Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
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.
Drugs that bind to and activate dopamine receptors.
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.
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.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
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.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
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.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
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.
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.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
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.
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.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
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.
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.
Drugs that selectively bind to and activate beta-adrenergic receptors.
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.
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.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
Drugs that bind to and activate adrenergic receptors.
A selective D1 dopamine receptor agonist used primarily as a research tool.
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.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
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.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
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).
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.
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.
A dopamine D2/D3 receptor agonist.
Drugs that bind to and activate excitatory amino acid receptors.
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.
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.
A family of hexahydropyridines.
Compounds with BENZENE fused to AZEPINES.
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
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.
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.
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.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
Drugs that selectively bind to and activate alpha adrenergic receptors.
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.
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.
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.
Established cell cultures that have the potential to propagate indefinitely.
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.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
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.
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)
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.
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.
A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.
Drugs that bind to and activate cholinergic receptors.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
OXAZINES with a fused BENZENE ring.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
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.
A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.
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.
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.
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.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.
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.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.
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.
Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.
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.
The observable response an animal makes to any situation.
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.
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.
A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
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.
A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.
A series of structurally-related alkaloids that contain the ergoline backbone structure.
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.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
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.
Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.
Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.
Purine bases found in body tissues and fluids and in some plants.
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.
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)
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.
Elements of limited time intervals, contributing to particular results or situations.
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.
Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.
Agents inhibiting the effect of narcotics on the central nervous system.
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.
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.
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.
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.
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.
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.
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.
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.
The rate dynamics in chemical or physical systems.
A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.
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.
The physical activity of a human or an animal as a behavioral phenomenon.
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.
Peptides composed of between two and twelve amino acids.
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
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.
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.
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)
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.
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.
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.
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.
Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.
Compounds that bind to and activate PURINERGIC RECEPTORS.
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.-.
The most common inhibitory neurotransmitter in the central nervous system.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
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.
A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.
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.
Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.
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.
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.
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
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 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.
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.
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.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
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.
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.
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.
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.
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).
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
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.
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)
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
Proteins prepared by recombinant DNA technology.
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 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.
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.
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.
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.
Use of electric potential or currents to elicit biological responses.
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.
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.
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)
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.
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.
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
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.
A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.
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.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
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.
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.
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.
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.
Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
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.
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.
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.
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.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
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.
A histamine H2 receptor agonist that is often used to study the activity of histamine and its receptors.
Compounds containing the PhCH= radical.
A group of compounds that contain the structure SO2NH2.
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 into the cerebral ventricles.
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.
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
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).
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.
Morphine derivatives of the methanobenzazocine family that act as potent analgesics.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.

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.
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Read about the chemical and physical properties of [{2-[[(2-Fluoro-4-sulfamoyl-phenylcarbamoyl)-methyl]-(2-hydroxy-phenyl)-amino]-ethyl}-(2-hydroxy-phenyl)-amino]-acetic acid. Get [{2-[[(2-Fluoro-4-sulfamoyl-phenylcarbamoyl)-methyl]-(2-hydroxy-phenyl)-amino]-ethyl}-(2-hydroxy-phenyl)-amino]-acetic acid molecular formula, CAS number, boiling point, melting point, applications, synonyms and more here.
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.
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-[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...
MN-221 is a novel, highly selective ß2-adrenergic receptor agonist being developed for the treatment of exacerbations of asthma/COPD. We licensed MN-221 from Kissei Pharmaceutical Co., Ltd. Preclinical studies conducted in vitro and in vivo showed MN-221 to be highly selective for the ß2-adrenergic receptor. In these studies, the ß1-adrenergic receptor stimulating activity of MN-221 was less than that of other ß2-adrenergic receptor agonists in isolated rat atrium and in vivo cardiac function tests in rats, dogs and sheep, thereby suggesting that MN-221 may stimulate the heart less than older, less selective ß2-adrenergic receptor agonists. In addition, in vitro studies also suggested that MN-221 may act as only a partial ß1-adrenergic receptor agonist in cardiac tissue, while acting as a full ß2-adrenergic receptor in lung tissue. We believe that this improved receptor binding and functional selectivity may result in fewer cardiovascular side effects than are commonly observed with other ...
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.
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Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic
2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydrofuran-2-yl]methyl (3R)-3-hydroxy-4-({3-oxo-3-[(2-sulfanylethyl)amino]propyl}amino)-2,2-dimethyl-4-oxobutyl dihydrogen ...
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. ...
Find quality suppliers and manufacturers of 1694-06-0(Benzenesulfonamide,N-(aminocarbonyl)-4-methyl-) for price inquiry. where to buy 1694-06-0(Benzenesulfonamide,N-(aminocarbonyl)-4-methyl-).Also offer free database of 1694-06-0(Benzenesulfonamide,N-(aminocarbonyl)-4-methyl-) including MSDS sheet(poisoning, toxicity, hazards and safety),chemical properties,Formula, density and structure, solution etc.
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Structure, properties, spectra, suppliers and links for: 2-({2-[(5-Chloro-2-pyridinyl)amino]ethyl}amino)-1-(1,3-thiazolidin-3-yl)ethanone.
Record for ((4-Methoxyphenyl){2-oxo-2-[(2-pyridin-2-ylethyl)-amino]ethyl}amino)acetic acid, CAS Number , MDL Number MFCD12027579.
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2-amino-N-(quinolin-8-yl)benzenesulfonamide; CAS Number: 16082-64-7; Linear Formula: C15H13N3O2S; find Liverpool ChiroChem-LIVH93E9FC02 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich
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Buy high quality 1,1,2,2,3,3,4,4,5,5,5-Undecafluoro-1-pentanesulfonic Acid Sodium Salt 630402-22-1 from toronto research chemicals Inc.
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 ...
As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
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]. ...
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]. ...
Methods and kits for treating or preventing psoriasis or a symptom associated with psoriasis in a subject are described. The methods involve topical applications to the subject a therapeutically effective amount of an α2 adrenergic receptor agonist, such as brimonidine.
China Concrete Admixture Retarder Gluconic Acid Sodium Salt, Find details about China Gluconic Acid Sodium Salt, Sodium Gluconate from Concrete Admixture Retarder Gluconic Acid Sodium Salt - Shandong Jufu Chemical Technology Co., Ltd.
Development policies and plans are also discussed as well as manufacturing processes and cost structures. Humic Acid Sodium market report also states import/export, supply and figures as well as cost, price, revenue and gross margin by regions (United States, EU, China and Japan), and other regions can be added.. For Pre-Order Enquiry on Humic Acid Sodium market, [email protected] http://www.360marketupdates.com/enquiry/pre-order-enquiry/10478147 Then, Humic Acid Sodium market report focuses on major leading industry players with information such as company profiles, product picture and specification, capacity, production, price, cost, revenue and contact information. Upstream raw materials, and downstream consumers analysis is also carried out. Whats more, the Humic Acid Sodium industry development trends and marketing channels are analysed.. For each player, product details, capacity, price, cost, gross and revenue numbers are given. Their contact information is provided for better ...
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TY - JOUR. T1 - A potent juvenile hormone mimic, 1-(4′-ethylphenoxy)-6,7-epoxy-3,7-dimethyl-2-octene, labeled with tritium in either the ethylphenyl- or geranyl-derived moiety. AU - Kamimura, Hideo. AU - Hammock, Bruce D.. AU - Yamamoto, Izuru. AU - Casida, John E.. PY - 1972. Y1 - 1972. N2 - Reduction of citral with sodium borotritide, conversion of the alcohol product to the bromo derivative, formation of the ether by reaction with 4-ethyl-phenol, and epoxidation yields 1-(4′-ethylphenoxy)-6,7 - epoxy - 3,7 - dimethyl - 2 - octene-1 -3H. Alternatively, tritiation of 4-ethylphenol with tritium water in sulfuric acid, reaction of the recovered phenol with geranyl bromide, and epoxidation yields 1 - (4′-ethylphen-3H-oxy)-6,7-epoxy-3,7-dimethyl-2-octene. the products have a high specific activity (33 to 654 mCi per mmol) and are useful in studies on the degradation and mode of action of this potent juvenile hormone mimic.. AB - Reduction of citral with sodium borotritide, conversion of the ...
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Press Release issued Oct 19, 2016: The Global and Chinese Dichloroisocyanuric Acid Sodium Market, 2011-2021 Market Research Report is a professional and in-depth study on the current state of the global Dichloroisocyanuric Acid Sodium industry with a focus on the Chinese market.
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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 = ...
