Buus Lassen J
Psychopharmacologia. 1975 Jul 23;43(1):25-9. doi: 10.1007/BF00437610.
The effect of H 77/77 (5 mg/kg s.c.) on motility of rats kept in a familiar cage was investigated. H 77/77 produced hypermotility, which was reduced by oral pretreatment with chlorpromazine, haloperidol, clozapine and thioridazine. The 4 neuroleptics were administered acutely and for a 14 day period. H 77/77 was given 30 min after the single or last dose of neuroleptc (chronic treatment) condition. After both single and repeated administration the neuroleptics showed H 77/77-antagonism in doses ranging from 0.1-2.0 mg/kg. The effect on H 77/77 activity did not change significantly after repeated treatment. Clozapine and thioridazine, which clinically produce only minor extrapyramidal side effects, exert a weak effect or none at all in tests commonly used for neuroleptic activity. These 2 neuroleptics were potent H 77/77-antagonists. Inhibition of H 77/77-hypermotility may possibly be used as a test for neuroleptics.
研究了H 77/77(5毫克/千克,皮下注射)对饲养在熟悉笼子里的大鼠活动能力的影响。H 77/77引起活动亢进,口服氯丙嗪、氟哌啶醇、氯氮平和硫利达嗪进行预处理可使其减轻。这4种抗精神病药物分别急性给药和连续给药14天。在单次或最后一剂抗精神病药物(慢性治疗)给药30分钟后给予H 77/77。单次给药和重复给药后,抗精神病药物在0.1 - 2.0毫克/千克的剂量范围内均表现出对H 77/77的拮抗作用。重复治疗后对H 77/77活性的影响没有显著变化。临床上仅产生轻微锥体外系副作用的氯氮平和硫利达嗪,在常用于检测抗精神病活性的试验中作用微弱或无作用。这两种抗精神病药物是强效的H 77/77拮抗剂。抑制H 77/77引起的活动亢进可能可用作抗精神病药物的一种检测方法。