SPECIFIC BINDING-SITES FOR [H-3] RO-5-4864 IN RAT PROSTATE AND SEMINAL-VESICLE

被引：12

作者：

CAMINS, A ^{[1
]}

SUREDA, FX ^{[1
]}

CAMARASA, J ^{[1
]}

ESCUBEDO, E ^{[1
]}

机构：

[1] UNIV BARCELONA,FAC PHARM,PHARMACOL & PHARMACOGNOSY,ZONA UNIV PEDRALBES,E-08028 BARCELONA,SPAIN

来源：

GENERAL PHARMACOLOGY | 1992年 / 23卷 / 03期

关键词：

D O I：

10.1016/0306-3623(92)90098-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. The peripheral-type benzodiazepine receptor was characterized in rat prostate and seminal vesicle using [H-3]Ro 5-4864 as radioligand. 2. The affinity of this radioligand for this receptor was higher in rat prostate (K(D) = 4.36 +/- 1.02 nM) than in seminal vesicle (K(D) = 8.45 +/- 1.34 nM). 3. The density of binding sites obtained in these two tissues was B(max) = 4164 +/- 873 fmol/mg in prostate and 5978 +/- 1022 fmol/mg in seminal vesicle. 4. The [H-3]Ro 5-4864 binding was inhibited non-competitively by atractyloside and alpha,beta-methyleneATP, suggesting a modulation by the ADP/ATP mitochondrial carrier. 5. Flutamide was able to displace bound [H-3)Ro 5-4864 with an IC50 similar to protoporphyrin IX.

引用

页码：381 / 384

页数：4

共 16 条

[1] BINDING OF [H-3] RO 5-4864 AND [H-3] PK 11195 TO CEREBRAL-CORTEX AND PERIPHERAL-TISSUES OF VARIOUS SPECIES - SPECIES-DIFFERENCES AND HETEROGENEITY IN PERIPHERAL BENZODIAZEPINE BINDING-SITES [J].