Scavone C, De Lucia R, Bernardi M M, Aizenstein M L
Eur J Pharmacol. 1985 May 28;112(1):11-6. doi: 10.1016/0014-2999(85)90233-x.
Dopamine (DA) receptor sensitivity was assessed in the rat striatal system following subchronic treatment with fencamfamine or saline for 7 days (10 mg/kg i.p.). Seventy-two hours after the last injection the stereotyped behaviour and general activity induced by apomorphine or saline were evaluated. Apomorphine (2.0 mg/kg s.c.) induced a decrease of the stereotypic response when fencamfamine-pretreated animals were compared to saline-treated ones while apomorphine (0.02 mg/kg s.c.) failed to alter the general activity of animals, treated with fencamfamine or not. In biochemical experiments subchronic fencamfamine did not alter the effects of apomorphine (0.02 mg/kg s.c.) in reducing homovanillic acid (HVA) and dihydroxyphenylacetic acid (DOPAC) striatal levels, when compared to saline. In addition we observed a slight but significant reduction in the total dopamine receptor content in the striatum labelled by [3H]spiroperidol. These findings indicate that subchronic fencamfamine treatment leads to a desensitization of postsynaptic DA receptors in rat striatum.
在大鼠纹状体系统中,用芬坎法明或生理盐水进行为期7天(10毫克/千克腹腔注射)的亚慢性治疗后,评估多巴胺(DA)受体敏感性。末次注射72小时后,评估阿扑吗啡或生理盐水诱导的刻板行为和一般活动。与生理盐水处理的动物相比,当比较芬坎法明预处理的动物时,阿扑吗啡(2.0毫克/千克皮下注射)诱导刻板反应降低,而阿扑吗啡(0.02毫克/千克皮下注射)未能改变是否用芬坎法明处理的动物的一般活动。在生化实验中,与生理盐水相比,亚慢性芬坎法明处理并未改变阿扑吗啡(0.02毫克/千克皮下注射)降低纹状体中高香草酸(HVA)和二羟基苯乙酸(DOPAC)水平的作用。此外,我们观察到用[3H]螺哌啶醇标记的纹状体中总多巴胺受体含量略有但显著降低。这些发现表明,亚慢性芬坎法明治疗导致大鼠纹状体中突触后DA受体脱敏。