Szabadi E, Bradshaw C M, Gaszner P
Psychopharmacology (Berl). 1980;68(2):125-34. doi: 10.1007/BF00432129.
Eight healthy male volunteers participated in four experimental sessions in which they ingested either DL-308 (10 mg), DL-308 (20 mg), thioridazine (50 mg) or placebo. Drugs were allocated to subjects and sessions in a double-blind fashion according to a balanced cross-over design. Both DL-308 and thioridazine displayed sedative properties, as indicated by the sedated appearance of the subjects, by a decrease in subjectively rated alertness and by an impairment of performance on psychomotor tests. DL-308 appeared to be a more potent sedative than thioridazine. DL-308 (10 mg) caused an increase in subjectivey rated sweating and objectively measured heart rate, suggesting a sympathomimetic property for the drug. DL-308, similarly to thioridazine, had effects consistent with an alpha-adrenolytic action; both drugs caused miosis, hypotension and a decrease in salivation. The decrease in salivation may also be consistent with an anticholinergic effect. When equisedative doses of the two drugs were compared, DL-308 had a much smaller influence on autonomic functions than thioridazine. DL-308 had a faster time-course of action than thioridazine. Peak effects were attained 1-3 h post-drug and the effects almost completely dissipated within 5 h. DL-308, similarly to thioridazine, had little effect on the motor system, as indicated by conventional clinical neurological examination.
八名健康男性志愿者参加了四个实验环节,在这些环节中他们分别服用了DL - 308(10毫克)、DL - 308(20毫克)、硫利达嗪(50毫克)或安慰剂。药物按照平衡交叉设计以双盲方式分配给受试者和实验环节。DL - 308和硫利达嗪均表现出镇静特性,这体现在受试者呈现出镇静的外观、主观评定的警觉性降低以及精神运动测试表现受损。DL - 308似乎是一种比硫利达嗪更强效的镇静剂。DL - 308(10毫克)导致主观评定的出汗增加以及客观测量的心率加快,表明该药物具有拟交感神经特性。与硫利达嗪类似,DL - 308具有与α - 肾上腺素能阻断作用一致的效应;两种药物均引起瞳孔缩小、低血压和唾液分泌减少。唾液分泌减少也可能与抗胆碱能效应一致。当比较两种药物的等效镇静剂量时,DL - 308对自主神经功能的影响比硫利达嗪小得多。DL - 308的作用时程比硫利达嗪更快。给药后1 - 3小时达到峰值效应,且效应在5小时内几乎完全消散。与硫利达嗪类似,常规临床神经学检查表明DL - 308对运动系统几乎没有影响。