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.

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

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

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

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

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

The possible existence of a beta3-adrenergic receptor (beta3-AR) in the human detrusor muscle was investigated by in vitro functional studies and analysis of mRNA expression. Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of the human detrusor. The rank order for their relaxing potencies was isoprenaline (pD2 6.37+/-0.07) > or = noradrenaline (pD2 6.07+/-0.12) > or = adrenaline (pD2 5.88< or =0.11). Neither dobutamine (beta1- and beta2-AR agonist) nor procaterol (beta2-AR agonist) produced any significant relaxation at concentrations up to 10(-5) M. BRL37344A, CL316243 and CGP-12177A (beta3-AR agonists), relaxed the preparations significantly at concentrations higher than 10(-6) M. The pD2 values for BRL37344A, CL316243 and CGP-12177A were 6.42+/-0.25, 5.53+/-0.09 and 5.74+/-0.14, respectively. CGP-20712A (10(-7) - 10(-5) M), a beta1-AR antagonist, did not affect the isoprenaline-induced relaxation. On the other hand, ICI-118,551, a beta2-AR antagonist, produced a rightward parallel shift of the concentration-relaxation curve for isoprenaline only at the highest concentration used (10(-5) > M) and its pKB value was 5.71+/-0.19. Moreover, SR58894A (10(-7) - 10(-5) M), a beta3-AR antagonist, caused a rightward shift of the concentration-relaxation curve for isoprenaline in a concentration-dependent manner. The pA2 value and slope obtained from Schild plots were 6.24+/-0.20 and 0.68+/-0.31. The beta1-, beta2- and beta3-AR mRNAs were all positively expressed in detrusor smooth muscle preparations in a reverse transcription polymerase chain reaction assay. In conclusion, the present results provide the first evidence for the existence of the beta3-AR subtype in the human detrusor. They also suggest that the relaxation induced by adrenergic stimulation of the human detrusor is mediated mainly through beta3-AR activation.  (+info)

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

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

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

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

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

We provide the first evidence that point mutations can constitutively activate the beta(1)-adrenergic receptor (AR). Leucine 322 of the beta(1)-AR in the C-terminal portion of its third intracellular loop was replaced with seven amino acids (I, T, E, F, C, A and K) differing in their physico-chemical properties. The beta(1)-AR mutants expressed in HEK-293 cells displayed various levels of constitutive activity which could be partially inhibited by some beta-blockers. The results of this study might have interesting implications for future studies aiming at elucidating the activation process of the beta(1)-AR as well as the mechanism of action of beta-blockers.  (+info)

Dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization. (7/484)

The use of dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization was investigated in 20 men. At 2.5, 5, and 10 microg x kg(-1) x min(-1), dobutamine induced significant increases in energy expenditure, lipid oxidation, and lipolysis. The beta(1)-adrenoceptor antagonist atenolol (bolus: 42.5 microg/kg, infusion: 1.02 microg x kg(-1) x min(-1)) blocked all dobutamine-induced effects on thermogenesis and lipid utilization. All parameters remained at levels comparable to those during saline infusion. The dose of atenolol used did not inhibit beta(2)-adrenoceptor-specific changes in energy expenditure, lipid oxidation, and lipolysis during salbutamol infusion (85 ng x kg(-1) x min(-1)). This indicates that atenolol was specific for beta(1)-adrenoceptors and did not camouflage concomitant beta(2)-adrenoceptor stimulation during dobutamine infusion. Therefore, we conclude that dobutamine can be used as a selective beta(1)-adrenoceptor agonist at dosages +info)

