Effects of synthetic ergot derivatives on the two identifiable giant neurons, sensitive to dopamine, of Achatina fulica Ferussac.

B S Ku, H Takeuchi
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Abstract

On the two dopamine (DA)-sensitive giant neurones, PON (periodically oscillating neuron, excited by DA) and TAN (tonically autoactive neuron, inhibited by DA), of an African giant snail (Achatina fulica Férussac), effects of synthetic ergot derivatives, including lisuride and pergolide, which are considered to be dopamine agonists, were examined. Of the substances examined, three of the ergot derivatives related to pergolide, D-8,9-didehydro-6-propylergoline-8-methanol (LY149174), D-6-methyl-8 beta-(2-(methylsulfinyl)ethyl)ergoline (LY116470) and D-2-chloro-6-methyl-8 beta-(2-(methylsulfinyl)ethyl)ergoline (LY127817), showed excitatory effects on PON, while pergolide (D-8 beta-( (methylthio)methyl)-6-propylergoline, LY127809) and lisuride (N-D-6-methyl-8-isoergolenyl-N',N'-diethylcarbamide) had no effect. On the other hand, only D-6-methyl-8 beta-(2-(methylsulfinyl)ethyl)ergoline (LY116470) had any excitatory effects on TAN.

合成麦角衍生物对黄颡鱼两种可识别的多巴胺敏感大神经元的影响。
在非洲巨蜗牛(Achatina fulica f russac)的两个多巴胺(DA)敏感的巨型神经元PON (DA兴奋的周期性振荡神经元)和TAN (DA抑制的强直性自活动神经元)上,研究了合成麦角衍生物(包括被认为是多巴胺激动剂的lisuride和pergolide)的作用。在所检测的物质中,与培高利酯相关的3种麦角衍生物d -8,9-二脱氢-6-丙麦角碱-8-甲醇(LY149174)、d -6-甲基-8-(2-(甲基亚砜基)乙基)麦角碱(LY116470)和d -2-氯-6-甲基-8-(2-(甲基亚砜基)乙基)麦角碱(LY127817)对PON有兴奋作用,而培高利酯(D-8 -(甲基硫基)甲基)-6-丙麦角碱,LY127809)和lisuride (N- d -6-甲基-8-异麦角烯基-N′,N′-二乙基氨基)对PON没有作用。另一方面,只有d -6-甲基-8 β -(2-(甲基亚砜基)乙基)麦角碱(LY116470)对TAN有兴奋作用。
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