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).

Effects of monosodium glutamate-induced obesity in spontaneously hypertensive rats vs. Wistar Kyoto rats: serum leptin and blood flow to brown adipose tissue. (1/90)

We compared the effects of hypothalamic obesity induced by neonatal monosodium glutamate (MSG) treatment between spontaneously hypertensive rats (SHR) and normotensive Wistar Kyoto rats (WKY). Newborn WKY and SHR were injected intraperitoneally with 4 mg/kg body weight of MSG daily for 5 days. At 6 months of age, the obesity of SHR was more advanced than that of WKY, but at 14 months of age the severity of obesity was similar between the two strains. Hypertriglyceridemia was enhanced in MSG-treated SHR as compared with MSG-treated WKY. Systolic blood pressure measured by the tail-cuff method was consistently lower in MSG-treated SHR than in control SHR, whereas blood pressure was not affected by neonatal MSG treatment in WKY. Food restriction reduced body weight more in control SHR than in control WKY, with the former also showing enhanced ketogenesis. Neonatal MSG treatment abolished the accelerated reduction of body weight in SHR. Serum leptin concentration was markedly increased in MSG-treated obese rats, though no differences were seen between WKY and SHR in the control or MSG-treated groups. Serum leptin was closely correlated with both Lee obese index and mesenteric fat weight over the strain. Blood flow in interscapular brown adipose tissue (BAT) measured by Laser Doppler flowmetry was significantly increased in response to beta3-adrenoceptor agonist BRL26830A in both the control and MSG-treated rats. However, the response of blood flow was not affected by MSG treatment or strain difference. The present study demonstrated some strain differences in response to neonatal MSG treatment between WKY and SHR. These differences could not be explained by the difference in serum leptin level or beta3-adrenergic reactivity in BAT.  (+info)

CCAAT/enhancer-binding protein alpha is required for transcription of the beta 3-adrenergic receptor gene during adipogenesis. (2/90)

The beta(3)-adrenergic receptor (beta(3)AR) is expressed predominantly in adipocytes, and it plays a major role in regulating lipolysis and adaptive thermogenesis. Its expression in a variety of adipocyte cell models is preceded by the appearance of CCAAT/enhancer-binding protein alpha (C/EBP alpha), which has been shown to regulate a number of other adipocyte-specific genes. Importantly, it has been demonstrated that several adipocyte cell lines that fail to express C/EBP alpha exhibit reduced insulin sensitivity, despite an apparent adipogenic phenotype. Here we show that transcription and function of the beta(3)AR correlates with C/EBP alpha expression in these adipocyte models. A 5.13-kilobase pair fragment of the mouse beta(3)AR promoter was isolated and sequenced. This fragment conferred a 50-fold increase in luciferase reporter gene expression in adipocytes. Two putative C/EBP binding sites exist at -3306 to -3298 and at -1462 to -1454, but only the more distal site is functional. Oligonucleotides corresponding to both the wild-type and mutated -3306 element were inserted upstream of a thymidine kinase luciferase construct. When cotransfected in fibroblasts with a C/EBP alpha expression vector, reporter gene expression increased 3-fold only in the wild-type constructs. The same mutation, when placed into the intact 5.13-kilobase pair promoter, reduced promoter activity in adipocytes from 50-fold to <10-fold. Electrophoretic mobility shift analysis demonstrated that the site at -3306 generated a specific protein-oligonucleotide complex that was supershifted by C/EBP alpha antibody, while a probe corresponding to a putative site at -1462 did not. These results define C/EBP alpha as a key transcriptional regulator of the mouse beta(3)AR gene during adipogenesis.  (+info)

(+/-)-Pindolol acts as a partial agonist at atypical beta-adrenoceptors in the guinea pig duodenum. (3/90)

The agonistic and antagonistic effects of (+/-)-pindolol (1-(1H-indol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanol) were estimated to clarify whether (+/-)-pindolol acts as a partial agonist on atypical beta-adrenoceptors in the guinea pig duodenum. (+/-)-Pindolol induced concentration-dependent relaxation with a pD2 value of 5.10 +/- 0.03 and an intrinsic activity of 0.83 +/- 0.03. However, the relaxations to (+/-)-pindolol were not antagonized by the non-selective beta1- and beta2-adrenoceptor antagonist (+/-)-propranolol (1 microM). In the presence of (+/-)-propranolol (1 microM), the non-selective beta1-, beta2- and beta3-adrenoceptor antagonist (+/-)-bupranolol (30 microM) induced a rightward shift of the concentration-response curves for (+/-)-pindolol (apparent pA2 = 5.41 +/- 0.06). In the presence of (+/-)-propranolol, (+/-)-pindolol (10 microM) weakly but significantly antagonized the relaxant effects to catecholamines ((-)-isoprenaline, (-)-noradrenaline and (-)-adrenaline), a selective beta3-adrenoceptor agonist BRL37344 ((R*,R*)-(+/-)-4-[2-[(2-(3-chlorophenyl)-2-hydroxyethyl) amino]propyl]phenoxyacetic acid sodium salt) and a non-conventional partial beta3-adrenoceptor agonist (+/-)-CGP12177A([4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H -benzimidazol-2-one] hydrochloride). These results demonstrate that (+/-)-pindolol possesses both agonistic and antagonistic effects on atypical beta-adrenoceptors in the guinea pig duodenum.  (+info)

Beta(3)-adrenoceptor agonist-induced increases in lipolysis, metabolic rate, facial flushing, and reflex tachycardia in anesthetized rhesus monkeys. (4/90)

