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二氢埃托啡对大鼠脑阿片受体的结合特性
引用本文:王丹心,黄矛.二氢埃托啡对大鼠脑阿片受体的结合特性[J].中国药理学与毒理学杂志,1991,5(3):161-163.
作者姓名:王丹心  黄矛
作者单位:军事医学科学院毒物药物研究所,军事医学科学院毒物药物研究所,军事医学科学院毒物药物研究所 北京 100850,北京 100850,北京 100850
摘    要:本文在大鼠脑匀浆P_2膜上,观察了二氢埃托啡(DHE)对~3H]纳洛酮,~3H]DPDPE和~3H]埃托啡(预先用30nmol/L吗啡和100nmol/L DADLE阻断μ和δ受体)与阿片受体结合的抑制强度。结果表明:DHE对~3H]纳洛酮与阿片受体结合的抑制强度远远大于对~3H]DPDPE和~3H]埃托啡(预先阻断μ和δ受体后)。DHE对μ,δ和κ受体的相对亲和力之比为1951:2:1,提示DHE为μ受体相对选择性配体。

关 键 词:二氲埃托啡  [~3H]洛酮  [~3H](D-Pen~(2  5))-脑啡肽  [~3]埃托啡  μ-阿片受体  δ-阿片受体  K-阿片受体  大鼠脑匀浆

Binding characteristics of dihydroetorphine to opioid receptors in rat brain
WANG Dan-Xin,HUANG Mao,QIN Bo-Yi Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing.Binding characteristics of dihydroetorphine to opioid receptors in rat brain[J].Chinese Journal of Pharmacology and Toxicology,1991,5(3):161-163.
Authors:WANG Dan-Xin  HUANG Mao  QIN Bo-Yi Institute of Pharmacology and Toxicology  Academy of Military Medical Sciences  Beijing
Institution:WANG Dan-Xin,HUANG Mao,QIN Bo-Yi Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing 100850
Abstract:The inhibitory potency of dihydroe torphine against the binding of 3H]naloxone, 3H]DPDPE and 3H]etorphine (with mu and delta sites having been previously suppressed by 30 nmol / L morphine and 100 nmol / L DADLE) to homogenates of rat brain opioid receptors was studied. The results showed that the inhibitory potency of dihydroetorphine against the binding of 3H]naloxone was much greater than that of 3H]DPDPE and3H]etorphine. The relative affinity of dihydroetorphine to mu, delta and kappa receptors was 1951 : 2:1. This indicates that dihydroetorphine is a relative mu-receptor selective ligand.
Keywords:dihydroetorphine  [3H]naloxone  [3H](D-Pen2  5)-enkephalin  [3H]etorphine  mu-opioid receptor  delta-opioid receptor  kappa-opioid receptor  rat brain homogenates
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