Montanaro N, Dall'Olio R, Gandolfi O, Vaccheri A
Eur J Pharmacol. 1982 Jun 16;81(1):1-9. doi: 10.1016/0014-2999(82)90595-7.
Rat exploratory activity as well as apomorphine-induced hypermotility and stereotyped behavior were assayed following acute (60 min before) or chronic (21 days) administration of sulpiride stereoisomers and haloperidol. Parallel groups of rats were assayed for their hypermotility and stereotyped responses to challenging doses of apomorphine 7 and 21 days after discontinuation of chronic treatments. Following its acute administration, (-)-sulpiride fully antagonized apomorphine-induced hypermotility without affecting the level of animal spontaneous activity and partially counteracted stereotyped behavior. Haloperidol completely suppressed both apomorphine responses and also depressed exploratory activity. Some tolerance to the anti-apomorphine effect of (-)-sulpiride groups exhibited enhanced behavioral sensitivity to apomorphine only with respect to hypermotility, whereas haloperidol groups were supersensitive with respect to both hypermotility and stereotyped responses. The results are discussed in terms of differential dopamine receptor supersensitivity arising from prolonged administration of butyrophenone and substituted benzamide.
在急性(给药前60分钟)或慢性(21天)给予舒必利立体异构体和氟哌啶醇后,测定大鼠的探索活动以及阿扑吗啡诱导的运动亢进和刻板行为。在慢性治疗停药后7天和21天,对平行组大鼠测定其对挑战性剂量阿扑吗啡的运动亢进和刻板反应。急性给予(-)-舒必利后,它完全拮抗阿扑吗啡诱导的运动亢进,而不影响动物自发活动水平,并部分抵消刻板行为。氟哌啶醇完全抑制了阿扑吗啡的两种反应,还抑制了探索活动。对(-)-舒必利抗阿扑吗啡作用产生了一定耐受性,(-)-舒必利组仅在运动亢进方面对阿扑吗啡表现出增强的行为敏感性,而氟哌啶醇组在运动亢进和刻板反应方面均表现出超敏感性。根据丁酰苯类和取代苯甲酰胺类药物长期给药引起的多巴胺受体超敏感性差异对结果进行了讨论。