The effects of two beta(3)-adrenergic receptor agonists, (R)-4-[4-(3-cyclopentylpropyl)-4,5-dihydro-5-oxo-1H-tetrazol-1-yl]-N-[4-[2-[[2-hy droxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]benzenesulfonamide and (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)- ethyl]amino]ethyl]phenyl]-1-(4-octylthiazol-2-yl)-5-indolinesulfonamide, on indices of metabolic and cardiovascular function were studied in anesthetized rhesus monkeys. Both compounds are potent and specific agonists at human and rhesus beta(3)-adrenergic receptors. Intravenous administration of either compound produced dose-dependent lipolysis, increase in metabolic rate, peripheral vasodilatation, and tachycardia with no effects on mean arterial pressure. The increase in heart rate in response to either compound was biphasic with an initial rapid component coincident with the evoked peripheral vasodilatation and a second more slowly developing phase contemporaneous with the evoked increase in metabolic rate. Because both compounds exhibited weak binding to and activation of rhesus beta(1)-adrenergic receptors in vitro, it was hypothesized that the increase in heart rate may be reflexogenic in origin and proximally mediated via release of endogenous norepinephrine acting at cardiac beta(1)-adrenergic receptors. This hypothesis was confirmed by determining that beta(3)-adrenergic receptor agonist-evoked tachycardia was attenuated in the presence of propranolol and in ganglion-blocked animals, under which conditions there was no reduction in the evoked vasodilatation, lipolysis, or increase in metabolic rate. It is not certain whether the beta(3)-adrenergic receptor-evoked vasodilatation is a direct effect of compounds at beta(3)-adrenergic receptors in the peripheral vasculature or is secondary to the release or generation of an endogenous vasodilator. Peripheral vasodilatation in response to beta(3)-adrenergic receptor agonist administration was not attenuated in animals administered mepyramine, indomethacin, or calcitonin gene-related peptide(8-37). These findings are consistent with a direct vasodilator effect of beta(3)-adrenergic receptor agonists.  (+info)

Upregulation of beta(3)-adrenoceptors and altered contractile response to inotropic amines in human failing myocardium. (5/90)

BACKGROUND: Contrary to beta(1)- and beta(2)-adrenoceptors, beta(3)-adrenoceptors mediate a negative inotropic effect in human ventricular muscle. To assess their functional role in heart failure, our purpose was to compare the expression and contractile effect of beta(3)-adrenoceptors in nonfailing and failing human hearts. METHODS AND RESULTS: We analyzed left ventricular samples from 29 failing (16 ischemic and 13 dilated cardiomyopathic) hearts (ejection fraction 18.6+/-2%) and 25 nonfailing (including 12 innervated) explanted hearts (ejection fraction 64.2+/-3%). beta(3)-Adrenoceptor proteins were identified by immunohistochemistry in ventricular cardiomyocytes from nonfailing and failing hearts. Contrary to beta(1)-adrenoceptor mRNA, Western blot analysis of beta(3)-adrenoceptor proteins showed a 2- to 3-fold increase in failing compared with nonfailing hearts. A similar increase was observed for Galpha(i-2) proteins that couple beta(3)-adrenoceptors to their negative inotropic effect. Contractile tension was measured in electrically stimulated myocardial samples ex vivo. In failing hearts, the positive inotropic effect of the nonspecific amine isoprenaline was reduced by 75% compared with that observed in nonfailing hearts. By contrast, the negative inotropic effect of beta(3)-preferential agonists was only mildly reduced. CONCLUSIONS: Opposite changes occur in beta(1)- and beta(3)-adrenoceptor abundance in the failing left ventricle, with an imbalance between their inotropic influences that may underlie the functional degradation of the human failing heart.  (+info)

Beta 3-adrenergic agonist up-regulates uncoupling proteins 2 and 3 in skeletal muscle of the mouse. (6/90)

Chronic stimulation of the beta3-adrenergic receptor (AR) in obese animals resulted in a reduced adiposity associated with an increased expression of thermogenic uncoupling protein (UCP)1 in adipose tissues. In this study, the mRNA expression of newly cloned UCP isoforms (UCP2 and UCP3) were examined in obese yellow KK and C57BL control mice. UCP2 mRNA was found in all tissues examined, with higher levels in adipose tissues and skeletal muscle of the obese mice. UCP3 mRNA was expressed in skeletal muscle, heart and brown adipose tissue similarly in the two mouse strains. Daily injection of a selective beta3-adrenergic agonist, CL316,243 (0.1 mg/kg), for 10 days resulted in a marked reduction of white fat pad weight and 1.8-4.8-fold increase in the mRNA levels of UCP2 and UCP3 in skeletal muscle of obese mice. No noticeable change in the UCP2 and 3 mRNA levels was found in brown and white adipose tissues. It was also found that CL316,243 injection produced a marked and sustained elevation of the plasma free fatty acid level. These results, together with our previous findings of the fatty acid-induced UCP expression in a myocyte cell line in vitro, suggest that the beta3-AR agonist-induced UCP expression in skeletal muscle may be mediated through the elevated plasma free fatty acids. It was also suggested that anti-obesity effect of beta3-AR agonists is attributable to increased thermogenesis not only by UCP1 but also by UCP2 and UCP3.  (+info)

beta-Adrenergic activation of p38 MAP kinase in adipocytes: cAMP induction of the uncoupling protein 1 (UCP1) gene requires p38 MAP kinase. (7/90)

