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。
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.
出处
《中国药理学与毒理学杂志》
CAS
CSCD
北大核心
1991年第3期161-163,共3页
Chinese Journal of Pharmacology and Toxicology
关键词
二氢埃托啡
阿片受体
脑
大鼠
药理
dihydroetorphine
[3H]naloxone
[3H](D-Pen2,5)-enkephalin
[3H]etorphine
mu-opioid receptor
delta-opioid receptor
kappa-opioid receptor
rat brain homogenates
