Ku B S, Takeuchi H
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1983;76(2):291-6.
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.
在非洲大蜗牛(非洲大蜗牛费鲁萨克)的两种对多巴胺(DA)敏感的巨型神经元上,即周期性振荡神经元(PON,受DA兴奋)和紧张性自发放电神经元(TAN,受DA抑制),研究了合成麦角衍生物(包括被认为是多巴胺激动剂的利苏瑞和培高利特)的作用。在所研究的物质中,与培高利特相关的三种麦角衍生物,即D-8,9-二脱氢-6-丙基麦角灵-8-甲醇(LY149174)、D-6-甲基-8β-(2-(甲基亚磺酰基)乙基)麦角灵(LY116470)和D-2-氯-6-甲基-8β-(2-(甲基亚磺酰基)乙基)麦角灵(LY127817),对PON有兴奋作用,而培高利特(D-8β-((甲硫基)甲基)-6-丙基麦角灵,LY127809)和利苏瑞(N-D-6-甲基-8-异麦角烯基-N',N'-二乙基甲酰胺)则无作用。另一方面,只有D-6-甲基-8β-(2-(甲基亚磺酰基)乙基)麦角灵(LY116470)对TAN有兴奋作用。