1-Octanesulfonic Acid Sodium Salt HPLC - O0100-1 O0100-1 O0100-3 Chemicals, HPLC Assay (as C8H17SO3Na)(by acidimetry) .......... min 98.0% 260 nm .......... 0.02 max. 250 nm .......... 0.02 max. 240 nm .......... 0.02 max. 230 nm .......... 0.03 max. 220 nm .......... 0.04 max. 210 nm .......... 0.05 max. 200 nm .......... 0.10 max.
Chemicals - Water Treatment China, 2 Phosphonobutane 1 4 Tricarboxylic Acid Sodium Salt Pbtca Na4, 2-Phosphonobutane -1, 2, 4-Tricarboxylic Acid, Sodium salt (PBTCA•Na4) CAS No. 40372-66-5 Molecular Formula: C7H7O9P•Na4...
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Mirabegron may cause increased heart rate, headaches, increased blood pressure, nausea, diarrhoea, constipation, urinary tract infection, dizziness. Inform your healthcare professional if you are allergic to Mirabegron.
TY - JOUR. T1 - α-Adrenergic receptor agonists, but not antagonists, alter the tail-flick latency when microinjected into the rostral ventromedial medulla of the lightly anesthetized rat. AU - Haws, C. M.. AU - Heinricher, Mary. AU - Fields, H. L.. PY - 1990/11/19. Y1 - 1990/11/19. N2 - The present experiments, part of an ongoing study designed to characterise the role norepinephrine (NE) in regulating the activity of putative nociceptive modulatory neurons in the rostral ventromedial medulla (RVM), assessed the effects of α-adrenergic receptor-selective agents on the nociceptive threshold (as measured by the tail-flick withdrawal response on noxious heat). These microinjection studies were carried out in the barbiturate-anesthetized rat, a preparation which is favourable for acute neurophysiological studies. The data obtained demonstrate that, as observed by others in the awake animal, activation of α2-adrenergic receptors in the RVM produces hypoalgesia. However, unlike in the awake animal, ...
Betmiga prolonged-release tablets contain the active ingredient mirabegron, which is a type of medicine called a selective beta3 adrenoceptor agonist. It is used to treat the symptoms of an overactive bladder (OAB).
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Quinoline derivatives have diverse biological activities including anticancer activity. On the other hand, many sulfonamide derivatives exhibited good cytotoxic activity. Hybrids of both moieties may present novel anticancer agents. Chloroquinoline incorporating a biologically active benzene-sulfonamide moieties 5-21 and diarylsulfone derivatives 22 and 23 were prepared using (E)-1-(4-((E)-7-chloro-1-methylquinolin-4(1H)-ylideneamino)phenyl)-3-(dimethyl-amino)prop-2-en-1-one 4 as strategic starting material. The structure of the newly synthesized compounds were confirmed by elemental analyses and spectral data. Compound 4 was confirmed by X-ray crystallographic analysis. The prepared compounds were evaluated for their anticancer activity against Lung, HeLa, Colorectal and breast cancer cell lines. Compounds 2, 4, 7, 11, 14 and 17 showed better or comparable activity to 2′, 7′-dichlorofluorescein (DCF) as reference drug. Molecular docking of the active compounds on the active site of PI3K enzyme was
As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
The information provided herein should not be used during any medical emergency or for the diagnosis or treatment of any medical condition. A licensed medical professional should be consulted for diagnosis and treatment of any and all medical conditions. Call 911 for all medical emergencies. Links to other sites are provided for information only -- they do not constitute endorsements of those other sites ...
TYTU : Synthesis, QSAR studies, and metabolic stability of novel 2-alkylthio-4-chloro-N-(5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)benzenesulfonamide derivatives as potential anticancer and apoptosis-inducing agents ...
Sulfalene Sulfalene Systematic (IUPAC) name 4-amino-N-(4-methoxypyrimidin-5-yl)benzenesulfonamide Identifiers CAS number  ? ATC code J01ED02 PubChem
Sulfisomidine Sulfisomidine Systematic (IUPAC) name 4-amino-N-(2,6-dimethylpyrimidin-4-yl)benzenesulfonamide Identifiers CAS number 515-64-0 ATC code J01EB01
TAK-677 has no effect on 24-h RQ or fat oxidation but does slightly increase 24-h EE at the highest dose (0.5 mg BID). The acute studies showed large interindividual variability in plasma concentrations of TAK-677 indicating some possible problems with bioavailability and therefore efficacy.
The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7- tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a β 2 -adrenergic receptor agonist.
January 2016). "Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive ... Vibegron is the international nonproprietary name (INN). Vibegron is a selective agonist for the beta-3 adrenergic receptor (β3 ... receptor. The receptors are located in the kidneys, urinary tract and bladder tissue. Upon binding, the β3 receptor undergoes a ... The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment ...
It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific ... "Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes". Canadian Journal of Physiology and ... a new β-adrenergic blocking agent]. Folia Pharmacologica Japonica (English abstract) (in Japanese). 75 (7): 707-720. doi: ... Takahashi H, Yoshida T, Nishimura M, Nakanishi T, Kondo M, Yoshimura M (September 1992). "Beta-3 adrenergic agonist, BRL-26830A ...
"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 ...
Clenbuterol remains banned not as a beta-agonist, but rather an anabolic agent. Heart muscle contraction Increase cardiac ... 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 ...
... (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- ... May 2008). "Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel ... October 2007). "GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and ...
"Three-dimensional models for beta-adrenergic receptor complexes with agonists and antagonists". Journal of Medicinal Chemistry ... Beta-adrenergic agonist Beta2-adrenergic agonist "Betmiga , European Medicines Agency". www.ema.europa.eu. Retrieved 2018-10-02 ... adrenergic receptor agonist or β3-adrenoceptor agonist, also known as β3-AR agonist, are a class of medicine that bind ... In 1984 the β3 receptor was described as the third group of beta receptors in adipose tissue. This led to the development of ...
"The beta-adrenergic receptors". PMID 12439640. Yoo, B.; et al. "Beta1-adrenergic receptors stimulate cardiac contractility and ... 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, causing widening of the airways ... Most agonists of the beta receptors are selective for one or more beta-adrenoreceptors. For example, patients with low heart ...
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 ...
It works by activating the β3 adrenergic receptor in the bladder, resulting in its relaxation. Mirabegron is the first ... clinically available beta-3 agonist with approval for use in adults with overactive bladder. Mirabegron was approved for ...
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 ...
... , 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 is crucial for the development of ... "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 ...
"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. ICI binds to the β2 subtype with ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... Branca C, Wisely EV, Hartman LK, Caccamo A, Oddo S (December 2014). "Administration of a selective β2 adrenergic receptor ...
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 ...
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 ...
... but also many medications like beta blockers, β2 agonists and α2 agonists, which are used to treat high blood pressure and ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 There is no α1C receptor. There was a subtype known as C, but ... and β-Adrenergic Receptors Theory of receptor activation Desensitization of β1 receptors. ... Sep 2010). "Ghrelin secretion stimulated by {beta}1-adrenergic receptors in cultured ghrelinoma cells and in fasted mice". ...
January 2011). "The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329 ... "The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta 2-adrenergic receptor into ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, 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 ...
... where it serves as a full agonist to murine TAAR1 (not necessarily human). It is also an agonist to beta-adrenergic receptors. ... it is a phenol-based TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors. It is most ... In October 2006, Taiwan banned ractopamine along with other beta-adrenergic agonists. In a 2012 climb-down, its legislature ... "Beta-agonists hog the limelight". The Star. November 5, 2006. Archived from the original on June 29, 2011. Retrieved January 25 ...
... 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. ...
... 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 ...
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. ...
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 adrenoceptor), 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 ...
"Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists". PLOS ONE. 6 (10 ... Isoprenaline is a β1 and β2 adrenoreceptor agonist and has almost no activity on alpha adrenergic receptors. Its agonist ... Jalba, MS (2008). "Three generations of ongoing controversies concerning the use of short acting beta-agonist therapy in asthma ... Pierce, Neil; Hensley, Michael J. (1998). "Epidemiologic Studies of Beta Agonists and Asthma Deaths" (PDF). Epidemiologic ...
GRK2 was first identified as an enzyme that phosphorylated the beta-2 adrenergic receptor, and was originally called the beta ... "A polymorphism of G-protein coupled receptor kinase5 alters agonist-promoted desensitization of beta2-adrenergic receptors". ... "Regulation of beta-adrenergic receptor signaling by S-nitrosylation of G-protein-coupled receptor kinase 2". Cell. 129 (3): 511 ... Dorn GW 2nd, Liggett SB (2008). "Pharmacogenomics of beta-adrenergic receptors and their accessory signaling proteins in heart ...
