Cyproterone acetate displaces opiate binding in mouse brain.
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), 5alpha-dihydrotestosterone and progesterone. Only cyproterone acetate inhibited [3H]diprenorphine binding (IC50 = (1.62 +/- 0.33) x 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.
Gutiérrez
M
M
Departamento de Medicina, Facultad de Medicina, Oviedo, Spain.
Menéndez
L
L
Ruiz-Gayo
M
M
Hidalgo
A
A
Baamonde
A
A
D000726:Androgen Antagonists / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D017373:Cyproterone Acetate / Q000378:metabolism / Q000494:pharmacology*; D013196:Dihydrotestosterone / Q000378:metabolism / Q000494:pharmacology; D004174:Diprenorphine / Q000378:metabolism* / Q000494:pharmacology; D005485:Flutamide / Q000378:metabolism / Q000494:pharmacology; D007553:Isotope Labeling; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009292:Narcotic Antagonists / Q000378:metabolism* / Q000494:pharmacology; D011374:Progesterone / Q000378:metabolism / Q000494:pharmacology; D011957:Receptors, Opioid / Q000187:drug effects* / Q000378:metabolism
D000726:Androgen Antagonists; D009292:Narcotic Antagonists; D011957:Receptors, Opioid; D013196:Dihydrotestosterone; D004174:Diprenorphine; D011374:Progesterone; D017373:Cyproterone Acetate; D005485:Flutamide