Hashimoto T, Katsura M, Kuriyama K
Department of Pharmacology, Kyoto Prefectural University of Medicine, Japan.
Eur J Pharmacol. 1991 Jun 6;198(2-3):121-7. doi: 10.1016/0014-2999(91)90610-3.
The effect of mergocryptine, a new ergot alkaloid, on the cerebral dopaminergic systems was examined using Wistar rats. The administration of mergocryptine (1 and 10 mg/kg i.p.) induced a significant suppression of striatal dopamine (DA) turnover. In vitro addition of mergocryptine (0.01-100 microM) induced a dose-dependent suppression of the release of [3H]DA from striatal slices. Mergocryptine inhibited [3H]apomorphine binding to a striatal synaptosomal fraction, and its IC50 value was found to be 0.23 microM. Pretreatment with apomorphine (100 micrograms/kg s.c.) showed an additive effect on the mergocryptine (10 mg/kg)-induced suppression of DA turnover. These results suggest that mergocryptine may induce the suppression of striatal DA turnover by reducing DA release via the stimulation of presynaptic dopaminergic autoreceptors.
使用Wistar大鼠研究了一种新型麦角生物碱麦戈隐亭对脑多巴胺能系统的影响。腹腔注射麦戈隐亭（1和10毫克/千克）可显著抑制纹状体多巴胺（DA）的周转。体外添加麦戈隐亭（0.01 - 100微摩尔）可剂量依赖性地抑制纹状体切片中[3H]DA的释放。麦戈隐亭抑制[3H]阿扑吗啡与纹状体突触体部分的结合，其IC50值为0.23微摩尔。阿扑吗啡（100微克/千克皮下注射）预处理对麦戈隐亭（10毫克/千克）诱导的DA周转抑制具有相加作用。这些结果表明，麦戈隐亭可能通过刺激突触前多巴胺能自身受体减少DA释放，从而抑制纹状体DA的周转。