... is a drug which acts as a selective agonist of the β3 adrenergic receptor, which has been investigated for various ... and beta-subtypes". British Journal of Pharmacology. 95 (3): 723-34. doi:10.1111/j.1476-5381.1988.tb11698.x. PMC 1854239. PMID ... Afeli SA, Rovner ES, Petkov GV (September 2013). "BRL37344, a β3-adrenergic receptor agonist, decreases nerve-evoked ... September 2018). "β3-adrenergic receptor activation induces TGFβ1 expression in cardiomyocytes via the PKG/JNK/c-Jun pathway". ...
... he called beta adrenotropic receptor (now β-adrenoceptor or β-adrenergic receptor). ″This concept of two fundamental types of ... β2 and β3 and the five dopamine receptors D1, D2, D3, D4 und D5. Their fine structure, without agonist or agonist-activated, is ... he called alpha adrenotropic receptor (now α-adrenoceptor or α-adrenergic receptor), while the receptor with the second rank ... J. W. Black; A. F. Crowther; R. G. Shanks; A. C. Dornhorst (1964). "A new adrenergic beta-receptor antagonist". The Lancet. 283 ...
For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta ... Sawa M, Harada H (2006). "Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists". Current ... Nebivolol while selectively blocking beta(1) receptor acts as a beta(3)-agonist. β3 receptors are found in the gallbladder, ... It works by blocking β1-adrenergic receptors in the heart and dilating blood vessels. Nebivolol was patented in 1983 and came ...
"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. ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... norepinephrine then acting on lipolysis-inducing beta receptors.. Muscle mass[edit]. Males typically have more skeletal muscle ...
... mesylate (Tornalate) is a short-acting β2 adrenergic receptor agonist used for the relief of bronchospasm in ... Walker, Susannah B.; Kradjan, Wayne A.; Bierman, C. Warren (6 May 1985). "Bitolterol Mesylate: A Beta-adrenergic Agent; ... 5 (3): 127-137. doi:10.1002/j.1875-9114.1985.tb03410.x. PMID 3895171. "ChEBI: Bitolterol". Chemical Entities of Biological ...
... β-adrenergic, as well as at SERT and VMAT (Ki = all , 1 μM), but it does have some affinity for the α2-adrenergic receptor (Ki ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... α1-adrenergic receptor antagonist (Ki = 75 nM and 86 nM, respectively).[12] It possesses low or no affinity for the 5-HT1A, 5- ...
... fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is evidence that it may have ... Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ... Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". ... is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.[1] Fenoldopam is used as ...
February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT ... 8 (3-4): 357-69. doi:10.1002/dta.1849. PMID 26391406.. *^ a b c d e f g h i j k l m Betz JM (2010). "Yohimbe". In Coates PM, ...
... a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. ... Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... Antagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol ... agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". ...
Beta-adrenergic agonist drugs have been proposed as a treatment for their effects on muscle growth and neuroprotection, but ... the AMPA receptor) that is more permeable to calcium. In ALS, there are decreased levels of excitatory amino acid transporter 2 ... 3 (17071): 17071. doi:10.1038/nrdp.2017.71. PMID 28980624.. *^ a b c d e f g h i j k l m n o p q r s t u v van Es MA, Hardiman ... Bartus RT, Bétourné A, Basile A, Peterson BL, Glass J, Boulis NM (January 2016). "β2-Adrenoceptor agonists as novel, safe and ...
Antagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol ... a new antipsychotic with combined dopamine and serotonin receptor antagonist activity". J Pharmacol Exp Ther 275 (1): 101-13. ... α1-adrenergic Antagonist (Ki = 10 nM). *mACh (IC50 ,1000 nM) [neznatan afinitet] ... 5-HT2A antagonist/inverzni agonist (Ki = 0.4 nM). *5-HT2C (Ki = 1.3 nM) ...
Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine). *Beta blockers (e.g., propranolol) ... See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... enhances hypothalamic BDNF expression in vivo by synergistic 5-HT2c receptor antagonism and sigma-1 receptor agonism". J. ...
Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ... beta-receptor agonists, follicle stimulating hormone, luteinising hormone, LHRH. gamolenic acid, gonadotropin release inhibitor ... General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ... Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ...
... has been shown to bind to two human trace amine-associated receptors, hTAAR1 and hTAAR2, as an agonist.[2] ... or by cross-coupling with beta-amino organozinc reagents, or reacting a brominated arene with beta-aminoethyl organolithium ... Leffler, Esther B.; Spencer, Hugh M.; Burger, Alfred (1951). "Dissociation Constants of Adrenergic Amines". Journal of the ... Receptors. Varies greatly across species;. Human receptors: hTAAR1[2] and hTAAR2[2]. ...
Drugs such as bromocriptine interact with the dopaminergic receptor sites as agonists with selectivity for D2 receptors, making ... beta-Ergocryptine. CH(CH3)2. CH(CH3)CH2CH3 (S). Isoleucine ... Adrenergic receptor modulators. α1. *Agonists: 6-FNE. * ... Drugs such as bromocriptine act as a dopamine receptor agonist, stimulating the nerves that control movement.[13] Newer ... at the postsynaptic level at the D2 receptor site or an agonist of dopamine at the presynaptic level at the D1 receptor site.[ ...
Re dhe vetëm beta receptor antagonist adrenergic, dichloroisoproterenol, gjithashtu ishte e pershkruara me larte dhe do të ... l epinephrine dhe-l norepinephrina me ndalim nga dichloroisoproterenol dhe dështimi i alfa blockers dhe agonist të kenë efekte ... Alquist kishte raportuar më parë se efektet adrenergic mund të klasifikohen si alfa ose beta varësi të potencë relative të ... për shkak të efekteve beta adrenergic siç tregohet nga potencies relative e-isoproterenol l,- ...
Angiotensin II receptor antagonist. *ACE inhibitor. *Alpha-adrenergic agonist. *Beta blocker. *Dopamine agonist ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ... Conversely not all PPAR agonists are fibrates, not all triglyceride lowering agents are PPAR agonists, and not all drugs that ... PPAR agonist), mode of action (reducing blood triglycerides), and are used to prevent and to treat the same disease ( ...
Ionotropic glutamate receptor modulators. AMPAR. *Agonists: Main site agonists: 5-Fluorowillardiine. *Acromelic acid ( ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... Receptor/signaling modulators. GABA receptor modulators. GABAA receptor positive modulators. Ionotropic glutamate receptor ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ...
... with gamma decay following rapidly after beta decay: I. 53. 131. ⟶. β. +. ν. ¯. e. +. Xe. ∗. 54. 131. +. 606. keV. {\ ... Meta-[I-131]iodobenzylguanidine is a radio-labeled analog of the adrenergic blocking agent guanethidine.[37] Radioactivity is ... Thyroid hormone receptor modulators. Receptor. (ligands). THR. *Agonists: Dextrothyroxine. *DIMIT. *DITPA. *Eprotirome (KB-2115 ... displaystyle {\ce {^{131}_{53}I-,\beta +{\bar {\nu }}_{e}+{^{131}_{54}Xe^{\ast }}+606keV}}}. Xe. ∗. 54. 131. ⟶. Xe. 54. 131. + ...
... an alpha-2 adrenergic agonist Irbesartan, an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH agonist, but is now ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ...
Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors.[22] ... Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine). *Beta blockers (e.g., propranolol) ... In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ...
Partial agonist at the mu opioid receptor; agonist at delta opioid receptor; antagonist at kappa opioid receptor.. Sublingual, ... "Combining opioid and adrenergic mechanisms for chronic pain". Postgraduate Medicine. 126 (4): 98-114. doi:10.3810/pgm.2014.07. ... Full agonist at kappa opioid receptors, partial agonist/antagonist at the mu opioid receptors.[39]. IM, IV, SC.. Protein ... Beta blockers. *Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... History: 2,5-DMA was first synthesized in Tuckahoe, New York by Richard Baltzly and Johannes S. Buck in 1939.[3] ... History: Experiments on psychiatric patients who were given 3,4-DMA at dosages of 70 mg to 700 mg by IV injection took place at ...
Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... "Miscellaneous Sympathomimetic Agonists". In Brunton LL, Chabner BA, Knollmann BC (eds.). Goodman & Gilman's Pharmacological ... Beta blockers. *Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... on adrenergic receptors.[83] It is most usually marketed as the hydrochloride or sulfate salt. ...