Because of increasing evidence that G protein-coupled receptors activate multiple signaling pathways, it becomes important to determine the coordination of these pathways and their physiological significance. Here we show that the beta(3)-adrenergic receptor (beta(3)AR) stimulates p38 mitogen-activated protein kinase (p38 MAPK) via PKA in adipocytes and that cAMP-dependent transcription of the mitochondrial uncoupling protein 1 (UCP1) promoter by beta(3)AR requires p38 MAPK. The selective beta(3)AR agonist CL316,243 (CL) stimulates phosphorylation of MAP kinase kinase 3/6 and p38 MAPK in a time- and dose-dependent manner in both white and brown adipocytes. Isoproterenol and forskolin mimicked the effect of CL on p38 MAPK. In all cases activation was blocked by the specific p38 MAPK inhibitor SB202190 (SB; 1-10 microm). The involvement of PKA in beta(3)AR-dependent p38 MAPK activation was confirmed by the ability of the PKA inhibitors H89 (20 microm) and (R(p))-cAMP-S (1 mm) to block phosphorylation of p38 MAPK. Treatment of primary brown adipocytes with CL or forskolin induced the expression of UCP1 mRNA levels (6.8- +/- 0.8-fold), and this response was eliminated by PKA inhibitors and SB202190. A similar stimulation of a 3.7-kilobase UCP1 promoter by CL and forskolin was also completely inhibited by PKA inhibitors and SB202190, indicating that these effects on UCP1 expression are transcriptional. Moreover, the PKA-dependent transactivation of the UCP1 promoter, as well as its sensitivity to SB202190, was fully reproduced by a 220-nucleotide enhancer element from the UCP1 gene. We similarly observed that increased phosphorylation of ATF-2 by CL was sensitive to both H89 and SB202190, while phosphorylation of cAMP-response element-binding protein was inhibited only by H89. Together, these studies illustrate that p38 MAPK is an important downstream target of the beta-adrenergic/cAMP/PKA signaling pathway in adipocytes, and one of the functional consequences of this cascade is stimulation of UCP1 gene expression in brown adipocytes.  (+info)

Dual action of octopamine on glucose transport into adipocytes: inhibition via beta3-adrenoceptor activation and stimulation via oxidation by amine oxidases. (8/90)

Octopamine, which is closely related to norepinephrine, acts as a neurotransmitter in invertebrates and is a trace amine with undefined properties in vertebrates. The octopaminergic receptors identified in insects are targets of various pesticides but are absent in vertebrates. We have established that octopamine stimulates fat cell lipolysis in mammals via activation of beta3-adrenoceptors (ARs), whereas this amine has been described elsewhere as an alpha2-AR agonist and as a substrate for monoamine oxidase (MAO) or semicarbazide-sensitive amine oxidase (SSAO). Because we have recently reported that amine oxidase substrates promote glucose transport in rat and human adipocytes, the in vitro octopamine effects on lipolysis and glucose uptake were reassessed by using adipocytes from beta3-AR-deficient mice. The lipolytic effect and the counter-regulation of insulin action on glucose transport provoked by 0.1 to 1 mM octopamine or by 1 microM beta3-AR agonists found in control animals disappeared in adipocytes from beta3-AR-deficient mice. This revealed an insulin-like effect of octopamine on glucose uptake, which was dependent on its oxidation by MAO or SSAO, as was the case for tyramine and benzylamine, devoid of beta3-adrenergic agonism. Similarly, octopamine promoted glucose transport in human adipocytes and exhibited a weaker lipolytic stimulation than in rodent adipocytes. These findings indicate that, besides its lipolytic activity, octopamine exerts, at millimolar dose, dual effect on glucose transport in adipocytes: counteracting insulin action via beta3-AR activation and stimulating basal transport via its oxidation by MAO or SSAO.  (+info)