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

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

COPD is a major cause of morbidity and mortality with a rising incidence worldwide. Large RCTs and meta-analyses show that currently available pharmacotherapy may improve symptoms and perhaps even survival. Appleton and colleagues provided an in-depth systematic review of the role of LABAs in the management of stable COPD. LABAs led to small statistically significant increases in lung function (FEV1) and improvement in some measures of health status compared with placebo. These findings further support current guideline recommendations for use of LABAs in stable moderate-to-severe COPD. However, the story does not end here. In light of recent concerns and the continued debate about LABAs and increased asthma-related deaths (1), is it possible that LABAs also increase deaths in patients with COPD? The meta-analysis by Salpeter and colleagues shows the effectiveness of anticholinergics in reducing COPD exacerbations and hospitalizations. Interestingly, compared with placebo, anticholinergics ...
A Moderate Drug Interaction exists between indacaterol and olodaterol. View detailed information regarding this drug interaction.
oh loe da ter ol). Brand Name(s): Striverdi® Respimat®, Stiolto ® Respimat® (as a combination product containing olodaterol and tiotropium). WHY is this medicine prescribed?. Olodaterol oral inhalation is used to control wheezing, shortness of breath, coughing, and chest tightness caused by chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs and airways, which includes chronic bronchitis and emphysema). Olodaterol oral inhalation is in a class of medications called long-acting beta-agonists (LABAs). It works by relaxing and opening air passages in the lungs, making it easier to breathe.. Are there OTHER USES for this medicine?. This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.. HOW should this medicine be used?. Olodaterol inhalation comes as a solution to inhale by mouth using a special inhaler. It is usually used once a day. Inhale olodaterol at around the same time every day. Follow the directions on ...
A list of combination inhalers including a long acting beta agonist (LABA) and an inhaled corticosteroid (ICS) preparations at VMP and AMP from the NHS Dictionary of Medicines and Devices.. ...
Advisors to the US Food and Drug Administration has recommended approval of Boehringer Ingelheims chronic obstructive pulmonary disease drug olodaterol. - News - PharmaTimes
本次文獻回顧找到71篇相關試驗,但並非所有試驗均包含我們所關注的結果。生活品質分析 (使用聖喬治呼吸問卷測量) 納入42篇試驗,肺功能分析則納入46篇試驗。. 品質優良的相似試驗所得到的證據,支持LABA/ICS合併療法為最適當的治療策略,患者的生活品質和肺功能改善幅度最高。於6個月時,合併療法的平均療效較安慰劑高3.9個單位。於6個月時LAMA排名第二 (-2.63個單位),LABA排名第三 (-2.29 個單位),尤其是將不可靠的試驗予以排除時,但估計值的重疊度很高。. 對最低第一秒用力吐氣肺容積 (FEV11) 而言,LABA/ICS合併療法為排序最高的治療類別,相對於安慰劑,於6個月時的平均改善幅度為133.3 mL (95% 可靠區間 [CrI] 為101至164)。如同SGRQ的結果,於6個月時LAMA (平均差 [MD] 為104,95% CrI為82至125) 的排序,恰在LABA (MD為99,95% CrI為72至128) ...
This is a 4-week, multicenter, randomized, double-blind, parallel group and active controlled study.. Patients will be randomized (1 to 1 ratio) to a 4-week double-blind treatment period of either FDC (fixed-dose combination) of tiotropium + olodaterol (5/5 µg) plus placebo or the free combination of tiotropium 5 µg and olodaterol 5 µg; all administered via the Respimat® inhaler. The purpose is to show non-inferiority between the FDC and the free combination of tiotropium and olodaterol in patients with COPD. ...
A Moderate Drug Interaction exists between CPM-PSE DM Drops and olodaterol. View detailed information regarding this drug interaction.
Long-Acting Beta2-AgonistsLong-acting bronchodilators (LABA) are not used for the treatment of acute bronchospasm. They are used for the preventive treatment of nocturnal asthma or exercise-induced as... more
An article in the Cochrane Library highlights five studies on cessation of LABA compared to continued use of LABA/ICS for adults with well-controlled asthma to determine whether stopping LABA treatment has an impact on asthma control, exacerbations, and other serious adverse events.
Bronchodilators are a type of medication that make breathing easier by relaxing the muscles in the lungs and widening the airways (bronchi). Theyre often used to treat long-term conditions where the airways may become narrow and inflamed, such as: asthma, a common lung condition caused by inflammation of the airways ...
The beta-2 agonist Clenbuterol is used for treating asthma, since it is a bronchodilator, in many countries. However, it is more commonly used to burn fat
Langtidsvirkende sympatomimetikum med stimulerende virkning overvejende på β2-receptorer (LABA), anvendes som bronkodilaterende middel.
In treatment period 1, patients received indacaterol 300 μg once daily for 14 days via single-dose dry-powder inhaler (SDDPI); in treatment period 2, patients received placebo to indacaterol once daily for 14 days via SDDPI; and in treatment period 3, patients received salmeterol 50 μg twice daily for 14 days via multi-dose dry-powder inhaler (MDDPI). There was a washout period of 14 days between each treatment period. Indacaterol and placebo to indacaterol were administered double-blind; salmeterol was administered open-label. Daily inhaled corticosteroid treatment (if applicable) was to remain stable throughout the study. The short-acting β2-agonist salbutamol/albuterol was available for rescue use throughout the study ...
Comparative efficacy of inhaled medications (ICS/LABA, LAMA, LAMA/LABA and SAMA) for COPD: a systematic review and network meta-analysis Mohamed Ismail Abdul Aziz,1,* Ling Eng Tan,1,* David Bin-Chia Wu,1 Fiona Pearce,1 Gerald Seng Wee Chua,2 Liang Lin,1 Ping-Tee Tan,1 Kwong Ng1 1Agency for Care Effectiveness, Ministry of Health, Singapore; 2Division of Medicine, Ng Teng Fong General Hospital, Singapore *These authors contributed equally to this work Purpose: To assess the comparative efficacy of short-acting muscarinic antagonists (SAMAs), long-acting muscarinic antagonists (LAMAs), LAMA in combination with long-acting beta-agonists (LABAs; LAMA/LABAs) and inhaled corticosteroids (ICS) in combination with LABA (ICS/LABAs) for the maintenance treatment of COPD.Materials and methods: We systematically reviewed 74 randomized controlled trials (74,832 participants) published up to 15 November 2017, which compared any of the interventions (SAMA [ipratropium], LAMA [aclidinium, glycopyrronium, tiotropium,
The principal mechanism by which bronchodilator β-adrenoceptor agonists act is to relax airways smooth muscle although they may also be anti-inflammatory. However, the extent of anti-inflammatory activity and the cell types affected by these agonists are uncertain. The purpose of this study was to evaluate whether β-adrenoceptor agonists prevent pro-inflammatory cytokine generation from activated human lung macrophages. Macrophages were isolated and purified from human lung. The cells were pre-treated with both short-acting (isoprenaline, salbutamol, terbutaline) and long-acting (formoterol, salmeterol, indacaterol) β-agonists before activation with lipopolysaccharide (LPS) to induce cytokine (TNFα, IL-6, IL-8 and IL-10) generation. The experiments showed that short-acting β-agonists were poor inhibitors of cytokine generation. Of the long-acting β-agonists studied, formoterol was also a weak inhibitor of cytokine generation whereas only indacaterol and salmeterol showed moderate ...
Long-acting bronchodilators (LABD) are similar in structure to short-acting selective beta2-adrenoceptor agonists, but have much longer side chains resulting in a 12-hour effect, and are used to give a smoothed symptomatic relief (used morning and night). While patients report improved symptom control, these drugs do not replace the need for routine preventers, and their slow onset means the short-acting dilators may still be required. In November 2005, the American FDA released a health advisory alerting the public to findings that show the use of long-acting β2-agonists could lead to a worsening of symptoms, and in some cases death. Currently available long-acting beta2-adrenoceptor agonists include salmeterol, formoterol, bambuterol, and sustained-release oral albuterol. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread; the most common combination currently in use is fluticasone/salmeterol (Advair in the United States, and Seretide in the United ...
The Stiolto Respimat inhaler, also known as tiotropium and olodaterol, is used to manage Chronic Obstructive Pulmonary Disease or COPD.
Olodaterol (oh-loe-DA-ter-ol), Tiotropium Bromide (tye-oh-TROE-pee-um BROE-mide) Treats chronic obstructive pulmonary disease (COPD). Brand Name(s): Stiolto Respimat
Indacaterol is a long-acting bronchodilator. Bronchodilators are medicines that are breathed in through the mouth to open up the bronchial tubes (air passages) in the lungs. They relieve cough, wheezing, shortness of breath, and troubled breathing by increasing the flow of air through the bronchial tubes. This medicine is available only with your doctors prescription. This product is available in the following dosage forms:. ...
Bronchodilators are medications commonly used by people with asthma. They relax the muscles that surround the airways and allow the airways (the tubes that carry air into and out of the lungs) to open up. Some bronchodilators act quickly to stop asthma symptoms (such as wheezing, coughing, or shortness of breath) that are often caused by narrowed airways. Known as rescue, quick-relief, or fast-acting medications, these bronchodilators are meant to be used when a person first notices symptoms, but their effect doesnt last long. Other bronchodilators, known as controller medications, are longer acting and are used to control, or prevent, asthma symptoms.. Back To Top. ...
The species, which eluted at 6.75 min and produced a molecular ion of m/z 255.13 (Fig. 4E), was assigned to a mono-nitrated salbutamol derivative 3 (Fig. 1). This assignment is consistent with elemental analysis (C12H19N2O4+, exact mass 255.13397) and further supported by MS/MS spectrum obtained from this molecular ion (Fig. 4G). Formation of this nitrophenol was unexpected as it required the side chain at C3 of the aromatic ring, -CH2OH, to be eliminated. We verified that the putative phenolic precursor of 3, a salbutamol analog, in which the -CH2OH moiety was replaced with -H, (m/z 210), was not present as an impurity in salbutamol samples. This indicates that the corresponding radical (1d in Fig. 11) had to be produced in situ, during enzymatic oxidation of salbutamol itself. In the proposed mechanism (Fig. 11), the initially generated phenoxyl radical, 1a, undergoes intramolecular hydrogen atom transfer from the adjacent -CH2OH moiety to generate the aryl-methoxyl-type radical 1c. After ...
Long-acting bronchodilators are the basis of treatment for COPD [1]; however, there are some patients who suffer from frequent or severe exacerbations, despite maximal bronchodilation [2]. These patients are at increased risk of death and represent a great challenge in clinical practice [3]. Inhaled corticosteroids (ICS) are the basis of the treatment of asthma and are also effective, albeit to a lesser extent, in some patients with COPD [4]. Generally speaking, ICS are indicated in patients with COPD and exacerbations, despite bronchodilator treatment [1]. However, not all COPD patients respond to ICS and the long-term use of ICS in COPD may be associated with several side-effects [5, 6]. Therefore, the use of ICS for the prevention of exacerbations in COPD should not be a treatment by default and must be guided by criteria based on evidence [7]. In this respect, the InforMing the PAthway of COPD Treatment (IMPACT) study has provided very relevant information about the proper use of ICS, ...
COPD is a major cause of morbidity and mortality with a rising incidence worldwide. Large RCTs and meta-analyses show that currently available pharmacotherapy may improve symptoms and perhaps even survival. Appleton and colleagues provided an in-depth systematic review of the role of LABAs in the management of stable COPD. LABAs led to small statistically significant increases in lung function (FEV1) and improvement in some measures of health status compared with placebo. These findings further support current guideline recommendations for use of LABAs in stable moderate-to-severe COPD. However, the story does not end here. In light of recent concerns and the continued debate about LABAs and increased asthma-related deaths (1), is it possible that LABAs also increase deaths in patients with COPD? The meta-analysis by Salpeter and colleagues shows the effectiveness of anticholinergics in reducing COPD exacerbations and hospitalizations. Interestingly, compared with placebo, anticholinergics ...
The ß-adrenergic receptors are linked to G proteins. The ß-receptor has three known subtypes. Beta-1 receptors primarily regulate myocardial tissue and affect the rate of contraction via impulse conduction. Beta-2 receptors regulate smooth muscle tone and influence vascular and bronchiolar rela...
Indacaterol helps people with asthama or COPD to breathe more easily, relaxing the muscles surrounding the airways so that air can pass through more easily.
Medscape - COPD dosing for Arcapta Neohaler (indacaterol inhaled), frequency-based adverse effects, comprehensive interactions, contraindications, pregnancy & lactation schedules, and cost information.
Despite being an irreversible airflow obstruction disorder, bronchodilators are still used in the treatment of COPD. Different patients of bronchitis need
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Teva (previously NuPathe) is developing long-acting compounds for the treatment of neurological and psychiatric disorders, using Long-Acting Delivery (LAD™)