Propranolol - Sympatholytic, beta blocker.. *Clonidine - Sympatholytic, α2-adrenergic receptor agonist.. *Guanfacine - ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ... 46 (3): 424-9. doi:10.1345/aph.1Q405. PMID 22395254.. *^ Rif S. El-Mallakh; S. Nassir Ghaemi (2 April 2007). Bipolar Depression ... 11 (3): 171-83. doi:10.2165/00148581-200911030-00003. PMID 19445546.. *^ Schacter, Daniel L.; Gilbert, Daniel T.; Wegner, ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... 3,4-Methylenedioxyphenethylamine ("3,4-MDPEA" or just "MDPEA"), also known as homopiperonylamine, is a substituted ... InChI=1S/C9H11NO2/c10-4-3-7-1-2-8-9(5-7)12-6-11-8/h1-2,5H,3-4,6,10H2 ...
Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine). *Beta blockers (e.g., propranolol) ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... InChI=1S/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ... InChI=1/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ...
α-Adrenergic receptor agonists[edit]. Main article: α-Adrenergic receptor agonist. Common or widely marketed[edit]. * ... Beta blockers. *Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... Pseudoephedrine acts indirectly on the adrenergic receptor system, whereas phenylephrine and oxymetazoline are direct agonists ... α1-adrenergic receptor since they mediate vasoconstriction and constricting nasal vasculature causes decongestion of nasal ...
Epinephrine acts by binding to a variety of adrenergic receptors. Epinephrine is a nonselective agonist of all adrenergic ... Epinephrine does this by its effects on alpha and beta receptors.[7] It is found in many animals and some one cell organisms.[8 ... Epinephrine's binding to these receptors triggers a number of metabolic changes. Binding to α-adrenergic receptors inhibits ... Its actions vary by tissue type and tissue expression of adrenergic receptors. For example, high levels of epinephrine causes ...
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Frequent infusions of beta-lactam antibiotics without exceeding total daily dose would help to keep the antibiotics level above ... the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I-like receptors. Invariably, the ... This forced receptor interaction induces the production of pro-inflammatory chemical signals (cytokines) by T-cells.[40] ...
Serotonin receptor agonists. *Serotonin-norepinephrine-dopamine releasing agents. *Substituted amphetamines. Hidden categories ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... Adrenergic release blockers: Bethanidine. *Bretylium. * ...
... 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 ...
The elevation of TH activity elicited in SCG by beta adrenergic receptor agonists is always preceded by an increase of cAMP ... Induction of tyrosine hydroxylase elicited by beta adrenergic receptor agonists in normal and decentralized sympathetic ganglia ... Induction of tyrosine hydroxylase elicited by beta adrenergic receptor agonists in normal and decentralized sympathetic ganglia ... Induction of tyrosine hydroxylase elicited by beta adrenergic receptor agonists in normal and decentralized sympathetic ganglia ...
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 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 ... History of smoking more than 10 cigarettes (or equivalent amount of tobacco) per day within 3 months prior to admission to the ... Johns wort) in the 2 weeks prior to admission to the Clinical Unit, except for paracetamol (up to 3 g/day) ... Any use of drugs of abuse within 3 months prior to admission to the clinical unit ...
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 ...
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 ...
... 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. ...
Based on the example of the β3-adrenoceptor agonist m … ... "β3-Adrenoceptor agonists were originally considered as a ... Receptors, Adrenergic, beta-3 / genetics * Receptors, Adrenergic, beta-3 / physiology* * Syndrome * Translational Medical ... a paucity of public domain tools for the study of the drug target and aspects of receptor agonists as drugs had to be addressed ... β3-Adrenoceptor agonists were originally considered as a promising drug class for the treatment of obesity and/or type 2 ...
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 ...
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 ...
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 ...
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 ...
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); ...
"The beta-adrenergic receptors". PMID 12439640. Yoo, B.; et al. "Beta1-adrenergic receptors stimulate cardiac contractility and ... 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, causing widening of the airways ... Most agonists of the beta receptors are selective for one or more beta-adrenoreceptors. For example, patients with low heart ...
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 ...
January 2016). "Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive ... Vibegron is the international nonproprietary name (INN). Vibegron is a selective agonist for the beta-3 adrenergic receptor (β3 ... receptor. The receptors are located in the kidneys, urinary tract and bladder tissue. Upon binding, the β3 receptor undergoes a ... The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment ...
Weight Loss and Maintenance Related to the Mechanism of Action of Glucagon-Like Peptide 1 Receptor Agonists. Advances in ... Beta-3 adrenergic receptor agonists. This class of drugs increases energy expenditure. So far, one drug in this class has been ... Glucagon-like peptide-1 receptor agonists. Semaglutide is a medication that targets the glucagon-like peptide-1 (GLP-1) ... Sweet-sensitive taste receptors are known to be present in the mouth, gut lining, pancreas, and brain.119 By activating taste ...
... 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 ...
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 ...
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 ...
Iii beta-3 adrenergic receptor agonist. In practice, the physician during pregnancy. Anaesth intensive care unit to deliver ... Pegfilgrastim is filgrastim conjugated to polyethylene glycol epoetin beta is an acceptable treatment option for patients with ...
... 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 ...
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- ...
The effects of various adrenergic beta receptor agonists and antagonists on lipolysis (measured as glycerol release) in human ... Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs.. M Frisk-Holmberg and ... Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs.. M Frisk-Holmberg and ... Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs.. M Frisk-Holmberg and ...
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 ...
A novel combination comprising a .beta.-hairpin peptidomimetic of the formula cyclo(-Thr-Trp-Ile-Dab-Orn-.sup.DDab-Dab-Trp-Dab- ... Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart.... This ... Methods and compositions comprising desmopressin in combination with a beta-3-adrenergic receptor agonist. The invention ... in combination with a beta-3-adrenergic receptor agonist. The methods and compositions... ...
  • Dopamine receptor antagonists.iv. (bireme.br)
  • Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. (nih.gov)
  • The effects of various adrenergic beta receptor agonists and antagonists on lipolysis (measured as glycerol release) in human adipose tissue in vitro were studied. (aspetjournals.org)
  • Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. (els.net)
  • Tone in the smooth muscles of the bladder neck and proximal sphincter is decreased with alpha adrenergic antagonists. (auanet.org)
  • Our previous work has shown that alpha- and beta-adrenergic agonists activated purified and red cell CA while adrenergic antagonists inhibited CA and reduced the activating effect of agonists on this enzyme (15,16). (scielo.br)
  • Functional identification of rat atypical beta-adrenoceptors by the first beta 3-selective antagonists, aryloxypropanolaminotetralins. (abcam.com)
  • Removal of extracellular Ca2+ or addition of the Ca2+ channel antagonists nifedipine and verapamil almost totally abolished stimulations elicited by high K+ and partially attenuated receptor- and fluoroaluminate-mediated increases in inositol phosphates. (aspetjournals.org)
  • Newer drugs, such as darifenacin and solifenacin are M3 selective receptor antagonists and may be more bladder-specific and have fewer side effects such as dry mouth. (thedoctorweighsin.com)
  • The results obtained from previous studies have shown that beta-receptor antagonists stimulate food consumption in rats [ 3 ]. (zjrms.com)
  • Stereoisomers of beta-adrenergic agonists and antagonists were 9- to 300-fold more potent than their corresponding (+) stereoisomers. (duke.edu)
  • Anticholinergic agents acting as muscarinic receptor antagonists have been the primary treatment and include tolterodine, oxybutynin (e.g. (pharmacistactivist.com)
