Heymans F, Steiner E, Jouquey S, Godfroid J J
Laboratoire de Pharmacochimie Moléculaire, Université Paris, France.
J Lipid Mediat. 1989 Sep-Oct;1(5):303-12.
In order to undertake a quantitative assessment of the contribution of the hydrophobic effect of the etheroxid chain to agonistic activity, it was necessary to include in the calculated data a highly lipophilic platelet-activating factor (PAF) analogue. The synthesis of such a compound--racemic 1-O-docosyl-2-O-acetylglycero-3-phosphocholine (C22 PAF)--is described. The regression analysis performed with data of 14 etheroxid analogues (reviewed by Godfroid et al., 1987), combined with data obtained with C22 PAF, is significant with respect to a parabolic evolution between lipophilicity of the chain and the logarithm of relative platelet stimulation. This result is characteristic of a hydrophobic interaction between the agonist and the PAF receptor.
为了对醚氧化链的疏水作用对激动活性的贡献进行定量评估，有必要在计算数据中纳入一种高度亲脂性的血小板激活因子（PAF）类似物。本文描述了此类化合物——外消旋1-O-二十二烷基-2-O-乙酰甘油-3-磷酸胆碱（C22 PAF）的合成。对14种醚氧化类似物的数据（Godfroid等人于1987年综述）以及C22 PAF获得的数据进行回归分析，结果表明链的亲脂性与相对血小板刺激对数之间呈抛物线演变，具有显著性。该结果是激动剂与PAF受体之间疏水相互作用的特征。