Positive new findings from two studies of the investigational, long-acting regimen of cabotegravir and rilpivirine for treatment of HIV.
Inhaled bronchodilators are the primary medications used,[2] and result in a small overall benefit.[121] The two major types are β2 agonists and anticholinergics; both exist in long-acting and short-acting forms.[122] They reduce shortness of breath, wheeze, and exercise limitation, resulting in an improved quality of life.[123] It is unclear if they change the progression of the underlying disease.[2] In those with mild disease, short-acting agents are recommended on an as needed basis.[2] In those with more severe disease, long-acting agents are recommended.[2] Long-acting agents partly work by reducing hyperinflation.[74] If long-acting bronchodilators are insufficient, then inhaled corticosteroids are typically added.[2] Which type of long-acting agent, long-acting muscarinic antagonist (LAMA) such as tiotropium or a long-acting beta agonist (LABA) is better is unclear, and trying each and continuing with the one that works best may be advisable.[124] Both types of agent appear to reduce ...
This pair of replicate, 52-week studies of the effects of once-daily combination of tiotropium+olodaterol administered via the Respimat Soft Mist Inhaler in patients with moderate to very severe COPD confirm statistically significant increases for the primary lung-function end points of trough FEV1 and FEV1 AUC0-3 response after 24 weeks versus either tiotropium or olodaterol alone. These results are supported by a range of secondary lung-function end points over 52 weeks. FEV1 AUC0-3 and trough FEV1 reflect bronchodilator benefit at the beginning and end of a 24-h cycle and are important measures in the selection of optimum doses and dosing frequency.. Long-acting bronchodilators remain the cornerstone of COPD maintenance therapy [2]. However, the combination of bronchodilators with different modes of action has not been commonly prescribed in clinical practice [1] due, in part, to the lack, until recently, of available FDCs of LAMA+LABA. Olodaterol is a novel once-daily LABA that has been ...
Indacaterol - Get up-to-date information on Indacaterol side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about Indacaterol
Chronic obstructive pulmonary disease (COPD) is a progressive lung disease that is associated with airway obstruction. COPD is a major cause of chronic morbidity and mortality throughout the world. It is a progressive condition, but is partially reversible through treatment, especially when diagnosed early in its clinical course. Bronchodilators are important in treating the symptoms of COPD. Long-acting bronchodilators provide sustained symptom relief and are usually preferred in patients with COPD. Combining bronchodilators with different mechanisms of action appears to improve efficacy.
Similar to the scenario in neonatal rat cardiomyocytes, β1-AR stimulation with isoproterenol induces a robust increase in cAMP accumulation that is associated with an increase in the amplitude and an acceleration of the kinetics of both the calcium transient and the twitch in adult rat ventricular myocytes. In contrast, only rather high concentrations of the β2-AR agonist zinterol (10-5 mol/L) modulate contractile function in adult rat ventricular myocytes (Figure 2⇑). Parenthetically, 2 laboratories have presented data to support the theoretical argument that 10-5 mol/L zinterol (in the absence of a β1-AR blocker) acts as a mixed β1-/β2-AR agonist; β2-AR selectivity is achieved only if a β1-AR blocker (such as CGP 20712A) is included in the assay.11 73 In contrast, Xiao and Lakatta74 maintain that the effects of high concentrations of zinterol (even without a β1-AR blocker) are attributable entirely to the minor population of β2-ARs in the preparation, and they present results to ...
Ultibro breezhaler contains the two active ingredients, indacaterol and glycopyrronium. These medicines work in two different ways to open the airways and make it easier to breathe.
Once-daily inhaled medication is the first approved fixed-dose combination of a long-acting beta agonist and a long-acting muscarinic antagonist.
Ultibro Breezhaler: This combination product contains two medications glycopyrronium and indacaterol. Glycopyrronium belongs to the group of medications known as anticholinergics. Indacaterol belongs to the group of medications known as long-acting bronchodilators. These medications work in different ways to relax the muscles in the walls of the small air passages in the lung, keeping the air passage open and making it easier to breathe.
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A type of drug that causes small airways in the lungs to open up. Bronchodilators are inhaled and are used to treat breathing disorders, such as asthma or emphysema ...
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This study compared the efficacy and tolerability of glycopyrrolate/indacaterol [QVA 149], glycopyrrolate, and indacaterol, in patients with stable
BioAssay record AID 640205 submitted by ChEMBL: Intrinsic activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay.
Symptomatic treatment of patients with severe COPD (FEV1 < 50% predicted normal) and a history of repeated exacerbations, who have significant symptoms despite regular therapy with long-acting bronchodilators. Strength ...
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A drug currently used to treat asthma and COPD improved cognitive abilities in mice with a model form of Down syndrome. Also this week: preventing post-infection cancer metastasis.
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Salmeterol- ന്റെ ഉപയോഗങ്ങൾ, ഡോസേജ്, പാർശ്വഫലങ്ങൾ, പ്രയോജനങ്ങൾ, പ്രതിപ്രവർത്തനങ്ങൾ, മുന്നറിയിപ്പ് എന്നിവ കണ്ടെത്തുക
Salmeterol- નાં ઉપયોગો, ડોઝ, આડઅસરો, ફાયદાઓ, ક્રિયાપ્રતિક્રિયાઓ અને ચેતવણી વિશે જાણો
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IBMC does research in Life Sciences and Biomedicine, training of postgraduate researchers, technology transfer and public engagement with science.
IBMC does research in Life Sciences and Biomedicine, training of postgraduate researchers, technology transfer and public engagement with science.
The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... Agonism of beta-2 receptors causes vasodilation and low blood pressure (i.e. the effect is opposite of the one resulting from ... Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). ... Agonists of alpha-2 receptors in the vascular smooth muscle lead to vasoconstriction. However, in clinical practice drugs ...
Beta2-adrenergic agonists act on beta-2 receptors to drive potassium into the cells. Therefore, beta blockers can raise ... Examples of medications that can cause hyperkalemia include ACE inhibitors, angiotensin receptor blockers, beta blockers, and ... Examples of drugs that can raise the serum potassium are non-selective beta-blockers such as propranolol and labetalol. Beta-1 ... Note that 12-40% of patients do not respond to salbutamol therapy for reasons unknown, especially if on beta-blockers, so it ...
... include substances that effect the adrenergic receptor in humans, increase insulin levels and stabilise breathing function. ... Billington, Charlotte K.; Penn, Raymond B.; Hall, Ian P. (2016), "β2 Agonists", Handbook of Experimental Pharmacology, Springer ... Beta-2 agonists: ...
Verhoeckx KC, Doornbos RP, Witkamp RF, van der Greef J, Rodenburg RJ (January 2006). "Beta-adrenergic receptor agonists induce ... Zilpaterol (zilpaterol hydrochloride; codenamed RU 42173) is a β2 adrenergic agonist. Under its trade name, Zilmax, it is used ... A. Plascencia; N. Torrentera & R.A. Zinn (1999). "Influence of the β-Agonist, Zilpaterol, on Growth Performance and Carcass ... the release of granulocyte chemotactic protein-2, oncostatin M, and vascular endothelial growth factor from macrophages". Int ...
"BET bromodomain inhibitors and agonists of the beta-2 adrenergic receptor identified in screens for compounds that inhibit DUX4 ... which encodes the protein ligand-dependent nuclear receptor-interacting factor 1 (LRIF1). LRIF1 is known to interact with the ... Oral albuterol, a β2 agonist, although it improved muscle mass and certain measures of strength in clinical trials, it did not ... Interestingly, after DUX4 was identified as an integral part of FSHD pathophysiology, drug screens showed that β2 agonists ...
Inhalation of an agonist for the beta-2 adrenergic receptor, such as Salbutamol, Albuterol (US), is the most common treatment ... adrenergic receptor on the response to regular use of albuterol in asthma" (PDF). American Journal of Respiratory and Critical ... a direct-acting beta agonist used in congestive heart failure, also demonstrates tachyphylaxis.[medical citation needed] ... Polymorphisms of the beta-2 receptor play a role in tachyphylaxis. Expression of the Gly-16 allele (glycine at position 16) ...
... a novel agonist at peripheral dopamine receptors and beta 2-adrenoceptors". British Journal of Pharmacology. 85 (3): 599-608. ... It is not an α-adrenergic agonist, does not cause vasoconstriction, and is not a pressor agent. As of 2004 there was some ... Effects of depexamine may be suppressed by concomitant use with ß2-adrenergic and dopamine receptor antagonists requires ... Dopexamine stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ...
Beta2-adrenergic agonist acts on beta-2 receptor to drive potassium into the cells. Therefore, beta blockers can cause the rise ... Examples of medications are: ACE inhibitors, angiotensin receptor blockers,[11] and calcineurin inhibitor immunosuppressants ... Examples of drugs that can raise the serum potassium are non-selective beta-blockers such as propanolol and labetalol. Beta-1 ... High levels of adrenaline and noradrenaline have a protective effect on the cardiac electrophysiology because they bind to beta ...
... is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ... Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. It was ... Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ... Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. ...
Causes of or contributors to ED include the following: Prescription drugs (e.g., SSRIs, beta blockers, alpha-2 adrenergic ... receptor agonists, thiazides, hormone modulators, and 5α-reductase inhibitors) Neurogenic disorders (e.g., diabetic neuropathy ... Men with type 2 diabetes are twice as likely to have lower levels of testosterone, and are three times more likely to ... Phentolamine (2 mg) is often added. Visual and tactile stimulation produces better results. Some authors recommend the use of ...
... 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. ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective beta 3-adrenergic receptor ...
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH agonist, but is now ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ...
Ferguson SS, Menard L, Barak LS, Koch WJ, Colapietro AM, Caron MG (1995). "Role of phosphorylation in agonist-promoted beta 2- ... beta-adrenergic-receptor] kinase, beta-adrenergic receptor-specific kinase, beta-AR kinase, beta-ARK, beta-ARK 1, beta-ARK 2, ... beta-adrenergic receptor] Thus, the two substrates of this enzyme are ATP and beta-adrenergic receptor, whereas its two ... beta-adrenergic receptor] phosphotransferase. Other names in common use include ATP:beta-adrenergic-receptor phosphotransferase ...
... is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high specificity (an antagonist ... ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... Fitzgerald, JD; Wale, JL (1983). "The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)". J Cardiovasc ... A Beta-2 adrenergic antagonist (β2-adrenoceptor antagonist) ...
Clenbuterol remains banned not as a beta-agonist, but rather an anabolic agent. Heart muscle contraction Increase cardiac ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... "Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta- ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... Agonists (activators) of the α2-adrenergic receptor are frequently used in veterinary anaesthesia where they affect sedation, ... where it sits alongside the more plentiful α1-adrenergic receptor. The α2-adrenergic receptor binds both norepinephrine ...
... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in ...
The β3 (beta 3) adrenergic receptor agonist or β3-adrenoceptor agonist, also known as β3-AR agonist, are a class of medicine ... Beta-adrenergic agonist Beta2-adrenergic agonist "Betmiga , European Medicines Agency". www.ema.europa.eu. Retrieved 2018-10-02 ... "Three-dimensional models for beta-adrenergic receptor complexes with agonists and antagonists". Journal of Medicinal Chemistry ... Coman, Oana Andreia; Păunescu, H.; Ghiţă, Isabel; Coman, L.; Bădărăru, Anca; Fulga, I. (2009). "Beta 3 adrenergic receptors: ...
... also known as Beta1-adrenergic receptor agonists, are a class of drugs that bind selectively to the beta-1 adrenergic receptor ... Epinephrine is a non-selective beta agonist, this means it also stimulates the beta 2 adrenergic receptor. Therefore, ... February 2001). "Beta1-adrenergic agonist is a potent stimulator of alveolar fluid clearance in hyperoxic rat lungs". Jpn. J. ... Beta-adrenoceptors typically bind to norepinephrine release by sympathetic adrenergic nerves and to circulating epinephrine. ...
"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 ...
Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. Postoje tri ... Adrenergički receptor. Reference[уреди]. *^ Ruuskanen JO, Xhaard H, Marjamäki A, Salaneck E, Salminen T, Yan YL, Postlethwait ...
