| 二氢埃托啡对大鼠脑阿片受体的结合特性 |
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| 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 |
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| 作者姓名： | 王丹心 黄矛 |
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| 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 |
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| 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。
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| 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 |
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| 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 |
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| Authors: | WANG Dan-Xin HUANG Mao QIN Bo-Yi Institute of Pharmacology Toxicology Academy of Military Medical Sciences Beijing |
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| Affiliation: | WANG Dan-Xin,HUANG Mao,QIN Bo-Yi Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing 100850 |
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| 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 and[3H]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. |
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| 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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