Add time:08/14/2019         Source:sciencedirect.com

Drugs acting on androgen receptors modify opioid transmission in the central nervous system. To investigate a direct interaction, we studied whether the binding of [3H]diprenorphine to mouse brain membranes was modified by cyproterone acetate (progesterone derivative with antiandrogen activity), flutamide (non-steroidal antiandrogen), 5α-dihydrotestosterone and progesterone. Only cyproterone acetate inhibited [3H]diprenorphine binding (IC50=(1.62±0.33)×10−6 M) without modifying its association rate. These results suggest that cyproterone acetate binds to opiate receptors independently of its classical androgenic intracellular receptor effect.

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