"The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329): 241-4. doi: ... Lohse MJ, Benovic JL, Codina J, Caron MG, Lefkowitz RJ (June 1990). "beta-Arrestin: a protein that regulates beta-adrenergic ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ... the receptor does not bind agonist and cannot initiate a response following exposure to agonist). Expression of the two ...
January 2011). "The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329 ... Lohse MJ, Benovic JL, Codina J, Caron MG, Lefkowitz RJ (June 1990). "beta-Arrestin: a protein that regulates beta-adrenergic ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors ( ... G protein-coupled receptors database List of MeSH codes (D12.776) Metabotropic receptor Orphan receptor Pepducins, a class of ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. Postoje tri ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
"Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta- ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation.". J. Biol. Chem. 263 (9): ... 1988). "Site-directed mutagenesis and continuous expression of human beta-adrenergic receptors. ... the contribution of genetic variability in beta adrenergic receptor and cytochrome P4502C9.". Clin. Pharmacol. Ther. 82 (2): ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... 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 ... "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. Bibcode:1989Sci...245.1118E ...
... is a selective agonist for the beta-3 adrenergic receptor (β3-AR) receptor. The receptors are located in the kidneys, ... The beta 3 adrenergic receptor was discovered in the late 1980s and initially beta3AR agonists were investigated as treatment ... Vibegron (other names: RVT-901; MK4618; KRP114V; URO-901) is a selective beta 3 adrenergic receptor agonist. The most common ... "Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor ...
... crossover study to evaluate efficacy and safety of the beta 3-adrenergic receptor agonist solabegron (SOL) in patients with ... Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel function, and ... 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 ...
... beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta-thromboglobulin - ... adrenergic receptor - adrenodoxin - aequorin - aerobic respiration - agonist - alanine - albumin - alcohol - alcoholic ... alpha adrenergic receptor - Alpha helix - alpha-1 adrenergic receptor - alpha-2 adrenergic receptor - alpha-beta T-cell antigen ... transforming growth factor beta - transforming growth factor beta receptor - transient receptor potential - translation ( ...
... 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; ... It has a rapid onset of action (2-5 minutes) and may last up to 6-8 hours. The drug, alone or in co-administration with ... 78 (2): 283-7. doi:10.1378/chest.78.2.283. PMID 6995040. Kemp, JP.; Chervinsky, P.; Orgel, HA.; Meltzer, EO.; Noyes, JH.; Mingo ...
... α1-adrenergic receptor antagonist (Ki = 75 nM and 86 nM, respectively).[12] It possesses low or no affinity for the 5-HT1A, 5- ... 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, ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... Agonists: Ergolines (e.g., 2-Br-LSD (BOL-148), ergotamine, LSD) ...
... 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 ...
... and dopamine D3 receptors.[31][32] It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B ... and as a partial agonist at 5-HT1A.[31][33][34][35] Yohimbine interacts with serotonin and dopamine receptors in high ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the ...
... agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". ... Antagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol ... On takođe deluje kao parcijalni agonist 5-HT1A receptora i antagonist 5-HT2A i 5-HT2B receptora.[3][4][5] ... receptor". Naunyn-Schmiedeberg's Archives of Pharmacology. 357 (1): 17-24. PMID 9459568. doi:10.1007/PL00005133.. ...
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 ... Retrieved 2 January 2015.. *^ a b c d e f g h i j k l m n o p q r s t u v w x y z aa Hardiman O, Al-Chalabi A, Chio A, Corr EM ... Retrieved 2 January 2015.. *^ a b c d e f g h i j k l m n o p q r s t u v w x Hobson EV, McDermott CJ (September 2016). " ...
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) ...
... σ1 receptor and D3 receptor agonist.[2] It produces antidepressant-like effects in rats.[2] However, captodiamine is unique ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... 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- ...
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 act as a dopamine receptor agonist, stimulating the nerves that control movement.[13] Newer ... beta-Ergocryptine. CH(CH3)2. CH(CH3)CH2CH3 (S). Isoleucine ... Adrenergic receptor modulators. α1. *Agonists: 6-FNE. * ... Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, ... For TAAR2 and TAAR5 agonists and inverse agonists, see TAAR for references. ...
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. + ...
In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ... Retrieved 2 September 2016.. *^ a b c d e f g h i j "Cymbalta (duloxetine delayed-release) Capsules for Oral Use. Full ...
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] ... 2,5-DMA is the alpha-methyl homologue of 2C-H and could be called "DOH" under the DO naming scheme. ...
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. ...
5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ... Hydroxyzine - Antihistamine, 5-HT2A receptor antagonist.. *Propranolol - Sympatholytic, beta blocker.. *Clonidine - ... 19 (2): 107-116.. ,access-date=. requires ,url=. (help). *^ a b Scott, E. L. (2011, September 6). Anxiety Disorders With ... 88 (2): 73-7. PMC 1295099 . PMID 7769598.. *^ Morissette, Sandra Baker; Tull, Matthew T.; Gulliver, Suzy Bird; Kamholz, Barbara ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... However, if MDPEA were either used in high enough of doses (e.g., 1-2 grams), or in combination with a monoamine oxidase ... InChI=1S/C9H11NO2/c10-4-3-7-1-2-8-9(5-7)12-6-11-8/h1-2,5H,3-4,6,10H2 ...
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. * ...
Highly specific receptor kinases, such as rhodopsin kinase and beta-adrenergic receptor kinase, which show stimulus-dependent ... Here we report that prevention of agonist-stimulated beta 2-adrenergic receptor (beta 2AR) phosphorylation by truncation of its ... the first direct evidence that one molecular mechanism of desensitization of G-protein-coupled receptors involves their agonist ... Removal of phosphorylation sites from the beta 2-adrenergic receptor delays onset of agonist-promoted desensitization.. Bouvier ...
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor. ...
beta-Adrenergic receptor mutants containing deletions within the sixth hydrophilic domain that failed to couple to Gs and ... Agonist-promoted sequestration of the beta 2-adrenergic receptor requires regions involved in functional coupling with Gs.. A H ... Agonist-promoted sequestration of the beta 2-adrenergic receptor requires regions involved in functional coupling with Gs.. A H ... Agonist-promoted sequestration of the beta 2-adrenergic receptor requires regions involved in functional coupling with Gs.. A H ...
A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor ... A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor ... beta 2AR-Y326A). This mutation completely abolishes agonist-mediated receptor sequestration without affecting the ability of ... a slower loss of total cellular receptors) associated with agonist-mediated desensitization of the beta 2-adrenergic receptor ...
Beta-2 Adrenergic Receptor Agonists Enhance AChR Clustering in C2C12 Myotubes: Implications for Therapy of Myasthenic Disorders ... Beta-2 Adrenergic Receptor Agonists Enhance AChR Clustering in C2C12 Myotubes: Implications for Therapy of Myasthenic Disorders ... Beta-2 Adrenergic Receptor Agonists Enhance AChR Clustering in C2C12 Myotubes: Implications for Therapy of Myasthenic Disorders ...
Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ... Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ... Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ... Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) ...
... on human lymphocytes alpha adrenergic receptor density. / Hasegawa, M.; Townley, R.. In: Journal of Allergy and Clinical ... on human lymphocytes alpha adrenergic receptor density, Journal of Allergy and Clinical Immunology, vol. 69, no. 1 II. ... on human lymphocytes alpha adrenergic receptor density. In: Journal of Allergy and Clinical Immunology. 1982 ; Vol. 69, No. 1 ... on human lymphocytes alpha adrenergic receptor density. Journal of Allergy and Clinical Immunology. 1982 Jan 1;69(1 II). ...
... on human lymphocytes alpha adrenergic receptor density. Together they form a unique fingerprint. * Sort by ... Effect of fenoterol (beta-2 agonist) on human lymphocytes alpha adrenergic receptor density. ... Fingerprint Dive into the research topics of Effect of fenoterol (beta-2 agonist) ...
... and beta-3 adrenergic receptors. Neither the beta-1 selective antagonist atenolol [38] nor the beta-3 selective antagonist L- ... To determine the relative roles of the three beta receptors in mediating reductions in DUX4 expression by beta agonists, we ... adrenergic receptor gene ADRB2 genetically confirmed that beta agonists are reducing DUX4 expression via the beta-2 adrenergic ... Together with the pharmacologic data, these results demonstrate that beta-adrenergic agonist compounds act through the beta-2 ...
Verhoeckx, K.C.M. ; Doornbos, R.P. ; Witkamp, R.F. ; de Greef, J. ; Rodenburg, R.J.T. / Beta-adrenergic receptor agonists ... title = "Beta-adrenergic receptor agonists induce the release of granulocyte chemotactic protein-2, oncostatin M, and vascular ... T1 - Beta-adrenergic receptor agonists induce the release of granulocyte chemotactic protein-2, oncostatin M, and vascular ... Beta-adrenergic receptor agonists induce the release of granulocyte chemotactic protein-2, oncostatin M, and vascular ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Mean change from Baseline (pre-dose on Day 1) in AM FEV1 from electronic flow meter over Days 2-15 [ Time Frame: Baseline (pre- ... and at 0-2 h, 0-4, and 0-24 h Days 1 and 14 ]. The forced expiratory volume in one second is the amount of air exhaled in one ... dose on Day 1), Day 2, and Day 15 ]. The forced expiratory volume in one second is the amount of air exhaled in one second ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Inhaled Corticosteroid (ICS)/Long Acting Beta Agonist (LABA). Drug: Fluticasone Furoate 100mcg/Vilanterol 25mcg Inhalation ... Inhaled Corticosteroid (ICS)/Long Acting Beta Agonist (LABA. Drug: Fluticaosne Propionate 500mcg/Salmeterol 50mcg Inhalation ... Subjects with history of hypersensitivity to study medications (e.g., beta-agonists, corticosteroid) or components of ...
Adrenergic beta-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Unwillingness of primary physician to discontinue inpatient beta agonist use. *Acute myocardial infarction or acute coronary ... Daily use (prior to study hospitalization) of inhaled beta agonist, corticosteroid, or oral leukotriene modifier ... Because beta-2 agonists have been shown to reduce permeability induced lung injury, it is anticipated that the severity of lung ...
These effects have traditionally been thought to be mediated exclusively by receptor activation of intrace … ... Stimulation of beta2-adrenergic receptors on the cell surface by adrenaline or noradrenaline leads to alterations in the ... Our findings indicate that agonist-dependent beta2-adrenergic receptor binding of NHERF plays a role in beta2-adrenergic ... Receptors, Adrenergic, beta-2 / genetics * Receptors, Adrenergic, beta-2 / metabolism* * Recombinant Fusion Proteins / genetics ...
... adrenergic receptor (beta(2)AR) is one of the most extensively studied. Previously, the X-ray crystal structure of beta(2)AR ... Crystal structure of the human beta2 adrenergic receptor in complex with the inverse agonist ICI 118,551. *DOI: 10.2210/pdb3NY8 ... Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography. Wacker, D., Fenalti, G., Brown, M.A., ... adrenergic receptor (beta(2)AR) is one of the most extensively studied. Previously, the X-ray crystal structure of beta(2)AR ...
INVOLVEMENT OF THE CARBOXYL TERMINAL DOMAIN OF THE BETA-2-ADRENERGIC RECEPTOR IN ITS AGONIST-INDUCED PHOSPHORYLATION AND ... INVOLVEMENT OF THE CARBOXYL TERMINAL DOMAIN OF THE BETA-2-ADRENERGIC RECEPTOR IN ITS AGONIST-INDUCED PHOSPHORYLATION AND ...
Adrenergic beta-2 Receptor Agonists / therapeutic use * Adult * Anti-Asthmatic Agents / administration & dosage ... Almost 62% of the women were dispensed at least one prescription for short-acting β2-agonist (SABA), 63% at least one inhaled ... Anna-Belle Beau 1 , Alain Didier 2 , Caroline Hurault-Delarue 1 , Jean-Louis Montastruc 1 , Isabelle Lacroix 1 , Christine ... corticosteroid (IC), 42% a fixed-combination of an IC and a long-acting β2-agonist (LABA) and 8% a LABA. An increase in SABA ...
Clenbuterol remains banned not as a beta-agonist, but rather an anabolic agent. Heart muscle contraction Increase cardiac ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... "Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta- ...
Beta-adrenergic agonists. Bronchodilation (Asthma); beneficial during P&PD. stimulate beta-2 receptors and cause relaxation. ... Alpha-1 agonists (adrenergic agonists); vasoconstrict nasal mucosa. Palpitations, headache, nausea, dependence, nervousness. ... Beta-Blockers (-olol). HTN, arrhythmia, angina, heart failure, MI (decrease HR and force of contraction). Block effects of ... Dopamine agonists. Parkinson disease. synthetic dopamine. GI distress, orthostatic hypotension, dyskinesias, psychotropic ...
