Hantraye P, Brouillet E, Fukuda H, Chavoix C, Guibert B, Dodd R H, Prenant C, Crouzel M, Naquet R, Mazière M
Département de Biologie, Hôpital d'Orsay, France.
Eur J Pharmacol. 1988 Aug 9;153(1):25-32. doi: 10.1016/0014-2999(88)90584-5.
After labelling the brain benzodiazepine receptors of sub-human primates with [11C]RO15-1788, the interactions of different benzodiazepine receptor antagonist ligands were studied by positron emission tomography (PET). Various doses of either RO15-1788, RO15-3505 or propyl beta-carboline-3-carboxylate were injected intravenously 20 min after the radiotracer, and induced an immediate and specific dose-dependent displacement of the brain radioactivity. However, a comparison of the dose-receptor occupancy patterns of these three antagonists established from the displacement experiments revealed that only propyl beta-carboline-3-carboxylate displayed clear biphasic dose-receptor occupancy curves. This indicates that, in the living primate brain, there are two different benzodiazepine receptor subpopulations (which can be either different benzodiazepine receptor subtypes or distinct conformational states of a single receptor).
在用[11C]RO15 - 1788标记亚人类灵长类动物的脑苯二氮䓬受体后，通过正电子发射断层扫描（PET）研究了不同苯二氮䓬受体拮抗剂配体的相互作用。在注射放射性示踪剂20分钟后，静脉注射不同剂量的RO15 - 1788、RO15 - 3505或丙基β - 咔啉 - 3 - 羧酸盐，它们立即引起脑放射性的特异性剂量依赖性位移。然而，根据位移实验建立的这三种拮抗剂的剂量 - 受体占据模式的比较表明，只有丙基β - 咔啉 - 3 - 羧酸盐显示出清晰的双相剂量 - 受体占据曲线。这表明，在活体灵长类动物脑中，存在两种不同的苯二氮䓬受体亚群（它们可以是不同的苯二氮䓬受体亚型，也可以是单个受体的不同构象状态）。
