氟马西尼和CGS 8216对氯雷唑抗焦虑样特性无影响。

Lack of effect of flumazenil and CGS 8216 on the anxiolytic-like properties of loreclezole.

作者信息

Dawson G R, Curnow R, Bayley P, Rambridge A, Tricklebank M D

机构信息

Merck, Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK.

出版信息

Eur J Pharmacol. 1994 Feb 11;252(3):325-8. doi: 10.1016/0014-2999(94)90180-5.

DOI:10.1016/0014-2999(94)90180-5

PMID:7909294

Abstract

Loreclezole is a novel antiepileptic that interacts in a unique way with the GABAA receptor complex. Its anticonvulsant effect in rats is reversed by benzodiazepine receptor partial inverse agonists, such as CGS 8216 but not by the competitive benzodiazepine receptor antagonist, flumazenil (Ro 15-1788). In this study loreclezole (30.0-50.0 mg/kg i.p.) was found to induce an anxiolytic-like effect in a rat conditioned emotional response test that was reversed neither by flumazenil (10.0 mg/kg) nor by CGS 8216 (2-phenylpyrazolo[4,3-c]quinolin-3(5H)-one, 0.3-3.0 mg/kg). The results suggest that the anxiolytic-like effects of loreclezole are not mediated by the benzodiazepine receptor.

摘要

洛雷唑是一种新型抗癫痫药物，它以独特的方式与GABAA受体复合物相互作用。在大鼠中，其抗惊厥作用可被苯二氮䓬受体部分反向激动剂（如CGS 8216）逆转，但不能被竞争性苯二氮䓬受体拮抗剂氟马西尼（Ro 15-1788）逆转。在本研究中，发现洛雷唑（腹腔注射30.0 - 50.0毫克/千克）在大鼠条件性情绪反应试验中诱导出抗焦虑样效应，该效应既不能被氟马西尼（10.0毫克/千克）逆转，也不能被CGS 8216（2-苯基吡唑并[4,3-c]喹啉-3(5H)-酮，0.3 - 3.0毫克/千克）逆转。结果表明，洛雷唑的抗焦虑样效应不是由苯二氮䓬受体介导的。