterol, formoterol, bambuterol, and sustained-release oral albuterol. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread; the most common combination currently in use is fluticasone/salmeterol (Advair in the United States, and Seretide in the United ...
The Stiolto Respimat inhaler, also known as tiotropium and olodaterol, is used to manage Chronic Obstructive Pulmonary Disease or COPD.
Olodaterol (oh-loe-DA-ter-ol), Tiotropium Bromide (tye-oh-TROE-pee-um BROE-mide) Treats chronic obstructive pulmonary disease (COPD). Brand Name(s): Stiolto Respimat
Indacaterol is a long-acting bronchodilator. Bronchodilators are medicines that are breathed in through the mouth to open up the bronchial tubes (air passages) in the lungs. They relieve cough, wheezing, shortness of breath, and troubled breathing by increasing the flow of air through the bronchial tubes. This medicine is available only with your doctors prescription. This product is available in the following dosage forms:. ...
The species, which eluted at 6.75 min and produced a molecular ion of m/z 255.13 (Fig. 4E), was assigned to a mono-nitrated salbutamol derivative 3 (Fig. 1). This assignment is consistent with elemental analysis (C12H19N2O4+, exact mass 255.13397) and further supported by MS/MS spectrum obtained from this molecular ion (Fig. 4G). Formation of this nitrophenol was unexpected as it required the side chain at C3 of the aromatic ring, -CH2OH, to be eliminated. We verified that the putative phenolic precursor of 3, a salbutamol analog, in which the -CH2OH moiety was replaced with -H, (m/z 210), was not present as an impurity in salbutamol samples. This indicates that the corresponding radical (1d in Fig. 11) had to be produced in situ, during enzymatic oxidation of salbutamol itself. In the proposed mechanism (Fig. 11), the initially generated phenoxyl radical, 1a, undergoes intramolecular hydrogen atom transfer from the adjacent -CH2OH moiety to generate the aryl-methoxyl-type radical 1c. After ...
COPD is a major cause of morbidity and mortality with a rising incidence worldwide. Large RCTs and meta-analyses show that currently available pharmacotherapy may improve symptoms and perhaps even survival. Appleton and colleagues provided an in-depth systematic review of the role of LABAs in the management of stable COPD. LABAs led to small statistically significant increases in lung function (FEV1) and improvement in some measures of health status compared with placebo. These findings further support current guideline recommendations for use of LABAs in stable moderate-to-severe COPD. However, the story does not end here. In light of recent concerns and the continued debate about LABAs and increased asthma-related deaths (1), is it possible that LABAs also increase deaths in patients with COPD? The meta-analysis by Salpeter and colleagues shows the effectiveness of anticholinergics in reducing COPD exacerbations and hospitalizations. Interestingly, compared with placebo, anticholinergics ...
The ß-adrenergic receptors are linked to G proteins. The ß-receptor has three known subtypes. Beta-1 receptors primarily regulate myocardial tissue and affect the rate of contraction via impulse conduction. Beta-2 receptors regulate smooth muscle tone and influence vascular and bronchiolar rela...
Indacaterol helps people with asthama or COPD to breathe more easily, relaxing the muscles surrounding the airways so that air can pass through more easily.
Medscape - COPD dosing for Arcapta Neohaler (indacaterol inhaled), frequency-based adverse effects, comprehensive interactions, contraindications, pregnancy & lactation schedules, and cost information.
Despite being an irreversible airflow obstruction disorder, bronchodilators are still used in the treatment of COPD. Different patients of bronchitis need
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Teva (previously NuPathe) is developing long-acting compounds for the treatment of neurological and psychiatric disorders, using Long-Acting Delivery (LAD™)
This pair of replicate, 52-week studies of the effects of once-daily combination of tiotropium+olodaterol administered via the Respimat Soft Mist Inhaler in patients with moderate to very severe COPD confirm statistically significant increases for the primary lung-function end points of trough FEV1 and FEV1 AUC0-3 response after 24 weeks versus either tiotropium or olodaterol alone. These results are supported by a range of secondary lung-function end points over 52 weeks. FEV1 AUC0-3 and trough FEV1 reflect bronchodilator benefit at the beginning and end of a 24-h cycle and are important measures in the selection of optimum doses and dosing frequency.. Long-acting bronchodilators remain the cornerstone of COPD maintenance therapy [2]. However, the combination of bronchodilators with different modes of action has not been commonly prescribed in clinical practice [1] due, in part, to the lack, until recently, of available FDCs of LAMA+LABA. Olodaterol is a novel once-daily LABA that has been ...
