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

, : Different types of steroids inhibit [3H]diprenorphine binding in mouse brain membranes. General Pharmacology 31(5): 747-751

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.


PMID: 9809473

DOI: 10.1016/s0306-3623(98)00110-4

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