... adrenergic agonist) increased CBF in a dose-dependent ... The beta(2)-adrenergic regulation of ciliary beat frequency ( ... 0/Adrenergic beta-Agonists; 0/Enzyme Inhibitors; 0/Receptors, Adrenergic, beta-2 ... Adrenergic beta-Agonists / pharmacology. Animals. Cell Size / drug effects, physiology. Cilia / drug effects, physiology. ... adrenergic agonist) increased CBF in a dose-dependent manner, and it also decreased the volume of the ciliary cells. These ...
The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. ... Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. ... regulation by beta-adrenergic receptors of Gq receptor signaling via phospholipase C underlies the airway beta-agonist paradox ... "beta 1-adrenergic receptor association with PSD-95. Inhibition of receptor internalization and facilitation of beta 1- ...
MOA for beta adrenergic agonists targets beta 2 receptors in airway - bronchodilation ... 1. Accolate - blocks leukotriene receptors. 2. Singulair - blocks leukotriene receptors. 3. Zyflo - Inhibits leukotriene ... 2. wheezing. 3. expanded chest. 4. sinusitis. 5. failure to grow. 6. thick stringy mucous ... What level of asthma would get one medium dose of inhaled corticosteroid or 2 daily medications ...
Beta2-adrenergic receptor agonist sympathomimetic; decreases free intracellular calcium ions. 0.25 to 0.5 mg SC every three to ... Beta2-adrenergic receptor agonist sympathomimetic; decreases free intracellular calcium ions. 0.25 to 0.5 mg SC every three to ... Figures 2 and 3 and Table 5 summarize the consensus management guidelines for the prevention of early-onset group B neonatal ... TABLE 2. Tocolytic Therapy for the Management of Preterm Labor. Medication. Mechanism of action. Dosage. ...
An inhaled long-acting beta2-adrenergic receptor agonist used as a bronchodilator in the management of asthma and COPD. ... An adrenergic beta agonist used to treat premature labor.. Terbutaline. A beta-2 adrenergic agonist used as a bronchodilator ... Adrenergic beta-Agonists. Accession Number. DBCAT000553. Description. Drugs that selectively bind to and activate beta- ... Etilefrine is an adrenergic agonist that appears to interact with beta-2 and some alpha adrenergic receptors. It has been used ...
... although beta2-agonist activity resides almost exclusively in the (R)-enantiomer. The enantioselective disposition of ... is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease ( ... Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. ... Levosalbutamol, also known as levalbuterol, is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma ...
Beta-2 adrenergic receptor agonists; Cromones; Glucocorticoids; Leukotriene receptor antagonists; Methyl xanthines; Omalizumab ...
... beta agonists may cause elevation in blood pressure and heart rate. Beta-2 agonists may also produce changes in ECG (eg, T wave ... Adrenergic bronchodilators. Related Drugs. albuterol, montelukast, Symbicort, Singulair, ProAir HFA, Ventolin, Spiriva, Breo ... Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Beta2-Agonists. Avoid combination ... Beta-Blockers (Beta1 Selective): May diminish the bronchodilatory effect of Beta2-Agonists. Of particular concern with ...
17 results for Category equals ADRENERGIC BETA-2 RECEPTOR AGONISTS Info. Please enable JavaScript in your browser. Row Number. ...
Drug-drug.Beta-adrenergic blockers: decreased salmeterol efficacy, increased risk of severe bronchospasm in patients with ... For children and adolescents with asthma who require addition of a long-acting beta2-adrenergic agonist to an inhaled ... Available data from controlled clinical trials suggest that long-acting beta2-adrenergic agonists increase risk of asthma- ... a fixed-dose combination product containing both an inhaled corticosteroid and a long-acting beta2-adrenergic agonist should ...
  • Most agonists of the beta receptors are selective for one or more beta-adrenoreceptors. (wikipedia.org)
  • 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)
  • 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)
  • 2, 3, 9, 10 Persistent severe asthma (Step 5) is treated with high-dose inhaled corticosteroid plus inhaled long-acting selective beta 2 ‑adrenergic receptor agonist. (dentalcare.com)
  • The dosing and strength selective beta-2 adrenergic receptor agonist (causes even being a steroid molecule. (cubeme.com)
  • Selective alpha 2-receptor that reduces aqueous humor formation and increases uveoscleral outflow. (medscape.com)
  • A relatively selective alpha-adrenergic agonist that does not have significant local anesthetic activity. (medscape.com)
  • Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral outflow. (medscape.com)
  • It is a selective beta-2 agonist, meaning it will stimulate your beta-2 adrenergic receptors. (ironmagazine.com)
  • 2010) Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist. (springer.com)
  • 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)
  • Currently MediciNova's MN-221, a highly selective beta(2)-adrenergic receptor agonist, is in a Phase 2 clinical trial for acute exacerbations of asthma. (bio-medicine.org)
  • These proteins are up-regulated after 16-24 h of exposure and this is mediated by the {\ss}2-AR, as determined by time course experiments and the use of a specific {\ss}2-AR antagonist (ICI 118551). (wur.nl)
  • In such cases, beta-2 stimulation with its consequent increase in humour production is highly contra-indicated, and conversely, a topical beta-2 antagonist such as timolol may be employed. (wikipedia.org)
  • CypHer5 has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor expressing cells (2). (bio-medicine.org)
  • This application note describes the validation of antagonist-format CypHer5E receptor internalization assays for high-throughput screening. (bio-medicine.org)
  • A β2adrenergic receptor antagonist screen was performed using the LOPAC ™ compound library, which consists of 640 well-characterized, pharmaceutically diverse compounds with known drug or drug-like activity. (bio-medicine.org)
  • The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 was able to identify all specific β2-adrenergic receptor antagonists and additional structurally related compounds present in the LOPAC compound library. (bio-medicine.org)
  • Agonist and antagonist controls were placed symmetrically in columns 1 and 12 of each plate. (bio-medicine.org)
  • Twelve replicate wells contained a known agonist, isoproterenol, and four replicate wells contai ned a known antagonist, alprenolol, each diluted in 0.01% DMSO. (bio-medicine.org)
  • Glycopyrronium bromide is a muscarinic receptor antagonist. (europa.eu)
  • GSK233705 is a high-affinity specific muscarinic receptor (mAChR) antagonist which is being developed for once daily treatment of chronic obstructive pulmonary disease (COPD). (bioportfolio.com)
  • From the Geodon page: 'Ziprasidone mesylate functions as an antagonist at the dopamine D2 and serotonin 5-HT2A and 5-HT1D receptors, and as an ag - 94% more. (medications.com)
  • Glycopyrronium is a muscarinic-receptor antagonist. (europa.eu)
  • atropine is a nicotinic receptor antagonist and should be given to treat symptomatic bradycardia. (brainscape.com)
  • Leukotriene receptor antagonist. (studystack.com)
  • This effect was blocked by co-injection of the alpha-2-receptor antagonist, yohimbine, demonstrating that the alpha-2-receptor is related to stimulation of feeding in layer-type chicks. (biomedsearch.com)
  • 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)
  • Using atomistic molecular dynamics (MD) simulations, we provide in-depth analysis to reveal structural signatures of wild and mutant complexes with their bound agonist and antagonist ligands. (springer.com)
  • Jatana N, Thukral L, Latha N (2015) Structure and dynamics of DRD4 bound to an agonist and an antagonist using in silico approaches. (springer.com)
  • The active component of Yohimbe extract, Yohimbine, works as alpha-2 antagonist. (doctor-clinic.org)
  • The β 2 adrenoceptor has been cloned and sequenced, and details of how agonist stimulation ultimately results in clinically evident effects are now known. (elsevier.com)
  • Stimulation of beta2-adrenergic receptors on the cell surface by adrenaline or noradrenaline leads to alterations in the metabolism, excitability, differentiation and growth of many cell types. (nih.gov)
  • However, certain physiological effects of beta2-adrenergic receptor stimulation, notably the regulation of cellular pH by modulation of Na+/H+ exchanger (NHE) function, do not seem to be entirely dependent on G-protein activation. (nih.gov)
  • The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that binds epinephrine (adrenaline), a hormone and neurotransmitter whose signaling, via adenylate cyclase stimulation through trimeric Gs proteins, increased cAMP, and downstream L-type calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation. (wikipedia.org)
  • Protein kinase A then goes on to phosphorylate (and thus inactivate) myosin light-chain kinase, which causes smooth muscle relaxation, accounting for the vasodilatory effects of beta 2 stimulation. (wikipedia.org)
  • In contrast, Beta-1 adrenergic receptors are coupled only to Gs, and stimulation of these results in a more diffuse cellular response. (wikipedia.org)
  • In the normal eye, beta-2 stimulation by salbutamol increases intraocular pressure via net: Increase in production of aqueous humour by the ciliary process, Subsequent increased pressure-dependent uveoscleral outflow of humour, despite reduced drainage of humour via the Canal of Schlemm. (wikipedia.org)
  • Upon agonist stimulation, a fluorescent signal is observed as the CypHer5E-antibody conjugate is internalized alongside the receptor into acidic endosomal vesicles. (bio-medicine.org)
  • The appreciation that chronic stimulation of βARs likely contributes to the pathogenesis of heart failure ( 4 ) has led to the use of β-adrenergic receptor antagonists (i.e., β-blockers) to competitively inhibit the harmful effects of chronic catecholamine stimulation ( 5 ). (pnas.org)
  • The stimulation of myotubes with the glycoprotein agrin or laminin-111 induces the clustering of postsynaptic machinery that contains acetylcholine receptors (AChRs). (nature.com)
  • Bbeta-adrenergic receptor kinase-1 levels in catecholamine-induced myocardial hypertrophy: regulation by beta- but not alpha1-adrenergic stimulation. (duke.edu)
  • The pharmacologic effects of beta-adrenergic agonists, including terbutaline, are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic 3',5'-adenosine monophosphate (cAMP). (nih.gov)
  • Stimulation of food intake caused by neuropeptide Y and beta-endorphin was attenuated by co-injection with yohimbine. (biomedsearch.com)
  • a site in a sympathetic effector cell that reacts to adrenergic stimulation. (thefreedictionary.com)
  • In general, stimulation of alpha receptors is excitatory of the function of the host organ or tissue, and stimulation of the beta receptors is inhibitory. (thefreedictionary.com)
  • However, it should be kept in mind that β-adrenergic stimulation of VEGF expression may not necessarily be of major significance in regulating physiological angiogenesis. (ahajournals.org)
  • Plays a central role in ADRB2 recycling and resensitization after prolonged agonist stimulation by constitutively binding ADRB2, mediating deubiquitination of ADRB2 and inhibiting lysosomal trafficking of ADRB2. (uniprot.org)
  • It is known that increased stimulation of beta-2 receptors will promote increased metabolic rate and thermogenesis. (alrindustries.com)
  • The principal mechanism of its action relies on its indirect stimulation of the adrenergic receptor system, which is part of the sympathetic nervous system (SNS), by increasing the activity of noradrenaline at the post-synaptic α- and β-receptors. (alrindustries.com)
  • Although immunologic mechanisms appear to prevail in asthma, β 2 receptor dysfunction may be important in some circumstances. (elsevier.com)
  • Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) with duration of action of 12 hours or more. (elsevier.com)
  • Statistical links between beta agonist use and asthma mortality or morbidity warrant careful examination for clinical relevance, but may not be dismissed. (elsevier.com)
  • Beta agonists are relatively safe and clearly effective in asthma, but anti-inflammatory management (including allergen avoidance and immunotherapy when appropriate) is indicated in patients who require chronic therapy. (elsevier.com)
  • Beta2-AR agonists are used as bronchodilators in the treatment of asthma, but appear to have no effect on the chronic inflammation of the disease. (wur.nl)
  • Different polymorphic forms, point mutations, and/or downregulation of this gene are associated with nocturnal asthma, obesity and type 2 diabetes. (wikipedia.org)
  • A beta-2 adrenergic agonist used to treat bronchospasm, asthma, and COPD. (drugbank.ca)
  • An inhaled long-acting beta2-adrenergic receptor agonist used as a bronchodilator in the management of asthma and COPD. (drugbank.ca)
  • A beta-2 adrenergic receptor agonist used to treat asthma, bronchitis, COPD, as well as prevent exercise induced bronchospasms. (drugbank.ca)
  • A beta-2 adrenergic agonist and bronchodilator used for the symptomatic treatment of asthma. (drugbank.ca)
  • A beta-2 adrenergic receptor agonist and bronchodilator used for the treatment of asthma and chronic obstructive pulmonary disease (COPD). (drugbank.ca)
  • Levosalbutamol, also known as levalbuterol, is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). (drugbank.ca)
  • For asthma control, long acting beta-2 agonists (LABAs) should be used in combination with inhaled corticosteroids and not as monotherapy. (drugs.com)
