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  • homologous
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs share many similarities in receptor phosphorylation, use of accessory proteins and sequestration of the receptors. (els.net)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (els.net)
  • catecholamine
  • Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions. (els.net)
  • Two approaches have been used to purify the β-adrenergic catecholamine receptor from turkey erythrocyte plasma membranes. (springer.com)
  • Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. (wikipedia.org)
  • The combination of these two properties can result in bimodal effects on receptor activity that are meaningful for basal activity and chronotropic catecholamine responses of human cardiomyocytes. (wikipedia.org)
  • insulin
  • Using [ 3 H]-yohimbine as a ligand for α 2 -adrenergic receptors, we have demonstrated that insulin is able to decrease [ 3 H]-yohimbine binding to glia in a time- and dose-dependent manner. (springer.com)
  • These results suggest that insulin, by modulating α 2 adrenergic receptor levels, is able to regulate the amount of NE present in the synaptic cleft. (springer.com)
  • Richards E.M., Raizada M.K., Sumners C. (1987) Insulin Downregulates Alpha-2 Adrenergic Receptors in Cultured Glial Cells. (springer.com)
  • In: Raizada M.K., Phillips M.I., LeRoith D. (eds) Insulin, Insulin-like Growth Factors, and Their Receptors in the Central Nervous System. (springer.com)
  • Indications of hypoglycemia were also reported due to secretion of insulin in the body from activation of β2 receptors. (wikipedia.org)
  • muscarinic
  • Other: Experimental studies observed that activating autoantibodies to the beta1/2-adrenergic and M2 muscarinic receptors are associated with atrial tachyarrhythmias in patients with hyperthyroidism. (wikipedia.org)
  • stimulate
  • Actions of the β1 receptor include: stimulate viscous, amylase-filled secretions from salivary glands Increase cardiac output Increase heart rate in sinoatrial node (SA node) (chronotropic effect) Increase atrial cardiac muscle contractility. (wikipedia.org)
  • Pharmacology
  • In June of that year, Raymond Ahlquist, Professor of Pharmacology at Medical College of Georgia, published a paper concerning adrenergic nervous transmission. (wikipedia.org)
  • In 1954, he was able to incorporate his findings in a textbook, Drill's Pharmacology in Medicine, and thereby promulgate the role played by α and β receptor sites in the adrenaline/noradrenaline cellular mechanism. (wikipedia.org)
  • contraction
  • It also induces contraction of the urinary bladder, although this effect is minor compared to the relaxing effect of β2-adrenergic receptors. (wikipedia.org)
  • Other effects on smooth muscle are contraction in: Ureter Uterus (when pregnant) Urethral sphincter Bronchioles (although minor to the relaxing effect of β2 receptor on bronchioles) Iris dilator muscle Seminal tract, resulting in ejaculation Activation of α1-adrenergic receptors produces anorexia and partially mediates the efficacy of appetite suppressants like phenylpropanolamine and amphetamine in the treatment of obesity. (wikipedia.org)
  • Actions of the β2 receptor include: Heart muscle contraction increase cardiac output (minor degree compared to β1). (wikipedia.org)
  • Increased heart rate and heart muscle contraction are also associated with the β2 receptors. (wikipedia.org)
  • Ligand
  • 1987) Ligand binding to the beta‐adrenergic receptor involves its rhodopsin‐like core. (els.net)
  • Due partly to the lack of reliable receptor structures, drug discovery efforts have been largely ligand-based. (pnas.org)
  • The recently determined X-ray structure of the β 2 -adrenergic receptor offers an opportunity to investigate the advantages and limitations inherent in a structure-based approach to ligand discovery against this and related GPCR targets. (pnas.org)
  • Despite the lack of crystal structures, adrenergic GPCRs have been successfully targeted for drug discovery by using ligand-based analoging. (pnas.org)
  • With the recent determination of the crystal structure of this receptor ( 9 , 10 ), we were interested to see how well the atomic model performed as a template for ligand discovery, using docking screens of large chemical libraries. (pnas.org)
  • Beta-2 adrenergic receptors have also been found to couple with Gi, possibly providing a mechanism by which response to ligand is highly localized within cells. (wikipedia.org)
  • cardiac
  • These animals still displayed markedly elevated cardiac contractility at 1 year of age and developed mild fibrosis late in life (≥1 year), 9 as would be expected from the dose-response curves for receptor expression now provided by Liggett et al. (ahajournals.org)
  • Associated pathologies: Cardiovascular diseases and events: Circulating autoantibodies to adrenergic receptors have been identified in numerous heart diseases and cardiac symptoms. (wikipedia.org)
  • In canine models inoculated with adrenergic autoantibodies, it has been shown that beta blockers can negate certain cardiac arrhythmias. (wikipedia.org)
  • It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue. (wikipedia.org)
  • Activation of β1 receptors induces positive inotropic, chronotropic output of the cardiac muscle, leading to increased heart rate and blood pressure, secretion of ghrelin from the stomach, and renin release from the kidneys. (wikipedia.org)

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