• selective
  • Ro40-2148 Solabegron (GW-427,353) Vibegron (MK-4618) L-748,328 L-748,337 SR 59230A was thought to be a selective β3 antagonist but later found to also be an antagonist of the α1 receptor. (wikipedia.org)
  • 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)
  • affinity
  • Affinity chromatography of digitonin-solubilized membranes yielded a 20,000-fold purified receptor which had conserved essentially all the pharmacological properties of the membrane-bound binding sites. (springer.com)
  • The neurotransmitter noradrenaline has higher affinity for the α1 receptor than does adrenaline (which is a hormone). (wikipedia.org)
  • Evidence for high and low affinity alpha 2-receptors. (wikipedia.org)
  • stimulate
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (els.net)
  • 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)

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  • 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)
  • 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)
  • 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)
  • 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)
  • stimulation
  • Myocardial alpha 1-adrenergic receptor stimulation. (ahajournals.org)
  • It is now generally accepted that chronically elevated stimulation of the cardiac β-adrenergic system is toxic to the heart and that such stimulation may contribute to the pathogenesis of congestive heart failure of various causes. (ahajournals.org)
  • 6 It is against this background that an article in this issue by Liggett et al 7 highlights several misconceptions and unfounded assumptions about β-adrenergic stimulation of the heart and points the way toward a more rational reconsideration of the potential for manipulating β-adrenergic signaling in the heart for therapeutic gain. (ahajournals.org)
  • These animals had remarkably elevated contractility unresponsive to further β-adrenergic stimulation. (ahajournals.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)
  • arrestin
  • Similarly to the βARK system, the phosphorylated rhodopsin residues will then bind to arrestin, resulting in receptor desensitization. (wikipedia.org)