Chronic obstructive pulmonary disease (COPD) is a progressive lung disease that is associated with airway obstruction. COPD is a major cause of chronic morbidity and mortality throughout the world. It is a progressive condition, but is partially reversible through treatment, especially when diagnosed early in its clinical course. Bronchodilators are important in treating the symptoms of COPD. Long-acting bronchodilators provide sustained symptom relief and are usually preferred in patients with COPD. Combining bronchodilators with different mechanisms of action appears to improve efficacy.
Similar to the scenario in neonatal rat cardiomyocytes, β1-AR stimulation with isoproterenol induces a robust increase in cAMP accumulation that is associated with an increase in the amplitude and an acceleration of the kinetics of both the calcium transient and the twitch in adult rat ventricular myocytes. In contrast, only rather high concentrations of the β2-AR agonist zinterol (10-5 mol/L) modulate contractile function in adult rat ventricular myocytes (Figure 2⇑). Parenthetically, 2 laboratories have presented data to support the theoretical argument that 10-5 mol/L zinterol (in the absence of a β1-AR blocker) acts as a mixed β1-/β2-AR agonist; β2-AR selectivity is achieved only if a β1-AR blocker (such as CGP 20712A) is included in the assay.11 73 In contrast, Xiao and Lakatta74 maintain that the effects of high concentrations of zinterol (even without a β1-AR blocker) are attributable entirely to the minor population of β2-ARs in the preparation, and they present results to ...
Ultibro breezhaler contains the two active ingredients, indacaterol and glycopyrronium. These medicines work in two different ways to open the airways and make it easier to breathe.
Once-daily inhaled medication is the first approved fixed-dose combination of a long-acting beta agonist and a long-acting muscarinic antagonist.
Ultibro Breezhaler: This combination product contains two medications glycopyrronium and indacaterol. Glycopyrronium belongs to the group of medications known as anticholinergics. Indacaterol belongs to the group of medications known as long-acting bronchodilators. These medications work in different ways to relax the muscles in the walls of the small air passages in the lung, keeping the air passage open and making it easier to breathe.
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A type of drug that causes small airways in the lungs to open up. Bronchodilators are inhaled and are used to treat breathing disorders, such as asthma or emphysema ...
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This study compared the efficacy and tolerability of glycopyrrolate/indacaterol [QVA 149], glycopyrrolate, and indacaterol, in patients with stable
BioAssay record AID 640205 submitted by ChEMBL: Intrinsic activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay.
Symptomatic treatment of patients with severe COPD (FEV1 < 50% predicted normal) and a history of repeated exacerbations, who have significant symptoms despite regular therapy with long-acting bronchodilators. Strength ...
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Role of combined indacaterol and glycopyrronium bromide (QVA149) for the treatment of COPD in Japan Nobuyuki Horita, Takeshi Kaneko Department of Pulmonology, Yokohama City University Graduate School of Medicine, Yokohama, Japan Abstract: Once-daily dual-bronchodilator therapy with combined indacaterol and glycopyrronium bromide in one device (Ultibro, Breezhaler), often called QVA149, was first approved in 2013 in Japan and Europe. As of November 2014, more than 40 countries had approved this medication except for the USA. This is the first dual bronchodilator in one device. Now, the Breezhaler is the only device that can provide long-acting muscarinic antagonist (glycopyrronium bromide), long-acting beta agonist (indacaterol), and a combination of the two medications (QVA149). The choice among the three medications allows a patient to use the same inhalation device even when the regimen is changed from single-bronchodilator therapy to dual-bronchodilator therapy. In addition, the quick
A study has investigated the effects on 24-h lung function and lung volume of a once-daily fixed-dose combination ( FDC ) of the long-acting muscarinic antagonist Tiotropium and the long-acting beta2- .... ...
