Cyproterone acetate displaces opiate binding in mouse brain

被引:5
作者
Gutierrez, M [1 ]
Menendez, L [1 ]
RuizGayo, M [1 ]
Hidalgo, A [1 ]
Baamonde, A [1 ]
机构
[1] FAC MED,DEPT MED,FARMACOL LAB,OVIEDO 33071,SPAIN
关键词
opioid; steroid; cyproterone acetate; binding;
D O I
10.1016/S0014-2999(97)83034-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Drugs acting on androgen receptors modify opioid transmission in the central nervous system. To investigate a direct interaction, we studied whether the binding of [H-3]diprenorphine to mouse brain membranes was modified by cyproterone acetate (progesterone derivative with antiandrogen activity), flutamide (non-steroidal antiandrogen), 5 alpha-dihydrotestosterone and progesterone. Only cyproterone acetate inhibited [H-3]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.
引用
收藏
页码:99 / 102
页数:4
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