γ-氨基丁酸（GABA）受体复合物拮抗剂的促冲突效应。地西泮的逆转作用。

Proconflict effect of GABA receptor complex antagonists. Reversal by diazepam.

作者信息

Corda M G, Biggio G

出版信息

Neuropharmacology. 1986 May;25(5):541-4. doi: 10.1016/0028-3908(86)90181-4.

Abstract

The effect of drugs which down-regulate the function of GABA at the level of the GABA/benzodiazepine receptor complex was studied on the conflict test in the rat. The GABA receptor antagonist, bicuculline, and the blockers of the GABA-receptor-coupled chloride channel, picrotoxin and pentylenetetrazol, produced a dose-dependent proconflict effect. This effect occurred at dose levels which failed to affect unpunished behaviour. The most effective compounds were bicuculline and picrotoxin. The proconflict effect of these drugs was prevented by diazepam but not by the specific benzodiazepine antagonist, Ro15-1788. The data indicate that a diminished GABAergic activity at different subunits of the GABA receptor complex resulted in an enhancement of punishment-suppressed behaviour in rats.

摘要

研究了在大鼠冲突试验中，下调γ-氨基丁酸（GABA）在GABA/苯二氮䓬受体复合物水平功能的药物的作用。GABA受体拮抗剂荷包牡丹碱，以及GABA受体偶联氯离子通道阻滞剂印防己毒素和戊四氮，产生了剂量依赖性的促冲突效应。这种效应出现在不影响未受惩罚行为的剂量水平。最有效的化合物是荷包牡丹碱和印防己毒素。这些药物的促冲突效应可被地西泮阻止，但不能被特异性苯二氮䓬拮抗剂Ro15 - 1788阻止。数据表明，GABA受体复合物不同亚基处GABA能活性的降低导致大鼠惩罚抑制行为增强。