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New use of either long-acting β-agonists or anticholinergics is associated with increased risks of cardiovascular events among older individuals with chronic obstructive pulmonary disease (COPD).
The post-market review of COPD medicines recommended by the PBAC in August is now open for public comment. The review was given the green light following concerns about the multiple use of a number of new combinations available on the PBS, including long-acting muscarinic antagonist (LAMA)/LABA and LABA/inhaled corticosteroid (ICS) combinations. The terms of reference .... ...
Beta2-adrenergic agonists act on beta-2 receptors to drive potassium into the cells. Therefore, beta blockers can raise ... Examples of medications that can cause hyperkalemia include ACE inhibitors, angiotensin receptor blockers, beta blockers, and ... Examples of drugs that can raise the serum potassium are non-selective beta-blockers such as propanolol and labetalol. Beta-1 ... High levels of adrenaline and noradrenaline have a protective effect on the cardiac electrophysiology because they bind to beta ...
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 ... the release of granulocyte chemotactic protein-2, oncostatin M, and vascular endothelial growth factor from macrophages". Int ...
Inhalation of an agonist for the beta-2 adrenergic receptor, such as Salbutamol, Albuterol (US), is the most common treatment ... adrenergic receptor on the response to regular use of albuterol in asthma". American Journal of Respiratory and Critical Care ... a direct-acting beta agonist used in congestive heart failure, also demonstrates tachyphylaxis.[medical citation needed] ... Polymorphisms of the beta-2 receptor play a role in tachyphylaxis. Expression of the Gly-16 allele (glycine at position 16) ...
... a novel agonist at peripheral dopamine receptors and beta 2-adrenoceptors". British Journal of Pharmacology. 85 (3): 599-608. ... It is not an α-adrenergic agonist, does not cause vasoconstriction, and is not a pressor agent. As of 2004 there was some ... Effects of depexamine may be suppressed by concomitant use with ß2-adrenergic and dopamine receptor antagonists requires ... Dopexamine stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ...
... a non-selective beta-adrenergic receptor inhibitor. Elevated IOP is considered the only modifiable risk factor in the ... It is a combination of brimonidine (an α2 adrenergic agonist) and timolol (a β adrenergic blocker), in concentrations of 0.2% ... 21 (2): 14. 2008. PMID 18326089. Lee, AJ; McCluskey, P (2008). "Fixed combination of topical brimonidine 0.2% and timolol 0.5% ... 2 (5): 705. doi:10.1586/17469899.2.5.705. ,access-date= requires ,url= (help) "BRIMONIDINE - brimonidine tartrate solution/ ...
... is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ... Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. It was ... Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ... Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. ...
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH agonist, but is now ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ...
Ferguson SS, Menard L, Barak LS, Koch WJ, Colapietro AM, Caron MG (1995). "Role of phosphorylation in agonist-promoted beta 2- ... beta-adrenergic-receptor] kinase, beta-adrenergic receptor-specific kinase, beta-AR kinase, beta-ARK, beta-ARK 1, beta-ARK 2, ... beta-adrenergic receptor] Thus, the two substrates of this enzyme are ATP and beta-adrenergic receptor, whereas its two ... beta-adrenergic receptor] phosphotransferase. Other names in common use include ATP:beta-adrenergic-receptor phosphotransferase ...
... is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high specificity (an antagonist ... ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... Fitzgerald, JD; Wale, JL (1983). "The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)". J Cardiovasc ... A Beta-2 adrenergic antagonist (β2-adrenoceptor antagonist) ...
Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... a Gq coupled receptor) and α2 (a Gi coupled receptor). Phenylephrine is a selective agonist of the α receptor. β receptors have ... Basic Neurochemistry: α- and β-Adrenergic Receptors Brief overview of functions of the β3 receptor Theory of receptor ... ISBN 0-443-06911-5. Alpha receptors illustrated The Adrenergic Receptors "Adrenoceptors". IUPHAR Database of Receptors and Ion ...
