James V, Gardner C R
Eur J Pharmacol. 1985 Jul 17;113(2):233-8. doi: 10.1016/0014-2999(85)90740-x.
Amphetamine-induced twitching of the suprahyoid muscle in nialamide-pretreated, urethane-anaesthetised rats was inhibited by the benzodiazepine agonists RU 32007, diazepam and chlordiazepoxide and the GABAA agonist muscimol. Ro15-1788 and CGS 8216 induced slight, or no reduction in twitching, respectively, but reversed the effect of RU 32007 and diazepam. Ro15-1788 did not reverse the effect of muscimol. Picrotoxin reversed both muscimol and RU 32007 effects at a dose which induced only a small increase in twitching alone. Higher doses of picrotoxin markedly increased amphetamine twitching and induced twitching in the absence of amphetamine. Ethyl-beta-carboline-3-carboxylate (BCE) weakly increased twitching and reversed the effect of RU 32007. CL 218872 weakly reduced twitching but also weakly antagonised RU 32007. In rats pretreated with a higher dose of nialamide methyl beta-carboline-3-carboxylate (BCM) and BCE induced twitching. BCE-induced twitching was antagonised by RU 32007, Ro15-1788, CGS 8216, muscimol and weakly by CL 218872. Thus, benzodiazepine agonists inhibit twitching and inverse agonists induce twitching, both being blocked by antagonists. Partial agonism (CL 218872) or partial inverse agonism (CGS 8216) may be detected by differential effects against different inducers of twitching.
在预先用烟肼酰胺处理、氨基甲酸乙酯麻醉的大鼠中，苯二氮䓬激动剂RU 32007、地西泮和氯氮䓬以及GABAA激动剂蝇蕈醇可抑制苯丙胺诱导的舌骨上肌群抽搐。Ro15 - 1788和CGS 8216分别使抽搐略有减轻或无减轻，但可逆转RU 32007和地西泮的作用。Ro15 - 1788不能逆转蝇蕈醇的作用。印防己毒素在仅引起抽搐小幅增加的剂量下可逆转蝇蕈醇和RU 32007的作用。更高剂量的印防己毒素可显著增加苯丙胺诱导的抽搐，并在无苯丙胺时诱发抽搐。β-咔啉-3-羧酸乙酯（BCE）可轻微增加抽搐，并逆转RU 32007的作用。CL 218872可轻微减轻抽搐，但也可轻微拮抗RU 32007。在用较高剂量烟肼酰胺预处理的大鼠中，β-咔啉-3-羧酸甲酯（BCM）和BCE可诱发抽搐。BCE诱发的抽搐可被RU 32007、Ro15 - 1788、CGS 8216、蝇蕈醇拮抗，CL 218872的拮抗作用较弱。因此，苯二氮䓬激动剂可抑制抽搐，反向激动剂可诱发抽搐，两者均可被拮抗剂阻断。通过对不同抽搐诱导剂的差异效应可检测到部分激动作用（CL 218872）或部分反向激动作用（CGS 8216）。
