Elliott J R, McElwee A A
Department of Physiology, University, Dundee.
Br J Anaesth. 1988 Jun;60(7):817-24. doi: 10.1093/bja/60.7.817.
We report the effects of n-alkanols (n-butanol to n-octanol), methyl carboxylic esters (methyl propionate to methyl octanoate) and n-alkyl ketones (2-pentanone to 2-nonanone) on a fast reflex escape response to a mechanical stimulus in Gammarus. ED50 concentrations and the relationships between In ED50 and chain length are given for each compound and series. For the n-alkanols, this relationship is well fit by a straight line (r2 = 1.000), with no evidence for a plateau between hexanol and heptanol. The standard free energy of transfer of a methylene group from water to a site of action in Gammarus is given for each series. The value for the esters is significantly smaller than that for the n-alkanols and ketones. These free energies are compared with those from other model systems, with the conclusion that further investigation of the differences between n-alkanols and esters will increase our understanding of the physico-chemical nature of the site(s) of action of general anaesthetics.
我们报告了正链烷醇(正丁醇至正辛醇)、甲基羧酸酯(丙酸甲酯至辛酸甲酯)和正烷基酮(2-戊酮至2-壬酮)对欧洲沼虾对机械刺激的快速反射逃避反应的影响。给出了每种化合物和系列的半数有效浓度(ED50)以及ED50的自然对数与链长之间的关系。对于正链烷醇,这种关系通过一条直线拟合良好(r2 = 1.000),没有证据表明己醇和庚醇之间存在平稳期。给出了每个系列中一个亚甲基从水转移到欧洲沼虾作用位点的标准自由能。酯类的值明显小于正链烷醇和酮类的值。将这些自由能与其他模型系统的自由能进行了比较,得出的结论是,进一步研究正链烷醇和酯类之间的差异将增进我们对全身麻醉药作用位点的物理化学性质的理解。