大鼠脑和血小板中的中枢及外周苯二氮䓬受体：地西泮和氯巴占治疗的影响

Central and peripheral benzodiazepine receptors in rat brain and platelets: effects of treatment with diazepam and clobazam.

作者信息

Larkin J G, Thompson G G, Scobie G, Brodie M J

机构信息

University Department of Medicine and Therapeutics, Western Infirmary, Glasgow, UK.

出版信息

Seizure. 1992 Sep;1(3):177-82. doi: 10.1016/1059-1311(92)90022-s.

DOI:10.1016/1059-1311(92)90022-s

PMID:1344764

Abstract

Tolerance to the effects of benzodiazepines (BZ) may be mediated by changes in benzodiazepine receptors (BZRs). Peripheral BZRs (in brain and platelets) and central BZRs (in brain) were measured in rats following intraperitoneal administration of diazepam and clobazam each for 4 and 12 days. BZRs were measured by binding assays using [3H] PK 11195 (peripheral) and [3H] flunitrazepam (central) as radioligands. Diazepam, but not clobazam, increased peripheral BZR numbers in platelets (both P < 0.005), but not in brain, after 4 and 12 days' treatment compared with appropriate controls. Neither drug altered central BZR affinities or numbers in rat brain. BZ effects on peripheral BZRs in platelets cannot be extrapolated to predict changes in brain receptors, either peripheral or central.

摘要

对苯二氮䓬（BZ）作用的耐受性可能由苯二氮䓬受体（BZR）的变化介导。在大鼠腹腔注射地西泮和氯巴占各4天和12天后，测量外周BZR（存在于脑和血小板中）和中枢BZR（存在于脑中）。使用[3H] PK 11195（外周）和[3H]氟硝西泮（中枢）作为放射性配体，通过结合测定法测量BZR。与相应对照组相比，在治疗4天和12天后，地西泮而非氯巴占增加了血小板中的外周BZR数量（两者P < 0.005），但未增加脑中的外周BZR数量。两种药物均未改变大鼠脑中中枢BZR的亲和力或数量。BZ对血小板中外周BZR的作用不能外推以预测脑受体（外周或中枢）的变化。