  • Beta blockers (β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, or beta adrenergic receptor antagonists ) are a class of drugs that are particularly used for the management of cardiac arrhythmias , protecting the heart from a second heart attack ( myocardial infarction ) after a first heart attack (secondary prevention), [1] and, in certain cases, hypertension . (netlibrary.net)
  • CL-316,243 group, beta-3 adrenergic receptor antagonist (SR59230A) pretreated CL-316,243 group and oxybutinin group. (auanet.org)
  • Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein. (nih.gov)
  • Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood-brain barrier, has not been investigated for this purpose. (frontiersin.org)
  • Propranolol is a non-selective beta-adrenergic antagonist that has good penetration of the blood-brain barrier ( 21 ). (frontiersin.org)
  • Rauwolscine is an alpha-2 adrenergic receptor antagonist with little to no activity on alpha-1. (drsharma.ca)
  • Potent, selective β 3 adrenoceptor antagonist (IC 50 values are 40, 408 and 648 nM for β 3, β 1 and β 2 , respectively). (abcam.com)
  • Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes. (abcam.com)
  • Here we report the raising of a mouse monoclonal antibody against human A(2A)AR that prevents agonist but not antagonist binding to the extracellular ligand-binding pocket, and describe the structure of A(2A)AR in complex with the antibody Fab fragment (Fab2838). (proteopedia.org)
  • The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. (curehunter.com)
  • Tamoxifen (Nolvadex, Istubal, Valodex) is an antagonist of estrogen receptors in breast tissue and is an agonist in the endometrium. (healthcmi.com)
  • montelukast, a cysteinyl leukotriene (CysLT)-receptor antagonist, is an alternative. (dentalcare.com)
  • low-dose inhaled corticosteroid plus montelukast, a cysteinyl leukotriene (CysLT)-receptor antagonist, is an alternative regimen. (dentalcare.com)
  • To identify directly and to quantitate these beta-adenergic receptors in human lymphocytes, (-) [3H] alprenolol, a potent beta-adrenergic antagonist, was used to label binding sites in homogenates of human mononuclear leukocytes. (duke.edu)
  • The beta-adrenergic antagonist, (-) propranolol, potently competed for the binding sites, causing half-maximal inhibition of binding at 9 nM. (duke.edu)
  • Based on the example of the β3-adrenoceptor agonist mirabegron, but also taking into consideration evidence obtained with ritobegron and solabegron, we discuss challenges facing a translational pharmacology program accompanying clinical drug development for a first-in-class molecule. (nih.gov)
  • Mirabegron (Myrbetriq), a beta-3 adrenergic receptor agonist, causes relaxation of the detrusor miuscle and increases bladder capacity. (medscape.com)
  • Mirabegron is the first FDA approved selective agonist that is currently used to treat overactive bladder (OAB). (wikipedia.org)
  • Mirabegron is a beta-3 adrenergic agonist . (rxlist.com)
  • Specifically, mirabegron is a beta - 3 adrenergic agonist which specifically targets the receptors in the detrusor muscle (97 percent of beta -3 mRNA produced by the body is produced in the detrusor muscle). (verywell.com)
  • Unlike antimuscarinic drugs, mirabegron doesn't interfere with beta-1 and beta-2 receptors in other parts of the body. (verywell.com)
  • Mirabegron is an oral [beta]3-adrenoreceptor agonist which has emerged as an alternative to antimuscarinics for the medical treatment of OAB. (thefreelibrary.com)
  • Mirabegron, a beta-3 adrenergic receptor agonist, another alternative to nonselective antimuscarinic drugs, appears to be less likely to cause dry mouth. (thedoctorweighsin.com)
  • SUMMARY Mirabegron is a kind of β3 adrenergic receptor agonist which is an effective drug for the treatment of overactive bladder. (bvsalud.org)
  • RESUMO Mirabegron é um tipo de agonista do receptor adrenérgico beta 3 que demonstra eficácia no tratamento de bexiga hiperativa. (bvsalud.org)
  • Mirabegron is a potent and selective β(3)-adrenoceptor agonist. (unboundmedicine.com)
  • A Japanese phase 3 study showed that mirabegron has excellent efficacy and safety for treating overactive bladder. (unboundmedicine.com)
  • Mirabegron is a beta-3 adrenergic receptor agonist and its activation of these receptors relaxes the detrusor muscle during the storage phase of the urinary bladder fill-void cycle, thereby increasing bladder capacity. (pharmacistactivist.com)
  • (D) They are used to stabilize the detrusor muscle, through binding and blocking muscarinic receptors. (scielo.br)
  • Recent studies suggest that antimuscarinics might suppress bladder afferent activity by blocking muscarinic receptors in the urothelium, myofibroblasts and detrusor, thereby improving overactive bladder symptoms. (unboundmedicine.com)
  • Comparisons of the Impact of Beta-3 Agonist Versus Antimuscarinics on Psychological Distress, Sexual Function, Bladder Wall Thickness and Blood Flow in Women With Overactive Bladder Syndrome: a Randomized Controlled Study. (clinicaltrials.gov)
  • MYRBETRIQ ® is a beta-3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence , urgency, and urinary frequency. (rxlist.com)
  • In three, 12-week, double-blind, placebo-controlled, safety and efficacy studies in patients with overactive bladder (Studies 1, 2, and 3), MYRBETRIQ ® was evaluated for safety in 2736 patients [see Clinical Studies ]. (rxlist.com)
  • Urovant Sciences, a biopharmaceutical company focused on developing and commercializing innovative therapies for urologic conditions, today announced the commercial launch of GEMTESA® (vibegron) 75 mg tablets, a beta-3 (β3) adrenergic receptor agonist, for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence (UUI), urgency, and urinary frequency in adults. (simonfoundation.org)
  • Urovant Sciences, Inc (Nasdaq: UROV) announced today that the U.S. Food and Drug Administration (FDA) has approved the New Drug Application (NDA) for once-daily 75 mg GEMTESA® (vibegron), a beta-3 adrenergic receptor (β3) agonist, for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence (UUI), urgency, and urinary frequency in adults. (simonfoundation.org)
  • Urovant Sciences has submitted a New Drug Application (NDA) to the Food and Drug Administration (FDA) for vibegron, a beta-3 adrenergic agonist, for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency. (simonfoundation.org)
  • Tolterodine and oxybutynin, drugs for the treatment of overactive bladder, were cited in 4 and 3 studies, respectively. (thedoctorweighsin.com)
  • Beta-3 adrenergic receptor agonist is known to alleviate rodent bladder microcontractions by inhibiting afferent pathway. (auanet.org)
  • We have investigated the effect of beta-3 adrenergic receptor agonist (CL-316,243) on micromotion of major pelvic ganglion disconnected rat bladder. (auanet.org)
  • We could observe that beta-3 adrenergic receptor agonist have effect in alleviating micromotions of MPG disconnected rat bladder. (auanet.org)
  • These results also suggest that the major action point of the beta 3 adrenergic receptor agonist is in the bladder. (auanet.org)
  • These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. (medscape.com)
  • The receptors are located in the kidneys, urinary tract and bladder tissue. (wikipedia.org)
  • Tone in the bladder neck and proximal sphincter is increased by alpha adrenergic agonists and can manifest with urinary retention, particularly in men with prostatism. (auanet.org)
  • GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. (wikipedia.org)
  • β(3)-Adrenoceptors are predominantly expressed in the human bladder and mediate relaxation of detrusor muscle. (unboundmedicine.com)
  • β(3)-Adrenoceptor agonists increase bladder capacity and prolong micturition interval. (unboundmedicine.com)
  • It is assumed that β(3)-adrenoceptor agonists could exert an inhibitory effect on bladder afferent through β(3)-adrenoceptors in the urothelium and detrusor, which eventually improve the symptom of urgency. (unboundmedicine.com)
  • Following intravenous administration to rats, the rodent selective β3AR agonist CL316243 reduces bladder pressure and in cystomeric studies increases bladder capacity leading to prolongation of micturition interval without increasing residual urine volume. (drugapprovalsint.com)
  • Gemtesa is a beta-3 adrenergic receptor agonist that activates beta-3 receptors in the bladder causing relaxation of the smooth muscle of the urinary bladder, increasing the bladder's storage capacity and helping alleviate urgency and frequency. (doctorpedia.com)
  • The pathophysiology of delirium is not fully understood, but several neurotransmitters are known to play an important role, including catecholamines ( 2 , 3 ). (frontiersin.org)
  • Adrenergic receptors (ARs) are members of the 7-transmembrane domain G-protein-coupled receptor superfamily that bind the endogenous catecholamines epinephrine and norepinephrine. (acris-antibodies.com)
  • They also provide an experimental approach to the study of states of altered sensitivity to catecholamines at the receptor level in man. (duke.edu)