ISBN 0-443-07145-4. Philipson, L. H. (December 2002). "beta-Agonists and metabolism". The Journal of Allergy and Clinical ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... "Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta- ...
The beta-adrenergic receptor kinase specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G ... The beta adrenergic receptor kinase-2 was cloned from mice and rats in 1991 and the human gene was cloned in 1993. Gene linkage ... Beta-adrenergic receptor kinase 2 (beta-ARK-2) also known as G-protein-coupled receptor kinase 3 (GRK3) is an enzyme that in ... "Entrez Gene: ADRBK2 adrenergic, beta, receptor kinase 2". Benovic JL, Onorato JJ, Arriza JL, Stone WC, Lohse M, Jenkins NA, ...
9 Beta Adrenergic Drugs beta-Adrenergic Receptor Agonists at the US National Library of Medicine Medical Subject Headings (MeSH ... adrenergic receptor agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic ... receptor. Like other β adrenergic agonists, they cause smooth muscle relaxation. β2 adrenergic agonists' effects on smooth ... Discovery and development of β2 agonists Ramanujan K. Common beta-agonist inhalers more than double death rate in COPD patients ...
"The beta-adrenergic receptors". Yoo, B.; et al. "Beta1-adrenergic receptors stimulate cardiac contractility and CaMKII ... In general, pure beta-adrenergic agonists have the opposite function of beta blockers. Beta adrenoreceptor agonist ligands ... Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, which widen the airways and result ... "WHAT ARE BETA-AGONISTS?". Thoracic.org. American Thoracic Society. Retrieved 17 October 2014. Adrenergic beta-Agonists at the ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... also acts as a moderate affinity 5-HT1A receptor agonist, and low affinity CB1 receptor antagonist). Clonidine (also I1 agonist ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... Agonists (activators) of the α2-adrenergic receptor are frequently used in veterinary anaesthesia where they affect sedation, ...
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 ... adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. Postoje tri ... Adrenergički receptor. Reference[уреди]. *^ Ruuskanen JO, Xhaard H, Marjamäki A, Salaneck E, Salminen T, Yan YL, Postlethwait ...
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 ... β-receptors are membrane-bound receptors coupled to G-proteins. Three types of β-receptors have been identified by molecular ...
"The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329): 241-4. doi: ... Lohse MJ, Benovic JL, Codina J, Caron MG, Lefkowitz RJ (June 1990). "beta-Arrestin: a protein that regulates beta-adrenergic ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... the receptor does not bind agonist and cannot initiate a response following exposure to agonist). Expression of the two ...
... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in ...
"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 ... adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. Postoje tri ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
"Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta- ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation.". J. Biol. Chem. 263 (9): ... 1988). "Site-directed mutagenesis and continuous expression of human beta-adrenergic receptors. ... the contribution of genetic variability in beta adrenergic receptor and cytochrome P4502C9.". Clin. Pharmacol. Ther. 82 (2): ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... September 1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. doi: ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist. ICI binds to the β2 subtype with at least 100 ...
"The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329): 241-4. doi: ... Lohse MJ, Benovic JL, Codina J, Caron MG, Lefkowitz RJ (June 1990). "beta-Arrestin: a protein that regulates beta-adrenergic ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... G protein-coupled receptors database List of MeSH codes (D12.776) Metabotropic receptor Orphan receptor Pepducins, a class of ...
The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... beta _{2}} receptors causes vasodilation and low blood pressure (i.e. the effect is opposite of the one resulting from ... Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). ... receptor agonists as hypotensive agents is less widespread due to adverse effects such as unnecessary bronchodilation in lungs ...
... a beta-adrenergic receptor antagonist Glaucoma Basic and clinical science course (2011-2012). Glaucoma. American Academy of ... Adrenergic antagonists (nonselective and selective Beta1-antagonists) Alpha 2 agonists Hyperosmotic agents Fotil is a ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... norepinephrine then acting on lipolysis-inducing beta receptors.. Muscle mass[edit]. Males typically have more skeletal muscle ...
