Messiha F S
Department of Pharmacology, University of North Dakota School of Medicine, Grand Forks 58203.
Neurotoxicology. 1991 Fall;12(3):571-81.
The separate and combined effects of successive administration of amantadine, 100 mg/kg, i.p., and chlorpromazine, 0.2 mg/kg, i.p., on motor activity and whole brain levels of certain biogenic amines and major metabolites were studied in four strains of mice. These were the albino ICR, the inbred BALB/C, C57BL/6 and the hybrid CDF-I mice. Amantadine produced a strain-dependent behavioral stimulation subsequent the fourth dose. This was apparent in ICR and C57BL/6 mouse strains and was followed by a behavioral depression phase occurring during the night in C57BL/6 mice which was antagonized by chlorpromazine. Administration of chlorpromazine alone affected only CDF-1 mouse mobility. Chlorpromazine reduced only ICR mouse brain dopamine without concomitant changes in major acid metabolites. Repeated administration of amantadine prior to chlorpromazine negated this effect. Chlorpromazine enhancement of BALB/C brain serotonin and 5-hydroxyindoleacetic acid was antagonised by pretreatment with amantadine. This antagonism was also evident in BALB/C mouse brain dihydroxyphenylacetic acid. The results suggest genotypic-dependent behavioral and cerebral effects by the drugs studied. The antagonism between amantadine and chlorpromazine on brain amines may explain the therapeutic efficacy of amantadine in modulating chlorpromazine-induced extrapyramidal disorders.
研究了腹腔注射100mg/kg金刚烷胺和0.2mg/kg氯丙嗪连续给药对四种品系小鼠运动活性以及某些生物胺和主要代谢产物全脑水平的单独和联合作用。这四种品系分别是白化ICR小鼠、近交系BALB/C小鼠、C57BL/6小鼠和杂交CDF-I小鼠。在第四次给药后,金刚烷胺产生了品系依赖性的行为兴奋作用。这在ICR和C57BL/6小鼠品系中很明显,随后C57BL/6小鼠在夜间出现行为抑制阶段,氯丙嗪可拮抗此阶段。单独给予氯丙嗪仅影响CDF-1小鼠的活动能力。氯丙嗪仅降低ICR小鼠脑内多巴胺水平,而主要酸性代谢产物无相应变化。在氯丙嗪之前重复给予金刚烷胺可消除此效应。金刚烷胺预处理可拮抗氯丙嗪对BALB/C小鼠脑内5-羟色胺和5-羟吲哚乙酸的增强作用。这种拮抗作用在BALB/C小鼠脑内二羟基苯乙酸中也很明显。结果表明所研究药物的行为和脑效应存在基因型依赖性。金刚烷胺和氯丙嗪对脑内胺类的拮抗作用可能解释了金刚烷胺在调节氯丙嗪所致锥体外系疾病方面的治疗效果。