Endomorphins fully activate a cloned human mu opioid receptor
作者: Jianhua GongJudith A StrongShengwen ZhangXia YueRobert N DeHavenJeffrey D DaubertJoel A CasselGuangling YuErik ManssonLei Yu
作者单位: 1Department of Cell Biology, Neurobiology and Anatomy,University of Cincinnati College of Medicine, 231 Bethesda Avenue, Cincinnati, OH 45267-0521, USA
2Department of Psychiatry, University of Cincinnati College of Medicine, Cincinnati, OH 45267-0521, USA
3Adolor Corporation, Malvern, PA 19355, USA
刊名: FEBS Letters, 1998, Vol.439 (1), pp.152-156
来源数据库: Elsevier Journal
DOI: 10.1016/S0014-5793(98)01362-3
关键词: EndomorphinHuman mu opioid receptor
原始语种摘要: Abstract(#br)Endomorphins were recently identified as endogenous ligands with high selectivity for mu opioid receptors. We have characterized the ability of endomorphins to bind to and functionally activate the cloned human mu opioid receptor. Both endomorphin-1 and endomorphin-2 exhibited binding selectivity for the mu opioid receptor over the delta and kappa opioid receptors. Both agonists inhibited forskolin-stimulated increase of cAMP in a dose-dependent fashion. When the mu opioid receptor was coexpressed in Xenopus oocytes with G protein-activated K + channels, application of either endomorphin activated an inward K + current. This activation was dose-dependent and blocked by naloxone. Both endomorphins acted as full agonists with efficacy similar to that of [ d -Ala 2 , N -Me-Phe 4...
全文获取路径: Elsevier  (合作)
影响因子:3.582 (2012)

  • opioid 鸦片样物质
  • receptor 接受体
  • activate 活化
  • naloxone 纳洛酮
  • potassium 
  • protein 蛋白质
  • blocked 分块
  • rectifying 精馏
  • cAMP 环腺苷酸
  • endogenous 内成的