Wettstein J G
Department of Psychiatry, Harvard Medical School, Boston, MA 02115.
Eur J Pharmacol. 1988 Oct 11;155(1-2):19-25. doi: 10.1016/0014-2999(88)90398-6.
Behavioral effects of the benzodiazepine agonist quazepam were compared with those of lorazepam in squirrel monkeys responding under a fixed-interval schedule of food presentation with a superimposed fixed-ratio schedule of response-produced shock. Low and intermediate i.v. doses of quazepam (0.1-1.0 mg/kg) and lorazepam (0.03-0.3 mg/kg) increased rates of suppressed responding, yet the maximal increases in rate were less after quazepam than after lorazepam. Higher doses of both drugs tended to increase responding less or decrease it and, with quazepam, frequent sleep was observed for 2-3 days afterwards. The dose-response curves for quazepam and lorazepam were shifted to the right following i.v. pretreatment with the benzodiazepine antagonists Ro 15-1788 (0.18-3.0 mg/kg) or AHR-11797 (1.0-5.6 mg/kg); in this regard, AHR-11797 was less potent than Ro 15-1788. Although the effects of quazepam on suppressed responding are likely due to actions at benzodiazepine receptors, these effects may be influenced by or reflect a more prominent sleep-promoting action of the drug.
在松鼠猴按固定间隔食物呈现时间表并叠加反应产生电击的固定比率时间表做出反应的实验中,比较了苯二氮䓬激动剂夸西泮与劳拉西泮的行为效应。低剂量和中等剂量静脉注射的夸西泮(0.1 - 1.0毫克/千克)和劳拉西泮(0.03 - 0.3毫克/千克)提高了抑制反应的速率,但夸西泮后的速率最大增幅低于劳拉西泮后的增幅。两种药物的较高剂量往往较少增加反应或降低反应,并且使用夸西泮后,在随后的2 - 3天观察到频繁睡眠。在用苯二氮䓬拮抗剂Ro 15 - 1788(0.18 - 3.0毫克/千克)或AHR - 11797(1.0 - 5.6毫克/千克)进行静脉预处理后,夸西泮和劳拉西泮的剂量 - 反应曲线向右移动;在这方面,AHR - 11797的效力低于Ro 15 - 1788。尽管夸西泮对抑制反应的影响可能归因于其对苯二氮䓬受体的作用,但这些影响可能受到该药物更显著的促睡眠作用的影响或反映了这种作用。