大鼠前列腺和精囊内[3H]Ro 5-4864的特异性结合位点

Specific binding sites for [3H]Ro 5-4864 in rat prostate and seminal vesicle.

Camins A, Sureda F X, Camarasa J, Escubedo E

Laboratory of Pharmacology and Pharmacognosy, Faculty of Pharmacy, University of Barcelona, Spain.

Gen Pharmacol. 1992 May;23(3):381-4. doi: 10.1016/0306-3623(92)90098-5.

Abstract

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

摘要

使用[3H]Ro 5-4864作为放射性配体，对大鼠前列腺和精囊中的外周型苯二氮䓬受体进行了表征。2. 这种放射性配体对该受体的亲和力在大鼠前列腺中（KD = 4.36 +/- 1.02 nM）高于精囊（KD = 8.45 +/- 1.34 nM）。3. 在这两种组织中获得的结合位点密度分别为：前列腺中Bmax = 4164 +/- 873 fmol/mg，精囊中为5978 +/- 1022 fmol/mg。4. [3H]Ro 5-4864的结合受到阿特拉津和α,β-亚甲基-ATP的非竞争性抑制，表明其受到ADP/ATP线粒体载体的调节。5. 氟他胺能够以与原卟啉IX相似的IC50取代结合的[3H]Ro 5-4864。