Structure, properties, spectra, suppliers and links for: {4-[(2R)-2-{[(2R)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino}propyl]phenoxy}acetic acid.
WATERNT Program (v1.01) was used to estimate the water solubility of the test substance 2-[[4-[bis(2-hydroxyethyl)amino]-o-tolyl]azo] -5-nitrobenzonitrile (CAS no. 12236-25-8). The estimated water solubility of the test substance 2-[[4-[bis(2-hydroxyethyl)amino]-o-tolyl]azo]-5-nitrobenzonitrile (CAS no. 12236-25-8) at 25 deg C was 61.338 mg/l. Based on the estimated value, the test substance 2-[[4-[bis(2-hydroxyethyl)amino]-o-tolyl]azo]-5-nitrobenzonitrile (CAS no. 12236-25-8) was considered to be slightly soluble in water. ...
91051-78-4 - Fatty acids, tallow, 2-(bis(2-hydroxyethyl)amino)ethyl esters - Searchable synonyms, formulas, resource links, and other chemical information.
You are viewing an interactive 3D depiction of the molecule (3z)-4-{[(2s)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}-3-[4-methyl-6-(4-morpholinyl)-1,3-dihydro-2h-benzimidazol-2-ylidene]-2(3h)-pyridinone (C24H17ClN5O3) from the PQR.
61361-60-2 - KBPURVPYVJJZGS-UHFFFAOYSA-N - Phenol, 2-(((2-hydroxyethyl)amino)methyl)-4-nitro- - Similar structures search, synonyms, formulas, resource links, and other chemical information.
2-[bis[2-(2,6-dioxomorpholin-4-yl)ethyl]amino]acetic acid 23911-26-4 route of synthesis, 2-[bis[2-(2,6-dioxomorpholin-4-yl)ethyl]amino]acetic acid chemical synthesis methods, 2-[bis[2-(2,6-dioxomorpholin-4-yl)ethyl]amino]acetic acid synthetic routes ect.
You are viewing an interactive 3D depiction of the molecule 2-[(8s,11s)-11-{(1r)-1-hydroxy-2-[(3-methylbutyl)(phenylsulfonyl)amino]ethyl}-6,9-dioxo-2-oxa-7,10-diazabicyclo[11.2.2]heptadeca-1(15),13,16-trien-8-yl]acetamide (C29H40N4O7S) from the PQR.
Phospholipids and lipid second messengers mediate mitogenic signal transduction and oncogenesis, but there have been few successful examples of small molecules that affect biologically important phospholipid metabolism. Here we investigated the actions of a previously described antitumor agent, 4-(benzyl-(2-[(2,5-diphenyloxazole-4-carbonyl)amino]ethyl)carbamoyl) -2-decanoylaminobutyric acid (SC-ααδ9), which has antisignaling properties, on phospholipases. Although SC-ααδ9 had been shown to be a potent and selective inhibitor of the Cdc25 family of dual-specificity phosphatases, many of its cellular effects are not readily reconciled with phosphatase inhibition. Molecular modeling studies suggested that SC-ααδ9 shared several structural features with membrane phospholipids. Enzyme inhibition studies in vitro revealed that SC-ααδ9 was a potent inhibitor of phospholipase C (PLC; IC50 = 25 μM) but did not inhibit phospholipase D activity at concentrations up to 100 μM. In H-ras ...
This page contains information on the chemical Glycine, N,N-bis(2-(bis(carboxymethyl)amino)ethyl)-, sodium salt including: 4 synonyms/identifiers.
Butanedioic acid, sulfo-, 4-[1-methyl-2-[(1-oxo-9-octadecenyl)amino]ethyl] ester, disodium salt | C25H43NNa2O8S | CID 106836 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
N-[3-[Bis-(2-hydroxyethyl)amino]propyl]hexadecan-1-amide/ACM66161657 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
N-{3-oxo-3-[(1,2,2,6,6-pentamethylpiperidin-4-yl)amino]propyl}furan-2-carboxamide | C18H29N3O3 | CID 1502175 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
[65 Pages Report] Check for Discount on [3-[(ethylimidocarbonyl)amino]propyl]trimethylammonium iodide Global Market and Forecast Research report by ChemReport. DescriptionWe provide independent and unbiased information on manufacturers, prices, production...
Learn more about [(2-{[2-(2,4-Dichlorophenyl)ethyl]amino}-2-oxoethyl)(4-methoxyphenyl)amino]acetic acid. We enable science by offering product choice, services, process excellence and our people make it happen.
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
Alfa Chemistry is the worlds leading provider for special chemicals. We offer qualified products for 86218-08-8((Z)-3-[2-(2-oxoimidazolidin-1-yl)ethylcarbamoyl]prop-2-enoic acid),please inquire us for 86218-08-8((Z)-3-[2-(2-oxoimidazolidin-1-yl)ethylcarbamoyl]prop-2-enoic acid).
reaction mass of N,N-ethane-1,2-diylbis(hexanamide) and 12-hydroxy-N-[2-[(1-oxyhexyl)amino]ethyl]octadecanamide and N,N-ethane-1,2-diylbis(12-hydroxyoctadecan amide) ...
Literature References: Selective a1-adrenergic receptor agonist. Prepn: GB 1145637; M. Giani et al., US 3646144 (1969, 1972 both to Zambeletti). Pharmacology: Scrollini et al., Atti Accad. Med. Lomb. 25, 193, 203 (1970), C.A. 76, 54270a, 54425e (1972). Pharmacokinetics and metabolism: P. Boselli et al., Arzneim.-Forsch. 26, 2038 (1976); M. S. Benedetti et al., ibid. 27, 158 (1977). TLC determn: G. Musumarra et al., J. Chromatogr. 350, 151 (1985). Double blind clinical evaluations: V. Baldrighi et al., Curr. Med. Res. Opin. 9, 78 (1984); U. Marini et al., ibid. 265. ...
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Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
N,N-butane-1,4-diylbis[1-hydroxy-N-(3-{[(1-hydroxy-6-oxo-1,6-dihydropyridin-2-yl)carbonyl]amino}propyl)-6-oxo-1,6-dihydropyridine-2-carboxamide ...
Product Number: C6750 CAS number: 960058-93-9 unlabeled free base Synonyms: [2H7]-2-Propenoic acid, 3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]. ...
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Antimuscarinic drugs form the mainstay of medical treatment for Overactive bladder Syndrome (OAB). With a proven efficacy but poor tolerability, other treatment modalities have been sought. Recent concerns regarding cumulative anticholinergic load and risk of dementia have provided further impetus to find novel OAB treatments. β3-adrenoceptor (β3-AR) agonists improve OAB symptoms by relaxing bladder tissue. As such, the search is underway to develop β3-AR agonist drugs for the treatment of OAB. Areas covered: The authors discuss studies on the only approved β3-AR agonist, mirabegron, followed by reports on β3-AR agonists in development, namely ritobegron and solabegron ...
