Different types of steroids inhibit [3H]diprenorphine binding in mouse brain membranes

被引：5

作者：

Gutiérrez, M ^{[1
]}

Menéndez, L ^{[1
]}

Brieva, R ^{[1
]}

Hidalgo, A ^{[1
]}

Baamonde, A ^{[1
]}

机构：

[1] Fac Med, Dept Med, Farmacol Lab, Oviedo 33071, Spain

来源：

GENERAL PHARMACOLOGY | 1998年 / 31卷 / 05期

关键词：

steroids; opiate; nongenomic effect; H-3]diprenorphine; mouse brain;

D O I：

10.1016/S0306-3623(98)00110-4

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. The binding of 60 drugs, mainly steroids, to opioid receptors was studied in crude membrane fractions from mouse brains. 2. Competition assays with the different drugs (5 x 10(-7)-10(-4) M) were performed by labeling opiate receptors with [H-3]diprenorphine (0.3-0.4 nM). 3. Only 7 drugs (alpha,5 beta-tetrahydrodeoxycorticosterone, megestrol acetate, mifepristone, 17 alpha-ethynlestradiol, diethylstilbestrol, clomiphene citrate and tamoxifen citrate) inhibited [H-3]diprenorphine binding more than 50% at the highest concentration assayed (10(-4) M). The IC50 values ranged between 6 x 10(-5) M. 4. Thus, the present results show that only a limited number of steroids, from diverse classes, bind to opiate receptors. (C) 1998 Elsevier Science Inc.

引用

页码：747 / 751

页数：5

共 29 条

[1] SEX-RELATED DIFFERENCES IN THE EFFECTS OF MORPHINE AND STRESS ON VISCERAL PAIN [J].