  • Adrenoceptors (also called adrenergic receptors) are the receptors for the catecholamines adreline and noradreline (called epinephrine and norepinephrine in the United States). (acris-antibodies.com)
  • Beta blockers block the action of endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors , of the sympathetic nervous system , which mediates the fight-or-flight response . (netlibrary.net)
  • Tocrisets contain 3-5 ligands supplied as lyophilized solids or pre-dissolved in DMSO at a specified concentration. (tocris.com)
  • Conformational changes induced by extracellular ligands binding to G-protein-coupled receptors result in a cellular response through the activation of G proteins. (proteopedia.org)
  • These cell surface receptors are acted on by a wide variety of ligands, including small molecules and soluble proteins. (technologynetworks.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)
  • A subcutaneous injection of an oil suspension of l-epinephrine (270 mumol/kg), dopamine (270 mumol/kg) or l-norepinephrine (270 mumol/kg), when administered with phenoxybenzamine (32 mumol/kg i.p.) to blocl alpha adrenergic effects, increases the cyclic 3', 5'-adenosine monophosphate (cAMP) content in superior cervical ganglia (SCG) of rats. (aspetjournals.org)
  • Of the agonists investigated, the potency rank order was isoproteronol greater than norepinephrine greater than salbutamol. (aspetjournals.org)
  • The norepinephrine provided by the LC acts at the medial septal area (MSA) and the medial preoptic area (MPOA) to activate waking-active neurons ( via alpha-1 adrenergic receptors) and inhibit sleep-active neurons ( via alpha-2 adrenergic receptors). (frontiersin.org)
  • It is an agonist at alpha and beta adrenergic receptors which causes the release of endogenous norepinephrine (noradrenaline). (healthcmi.com)
  • Adrenergic Fibers: Nerve fibers that synthesize and release norepinephrine. (cram.com)
  • Norepinephrine is generally considered to be a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. (abmole.com)
  • Selected examples are: Arformoterol Buphenine Clenbuterol Dopexamine (β1 and β2) Epinephrine (non-selective) Fenoterol Formoterol Isoetarine Isoprenaline (INN), isoproterenol (USAN) (β1 and β2) Levosalbutamol (INN), levalbuterol (USAN) Orciprenaline (INN), metaproterenol (USAN) Pirbuterol Procaterol Ritodrine Salbutamol (INN), albuterol (USAN) Salmeterol Terbutaline These agents are also listed as agonists by MeSH. (wikipedia.org)
  • The inhibitory effect of isoproterenol, similar to that of nifedipine, was counteracted by ionomycin and also by the Ca2+ channel agonist Bay K 8644. (aspetjournals.org)
  • Heart rate responsiveness to beta AR stimulation was blunted, with ED50, for isoproterenol increased 133% (p less than 0.001) after development of circulatory congestion. (ahajournals.org)
  • In first two experiments, rats received intraperitoneal injections of isoproterenol (0, 0.5, 1 and 2 mg/kg) and Nociceptin agonist 64 - 6198 (0, 1, 2 and 4 mg/kg) respectively. (zjrms.com)
  • Isoproterenol is a non-selective beta adrenergic agonist. (zjrms.com)
  • In the peripheral nervous system, as well as the brain, isoproterenol appears to have only beta-adrenergic activity. (zjrms.com)
  • Peripheral, but not central anorectic effect of isoproterenol is mediated by beta adrenergic receptors. (zjrms.com)
  • We have now correlated this functional impairment in beta-adrenergic response with a decreased generation of cAMP in response to isoproterenol. (elsevier.com)
  • Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions. (els.net)
  • G-protein-coupled receptors are the largest class of cell-surface receptors, and these membrane proteins exist in equilibrium between inactive and active states. (proteopedia.org)
  • Our objective was to test the safety and metabolic effects of a novel beta(3)-adrenoreceptor agonist (TAK-677) in humans. (nih.gov)
  • Though its yet to be tested in humans, animal studies have determined that Cimaterol is a more powerful beta-agonist than clenbuterol, promotes protein retention and accretion, and has shown powerful anti-catabolic properties in cases of cancer or burns. (steroid.com)
  • Interestingly, among the viral receptors there is a greater diversity in the DRY-motif compared to their endogenous receptor homologous. (pubmedcentralcanada.ca)
  • In this review we will focus on these two structural motifs and discuss their role in viral 7TM receptor signaling compared to their endogenous counterparts. (pubmedcentralcanada.ca)
  • Despite the structural diversity in the repertoire of the endogenous 7TM receptor agonists, the conformational changes that occur upon receptor activation are believed to be overall identical. (pubmedcentralcanada.ca)
  • The nociceptin/orphanin FQ (N/OFQ) peptide is the endogenous ligand for the N/OFQ peptide (NOP) receptor. (zjrms.com)
  • (Department of Pharmacology and Toxicology, University of Lausanne, Switzerland) Working with Professor Kaethi Geering and Dr Stephanie Bibert to identify the candidate cysteine residue on the beta 1 subunit of Na+-K+ pump subunit that mediates its oxidative regulation. (edu.au)
  • Operating via heterotrimeric G proteins, adrenergic receptors constitute one of the most intensely studied classes of membrane proteins, whose expression and function are subject to regulation at many different levels, including transcriptional, posttranscriptional and posttranslational. (els.net)
  • Hadcock JR and Malbon CC (1988) Down‐regulation of beta‐adrenergic receptors: agonist‐induced reduction in receptor mRNA levels. (els.net)
  • Kallal L, Gagnon AW, Penn RB and Benovic JL (1998) Visualization of agonist‐induced sequestration and down‐regulation of a green fluorescent protein‐tagged beta2‐adrenergic receptor. (els.net)
  • Kohout TA and Lefkowitz RJ (2003) Regulation of G protein‐coupled receptor kinases and arrestins during receptor desensitization. (els.net)
  • Krupnick JG and Benovic JL (1998) The role of receptor kinases and receptors in G‐protein‐coupled receptor regulation. (els.net)
  • Shenoy SK, McDonal PH, Kohout TA and Lefkowitz RJ (2001) Regulation of receptor fate by ubiquitination of activated beta2‐adrenergic receptor and beta‐arrestin. (els.net)
  • The beta-3-adrenergic receptor ( ADRB3 ), located on human chromosome 8p12-p11.2, is expressed predominantly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis 3 . (jrheum.org)
  • The A(2A) adenosine receptor (A(2A)AR) is responsible for regulating blood flow to the cardiac muscle and is important in the regulation of glutamate and dopamine release in the brain. (proteopedia.org)
  • Beta-adrenergic receptors and their regulation. (springermedizin.de)
  • Furthermore, we show that the regulation of NMII takes place downstream of guidance receptor signalling and is critical to ensure efficient collective migration. (visionsxrwabbitt36.cf)
  • Beta adrenergic receptors and N/OFQ are involved in the regulation of food intake through central and peripheral mechanisms. (zjrms.com)
  • What is the role of beta-adrenergic agonists in urinary incontinence treatment? (medscape.com)
  • Treatment of Postprostatectomy Male Urinary Incontinence With the Transobturator Retroluminal Repositioning Sling Suspension: 3-Year Follow-up. (medscape.com)
  • Cheng J, Gao S, Zhu C , Liu S, Li J, Kang J, Wang Z, Wang T. Typical Stress Granule proteins interact with the 3'-UTR of Enterovirus D68 to inhibit viral replication. (academictree.org)
  • Beta adrenergic receptors physiologically inhibit food intake in mammals. (zjrms.com)
  • Differential inhibition of lipolysis in human adipose tissue by adrenergic beta receptor blocking drugs. (aspetjournals.org)
  • Dexmedetomidine is a potent alpha-2 adrenergic agonist that binds to the alpha-2 adrenergic receptor subtype A at the LC, resulting in almost complete inhibition of the LC, which has a sedative effect ( 5 , 6 ). (frontiersin.org)
  • The beta-adrenergic receptor-induced inhibition was prevented by pertussis toxin and could not be reproduced by forskolin, indicating that cAMP was not involved. (aspetjournals.org)
  • Accumulation of inositol phosphates triggered by high K+ was insensitive to the beta-adrenergic receptor inhibition. (aspetjournals.org)
  • Signaling by 7TM receptors through G proteins leads to, for example, either inhibition (G αi ) or activation (G αs ) of adenylyl cyclase and cAMP production, activation of phospholipase C with inositol triphosphate turnover (G αq ), or activation of RhoGEF (G α 12/13 ) depending on which G protein the receptor is activating [ 3 ]. (pubmedcentralcanada.ca)
  • Seven transmembrane (7TM) receptors constitute the largest superfamily of membrane proteins and function as important mediators of extracellular signals to intracellular responses. (pubmedcentralcanada.ca)
  • The Adrenoceptors are members of the G-protein-coupled receptor (GPCR) superfamily of membrane proteins. (acris-antibodies.com)
  • Vibegron is a selective agonist for the beta-3 adrenergic receptor (β3-AR) receptor. (wikipedia.org)
  • Solabegron (GW-427,353) is a drug which acts as a selective agonist for the β3 adrenergic receptor. (drugbank.ca)