  • Because long-acting beta 2 -agonists (LABAs) may disguise poorly controlled persistent asthma, frequent or chronic use of LABAs for exercise-induced bronchospasm is discouraged by the NAEPP Asthma Guidelines (NAEPP 2007). (drugs.com)
  • Currently available data are inadequate to determine whether concurrent use of inhaled corticosteroids or other long-term asthma control drugs mitigates the increased risk of asthma-related death from long-acting beta 2 -adrenergic agonists. (thefreedictionary.com)
  • Available data from controlled clinical trials suggest that long-acting beta 2 -adrenergic agonists increase risk of asthma-related hospitalization in children and adolescents. (thefreedictionary.com)
  • For children and adolescents with asthma who require addition of a long-acting beta 2 -adrenergic agonist to an inhaled corticosteroid, a fixed-dose combination product containing both an inhaled corticosteroid and a long-acting beta 2 -adrenergic agonist should ordinarily be used to ensure adherence with both drugs. (thefreedictionary.com)
  • In cases in which use of a separate long-term asthma-control medication (for example, inhaled corticosteroid) and a long-acting beta 2 -adrenergic agonist is clinically indicated, take appropriate steps to ensure adherence with both treatment components. (thefreedictionary.com)
  • It is used for maintenance (regular) treatment in adults whose asthma is not controlled well enough with inhaled long-acting beta-2 agonist together with a high dose of an inhaled corticosteroid. (europa.eu)
  • A main study involved 3,092 patients whose asthma was not well controlled on a combination of a long-acting beta-2 agonist and a corticosteroid used by inhalation. (europa.eu)
  • In patients whose asthma is not controlled well enough on a combination of an inhaled long-acting beta-2 agonist and high-dose corticosteroid and who have had an exacerbation in the previous year, the improvement in FEV1 with Zimbus Breezhaler was modest but considered to be clinically important. (europa.eu)
  • 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)
  • Patients with asthma should not normally be treated with beta-blockers. (nih.gov)
  • Bronchospasm, asthma-associated (prophylaxis)- Salmeterol and formoterol are indicated to prevent bronchospasm and reduce the frequency of acute asthma exacerbations in patients with chronic asthma {27} {30} {38} {46} {47} who require regular treatment with an inhaled shorter-acting beta-adrenergic bronchodilator. (drugs.com)
  • FDA has already concluded that monotherapy with long-acting adrenergic receptor beta 2 (ADRB2) agonists (LABAs) increases the risk of asthma-related exacerbations, including hospitalizations and death. (biocentury.com)
  • Short-acting adrenergic receptor beta 2 (ADRB2) agonists (SABAs) were first marketed to treat asthma in the 1930s. (biocentury.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)
  • New York, 2 December 2009 - Commonly prescribed beta 2 adrenergic agonist drugs for the treatment of asthma in pregnant women as well as pre-term labor may increase the incidence of autism-spectrum disorders, psychiatric pathology, cognitive problems and poor school performance in their children, according to a new study published in the December 2009 issue of the American Journal of Obstetrics & Gynecology . (elsevier.com)
  • Genetic variation of the beta(2)-adrenoceptor: its functional and clinical importance in bronchial asthma. (wikipedia.org)
  • The two companies also are working together on a Phase 2 trial studying MediciNova's compound MN-221 to combat asthma and chronic obstructive pulmonary disease (COPD). (bio-medicine.org)
  • After the SMART trial evaluating the safety of salmeterol (long-acting beta-2-agonist (LABA)) in asthma patients, regulatory actions were taken to promote a guideline-adherent prescribing of LABA only to patients receiving inhaled corticosteroids (ICS). (biomedcentral.com)
  • The Salmeterol Multicentre Asthma Research Trial (SMART) [ 1 ] was a large randomized controlled trial in asthma patients evaluating the safety of salmeterol (i.e., a long-acting beta-2-agonist [LABA]) compared to placebo in addition to usual asthma care. (biomedcentral.com)
  • Genetic polymorphisms of the beta 2-adrenergic receptor in nocturnal and nonnocturnal asthma. (jci.org)
  • The basis for this phenotype of asthma is not known, but beta 2-adrenergic receptors (beta 2AR) are known to downregulate overnight in nocturnal asthmatics but not normal subjects or nonnocturnal asthmatics. (jci.org)
  • Thus the Gly16 polymorphism of the beta 2AR, which imparts an enhanced downregulation of receptor number, is overrepresented in nocturnal asthma and appears to be an important genetic factor in the expression of this asthmatic phenotype. (jci.org)
  • The study, called the Long-Acting Beta Agonist Response by Genotype (LARGE) trial was conducted by the Asthma Clinical Research Network established by the National Institutes of Health. (healthcanal.com)
  • This study is important as it provides reassurance that the use of combination medications, inhaled steroids and long-acting beta-agonists (tradenames Advair or Symbicort), which are widely prescribed for asthma, are safe in patients that have this genetic variation," he says. (healthcanal.com)
  • The genetic variation relates to the beta-2-adrenergic receptor, the receptor that asthma bronchodilators bind to in order to exert their effects. (healthcanal.com)
  • The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. (uniprot.org)
  • The beta-agonist effects of epinephrine include bronchodilatation, chronotropic cardiac activity, and positive inotropic effects. (medscape.com)
  • Beta adrenergic receptors are found distributed throughout the body, in both muscle and fat, and are regulated through various natural hormones (triiodothyronine or T3, thyroxine or T4, testosterone, etc…) and catecholamines (such as norepinephrine and epinephrine). (ironmagazine.com)
  • The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (harvard.edu)
  • Furthermore, receptor ligand cross-docking experiments revealed that a single beta(2)AR complex can be suitable for docking of a range of antagonists and inverse agonists but also indicate that additional ligand-receptor structures may be useful to further improve performance for in-silico docking or lead-optimization in drug design. (rcsb.org)
  • Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( Introduction. (bio-medicine.org)
  • CypHer5E, consequently, can be used to screen for novel antagonists of known receptors and for potential ligands of non-G-protein coupled receptors (5) and orphan receptors. (bio-medicine.org)
  • Our findings demonstrate that Alp and Car are ligands that not only act as classical receptor antagonists, but can also stimulate signaling pathways in a G protein-independent, β-arrestin-dependent fashion. (pnas.org)
  • Muscarinic receptor antagonists and long-acting beta-2-adrenergic agonists are commonly combined in the management of COPD. (europa.eu)
  • In clinical practice, most experience has been gained with the use of nifedipine, whose efficacy is superior or comparable to those of β-agonists and oxytocin antagonists. (mdpi.com)
  • It contains a microcrystalline suspension of albuterol sulfate in propellant HFA-134a (1, 1, 1, 2- tetrafluoroethane) and ethanol. (rxlist.com)
  • Albuterol sulfate is a beta 2 -adrenergic agonist. (rxlist.com)
  • Under standardized in vitro test conditions with fixed flow rates ranging from 58 to 71 L/min, and with a total air volume of 2 L, ProAir Digihaler inhaler delivers 108 mcg of albuterol sulfate (equivalent to 90 mcg of albuterol base) with lactose from the mouthpiece. (rxlist.com)
  • The patient experiences prompt relief with inhaled short-acting beta 2 ‑adrenergic receptor agonist such as albuterol. (dentalcare.com)
  • Albuterol mainly acts on beta2 receptors, which predominate in the smooth muscles of the bronchi (respiratory tubes) It contains a generic form of levalbuterol, the active ingredient in non-generic Xopenex, and is just as effective as the non-generic, but at a lower cost. (liberalconspiracy.org)
  • Albuterol (Generic Ventolin tablets) is a beta-2-adrenergic agonist, which stimulates the beta-2-adrenergic receptors in the lungs resulting in the relaxation of bronchial smooth muscles. (liberalconspiracy.org)
  • beta-Adrenergic receptor mutants containing deletions within the sixth hydrophilic domain that failed to couple to Gs and stimulate adenylyl cyclase did not undergo agonist-mediated sequestration. (aspetjournals.org)
  • This mutation completely abolishes agonist-mediated receptor sequestration without affecting the ability of the receptor to activate maximally adenylyl cyclase, to undergo rapid desensitization, and to down-regulate in response to agonist. (duke.edu)
  • Mutation of the final residue of the beta2-adrenergic receptor from leucine to alanine abolishes the receptor's interaction with NHERF and also markedly alters beta2-adrenergic receptor regulation of NHE3 in cells without altering receptor-mediated activation of adenylyl cyclase. (nih.gov)
  • This receptor-channel complex is coupled to the Gs G protein, which activates adenylyl cyclase, catalysing the formation of cyclic adenosine monophosphate (cAMP) which then activates protein kinase A, and counterbalancing phosphatase PP2A. (wikipedia.org)
  • The dopamine D2 receptor is expressed and sensitizes adenylyl cyclase activity in airway smooth muscle. (ndriresource.org)
  • The beta(2) adrenergic receptor (beta(2)AR) activation of Gs, the stimulatory G protein for adenylyl cyclase, has long been a model system for GPCR signalling. (proteopedia.org)
  • During therapy with salmeterol or formoterol, it is important for patients to have a fast-acting inhaled beta-adrenergic bronchodilator available for relief of acute attacks {17} {117} {120} . (drugs.com)
  • Some studies suggest that patients with two genes coding for the amino-acid arginine at a certain position in this receptor (termed B16 Arg/Arg) benefit less from treatment with long-acting beta-2 agonists such as salmeterol and inhaled corticosteroids than do those with two genes coding for amino acid glycine (termed B16 Gly/Gly) at this position. (healthcanal.com)
  • Individuals in a matched pair were assigned to receive inhaled long-acting beta-2 agonist (salmeterol 50 μg twice a day) or placebo for two 18-week periods. (healthcanal.com)
  • In contrast, all receptor mutants that displayed Gs coupling were sequestered away from the cell surface in response to isoproterenol. (aspetjournals.org)
  • In testing this model, we examined the in vivo down-regulation and recovery of rat renal cortical membrane beta 1- and beta 2-adrenergic receptors in response to infusion of the agonist isoproterenol from subcutaneously implanted osmotic minipumps. (aspetjournals.org)
  • In the absence of agonist, EGFR had a uniform membrane distribution ( Fig. 1 A ). In contrast, the βAR agonists dobutamine (Dob) and isoproterenol (Iso) resulted in internalization of EGFRs as visualized by marked redistribution into cellular aggregates, similar to that seen with EGF ( Fig. 1 A Upper ). (pnas.org)
  • Caspase-3 and TNF-α levels were significantly reduced at 50nM in cultured cells, a dose lower than that of a non-specific beta-adrenergic agonist, isoproterenol. (arvojournals.org)
  • Beta-agonists relax bronchial smooth muscle by action on beta 2 -receptors, with little effect on cardiac muscle contractility. (medscape.com)
  • Terbutaline exerts a preferential effect on beta 2-adrenergic receptors which are the predominant receptors in bronchial smooth muscle. (pediatriconcall.com)
  • These findings provide reassurance that in the general population, patients should continue to be treated with long-acting beta-2 agonists plus moderate-dose inhaled corticosteroids irrespective of B16 genotype. (healthcanal.com)
  • The double-blind trial compared Serevent vs. placebo when added to standard therapy, such as ICS, methylxanthines, leukotriene modifiers and other ADRB2 agonists. (biocentury.com)
  • These data provide the first direct evidence that one molecular mechanism of desensitization of G-protein-coupled receptors involves their agonist-induced phosphorylation. (nih.gov)
  • A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor sequestration. (duke.edu)
  • An aromatic residue, tyrosine 326 in the prototypical human beta 2-adrenergic receptor, exists in a highly conserved sequence motif in virtually all members of the G protein-coupled receptor family. (duke.edu)
  • These results imply that this tyrosine residue, which is part of a highly conserved sequence motif in G protein-coupled receptors, may be responsible for their agonist-mediated sequestration and that sequestration and down-regulation of the receptor are dissociable phenomena. (duke.edu)
  • The lack of resensitization in the sequestration-defective beta 2-adrenergic receptor mutant strongly suggests that the sequestration pathway is an important mechanism by which cells re-establish the normal responsiveness of G protein-coupled receptors following the removal of agonist. (duke.edu)
  • We report here a direct agonist-promoted association of the beta2-adrenergic receptor with the Na+/H+ exchanger regulatory factor (NHERF), a protein that regulates the activity of the Na+/H+ exchanger type 3 (NHE3). (nih.gov)
  • Vascular endothelial growth factor (VEGF), oncostatin M (OSM), and granulocyte chemotactic protein-2 (GCP-2/CXCL6) are up-regulated in U937 macrophages and peripheral blood macrophages exposed to LPS, beta-adrenergic receptor (ß2-AR) agonists (e.g. zilpaterol, and clenbuterol) and some other agents that induce intracellular cAMP (prostaglandin E2, forskolin, and butyryl cAMP). (wur.nl)