Highly specific receptor kinases, such as rhodopsin kinase and beta-adrenergic receptor kinase, which show stimulus-dependent ... Here we report that prevention of agonist-stimulated beta 2-adrenergic receptor (beta 2AR) phosphorylation by truncation of its ... the first direct evidence that one molecular mechanism of desensitization of G-protein-coupled receptors involves their agonist ... Removal of phosphorylation sites from the beta 2-adrenergic receptor delays onset of agonist-promoted desensitization.. Bouvier ...
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor. ...
A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor ... A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor ... beta 2AR-Y326A). This mutation completely abolishes agonist-mediated receptor sequestration without affecting the ability of ... a slower loss of total cellular receptors) associated with agonist-mediated desensitization of the beta 2-adrenergic receptor ...
Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ... Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ... Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ... Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ...
... on human lymphocytes alpha adrenergic receptor density. / Hasegawa, M.; Townley, R.. In: Journal of Allergy and Clinical ... on human lymphocytes alpha adrenergic receptor density, Journal of Allergy and Clinical Immunology, vol. 69, no. 1 II. ... on human lymphocytes alpha adrenergic receptor density. In: Journal of Allergy and Clinical Immunology. 1982 ; Vol. 69, No. 1 ... on human lymphocytes alpha adrenergic receptor density. Journal of Allergy and Clinical Immunology. 1982 Jan 1;69(1 II). ...
... on human lymphocytes alpha adrenergic receptor density. Together they form a unique fingerprint. * Sort by ... Effect of fenoterol (beta-2 agonist) on human lymphocytes alpha adrenergic receptor density. ... Fingerprint Dive into the research topics of Effect of fenoterol (beta-2 agonist) ...
... and beta-3 adrenergic receptors. Neither the beta-1 selective antagonist atenolol [38] nor the beta-3 selective antagonist L- ... To determine the relative roles of the three beta receptors in mediating reductions in DUX4 expression by beta agonists, we ... adrenergic receptor gene ADRB2 genetically confirmed that beta agonists are reducing DUX4 expression via the beta-2 adrenergic ... Together with the pharmacologic data, these results demonstrate that beta-adrenergic agonist compounds act through the beta-2 ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Mean change from Baseline (pre-dose on Day 1) in AM FEV1 from electronic flow meter over Days 2-15 [ Time Frame: Baseline (pre- ... and at 0-2 h, 0-4, and 0-24 h Days 1 and 14 ]. The forced expiratory volume in one second is the amount of air exhaled in one ... dose on Day 1), Day 2, and Day 15 ]. The forced expiratory volume in one second is the amount of air exhaled in one second ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Inhaled Corticosteroid (ICS)/Long Acting Beta Agonist (LABA). Drug: Fluticasone Furoate 100mcg/Vilanterol 25mcg Inhalation ... Inhaled Corticosteroid (ICS)/Long Acting Beta Agonist (LABA. Drug: Fluticaosne Propionate 500mcg/Salmeterol 50mcg Inhalation ... Subjects with history of hypersensitivity to study medications (e.g., beta-agonists, corticosteroid) or components of ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Unwillingness of primary physician to discontinue inpatient beta agonist use. *Acute myocardial infarction or acute coronary ... Daily use (prior to study hospitalization) of inhaled beta agonist, corticosteroid, or oral leukotriene modifier ... Because beta-2 agonists have been shown to reduce permeability induced lung injury, it is anticipated that the severity of lung ...
These effects have traditionally been thought to be mediated exclusively by receptor activation of intrace … ... Stimulation of beta2-adrenergic receptors on the cell surface by adrenaline or noradrenaline leads to alterations in the ... Our findings indicate that agonist-dependent beta2-adrenergic receptor binding of NHERF plays a role in beta2-adrenergic ... Receptors, Adrenergic, beta-2 / genetics * Receptors, Adrenergic, beta-2 / metabolism* * Recombinant Fusion Proteins / genetics ...