  • The species orthologs of the human β-adrenoceptors found in the rat, mouse, and cow have significantly different agonist pharmacology. (guidetopharmacology.org)
  • Large differences exist in the pharmacology of agents within the class, thus not all beta blockers are used for all indications listed below. (netlibrary.net)
  • One of the mediators of the positive metabolic effects of endurance exercise is peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α). (anabolicminds.com)
  • We sought to determine the effects of activation of peroxisome proliferator-activated receptor-gamma (PPAR-gamma) on multilocularization of adipocytes in adult white adipose tissue (WAT). (bvsalud.org)
  • The most well studied models whereby brown adipocytes appear in white fat are upon cold exposure or after stimulation of the beta(3)-adrenoceptor pathways. (frontiersin.org)
  • 2004) Characterization of agonist stimulation of cAMP‐dependent protein kinase and G protein‐coupled receptor kinase phosphorylation of the beta2‐adrenergic receptor using phosphoserine‐specific antibodies. (els.net)
  • 2 These atypical receptors, now called β3-adrenoceptors, are found on the cell surface of both white and brown adipocytes where their stimulation promotes both lipolysis and energy expenditure in brown adipose tissue (BAT) and lipolysis in white adipose tissue (WAT). (dovepress.com)
  • β3 receptors are mainly located in adipose tissue. (wikipedia.org)
  • The results indicate that the adrenergic reciptor mediating lipolysis in human adipose tissue is of type beta-1. (aspetjournals.org)
  • The objective of this experiment was to study the effect of CL 316,243 (CL) (a highly selective ß3-adrenergic receptor agonist) on cellular changes occurring in retroperitoneal white adipose tissue (RWAT) of lean and obese rats. (dovepress.com)
  • 1996) The beta‐adrenergic receptor is a substrate for the insulin receptor tyrosine kinase. (els.net)
  • Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, in rats: identification of a novel isethionic acid conjugate. (nih.gov)
  • The pharmacokinetics of a thiazole benzenesulfonamide beta 3-adrenergic receptor agonist and its analogs in rats, dogs, and monkeys: improving oral bioavailability. (nih.gov)
  • Portal hypertension and liver cirrhosis in rats: effect of the ß3-adrenoceptor agonist SR58611A. (abcam.com)
  • Hajinezhad M R, Shohreh B. Possible Involvement of Beta-Adrenergic Receptors on Nociceptin/Orphanin FQ Induced Food Consumption in Male Rats, Zahedan J Res Med Sci. (zjrms.com)
  • The aim of this study was to determine the possible interaction between beta adrenergic and N/OFQ receptors on food consumption in male rats. (zjrms.com)
  • High dosages of beta adrenergic receptor agonists induce cardiomyocyte necrosis and interstitial fibrosis in rats [ 5 ]. (zjrms.com)
  • L-755,507 is also a very potent and selective β3-AR adrenergic receptor partial agonist, selective over both β1-AR and β2-AR adrenoceptor binding. (scbt.com)
  • Vibegron is a potent and selective beta 3 adrenergic receptor agonist. (abmole.com)
  • L-755,507 is a very potent and selective β 3 partial agonist. (abmole.com)
  • Fenoterol is a β2 adrenoreceptor agonist with bronchodilator activity. (abmole.com)
  • PI3Kγ is selectively recruited to G protein-coupled receptors implicated in inflammation and metabolic homeostasis, including chemokine receptors, β-adrenergic signaling, and angiotensin II receptors ( 13 - 17 ). (pnas.org)
  • A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. (scbt.com)
  • The lab also is working to determine the precise role of the "metabolic" beta-3 adrenergic receptor (ß3AR) in the heart and define the extent of its protective effect in obesity and in heart failure, including its role in maintaining nitric oxide synthase (NOS) coupling. (hopkinsmedicine.org)
  • A guideline from the American Urological Association recommends beta-3-adrenergic receptor agonists as second-line therapy in patients with an inadequate response to behavioral therapy. (medscape.com)
  • On activation, PI3Kγ controls two major second messengers: phosphatidylinositol(3,4,5)-tris-phosphate (PIP 3 ) through direct phosphorylation of phosphatidylinositol 4,5 bisphosphate and cAMP by a kinase-independent mechanism ( 18 ). (pnas.org)
  • We believe that adrenergic agonists may have a dual mechanism of action: the first one consists of a catecholamine action on its receptor with the formation of a stimulus-receptor complex. (scielo.br)
  • By this second component of the mechanism, the same stimulus directly acts on the carbonic anhydrase I isozyme (that might be functionally coupled with adrenergic receptors), so that its activation ensures an adequate pH for stimulus-receptor coupling for signal transduction into the cell, resulting in vasoconstriction. (scielo.br)
  • In the present investigation we studied the relationship between alpha- and beta-adrenergic agonists and CA activity in vasoconstriction mechanism. (scielo.br)
  • Beta blockers are known primarily for their reductive effect on heart rate, although this is not the only mechanism of action of importance in congestive heart failure. (netlibrary.net)
  • G-protein alpha-i family activation releases complex of G-protein beta/gamma , which activates c-src tyrosine kinase ( c-Src ) [ 12 ]. (bio-rad.com)
  • For example, patients with low heart rate are given beta agonist treatments that are more "cardio-selective" such as dobutamine, which increases the force of contraction of the heart muscle. (wikipedia.org)
  • Beta-2 adrenergic receptor activation also appears to be important in the MSA and MPOA, resulting in dose-dependent increases in time spent awake ( 4 ). (frontiersin.org)
  • Clenbuterol is a Beta(2) agonist similar in some structural respects to salbutamol. (drugbank.ca)
  • Thus, changes in beta-adrenergic receptor (beta AR) expression should reflect more directly the influence of neurohumoral adrenergic tone, clarifying the manner in which peripheral (neurohumoral) versus primary myocardial factors are operative in decreased beta AR-dependent signal transduction. (ahajournals.org)
  • Activation of β2 receptors induces smooth muscle relaxation in the lungs, gastrointestinal tract, uterus, and various blood vessels. (wikipedia.org)
  • Agonism of the beta(2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles. (drugbank.ca)
  • No differences in the extent or potency of β3AR agonist mediated relaxation were observed, consistent with the concept that the β3AR activation is an effective way of relaxing the detrusor in normal and pathogenic states. (drugapprovalsint.com)
  • 1987) Ligand binding to the beta‐adrenergic receptor involves its rhodopsin‐like core. (els.net)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs share many similarities in receptor phosphorylation, use of accessory proteins and sequestration of the receptors. (els.net)
  • Other studies have proved that binding of agonists to these receptors occurs when the catecholamine molecule is in the protonated state (6), all of these receptors being coupled with G proteins. (scielo.br)
  • The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. (proteopedia.org)
  • G protein-coupled receptors (GPCRs), one of the most commonly used and successful targets for drugs, are a large family of multi-transmembrane proteins and an important class of receptors. (technologynetworks.com)
  • Beta receptors are coupled to Gs proteins, which in turn are linked to adenylyl cyclase. (acris-antibodies.com)
  • 9, 10 In patients with intermittent asthma an inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol is preferred (Step 1). (dentalcare.com)
  • The patient experiences prompt relief with inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol. (dentalcare.com)
  • Indications of administration for β agonists include: Bradycardia (slow heart rate) Asthma Chronic obstructive pulmonary disease (COPD) Heart failure Allergic reactions Hyperkalemia Beta blocker poisoning Premature labor (this is an off-label use and could be detrimental) Although minor compared to those of epinephrine, beta agonists usually have mild to moderate adverse effects, which include anxiety, hypertension, increased heart rate, and insomnia. (wikipedia.org)
  • Beta receptors are found on cells of the heart muscles, smooth muscles , airways , arteries , kidneys , and other tissues that are part of the sympathetic nervous system and lead to stress responses, especially when they are stimulated by epinephrine (adrenaline). (netlibrary.net)
  • Beta blockers interfere with the binding to the receptor of epinephrine and other stress hormones, and weaken the effects of stress hormones. (netlibrary.net)
  • β3-Adrenoceptor agonists were originally considered as a promising drug class for the treatment of obesity and/or type 2 diabetes. (nih.gov)
  • β(3)-Adrenoceptor. (nih.gov)
  • 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)
  • Male C57BL/6 normal, db/db, and ob/ob mice were treated with agonists of PPAR-gamma, PPAR-alpha, or beta3-adrenoceptor for 3 weeks. (bvsalud.org)
  • Several herpes- and poxviruses have captured chemokine receptors from their hosts and modified these to their own benefit. (pubmedcentralcanada.ca)
