LOW DIHYDROPYRIDINE RECEPTOR DENSITY IN VASA DEFERENTIA OF CASTRATED RATS

被引:20
作者
CASTILLO, CJF
LAFAYETTE, S
CARICATINETO, A
SETTE, M
JURKIEWICZ, NH
GARCIA, AG
JURKIEWICZ, A
机构
[1] ESCOLA PAULISTA MED SCH,DEPT PHARMACOL,CAIXA POSTAL 20372,BR-04034 SAO PAULO,BRAZIL
[2] UNIV AUTONOMA MADRID,FAC MED,DEPT BIOCHEM,MADRID 34,SPAIN
[3] UNIV AUTONOMA MADRID,FAC MED,DEPT PHARMACOL,MADRID 34,SPAIN
关键词
DIHYDROPYRIDINE RECEPTORS; VAS DEFERENS; CALCIUM CHANNELS; CASTRATION;
D O I
10.1111/j.1476-5381.1992.tb14241.x
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
Radioligand binding studies in crude membrane preparations of vasa deferentia of normal rats, with the 1,4-dihydropyridine (+)-[H-3]-PN200-110 (isradipine) showed typical saturation isotherms. The binding exhibited a K(D) of 259 +/- 60 pM and B(max) of 144 +/- 20 fmol mg-1 protein. The low K(D) and the stereoselective displacement of (+)-[H-3]-PN200-110 binding by (+)- and (-)-PN200-110 and by nifedipine suggests that these tissues contain dihydropyridine receptors probably coupled to voltage-sensitive, L-type calcium channels. In membrane preparations from vasa deferentia from rats castrated 30 days previously the maximum specific binding was 25 +/- 10 fmol mg-1 protein, representing only 11% of total binding; thus, the calculation of reliable K(D) values was not feasible. These findings suggest that a testicular hormone, possibly testosterone, plays an important role in the regulation of dihydropyridine-sensitive, voltage-dependent calcium channels in the rat vas deferens.
引用
收藏
页码:257 / 258
页数:2
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