Specific binding of phospholipid platelet-activating factor by human platelets.

作者: E Coles , V R Reinhold , E J Goetzl , F H Valone

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摘要: The binding of the phospholipid platelet-activating factor 1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphorylcholine (AGEPC) to washed human platelets was more than 80% complete within 2 min, which coincided with time initiation platelet aggregation by AGEPC. Scatchard plot analysis [3H]AGEPC without and an excess unlabeled AGEPC revealed two distinct types sites. One site for exhibited a high affinity (KD = 37 +/- 13 nM, mean SD), saturable, had low maximal capacity 1399 498 (mean SD) molecules AGEPC/platelet. other demonstrated nearly infinite capacity, consistent nonreceptor uptake into cellular structures. specificity high-affinity assessed comparing several analogues inhibit induce aggregation. An ether linkage in position 1, short-chain fatty acid 2, choline moiety polar head group proved be critical both Exposure 5 min at degrees C functionally deactivated exposed subsequent stimulation AGEPC, as diminished aggregation, concomitantly reduced specific [3H]AGEPC. Evaluation course events deactivation loss response after 90 sec C, despite retention up 50% sites

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