  • The human and viral chemokine receptors belong to class A 7 transmembrane (TM) receptors which are characterized by several structural motifs like the DRY-motif in TM3 and the C-terminal tail. (pubmedcentralcanada.ca)
  • 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)
  • The region of i loop 3 highlighted in blue is implicated in signalling from receptor to G protein. (els.net)
  • Marchese A, Chen C, Kim YM and Benovic JL (2003) The ins and outs of G‐protein‐coupled receptor trafficking. (els.net)
  • Tao J, Wang HY and Malbon CC (2003) Protein kinase A regulates AKAP250 (gravin) scaffold binding to the beta2‐adrenergic receptor. (els.net)
  • 3 The thermogenesis function in BAT largely depends on an integral membrane protein located at the inner membrane of mitochondria that is called thermogenin or uncoupling protein one (UCP1). (dovepress.com)
  • For example, Beta-2 adrenergic receptor activate GNAS complex locus ( G-protein alpha-s )/ Adenylate cyclases, which leads to Adenosine 3',5'-cyclic phosphate ( cAMP ) production. (bio-rad.com)
  • PKA-cat phosphorylation of Beta-2 adrenergic receptor leads to its activation switch from G-protein alpha-i family to G-protein alpha-s . (bio-rad.com)
  • c-Src phosphorylates SHC transforming protein 1 ( Shc ) and Growth factor receptor-bound protein 2 ( GRB2 ), activating Son of sevenless homolog ( SOS )/ H-Ras / c-Raf-1 and subsequent MEK and Erk activation [ 12 ], [ 13 ]. (bio-rad.com)
  • CDR-H3 is located in a similar position to the G-protein carboxy-terminal fragment in the active opsin structure and to CDR-3 of the nanobody in the active beta(2)-adrenergic receptor structure, but locks A(2A)AR in an inactive conformation. (proteopedia.org)
  • These results suggest a new strategy to modulate the activity of G-protein-coupled receptors. (proteopedia.org)
  • G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody. (proteopedia.org)
  • hence, the name is G protein coupled receptors (GPCRs). (pubmedcentralcanada.ca)
  • In this review we will use the term 7TM receptors instead of GPCRs as these receptors also signal trough non-G protein-dependent pathways, like β -arrestin-mediated signaling [ 2 ]. (pubmedcentralcanada.ca)
  • Furthermore, the G βγ subunit is also involved in signaling and the 7TM receptors also signal via G protein-independent pathways like MAP-kinase activation-mediated by β -arrestins [ 4 ]. (pubmedcentralcanada.ca)
  • Beta adrenergic receptors (or β receptors) belong to the guanine nucleotide-binding G protein-coupled receptor (GPCR) superfamily. (zjrms.com)
  • Binding was rapid (t1/2 less than 30 s) and rapidly reversible (t1/2 less than 3 min) at 37 degrees C. Binding was a saturable process with 75 +/- 12 fmol (-) [3H] alprenolol bound/mg protein (mean +/- SEM) at saturation, corresponding to about 2,000 sites/cell. (duke.edu)
  • The focus of work in this laboratory is on the elucidation of the molecular properties and regulatory mechanisms controlling the function of G protein-coupled receptors. (duke.edu)
  • 1. Rekawiecki R, Nowocin A, Kotwica J. Relationship between concentrations of progesterone, oxytocin, noradrenaline, gene expression and protein level for their receptors in corpus luteum during estrous cycle in the cow. (acris-antibodies.com)
  • Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. (scbt.com)
  • 1989) Molecular characterization of the human beta 3‐adrenergic receptor. (els.net)
  • The new type of skin patch contains hundreds of micro-needles, each thinner than a human hair, which are loaded with the drug Beta-3 adrenergic receptor agonist or another drug called thyroid hormone T3 triiodothyronine. (eurekalert.org)
  • The team estimates that their prototype patch had a material cost of about S$5 (US$3.50) to make, which contains beta-3 adrenergic receptor agonist combined with Hyaluronic acid, a substance naturally found in the human body and commonly used in products like skin moisturisers. (eurekalert.org)
  • There are four known beta adrenergic receptors in the human body. (drsharma.ca)
  • 3vga is a 3 chain structure with sequence from Human and Mus musculus . (proteopedia.org)
  • AA2AR_HUMAN ] Receptor for adenosine. (proteopedia.org)
  • Also this region is more variable among virus-encoded 7TM receptors compared to human class A receptors. (pubmedcentralcanada.ca)
  • Identification of beta-adrenergic receptors in human lymphocytes by (-) (3H) alprenolol binding. (duke.edu)
  • Human lymphocytes are known to posessess a catecholamine-responsive adenylate cyclase which has typical beta-adrenergic specificity. (duke.edu)
  • These results demonstrate the feasibility of using direct binding methods to study beta-adrenergic receptors in a human tissue. (duke.edu)
  • Previous studies in human asthmatics have suggested a defect in the beta-adrenergic pathway leading to cyclic adenosine monophosphate (cAMP) generation. (elsevier.com)
  • Although these studies have suggested normal or increased numbers of beta-adrenergic receptors, limitations in the quantity of tissue available have not allowed further delineation of the biochemical or molecular mechanisms of human asthma. (elsevier.com)
  • The basenji-greyhound (BG) dog model of nonspecific airway hyperreactivity displays similarities to human asthma, and altered functional response to beta-adrenergic agonists has been previously shown in airway tissue from this model. (elsevier.com)
  • Myocardial beta-adrenergic receptor expression and signal transduction after chronic volume-overload hypertrophy and circulatory congestion. (ahajournals.org)
  • METHODS AND RESULTS We examined the beta-adrenergic receptor-responsive adenylyl cyclase pathway in hearts from pigs subjected to volume-overload hypertrophy with circulatory congestion. (ahajournals.org)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (els.net)
  • Beta-1 adrenergic receptor may also stimulate Rap guanine nucleotide exchange factor (GEF) 2 ( PDZ-GEF1 ) directly and/or via cAMP. (bio-rad.com)
  • Cimaterol, however may stimulate the beta-1, 2, and 3 receptors while clen only stimulates the beta 2 and 3 receptors. (steroid.com)
  • Tolerance to bronchodilation during treatment with long-acting beta-agonists, a randomised controlled trial. (springermedizin.de)
  • Agonist induced desensitization of the beta receptor linked adenylate cyclase. (springer.com)
  • Homologous desensitization of beta adrenergic receptor coupled adenylate cyclase. (springer.com)
  • Binding of (-) [3H] alprenolol to these sites demonstrated the kinetics, affinity, and stereospecificity expected of binding to adenylate cyclase-coupled beta-adrenergic receptors. (duke.edu)
  • Dopamine receptor agonists.iii. (bireme.br)
  • Structurally related compounds devoid of beta-adrenergic activity such as dopamine, dihydroxymandelic acid, normetanephrine, pyrocatechol, and phentolamine did not effectively compete for the binding sites. (duke.edu)
  • 6 It has been reported that a chronic administration of the β3-adrenergic agonists can induce the ectopic expression of UCP in white fat and skeletal muscle. (dovepress.com)
  • Activation of beta-adrenergic receptors inhibits Ca2+ entry-mediated generation of inositol phosphates in the guinea pig myometrium, a cyclic AMP-independent event. (aspetjournals.org)
  • Tamoxifen is an estrogen receptor agonist in bone and therefore inhibits osteoclasts. (healthcmi.com)
  • The C-terminal receptor tail constitutes another regulatory region that through a number of phosphorylation sites is involved in signaling, desensitization, and internalization. (pubmedcentralcanada.ca)
  • The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment for obesity and diabetes. (wikipedia.org)
  • previous studies suggested that ADRB3 -selective agonists had an antidiabetic effect in rodent models of obesity and diabetes 4 . (jrheum.org)
  • Ultimately, this work will enable the exploration of a possible therapeutic role of ß3AR agonists and re-coupling of NOS in preventing adverse ventricular remodeling in obesity and in heart failure. (hopkinsmedicine.org)
  • Activation of β1 receptors induces positive inotropic, chronotropic output of the cardiac muscle, leading to increased heart rate and blood pressure, secretion of ghrelin from the stomach, and renin release from the kidneys. (wikipedia.org)
  • The patient experiences partial relief from frequent inhaled short-acting beta 2 ‑adrenergic receptor agonist and should be referred to an emergency room. (dentalcare.com)
  • For the combined Studies 1, 2, and 3, 432 patients received MYRBETRIQ ® 25 mg, 1375 received MYRBETRIQ ® 50 mg, and 929 received MYRBETRIQ ® 100 mg once daily. (rxlist.com)
  • The beta-3 agonist class of medication has numerous advantages over the anti-cholinergic class (Detrol, Ditropan, VESIcare, Enablex, Sanctura, Toviaz) and Gemtesa affords some advantages over Myrbetriq including simple dosing, ability to crush, no worries about blood pressure and less drug-drug interactions, but has not yet been approved for pediatric indications as has Myrbetriq. (doctorpedia.com)