Adrenergic beta-2 Receptor Agonists / therapeutic use * Adult * Anti-Asthmatic Agents / administration & dosage ... Almost 62% of the women were dispensed at least one prescription for short-acting β2-agonist (SABA), 63% at least one inhaled ... Anna-Belle Beau 1 , Alain Didier 2 , Caroline Hurault-Delarue 1 , Jean-Louis Montastruc 1 , Isabelle Lacroix 1 , Christine ... corticosteroid (IC), 42% a fixed-combination of an IC and a long-acting β2-agonist (LABA) and 8% a LABA. An increase in SABA ...
INVOLVEMENT OF THE CARBOXYL TERMINAL DOMAIN OF THE BETA-2-ADRENERGIC RECEPTOR IN ITS AGONIST-INDUCED PHOSPHORYLATION AND ... INVOLVEMENT OF THE CARBOXYL TERMINAL DOMAIN OF THE BETA-2-ADRENERGIC RECEPTOR IN ITS AGONIST-INDUCED PHOSPHORYLATION AND ...
... adrenergic agonist) increased CBF in a dose-dependent ... The beta(2)-adrenergic regulation of ciliary beat frequency ( ... 0/Adrenergic beta-Agonists; 0/Enzyme Inhibitors; 0/Receptors, Adrenergic, beta-2 ... Adrenergic beta-Agonists / pharmacology. Animals. Cell Size / drug effects, physiology. Cilia / drug effects, physiology. ... adrenergic agonist) increased CBF in a dose-dependent manner, and it also decreased the volume of the ciliary cells. These ...
ISBN 0-443-07145-4. Philipson, L. H. (December 2002). "beta-Agonists and metabolism". The Journal of Allergy and Clinical ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... "Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta- ...
MOA for beta adrenergic agonists targets beta 2 receptors in airway - bronchodilation ... 1. Accolate - blocks leukotriene receptors. 2. Singulair - blocks leukotriene receptors. 3. Zyflo - Inhibits leukotriene ... 2. wheezing. 3. expanded chest. 4. sinusitis. 5. failure to grow. 6. thick stringy mucous ... What level of asthma would get one medium dose of inhaled corticosteroid or 2 daily medications ...
Beta-adrenergic agonists. Bronchodilation (Asthma); beneficial during P&PD. stimulate beta-2 receptors and cause relaxation. ... Alpha-1 agonists (adrenergic agonists); vasoconstrict nasal mucosa. Palpitations, headache, nausea, dependence, nervousness. ... Beta-Blockers (-olol). HTN, arrhythmia, angina, heart failure, MI (decrease HR and force of contraction). Block effects of ... Dopamine agonists. Parkinson disease. synthetic dopamine. GI distress, orthostatic hypotension, dyskinesias, psychotropic ...
Beta2-adrenergic receptor agonist sympathomimetic; decreases free intracellular calcium ions. 0.25 to 0.5 mg SC every three to ... Beta2-adrenergic receptor agonist sympathomimetic; decreases free intracellular calcium ions. 0.25 to 0.5 mg SC every three to ... Figures 2 and 3 and Table 5 summarize the consensus management guidelines for the prevention of early-onset group B neonatal ... TABLE 2. Tocolytic Therapy for the Management of Preterm Labor. Medication. Mechanism of action. Dosage. ...
... although beta2-agonist activity resides almost exclusively in the (R)-enantiomer. The enantioselective disposition of ... is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease ( ... Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. ... Levosalbutamol, also known as levalbuterol, is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma ...
Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline . ... In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors ... Agonist. General Function. Protein homodimerization activity. Specific Function. Beta-adrenergic receptors mediate the ... Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.. Gene Name. ...
Beta-2 adrenergic receptor agonists; Cromones; Glucocorticoids; Leukotriene receptor antagonists; Methyl xanthines; Omalizumab ...
"The beta-adrenergic receptors". Yoo, B.; et al. "Beta1-adrenergic receptors stimulate cardiac contractility and CaMKII ... In general, pure beta-adrenergic agonists have the opposite function of beta blockers. Beta adrenoreceptor agonist ligands ... Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, which widen the airways and result ... "WHAT ARE BETA-AGONISTS?". Thoracic.org. American Thoracic Society. Retrieved 17 October 2014. Adrenergic beta-Agonists at the ...
