血小板活化因子-氨基膦酸酯（PAF-AP）的生物活性，一种新型的血小板活化因子（PAF）膦脂选择性抑制剂。

Biological activity of platelet activating factor-amidophosphonate (PAF-AP), a novel phosphonolipid selective inhibitor of platelet activating factor (PAF).

作者信息

Steiner M, Landolfi R, Motola N C, Turcotte J G

出版信息

Biochem Biophys Res Commun. 1985 Dec 31;133(3):851-5. doi: 10.1016/0006-291x(85)91212-4.

Abstract

A novel amidophosphonate analog of Platelet Activating Factor (PAF), trimethyl (3-phosphonopropyl) ammonium hydroxide (R)-mono[2-acetamido-3-(hexadecyloxy)propyl] ester (PAF-AP), was synthesized. A potent inhibitor of aggregation induced by Platelet Activating Factor, arachidonic acid, Ca2+-ionophore, ADP, and thrombin, PAF-AP had no or very little effect on aggregation induced by epinephrine and collagen. Inhibition of phospholipase A2 and C2 activity was suggested from suppression of release of [14C]-arachidonic acid from pre-labeled platelet glycerophospholipids.

摘要

合成了一种新型的血小板活化因子（PAF）的氨基膦酸类似物，即氢氧化三甲基（3-膦酰丙基）铵（R）-单[2-乙酰氨基-3-（十六烷氧基）丙基]酯（PAF-AP）。PAF-AP是血小板活化因子、花生四烯酸、钙离子载体、ADP和凝血酶诱导的聚集的强效抑制剂，对肾上腺素和胶原蛋白诱导的聚集没有或几乎没有影响。从预先标记的血小板甘油磷脂中[14C]-花生四烯酸释放的抑制作用提示其对磷脂酶A2和C2活性有抑制作用。