  • G protein-coupled receptors (GPCRs) represent a large fraction of current pharmaceutical targets, and of the GPCRs, the beta(2) adrenergic receptor (beta(2)AR) is one of the most extensively studied. (rcsb.org)
  • The 3D crystallographic structure (see figure and links to the right) of the β2-adrenergic receptor has been determined by making a fusion protein with lysozyme to increase the hydrophilic surface area of the protein for crystal contacts. (wikipedia.org)
  • An alternative method, involving production of a fusion protein with an agonist, supported lipid-bilayer co-crystallization and generation of a 3.5 Å resolution structure. (wikipedia.org)
  • Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs) (4). (bio-medicine.org)
  • 2004. Cannabinoid CB1 receptor protein expression in the rat choroid plexus: a possible involvement of cannabinoids in the regulation of cerebrospinal fluid. (springer.com)
  • 2000. Crystal structure of rhodopsin: A G protein-coupled receptor. (springer.com)
  • 2008. Crystal structure of the ligand-free G-protein-coupled receptor opsin. (springer.com)
  • Recent evidence suggests that binding of agonist to its cognate receptor initiates not only classical G protein-mediated signaling, but also β-arrestin-dependent signaling. (pnas.org)
  • To determine whether β-adrenergic ligands that do not activate G protein signaling (i.e., β-blockers) can stabilize the β 1 AR in a signaling conformation, we screened 20 β-blockers for their ability to stimulate β-arrestin-mediated EGFR transactivation. (pnas.org)
  • By using mutants of the β 1 AR lacking G protein-coupled receptor kinase phosphorylation sites and siRNA directed against β-arrestin, we show that Alp- and Car-stimulated EGFR transactivation requires β 1 AR phosphorylation at consensus G protein-coupled receptor kinase sites and β-arrestin recruitment to the ligand-occupied receptor. (pnas.org)
  • Beta-adrenergic receptors (βARs) are members of the seven transmembrane receptor (7TMR) family that become activated upon catecholamine binding to stimulate G protein-dependent signaling. (pnas.org)
  • Turning off the G protein signal by a process known as desensitization occurs through G protein-coupled receptor kinase (GRK) phosphorylation of the 7TMR, and subsequent binding of β-arrestin ( 1 , 2 ). (pnas.org)
  • Nerve-derived agrin binds to the surface of low-density lipoprotein receptor-related protein (Lrp4), which activates muscle-specific kinase (MuSK) 13 . (nature.com)
  • An approach to the study of G-protein-coupled receptor kinases: an in vitro-purified membrane assay reveals differential receptor specificity and regulation by G beta gamma subunits. (duke.edu)
  • Phosphorylation of GTP-binding-regulatory (G)-protein-coupled receptors by specific G-protein-coupled receptor kinases (GRKs) is a major mechanism responsible for agonist-mediated desensitization of signal transduction processes. (duke.edu)
  • Beta-adrenergic receptor kinase: identification of a novel protein kinase that phosphorylates the agonist-occupied form of the receptor. (duke.edu)
  • cDNA for the human beta 2-adrenergic receptor: a protein with multiple membrane-spanning domains and encoded by a gene whose chromosomal location is shared with that of the receptor for platelet-derived growth factor. (duke.edu)
  • In transfected cell lines, these amino-terminus SNPs alter cellular trafficking of the receptor protein, resulting in variation in agonist-promoted receptor downregulation. (ahajournals.org)
  • ALRI Industries recommends that you take 1 serving of Humapro 25 minutes before taking in any type of protein or amino acids or at least 2 hours after you ingest any sort of protein or amino acid. (bestpricenutrition.com)
  • Alfa-2 ( α 2 ) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje G i heterotrimerni G protein . (wikipedia.org)
  • Beta receptors are divided into beta1, beta2, beta3, which are linked to Gs, and adenylate cyclase, increasing cAMP, which in turn drives cAMP-dependent protein kinase that mediates intracellular events. (thefreedictionary.com)
  • Additionally, these mutations lead to compact ICL3 region compared to the wild type, indicating that the receptor would be inaccessible for G protein coupling. (springer.com)
  • Li Y, Hou T, Goddard I (2010) Computational modeling of structure-function of G protein-coupled receptors with applications for drug design. (springer.com)
  • Probst WC, Snyder LA, Schuster DI, Brosius J, Sealfon SC (1992) Sequence alignment of the G protein-coupled receptor superfamily. (springer.com)
  • Tuteja N (2009) Signaling through G protein coupled receptors. (springer.com)
  • Protein kinase A-mediated phosphorylation of the beta 2-adrenergic receptor regulates its coupling to Gs and Gi. (wikipedia.org)
  • Although the cellular origin of NETs of the GI tract is uncertain, consistent expression of cytokeratins in NETs and the expression of the caudal-related homeodomain protein 2 (CdX2 protein), an intestinal transcription factor in endocrine tumors of the small intestine, suggests an origin from an epithelial precursor cell. (uwhealth.org)
  • K2 and other newly popularized drugs laced with synthetic cannabinoids, which mimic those found in marijuana, bind similarly to G protein-coupled receptors found throughout the body and nervous system. (proteopedia.org)
  • Acts as a regulator of G-protein coupled receptor (GPCR) signaling by mediating the deubiquitination of beta-arrestins (ARRB1 and ARRB2) and beta-2 adrenergic receptor (ADRB2). (uniprot.org)
  • We reported that surface CD23 expression remained constant on primed B cells exposed to a β2AR agonist, while CD23 mRNA, total CD23 protein, and soluble CD23 (sCD23) increased. (jimmunol.org)
  • The nanoparticle coating contained osteoconductive hydroxyapatite (HAP) and osteoinductive bone morphogenetic protein-2 (BMP-2), and induced osteoblastic differentiation of endogenous progenitor cells within the bone marrow without eliciting a foreign-body response. (medpagetoday.com)
  • The G(s) protein is involved in hormonal regulation of adenylate cyclase: it activates the cyclase in response to beta-adrenergic stimuli. (proteopedia.org)
  • The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. (proteopedia.org)
  • G protein-coupled receptors (GPCRs) are responsible for the majority of cellular responses to hormones and neurotransmitters as well as the senses of sight, olfaction and taste. (proteopedia.org)
  • The paradigm of GPCR signalling is the activation of a heterotrimeric GTP binding protein (G protein) by an agonist-occupied receptor. (proteopedia.org)
  • Chromosomal organization of adrenergic receptor genes. (duke.edu)
  • Molecular pharmacology and modeling of vasopressin receptors. (wikipedia.org)
  • Terbutaline (a beta(2)-adrenergic agonist) increased CBF in a dose-dependent manner, and it also decreased the volume of the ciliary cells. (biomedsearch.com)
  • Terbutaline sulfate, USP, the active ingredient of terbutaline sulfate injection, is a beta-adrenergic agonist bronchodilator available as a sterile, nonpyrogenic, aqueous solution in vials, for subcutaneous administration. (nih.gov)
  • Terbutaline sulfate is (±)-α-[(tert-butylamino)methyl]-3,5-dihydroxybenzyl alcohol sulfate (2:1) (salt). (nih.gov)
  • Terbutaline sulfate injection is a beta-adrenergic receptor agonist. (nih.gov)
  • In vitro and in vivo pharmacologic studies have demonstrated that terbutaline exerts a preferential effect on beta 2 -adrenergic receptors. (nih.gov)
  • Controlled clinical studies in patients given terbutaline subcutaneously have not revealed a preferential beta 2 -adrenergic effect. (nih.gov)
  • Monoamine Oxidase Inhibitors or Tricyclic Antidepressants: Terbutaline should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents, since the action of terbutaline on the vascular system may be potentiated. (pediatriconcall.com)
  • Almost 62% of the women were dispensed at least one prescription for short-acting β2-agonist (SABA), 63% at least one inhaled corticosteroid (IC), 42% a fixed-combination of an IC and a long-acting β2-agonist (LABA) and 8% a LABA. (nih.gov)
  • To explore the effects of currently available noradrenergic drugs in these mice, Salehi and colleagues administered formoterol, a long-acting beta-2 adrenergic receptor agonist (LABA). (medpagetoday.com)
  • Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. (uniprot.org)
  • It is therefore likely that brain adrenergic alpha-2-receptors mediate the orexigenic effects of neuropeptide Y and beta-endorphin in layer-type chicks. (biomedsearch.com)
  • They are a class of sympathomimetic agents, each acting upon the beta adrenoceptors. (wikipedia.org)
  • Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs: May potentiate effect. (nih.gov)
  • alpha-adrenergic, which act in response to sympathomimetic stimuli, and beta-adrenergic, which block sympathomimetic activity. (thefreedictionary.com)
  • Beta-adrenergic blocker that has little or no intrinsic sympathomimetic effects and membrane-stabilizing activity. (medscape.com)
  • Blocks beta 1- and beta 2-receptors and has mild intrinsic sympathomimetic effects. (medscape.com)
  • Cells stably expressing WT β 1 ARs were transfected with GFP-tagged EGFR (EGFR-GFP) and stimulated with several agonists or 20 different β-blockers. (pnas.org)
  • ACE inhibitors , angiotensin receptor blockers , [11] and calcineurin inhibitor immunosuppressants such as ciclosporin and tacrolimus . (wikipedia.org)
  • Beta-blockers: May block bronchodilatory effects of beta-agonists and produce severe bronchospasm. (nih.gov)
  • They are constantly gaining in importance, and increasingly more significant than traditional tocolytics such as beta-adrenergic receptor (β-AR) blockers or magnesium sulphate. (mdpi.com)
  • Medications used to decrease aqueous production include beta-blockers (topical), carbonic anhydrase inhibitors (topical and/or oral), and alpha 2-agonists. (medscape.com)
  • Beta-blocking agents have been less well studied for ICU delirium, although beta-blockers are known to have beneficial effects on anxiety, posttraumatic Stress Disorder (PTSD) and aggressive behavior in a variety of populations ( 16 - 20 ). (frontiersin.org)
  • Beta-Blockers: Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-agonists, but may produce severe bronchospasm in asthmatic patients. (pediatriconcall.com)
  • Recent evidence suggests that binding of different ligands promotes distinct receptor conformations leading to specific signaling events ( 9 - 12 ). (pnas.org)
  • We screened β-adrenergic ligands to determine if any could lead to β 1 AR-mediated EGFR transactivation. (pnas.org)
  • A long-acting beta2-adrenergic agonist used in the management of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema. (drugbank.ca)
  • To the extent that the kinetics of recovery from down-regulation reflect "basal" receptor metabolism, the data indicate that enhanced receptor clearance of both receptor subtypes from the plasma membrane contribute to down-regulation, but changes in rates of receptor appearance may occur as well. (aspetjournals.org)
  • There are three families of adrenergic receptors, alpha 1 , alpha 2 and beta, and each family contains three distinct subtypes. (thefreedictionary.com)
  • Pharmacologic, biochemical, and genetic analyses have demonstrated the existence of multiple alpha 2-adrenergic receptor (alpha 2AR) subtypes. (duke.edu)
  • Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. (wikipedia.org)
  • In 2013, zilpaterol, a β agonist sold by Merck, was temporarily withdrawn due to signs of sickness in some cattle that were fed the drug. (wikipedia.org)
  • 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)
  • Activation of β2 adrenergic receptors on airway smooth muscle leads to the activation of adenylate cyclase and to an increase in the intracellular concentration of 3',5'-cyclic adenosine monophosphate (cyclic AMP). (drugbank.ca)
  • Agonist-promoted desensitization of adenylate cyclase is intimately associated with phosphorylation of the beta-adrenergic receptor in mammalian, avian, and amphibian cells. (duke.edu)
  • Beta-agonist- and prostaglandin E1-induced translocation of the beta-adrenergic receptor kinase: evidence that the kinase may act on multiple adenylate cyclase-coupled receptors. (duke.edu)
  • 2006. Cannabinoid receptors as therapeutic targets for obesity and metabolic diseases. (springer.com)
  • 2007. Cannabinoid-1 receptor blockade in cardiometabolic risk reduction: Safety, tolerability, and therapeutic potential. (springer.com)
  • The therapeutic potential of drugs that target cannabinoid receptors or modulate the tissue levels or actions of endocannabinoids. (springer.com)
  • The alpha adrenergic receptor system, which responds to the neurotransmitter adrenaline, is an important signaling mechanism in the body and is believed to be involved in such diverse therapeutic indications as cardiovascular disease, benign prostatic hyperplasia (BPH), pain and glaucoma. (thefreedictionary.com)
  • Beta-2 adrenergički receptor (β 2 adrenoreceptor), takođe poznat kao ADRB2 , je beta-adrenergički receptor . (wikipedia.org)
  • Deubiquitinating enzyme involved in various processes such as centrosome duplication, cellular migration and beta-2 adrenergic receptor/ADRB2 recycling. (uniprot.org)
  • Upon dissociation, it is probably transferred to the translocated beta-arrestins, leading to beta-arrestins deubiquitination and disengagement from ADRB2. (uniprot.org)
  • This suggests the existence of a dynamic exchange between the ADRB2 and beta-arrestins. (uniprot.org)
  • Removal of phosphorylation sites from the beta 2-adrenergic receptor delays onset of agonist-promoted desensitization. (nih.gov)
  • The mechanisms for such processes, collectively referred to as desensitization, often involve alterations in the properties and number of cell-surface hormone receptors. (nih.gov)
