García-Sevilla J A, Areso P, Giralt M T, Ulibarri I
Department of Pharmacology, Faculty of Medicine, University of the Basque Country, Leioa, Spain.
Eur J Pharmacol. 1988 Jan 5;145(1):91-5. doi: 10.1016/0014-2999(88)90354-8.
Preincubation of platelet-rich plasma with N-ethylmaleimide (NEM) attenuated the inhibitory effect of the alpha 2-adrenoceptor agonist UK 14304 on basal and forskolin-stimulated adenylate cyclase activities. NEM also led to concomitant marked reductions of the specific binding of [3H]UK 14304 to platelet membranes and of the primary aggregation response induced by UK 14304. These results indicate that uncoupling of the receptor adenylate cyclase system by NEM induces down-regulation of platelet alpha 2-adrenoceptor density (3H-agonist binding sites) and of the associated functional response (platelet aggregation).
富含血小板的血浆与N - 乙基马来酰亚胺（NEM）预孵育可减弱α2 - 肾上腺素能受体激动剂UK 14304对基础和福斯可林刺激的腺苷酸环化酶活性的抑制作用。NEM还导致[3H]UK 14304与血小板膜的特异性结合以及UK 14304诱导的初级聚集反应显著降低。这些结果表明，NEM使受体 - 腺苷酸环化酶系统解偶联，从而诱导血小板α2 - 肾上腺素能受体密度（3H - 激动剂结合位点）和相关功能反应（血小板聚集）的下调。