0085] wherein R1 is unsubstituted hydroxy or amino, or hydroxy or amino substituted with one or more C1-6 hydroxyalkyl groups, R3 and R5 are each independently hydrogen, hydroxy, amino, or amino substituted with C1-6 alkyl, C1-6 alkoxy, or C1-6 hydroxyalkyl group; and R2, R4, and R6 are each independently hydrogen, C1-6 alkoxy, C1-6 hydroxyalkyl, or C1-6 alkyl, or R3 and R4 together may form a methylenedioxy or ethylenedioxy group. Examples of such compounds include meta-derivatives such as phenols, meta-aminophenols, meta-phenylenediamines, and the like, which may be unsubstituted, or substituted on the amino group or benzene ring with alkyl, hydroxyalkyl, alkylamino groups, and the like. Suitable couplers include m-aminophenol, 2,4-diaminotoluene, 4-amino, 2-hydroxytoluene, phenyl methyl pyrazolone, 3,4-methylenedioxyphenol, 3,4-methylenedioxy-1-[(β-hydroxyethyl)amino]benzene, 1-methoxy-2-amino-4-[(β-hydroxyethyl)amino]benzene, 1-hydroxy-3-(dimethylamino)benzene, ...
This in vitro study was performed to assess the corneal damage potential by means of the BCOP assay using fresh bovine corneae. After a first opacity measurement of the fresh bovine corneae (t0), the 20% (w/v) suspension in saline of the test item , the positive, and the negative controls were applied to corneae and incubated for 240 minutes at 32± 1 °C. After the incubation phase the test item, the positive, and the negative controls were each rinsed from the corneae andopacity was measured again (t240). After the opacity measurements permeability of the corneae was determined by measuring spectrophotometrically the transfer of sodium fluorescein after incubation in a horizontal position for 90 minutes at 32 ± 1 °C. With the negative control (saline) neither an increase of opacity nor permeability of the corneae could be observed (mean IVIS = 0.75). The positive control (10% (w/v) Benzalkonium chloride in saline) showed clear opacity and distinctive permeability of the corneae (mean IVIS = ...
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It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific ... Zhao, Jin; Golozoubova, Valeria; Cannon, Barbara; Nedergaard, Jan (July 2001). "Arotinolol is a weak partial agonist on beta 3- ... adrenergic receptors in brown adipocytes". Can J Physiol Pharmacol. 79 (7): 585-593. doi:10.1139/cjpp-79-7-585. PMID 11478592. ... Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. ...
... (code name GW-427,353) is a drug which acts as a selective agonist for the β3 adrenergic receptor. It is being ... 2008). "Randomized, double-blind, placebo (PLA)-controlled, crossover study to evaluate efficacy and safety of the beta 3- ... selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog". ... adrenergic receptor agonist solabegron (SOL) in patients with irritable bowel syndrome (IBS)". Neurogastroenterol Motil. 20 ( ...
Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel function, and ... Solabegron relaksira glatke mišiće bešike putem stimulacije beta-3 adrenoceptora. To je nov mehanizam u poređenju sa trenutno ... GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases ... Solabegron (GW-427,353) je lek koji deluje kao selektivni agonist za β3 adrenergički receptor. On je u razvoju za tretman ...
"Role of phosphorylation in agonist-promoted beta 2-adrenergic receptor sequestration. Rescue of a sequestration-defective ... 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 ...
ISBN 0-443-07145-4. Philipson, L. H. (December 2002). "beta-Agonists and metabolism". The Journal of Allergy and Clinical ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ...
"Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic ... is a beta-adrenergic receptor, and also denotes the human gene encoding it. Actions of the β3 receptor include Enhancement of ... Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through ...
The beta-adrenergic receptor kinase specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G ... Overall, the beta adrenergic receptor kinase 2 has 85% amino acid similarity with beta adrenergic receptor kinase 1, with the ... Beta-adrenergic receptor kinase 2 (beta-ARK-2) also known as G-protein-coupled receptor kinase 3 (GRK3) is an enzyme that in ... 1991). "Cloning, expression, and chromosomal localization of beta-adrenergic receptor kinase 2. A new member of the receptor ...
"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 ...
β adrenergic receptor antagonists (also called beta-blockers or β-blockers) were initially developed in the 1960s, for the ... partial adrenergic agonist activity (pindolol), concomitant α-adrenergic blocking activity (for example labetalol and ... β-blockers can be selective for either β1, β2 adrenergic receptor, or to be non-selective. By blocking β1 receptor it is ... β1-receptors are located in the heart and consist of about 75% of all β-receptors. β2-receptors can be found in the smooth ...
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 ...
... , like arrestin beta 1, was shown to inhibit beta-adrenergic receptor function in vitro. It is expressed at high ... The protein may interact with the agonist DOI in 5-HT2A receptor signaling. Arrestin beta 2 has been shown to interact with ... "Regulation of receptor fate by ubiquitination of activated beta 2-adrenergic receptor and beta-arrestin". Science. 294 (5545): ... Lefkowitz RJ (July 1998). "G protein-coupled receptors. III. New roles for receptor kinases and beta-arrestins in receptor ...
... are capable of exerting low-level agonist activity at the β-adrenergic receptor while simultaneously acting as a receptor site ... beta-blockers, β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor ... Beta blockers must not be used in the treatment of selective alpha-adrenergic agonist overdose. The blockade of only beta ... Beta blockers, due to their antagonism at beta-1 adrenergic receptors, inhibit both the synthesis of new melatonin and its ...
Selective agonists to the beta-1 receptor are: Denopamine Dobutamine (in cardiogenic shock) Xamoterol (cardiac stimulant) (Beta ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic ... The beta-1 adrenergic receptor (β1 adrenoreceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the ... "The cardiac beta-adrenergic receptor. Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by ...
ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... A Beta-2 adrenergic antagonist (β2-adrenoceptor antagonist) is an adrenergic antagonist which blocks the beta-2 adrenergic ... Fitzgerald, JD; Wale, JL (1983). "The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)". J Cardiovasc ... receptors of cells, with either high specificity (an antagonist which is selective for β2 adrenoceptors) like Butaxamine and ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... "A cell-based assay to assess the persistence of action of agonists acting at recombinant human beta(2) adrenoceptors". Journal ...
... is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... In particular, it is a partial agonist at beta2- receptors located in the vascular smooth muscle. Labetalol relaxes vascular ... Labetalol is a dual alpha (α1) and beta (β1/β2) adrenergic receptor blocker and competes with other Catecholamines for binding ... Labetalol was the first drug created that combined both alpha- and beta- adrenergic receptor blocking properties. It was ...
... where it serves as a full agonist at mouse (not necessarily human) TAAR1. It is also an agonist at beta-adrenergic receptors. A ... Pharmacologically, it is a TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors. It is the ... Taiwan banned ractopamine along with other beta-adrenergic agonists in October 2006, but in 2012, its legislature passed ... "Beta-agonists hog the limelight". The Star. November 5, 2006. Retrieved January 25, 2012. "Vet Dept seals 10 pig farms". The ...
1989). "Beta 1- and beta 2-adrenergic receptor-mediated adenylate cyclase stimulation in nonfailing and failing human ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation.". J. Biol. Chem. 263 (9): ... Beta-2 adrenergički receptor (β2 adrenoreceptor), takođe poznat kao ADRB2, je beta-adrenergički receptor.[3] ... Frielle T, Caron MG, Lefkowitz RJ (1989). "Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by ...
... a protein that regulates beta-adrenergic receptor function". Science. 248 (4962): 1547-50. doi:10.1126/science.2163110. PMID ... "Core engagement with β-arrestin is dispensable for agonist-induced vasopressin receptor endocytosis and ERK activation". ... Lefkowitz RJ, Shenoy SK (April 2005). "Transduction of receptor signals by beta-arrestins". Science. 308 (5721): 512-7. doi: ... Increased accessibility of these sites in receptor-bound arrestin targets the arrestin-receptor complex to the coated pit. ...
"The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor into ... "The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329): 241-4. doi: ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... Lohse MJ, Benovic JL, Codina J, Caron MG, Lefkowitz RJ (June 1990). "beta-Arrestin: a protein that regulates beta-adrenergic ...
... is a cytosolic protein and acts as a cofactor in the beta-adrenergic receptor kinase (BARK) mediated ... Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G protein- ... 1990). "beta-Arrestin: a protein that regulates beta-adrenergic receptor function". Science. 248 (4962): 1547-50. doi:10.1126/ ... 2000). "The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor ...
Limbird LE, Meyts PD, Lefkowitz RJ (June 1975). "Beta-adrenergic receptors: evidence for negative cooperativity". Biochem. ... "A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers". Proc. Natl. Acad. Sci. U.S.A. ... and hetero-oligomerization of β2-adrenergic receptor in receptor trafficking, signaling pathways and receptor pharmacology". ... "The size of the mammalian lung beta 2-adrenergic receptor as determined by target size analysis and immunoaffinity ...
The human beta-2 adrenergic receptor in complex with the partial inverse agonist carazolol.[1] ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... Crystal structure of activated beta-2 adrenergic receptor in complex with Gs(PDB entry 3SN6). The receptor is colored red, Gα ... "The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329): 241-4. doi: ...
"G(i)-dependent localization of beta(2)-adrenergic receptor signaling to L-type Ca(2+) channels". Biophys. J. 79 (5): 2547-56. ... Mechanism of agonist activation. J. Biol. Chem., 273, 17979-17982.. *Lefkowitz, R.J. (1998). G protein-coupled receptors. III. ... Biogeno aminski receptor - Eikozanoidni receptor (Prostaglandinski receptor) - G protein-spregnuti receptor - Imunski receptor ... New roles for receptor kinases and beta-arrestins in receptor signaling and desensitization. J. Biol. Chem., 273, 18677-18680. ...
The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group ... This is because adrenergic stimulation by agonists, results in normal calcium channel regulation. If these adrenergic receptors ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... Alpha blocker Beta blocker Adrenergic Receptor Antagonist Sympathetic nervous system Propanolol Beta-blockers and the treatment ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... Alfa-2 (α2) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. ...
... adrenergic receptor-mediated diseases, conditions, or disorders in a mammal which methods comprise administering to the mammal ... R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, X, and Y, are as defined herein.The invention further provides ... beta..sub.3 adrenergic receptor agonists of structural Formula (I), ##STR1##the stereoisomers and prodrugs thereof, and the ... beta..sub.1 and .beta..sub.2 Receptor Selectivity. In vivo selectivity for .beta..sub.1 and .beta..sub.2 receptors may be ...
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level relative to isoproterenol. ...
The Physiological Responses and Adaptation of Brown Adipose Tissue to Chronic Treatment With Beta-3-Adrenergic Receptor ... Agonists Next Previous Table of Contents * At a glance * Trial Overview * Purpose ... The Physiological Responses and Adaptation of Brown Adipose Tissue to Chronic Treatment With Beta-3-Adrenergic Receptor ...
Adrenergic beta-3 Receptor Antagonists* * Adrenergic beta-Antagonists / administration & dosage* * Adult * Body Weight / drug ... Objective: Our objective was to test the safety and metabolic effects of a novel beta(3)-adrenoreceptor agonist (TAK-677) in ... Lack of an effect of a novel beta3-adrenoceptor agonist, TAK-677, on energy metabolism in obese individuals: a double-blind, ... 3-((2R)-(((2R)-3-chlorophenyl)-2-hydroxyethyl)amino)propyl)-1H-indol-7-yloxy)acetic acid ...
Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Comparisons of the Impact of Beta-3 Agonist Versus Antimuscarinics on Psychological Distress, Sexual Function, Bladder Wall ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Adrenergic beta-3 Receptor Agonists. Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Regular use of any inducer of liver metabolism (e.g. barbiturates, rifampin) in the 3 months prior to admission to the Clinical ... History of smoking more than 10 cigarettes (or equivalent amount of tobacco) per day within 3 months prior to admission to the ... Male subject must agree to sexual abstinence and/or use a highly effective method of birth control from screening until 3 ...
... cholinergic agonists, anticancer drugs, immunosuppressive agents, antiviral agents, antibiotic agents, appetite suppressants, ... 60/22.5/10/2.5/2.5/2.5 25 3 5.52 1.38 EtOH/H.sub.2 O/Gly/GDO/ML/OA4. 60/22.5/10/2.5/2.5/2.5 75 8 3.35 2.18 EtOH/H.sub.2 O/Gly/ ... 60/28/10/1/1 30 3 13.03 3.35 EtOH/H.sub.2 O/Gly/GMO/ML3. 60/28/10/1/1 25 3 12.98 2.06 EtOH/H.sub.2 O/Gly/GMO/ML4. 60/28/10/1/1 ... 40/54/5/1 40 5 38.8 18.9 EtOH/H.sub.2 O/Gly/GMO 20 12 17.5 5.1 10 6 10.1 3.3 5 3 8.0 1.43. 30/63/5/2 40 6 23.9 10.0 EtOH/H.sub. ...
The effect of beta-3 adrenergic receptor agonist on micromotions of major pelvic ganglion disconnected rat bladder. View Poster ... Beta-3 adrenergic receptor agonist is known to alleviate rodent bladder microcontractions by inhibiting afferent pathway. ... These results also suggest that the major action point of the beta 3 adrenergic receptor agonist is in the bladder. ... We have investigated the effect of beta-3 adrenergic receptor agonist (CL-316,243) on micromotion of major pelvic ganglion ...
These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?) and What is the role of beta-adrenergic ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?. Updated: Sep 23, 2019 ...
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.. Parmee ER, Naylor EM, Perkins L, ... Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.. Weber AE, Mathvink RJ, Perkins L, ... Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.. Naylor EM, Parmee ER ... Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.. Brockunier LL, Candelore ...
"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 ...
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); DRB57K47QC (Celiprolol); Y41JS2NL6U (Bisoprolol). ... Dopamine receptor agonists.iii. Dopamine receptor antagonists.iv. Dopamine-depletor drugs.v. Drugs that increase the production ... 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); 0 (Cytokines); 0 (Interleukin-6); 0 (Lipids); ... 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Vasodilator Agents); 268B43MJ25 (Uric Acid); 2TN51YD919 (Hypoxanthine); ...
We recently described an important role played by the TGF-beta/Smad3 signaling pathway in modulating the appearance of brown ... We recently described an important role played by the TGF-beta/Smad3 signaling pathway in modulating the appearance of brown ... A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent. J. ... beta3-adrenergic receptors mediate CL 316,243 agonist-induced effects on energy expenditure, insulin secretion, and food intake ...
It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific ... Zhao, Jin; Golozoubova, Valeria; Cannon, Barbara; Nedergaard, Jan (July 2001). "Arotinolol is a weak partial agonist on beta 3- ... adrenergic receptors in brown adipocytes". Can J Physiol Pharmacol. 79 (7): 585-593. doi:10.1139/cjpp-79-7-585. PMID 11478592. ... Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. ...
Among the most significant are chemokine receptors, β-adrenergic receptors, and angiotensin II AT1 receptors (13-16). ... 2002) Beta(1)/beta(2)/beta(3)-adrenoceptor knockout mice are obese and cold-sensitive but have normal lipolytic responses to ... 2001) Agonist-dependent recruitment of phosphoinositide 3-kinase to the membrane by beta-adrenergic receptor kinase 1. A role ... including chemokine receptors, β-adrenergic signaling, and angiotensin II receptors (13-17). On activation, PI3Kγ controls two ...
... is a drug which acts as a selective agonist for the β3 adrenergic receptor. It is being developed for the treatment of ... Agonist. General Function. Protein homodimerization activity. Specific Function. Beta-adrenergic receptors mediate the ... Solabegron (GW-427,353) is a drug which acts as a selective agonist for the β3 adrenergic receptor. It is being developed for ... selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. J ...
Rasmussen, H., Figtree, G., Krum, H., Bundgaard, H. (2009). The use of beta3-adrenergic receptor agonists in the treatment of ... Beta 3 adrenergic receptor stimulation as a novel treatment for limb and wound complications associated with Type 2 diabetes; ... Rasmussen, H., Figtree, G., Krum, H., Bundgaard, H. (2009). The use of beta3-adrenergic receptor agonists in the treatment of ... No association of G-protein-coupled receptor kinase 5 or β-adrenergic receptor polymorphisms with Takotsubo cardiomyopathy in a ...
... of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides p... ... PHENYL AMINO SQUARATE AND THIADIAZOLE DIOXIDE BETA-3 ADRENERGIC RECEPTOR AGONISTS. This invention provides compounds of Formula ... The present invention provides non-steroidal compounds of formula (I) which are selective modulators (i.e., agonists and ... IL-8 RECEPTOR ANTAGONISTS. This invention relates to the novel use of dianilino squarates in the treatment of disease states ...
Beta-adrenergic agonists. These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder ... Alpha-adrenergic agonists. Alpha agonists, such as midodrine (Pro-Amatine) or pseudoephedrine (Sudafed), may improve symptoms ... They possess both a central and peripheral anticholinergic effect, as well as being alpha-adrenergic agonists and central ... Mirabegron (Myrbetriq), a beta-3 adrenergic receptor agonist, causes relaxation of the detrusor miuscle and increases bladder ...
Adrenergic Agonists. Phase 4. 18. Adrenergic beta-3 Receptor Agonists. Phase 4. ... Selective Estrogen Receptor Modulators. Phase 2. 38. Testosterone 17 beta-cypionate. Phase 2. ... 17-Hydroxy-(17-beta)-androst-4-en-3-one. 17-Hydroxy-10,13-dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro- ... 3. INS p.Arg46Gln. VAR_063729 rs121908260 ClinVar genetic disease variations for Maturity-Onset Diabetes of the Young, Type 10: ...
Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, ... The pharmacokinetics of a thiazole benzenesulfonamide beta 3-adrenergic receptor agonist and its analogs in rats, dogs, and ... Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role ... Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4- ...
... beta-adrenergic hormones, retinoids, PPARγ and PPARα agonists, and the liver X receptor.. Exercise and peroxisome proliferator- ... Liver X Receptor Beta (LXRβ). The Kuding in LipoMorph suppresses lipogenesis through antagonism of LXRβ.. * Beta- ... Unlike other beta adrenergic receptors, which are widely distributed about the body, being found in cardiac tissue, skeletal ... Retinoic acid is necessary for induction of human UCP1 by beta-adrenergic agonists. [28] ...
A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. J. Clin. Invest. 101(11): 2387- ... Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. Bioorg. Med. Chem. Lett. 8(9): 1107-1112. PMID ... L-755,507 is also a very potent and selective β3-AR adrenergic receptor partial agonist, selective over both β1-AR and β2-AR ... Synonym: 4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]- ...
... surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, ... Hadcock JR and Malbon CC (1988) Down‐regulation of betaadrenergic receptors: agonist‐induced reduction in receptor mRNA levels ... Shumay E, Gavi S, Wang HY and Malbon CC (2004) Trafficking of beta2‐adrenergic receptors: insulin and betaagonists regulate ... 1996) The betaadrenergic receptor is a substrate for the insulin receptor tyrosine kinase. Journal of Biological Chemistry 271 ...
  • Portal hypertension and liver cirrhosis in rats: effect of the ß3-adrenoceptor agonist SR58611A. (abcam.com)
  • Selection of 3 β-adrenoceptor agonists (Cat. (tocris.com)
  • If you know of a relevant reference for β -Adrenoceptor Agonist Tocriset™, please let us know . (tocris.com)
  • Do you know of a great paper that uses β -Adrenoceptor Agonist Tocriset™ from Tocris? (tocris.com)
  • Be the first to review β -Adrenoceptor Agonist Tocriset™ and earn rewards! (tocris.com)
  • Our work reported in this review focuses on a potential new target for tocolytic drugs, the β 3 -adrenoceptor (ADRB3). (biomedcentral.com)
  • Among these treatments, β 2 -adrenoceptor (ADRB2) agonists are becoming less used worldwide as tocolytic agents because of important maternal and fetal side effects. (biomedcentral.com)
  • Myocardial beta-adrenergic receptor expression and signal transduction after chronic volume-overload hypertrophy and circulatory congestion. (ahajournals.org)
  • Thus, a primary defect in intrinsic contractile function is not a necessary component for abnormalities of the myocardial beta AR-responsive adenylyl cyclase pathway. (ahajournals.org)
  • One patient who had suffered an acute myocardial infarction with heart failure resistant to vasodilators, beta-agonists, and balloon counterpulsation was stabilized with milrinone for 21 days. (springer.com)
  • Nadolol has no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, Nadolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action. (drugs.com)
  • Beta blockers ( beta-blockers , β-blockers , etc.) are a class of medications that are predominantly used to manage abnormal heart rhythms , and to protect the heart from a second heart attack ( myocardial infarction ) after a first heart attack (secondary prevention). (wikipedia.org)
  • Finally, we reported that contrary to ADRB2, the human myometrial ADRB3 is resistant to long-term agonist-induced desensitisation. (biomedcentral.com)
  • These compelling data confirm the clinical potential interest of ADRB3 agonists in the pharmacological management of preterm labour. (biomedcentral.com)
  • Tocrisets contain 3-5 ligands supplied as lyophilized solids or pre-dissolved in DMSO at a specified concentration. (tocris.com)
  • Another of our translational research projects is focused on Beta 1- adrenergic (β1-ADR) ligands as memory enhancers for cognitive disorders, and exploring the use of β1-ADR as a significant therapeutic target for AD. (stanford.edu)
  • Arbutamine Befunolol Bromoacetylalprenololmenthane Broxaterol Cimaterol Cirazoline Etilefrine Hexoprenaline Higenamine Isoxsuprine Mabuterol Methoxyphenamine Oxyfedrine Ractopamine Reproterol Rimiterol Tretoquinol Tulobuterol Zilpaterol Zinterol Alpha-adrenergic agonist "WHAT ARE BETA-AGONISTS? (wikipedia.org)
  • Ordinary white fat stores energy in the form of fat droplets, one droplet per adipocyte, which can be broken down by lipolysis into free fatty acids which are circulated into the blood stream and transported to the fuel-requiring tissue where they undergo beta-oxidation to acetyl-CoA which can be used to generate energy through the Krebs cycle. (anabolicminds.com)
  • Results showed that NNK, after 5-h treatment, stimulated cell proliferation, enhanced α7-nicotinic acetylcholine receptor (α7-nAChR) mRNA levels and nuclear factor-κB (NF-κB) DNA binding activity, as well as 5-lipoxygenase and cyclooxygenase-2 protein expressions. (aspetjournals.org)
  • The risk or severity of hypertension can be increased when 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid is combined with Solabegron. (drugbank.ca)
  • The risk or severity of hypertension can be increased when 3,4-Methylenedioxyamphetamine is combined with Solabegron. (drugbank.ca)
  • The most frequent adverse events (0.2%) leading to discontinuation in Studies 1, 2 and 3 for the 25 mg or 50 mg dose were nausea, headache, hypertension , diarrhea, constipation, dizziness and tachycardia . (rxlist.com)
  • For the treatment of primary hypertension, in comparison with other first-line anti-hypertensive drugs, first-line beta-blockers are not as effective in preventing stroke and total cardiovascular events as first-line diuretics , drugs inhibiting the renin-angiotensin system and calcium channel blockers . (netlibrary.net)
  • For the treatment of primary hypertension, meta-analyses of studies which mostly used atenolol have shown that although beta blockers are more effective than placebo in preventing stroke and total cardiovascular events, they are not as effective as diuretics , medications inhibiting the renin-angiotensin system (e.g. (wikipedia.org)