Tokumura A, Fukuzawa K, Yamada S, Tsukatani H
Arch Int Pharmacodyn Ther. 1980 May;245(1):74-83.
Lysophosphatidic acids stimulated isolated uterine smooth muscle dose-dependently. The contractions were not reduced by pretreatment with atropine or an anti-5-hydroxytryptaminic agent. The potency depended on the nature of the acyl chain in the molecule. Of the compounds with a saturated fatty acyl group tested, the most effective were myristoyl- and lauroyl-lysophosphatidic acid. In a series of unsaturated lysophosphatidic acids, the potency increased with the number of cis double bonds in the acyl chain, and linolenoyl-lysophosphatidic acid was the most active. When injected intravenously, these compounds induced an immediate rise in blood pressure and intrauterine pressure, like prostaglandin F2 alpha: The order of potency of their effects on the intact uterus was consistent with that of their effects on isolated uterine smooth muscle, but not with that of their hypertensive effects in rats.
溶血磷脂酸可剂量依赖性地刺激离体子宫平滑肌。用阿托品或抗5 - 羟色胺剂预处理并不会降低其收缩作用。其效力取决于分子中酰基链的性质。在所测试的具有饱和脂肪酰基的化合物中,最有效的是肉豆蔻酰基 - 和月桂酰基 - 溶血磷脂酸。在一系列不饱和溶血磷脂酸中,效力随酰基链中顺式双键数量的增加而增强,亚麻酸酰基 - 溶血磷脂酸最为活跃。静脉注射时,这些化合物会像前列腺素F2α一样使血压和子宫内压立即升高:它们对完整子宫的作用效力顺序与其对离体子宫平滑肌的作用顺序一致,但与它们对大鼠的升压作用顺序不一致。