抗惊厥苯二氮䓬受体的部分激动剂：CGS - 8216对Ro 15 - 1788抗惊厥作用的逆转。

A partial agonist at the anticonvulsant benzodiazepine receptor: reversal of the anticonvulsant effects of Ro 15-1788 with CGS-8216.

作者信息

Robertson H A, Riives M, Black D A, Peterson M R

出版信息

Brain Res. 1984 Jan 23;291(2):388-90. doi: 10.1016/0006-8993(84)91275-7.

PMID:6320966

Abstract

A benzodiazepine antagonist (Ro 15-1788) prevents the development of kindled seizures. CGS-8216, another benzodiazepine antagonist, prevents DMCM-induced seizures (indicating that CGS-8216 acts at a benzodiazepine receptor) but has no effect on kindling or kindled seizures. CGS-8216 prevents the anticonvulsant actions of Ro 15-1788 suggesting that Ro 15-1788 is a partial agonist at an anticonvulsant benzodiazepine receptor. These results support that idea of of distinct, separate receptors for anticonvulsant and sedative effects of benzodiazepines.

摘要

一种苯二氮䓬拮抗剂（Ro 15-1788）可预防点燃性癫痫发作的发展。另一种苯二氮䓬拮抗剂CGS-8216可预防DMCM诱导的癫痫发作（表明CGS-8216作用于苯二氮䓬受体），但对点燃或点燃性癫痫发作无影响。CGS-8216可阻断Ro 15-1788的抗惊厥作用，提示Ro 15-1788是抗惊厥苯二氮䓬受体的部分激动剂。这些结果支持了苯二氮䓬抗惊厥和镇静作用存在不同、独立受体的观点。