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

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 [3H]diprenorphine (0.3-0.4 nM). 3. Only 7 drugs (alpha,5beta-tetrahydrodeoxycorticosterone, megestrol acetate, mifepristone, 17alpha-ethynylestradiol, diethylstilbestrol, clomiphene citrate and tamoxifen citrate) inhibited [3H]diprenorphine binding more than 50% at the highest concentration assayed (10(-4) M). The IC50 values ranged between 6x10(-5) M. 4. Thus, the present results show that only a limited number of steroids, from diverse classes, bind to opiate receptors.