Drug-drug.Beta-adrenergic blockers: decreased salmeterol efficacy, increased risk of severe bronchospasm in patients with ... For children and adolescents with asthma who require addition of a long-acting beta2-adrenergic agonist to an inhaled ... Available data from controlled clinical trials suggest that long-acting beta2-adrenergic agonists increase risk of asthma- ... a fixed-dose combination product containing both an inhaled corticosteroid and a long-acting beta2-adrenergic agonist should ...
Insulin decreases atherosclerosis by inducing endothelin receptor B expression.. Park K, Mima A, Li Q, Rask-Madsen C, He P, ... Transforming growth factor beta-1 and incidence of heart failure in older adults: the Cardiovascular Health Study. ... Homozygous receptors for insulin and not IGF-1 accelerate intimal hyperplasia in insulin resistance and diabetes. ... Beta 2-adrenergic receptor agonists are novel regulators of macrophage activation in diabetic renal and cardiovascular ...
  • Almost 62% of the women were dispensed at least one prescription for short-acting β2-agonist (SABA), 63% at least one inhaled corticosteroid (IC), 42% a fixed-combination of an IC and a long-acting β2-agonist (LABA) and 8% a LABA. (nih.gov)
  • These findings provide reassurance that in the general population, patients should continue to be treated with long-acting beta-2 agonists plus moderate-dose inhaled corticosteroids irrespective of B16 genotype. (healthcanal.com)
  • The double-blind trial compared Serevent vs. placebo when added to standard therapy, such as ICS, methylxanthines, leukotriene modifiers and other ADRB2 agonists. (biocentury.com)
  • BROVANA (arformoterol tartrate) Inhalation Solution is supplied as 2 mL of arformoterol tartrate solution packaged in 2.1 mL unit-dose, low-density polyethylene (LDPE) unit-dose vials. (rxlist.com)
  • Cells stably expressing WT β 1 ARs were transfected with GFP-tagged EGFR (EGFR-GFP) and stimulated with several agonists or 20 different β-blockers. (pnas.org)
  • ACE inhibitors , angiotensin receptor blockers , and calcineurin inhibitor immunosuppressants such as ciclosporin and tacrolimus . (wikipedia.org)
  • They are constantly gaining in importance, and increasingly more significant than traditional tocolytics such as beta-adrenergic receptor (β-AR) blockers or magnesium sulphate. (mdpi.com)
  • 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)
  • Recent evidence suggests that binding of different ligands promotes distinct receptor conformations leading to specific signaling events ( 9 - 12 ). (pnas.org)
  • We screened β-adrenergic ligands to determine if any could lead to β 1 AR-mediated EGFR transactivation. (pnas.org)
  • The ligands that bind and activate these receptors include light-sensitive compounds, odors , pheromones , hormones , and neurotransmitters , and vary in size from small molecules to peptides to large proteins . (wikipedia.org)
  • Levosalbutamol acts as a functional agonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges. (drugbank.ca)
  • It relaxes the muscle around the airways into the lungs by activating targets called beta-2 receptors in the muscle cells. (europa.eu)
  • We have recently delineated three polymorphic loci within the coding block of the beta 2AR which alter amino acids at positions 16, 27, and 164 and impart specific biochemical and pharmacologic phenotypes to the receptor. (jci.org)
  • Deubiquitinating enzyme involved in various processes such as centrosome duplication, cellular migration and beta-2 adrenergic receptor/ADRB2 recycling. (uniprot.org)
  • Upon dissociation, it is probably transferred to the translocated beta-arrestins, leading to beta-arrestins deubiquitination and disengagement from ADRB2. (uniprot.org)
  • This suggests the existence of a dynamic exchange between the ADRB2 and beta-arrestins. (uniprot.org)
  • Western Blot analysis of ADRB2 expression in transfected 293T cell line ( H00000154-T02 ) by ADRB2 MaxPab polyclonal antibody.Lane 1: ADRB2 transfected lysate(45.43 KDa).Lane 2: Non-transfected lysate. (acris-antibodies.com)
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