Hsu C Y, Knapp D R, Halushka P V
J Pharmacol Exp Ther. 1979 Mar;208(3):366-70.
The effects of alpha adrenergic agonists and antagonists on human in vitro platelet aggregation were studied to characterize further the platelet alpha adrenergic receptor. Aggregation induced by ADP and U46619; a stable prostaglandin endoperoxide analog, was potentiated by alpha adrenergic agonists, an effect which was completely blocked by the alpha adrenergic antagonist phentolamine (1 X 10(-6) M) but not by prazosin (1 X 10(-6) M). The order of potency for the alpha adrenergic agonists in potentiating ADP-induced aggregation was clonidine greater than or equal to epinephrine greater than alpha-methylnorepinephrine greater than norepinephrine greater than phenylephrine greater than methoxamine. Epinephrine-induced platelet aggregation was blocked by phentolamine, yohimbine, dihydroergotamine, clonidine and lofexidine but not by phenoxybenzamine (1 X 10(-5) M). These findings suggest that: 1)clonidine and lofexidine are partial agonists and 2) that the alpha adrenergic receptor of the platelet is different from the classical postsynaptic alpha adrenergic receptor and more closely resembles presynaptic alpha adrenergic receptors.
研究了α肾上腺素能激动剂和拮抗剂对人离体血小板聚集的影响,以进一步表征血小板α肾上腺素能受体。由ADP和U46619(一种稳定的前列腺素内过氧化物类似物)诱导的聚集,被α肾上腺素能激动剂增强,这种效应被α肾上腺素能拮抗剂酚妥拉明(1×10⁻⁶M)完全阻断,但不被哌唑嗪(1×10⁻⁶M)阻断。α肾上腺素能激动剂增强ADP诱导聚集的效力顺序为可乐定≥肾上腺素>α-甲基去甲肾上腺素>去甲肾上腺素>去氧肾上腺素>甲氧明。肾上腺素诱导的血小板聚集被酚妥拉明、育亨宾、双氢麦角胺、可乐定和洛非西定阻断,但不被苯氧苄胺(1×10⁻⁵M)阻断。这些发现表明:1)可乐定和洛非西定是部分激动剂;2)血小板的α肾上腺素能受体不同于经典的突触后α肾上腺素能受体,更类似于突触前α肾上腺素能受体。