  • Direct evidence for a causal relationship between receptor phosphorylation and desensitization has been lacking however. (nih.gov)
  • Here we report that prevention of agonist-stimulated beta 2-adrenergic receptor (beta 2AR) phosphorylation by truncation of its serine and threonine-rich phosphate acceptor segment delays the onset of desensitization. (nih.gov)
  • The molecular basis for the desensitization of beta 2-adrenergic receptors was investigated by oligonucleotide-directed mutagenesis. (aspetjournals.org)
  • Progressive truncation of the C-terminus of the receptor resulted in decreases in the initial rates of receptor sequestration and functional uncoupling, although the final extent of these desensitization processes was not affected by the mutations. (aspetjournals.org)
  • The potential role of this conserved aromatic amino acid residue in the cellular processes of sequestration (a rapid internalization of the surface receptor) and down-regulation (a slower loss of total cellular receptors) associated with agonist-mediated desensitization of the beta 2-adrenergic receptor was assessed by replacing tyrosine residue 326 with an alanine residue (beta 2AR-Y326A). (duke.edu)
  • The only other major change associated with the mutated receptor is a complete loss of the ability to resensitize following rapid desensitization. (duke.edu)
  • Receptor desensitization by agonist is an almost universal process that can be prevented and reversed by corticosteroids. (elsevier.com)
  • delays onset of agonist-promoted desensitization. (cogprints.org)
  • The use of this computer modeling technique for defining kinetics of changes in receptor number from one steady state level to another should provide a generally useful means to assess hormone and neurotransmitter receptor metabolism in vivo. (aspetjournals.org)
  • The nerve terminal releases the neurotransmitter acetylcholine (ACh), which binds to postsynaptic ACh receptors (AChRs) that are located on the surface of muscle fibers. (nature.com)
  • If adherence can't be assured, a fixed-dose combination product containing both an inhaled corticosteroid and a long-acting beta 2 -adrenergic agonist is recommended. (thefreedictionary.com)
  • The authors investigated whether there is a genotype-specific response to treatment with a long-acting beta-2 agonist in combination with an inhaled corticosteroid. (healthcanal.com)
  • A beta-1 agonist used to treat cardiac decompensation in patients with organic heart disease or from cardiac surgery. (drugbank.ca)
  • 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)
  • Catecholamines, cardiac beta-adrenergic receptors, and heart failure. (duke.edu)
  • Background- Sympathetic activation influences the risk of ventricular arrhythmias and sudden cardiac death (SCD), mediated in part by the β2-adrenergic receptor (B2AR). (ahajournals.org)
  • [1] [2] An abnormal heart rate can occur which can result in cardiac arrest and death. (wikipedia.org)
  • Studies in laboratory animals (minipigs, rodents, and dogs) have demonstrated the occurrence of cardiac arrhythmias and sudden death (with histological evidence of myocardial necrosis) when beta-agonists and methylxanthines are administered concurrently. (nih.gov)
  • Highly specific receptor kinases, such as rhodopsin kinase and beta-adrenergic receptor kinase, which show stimulus-dependent phosphorylation of receptors have been described. (nih.gov)
  • Characterization of Glycolytic Enzymes and Pyruvate Kinase M2 in Type 1 and 2 Diabetic Nephropathy. (nih.gov)
  • A beta-adrenergic receptor kinase-like enzyme is involved in olfactory signal termination. (duke.edu)
  • beta-Adrenergic receptor kinase (beta-AR kinase) is a cytosolic enzyme that phosphorylates the beta-adrenergic receptor only when it is occupied by an agonist [Benovic, J. Strasser, R. H., Caron, M. G. & Lefkowitz, R. J. (duke.edu)
  • S.p. mice in response to beta-adrenergic receptor agonist stimuli. (lignol.ca)
  • Activation of β2 receptors induces smooth muscle relaxation in the lungs, gastrointestinal tract, uterus, and various blood vessels. (wikipedia.org)
  • Activation of the β3 receptors induces the metabolism of lipids. (wikipedia.org)
  • In airways, Tiotropium induces bronchodilation via inhibition of the M3 receptor on airway smooth muscle. (studystack.com)
  • Higenamine, being a beta-2 Adrenergic Agonist, induces lipolysis by stimulating beta-2 Adrenergic receptors. (doctor-clinic.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)
  • We have isolated and sequenced a cDNA encoding the human beta 2-adrenergic receptor. (duke.edu)
  • Involvement of tyrosine residues located in the carboxyl tail of the human beta 2-adrenergic receptor in agonist-induced down-regulation of the receptor. (duke.edu)
  • Alternatively, physiological behaviours are modelled with the aim of capturing the underlying control principles governing the behaviour of interest, with only key biological mechanisms characterized and parametrized in detail [ 2 ]. (royalsocietypublishing.org)
  • Different beta 1 and 2 adrenergic receptors agonists might have various biological and physiological effects on fish species. (magiran.com)
  • The present study showed that various beta1 and beta2 adrenergic receptor agonists had same physiological effects on rainbow trout but it seems ractopamine, as a beta1 adrenergic receptor, had more potential on fatty acid metabolism and growth response of rainbow trout. (magiran.com)
  • 1 Furthermore, numerous studies in vivo have shown that expression of VEGF and its receptors is upregulated during angiogenesis under physiological and pathological processes, such as development of the embryo, 2-4 estrous cycle, 5 tumor growth, 6,7 and wound healing. (ahajournals.org)
  • Long-acting β2 agonists such as clenbuterol (not used clinically in the United States) are frequently abused performance-enhancing drugs for their anabolic, lipolytic, and performance-enhancing effects. (wikipedia.org)
  • Clenbuterol remains banned not as a beta-agonist, but rather an anabolic agent. (wikipedia.org)
  • Clenbuterol (frequently described merely as 'Clen') is not a steroid, however a Beta 2 Sympathomitetic and main nerve system (CNS) stimulant. (mondotaitu.com)
  • The body is trying to compensate…clenbuterol is good but it only lasts 2-3 weeks at a time unless you jack up the dosage sky-high. (ironmagazine.com)
  • It relaxes the muscle around the airways into the lungs by activating targets called beta-2 receptors in the muscle cells. (europa.eu)
  • Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor subtype, the gene for which is located on chromosome 2. (duke.edu)
  • 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)
  • These effects have traditionally been thought to be mediated exclusively by receptor activation of intracellular G proteins. (nih.gov)
  • Levosalbutamol acts as a functional agonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges. (drugbank.ca)
  • Because these receptors help control the contraction of the airway muscles, blocking them causes the muscles to relax, helping to keep the airways open. (europa.eu)
  • It binds to (CysLT) type-1 receptors found in human airway (smooth muscle cells and macrophages), which prevents airway edema, smooth muscle contraction and other respiratory inflammation. (studystack.com)
  • beta-2-Adrenergic Receptor Agonists Modulate Human Airway Smooth Muscle Cell Migration via Vasodilator-Stimulated Phosphoprotein. (ndriresource.org)
  • β2AR agonists alleviate bronchoconstriction by targeting the β2AR expressed on bronchiolar smooth muscle cells to trigger airway relaxation, but these drugs also target the β2AR on primed B cells, potentially producing an IgE effect that may be counterproductive to the drugs intended use. (jimmunol.org)
  • Considering its widespread use in humans and positive effects on cognition in [these] mice, formoterol or similar beta-2 adrenergic receptor agonists with ability to cross the blood-brain barrier might be attractive candidates for clinical trials to improve cognitive function in individuals with Down syndrome," the researchers wrote in their paper in Biological Psychiatry . (medpagetoday.com)
  • For treatment of acute episodes of bronchospasm or prevention of symptoms associated with bronchospasm, the recommended dosage for adults and children 4 years of age or older is 2 inhalations repeated every 4 to 6 hours. (rxlist.com)
  • For prevention of exercise-induced bronchospasm, the recommended dosage for adults and children 4 years of age or older is 2 inhalations 15 to 30 minutes before exercise. (rxlist.com)
  • Our findings indicate that agonist-dependent beta2-adrenergic receptor binding of NHERF plays a role in beta2-adrenergic receptor-mediated regulation of Na+/H+ exchange. (nih.gov)
  • Beta 2-adrenergic regulation of ciliary beat frequency in rat bronchiolar epithelium: potentiation by isosmotic cell shrinkage. (biomedsearch.com)
  • The beta(2)-adrenergic regulation of ciliary beat frequency (CBF) was studied using video-optical microscopy. (biomedsearch.com)
  • Application to agonist-mediated down-regulation of rat renal cortical beta 1- and beta 2-adrenergic receptors. (aspetjournals.org)
  • We have developed a method for the assessment of agonist-induced down-regulation of receptors in vivo in terms of rates of receptor appearance and disappearance. (aspetjournals.org)
  • During recovery from down-regulation, the beta 1-receptors have a t 1/2 of 45 hr and a kappa ap of 1.6%/hr, and the beta 2-adrenergic receptors a t 1/2 of 18 hr and a kappa ap of 3.9%/hr. (aspetjournals.org)
  • During down-regulation, the t 1/2 for both receptors is 12 hr, while kappa ap for beta 1-receptors and beta 2-receptors are 3 and 2.3%/hr, respectively. (aspetjournals.org)
  • Even though NM receptor regulation is implicated in the pharmacological action of many drugs, and is also known to be influenced by various environmental factors, its functional consequences and modes of action are not well understood. (cogprints.org)
  • In this paper we summarize relevant experimental evidence on NM receptor regulation (specifically dopamine D1 and D2 receptors) in order to explore its significance for neural and synaptic plasticity. (cogprints.org)
  • We identify the relevant components of NM receptor regulation (receptor phosphorylation, receptor trafficking and sensitization of second-messenger pathways) gained from studies on cultured cells. (cogprints.org)
  • Key principles in the regulation and control of short-term plasticity (sensitization) are identified, and a model is presented which employs direct and indirect feedback regulation of receptor efficacy. (cogprints.org)
  • Finally, we discuss the implications of NM receptor regulation for models of brain plasticity and memorization.We emphasize that a realistic model of brain plasticity will have to go beyond Hebbian models of long-term potentiation and depression to include plasticity in the distribution and efficacy of NM receptors. (cogprints.org)
  • The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer-type chicks. (biomedsearch.com)
  • In this issue of Circulation Research , Muthig et al demonstrate a critical role for α 2B -adrenoceptors in VEGF-associated angiogenic regulation in the placenta via the suppression of expression of the VEGF receptor-1 (Flt-1) and its soluble splice variant (sFlt-1). (ahajournals.org)
  • We have recently delineated three polymorphic loci within the coding block of the beta 2AR which alter amino acids at positions 16, 27, and 164 and impart specific biochemical and pharmacologic phenotypes to the receptor. (jci.org)
  • 2-4 Animal studies suggest that the β2-adrenergic receptor (B2AR) partly mediates this response to sympathetic activation. (ahajournals.org)
  • subicular neurons via presynaptic D1-like dopamine receptors. (cogprints.org)
  • Human Dopamine Receptor D4 (DRD4) orchestrates several neurological functions and represents a target for many psychological disorders. (springer.com)
  • 2006) Genetic susceptibility to Parkinson's disease among south and north Indians: I. Role of polymorphisms in dopamine receptor and transporter genes and association of DRD4 120-bp duplication marker. (springer.com)
  • Seeman P, Guan HC, Van Tol HH (1993) Dopamine D4 receptors elevated in schizophrenia. (springer.com)
  • 2009) Investigation of dopamine receptors in susceptibility to behavioural and psychological symptoms in Alzheimer's disease. (springer.com)
  • 2003) Progressive striatal and cortical dopamine receptor dysfunction in Huntington's disease: a PET study. (springer.com)
  • American Journal of Respiratory Cell and Molecular Biology 49(2): 204-11. (ndriresource.org)
  • It blocks muscarinic receptors in muscle cells in the airways. (europa.eu)
  • It works by blocking some receptors called muscarinic receptors, which control the contraction of muscles. (europa.eu)
  • 1) Alpha receptors, which evoke an excitatory response of smooth muscle cells to catecholamines. (thefreedictionary.com)
  • Alpha receptors are divided into alpha1 (Gq) and alpha2 (Gi) coupled receptors. (thefreedictionary.com)
  • Beta 2 adrenergic agonist drugs as a class are widely used in obstetrics as tocolytics to inhibit or slow down labor and bronchodilators, but may act as functional and behavioral teratogens when given continuously in the mid to late second or early third trimesters. (elsevier.com)
  • Our screens identified several classes of molecules that include inhibitors of the bromodomain and extra-terminal (BET) family of proteins and agonists of the beta-2 adrenergic receptor. (biomedcentral.com)
  • Specificity determinants for lipids bound to beta-barrel proteins. (biomedsearch.com)