Bostwick J R, Abbe R, Sun J, Appel S H
Department of Neurology, Baylor College of Medicine, Houston, Texas 77030.
Neuroreport. 1992 May;3(5):425-8. doi: 10.1097/00001756-199205000-00012.
The synthesis and release of 3H-acetylcholine was measured in hippocampal slices of adult rat brain following acute in vitro exposure to ethanolamine. Evoked release of 3H-acetylcholine was elevated by 60-70% but 3H-acetylcholine synthesis was unaffected. Other amino alcohols were also found to significantly increase evoked 3H-acetylcholine release. The effect may be stereochemically mediated since only one of four possible propanolamine configurations, R-alaninol, was active. The most potent compound tested was R-prolinol which showed an EC50 nearly 10-fold lower than that of either R-alaninol or ethanolamine; S-prolinol was inactive. Slices taken from adult rats which had been fed active compounds for two weeks also exhibited enhancements in evoked 3H-acetylcholine release. These results indicate that amino alcohols modulate acetylcholine release in the rat hippocampus.
在成年大鼠脑海马切片中,急性体外暴露于乙醇胺后,对3H-乙酰胆碱的合成和释放进行了测定。3H-乙酰胆碱的诱发释放提高了60%-70%,但3H-乙酰胆碱的合成未受影响。还发现其他氨基醇也能显著增加3H-乙酰胆碱的诱发释放。这种作用可能是由立体化学介导的,因为在四种可能的丙醇胺构型中,只有R-丙氨醇具有活性。测试的最有效化合物是R-脯氨醇,其半数有效浓度(EC50)比R-丙氨醇或乙醇胺低近10倍;S-脯氨醇无活性。取自喂食活性化合物两周的成年大鼠的切片,其3H-乙酰胆碱的诱发释放也有所增强。这些结果表明,氨基醇可调节大鼠海马中乙酰胆碱的释放。