Thomas M E, Osmani A H, Scrutton M C
Thromb Res. 1983 Dec 15;32(6):557-66. doi: 10.1016/0049-3848(83)90057-9.
Aggregation of human platelets by vasopressin is potently inhibited by 1-[beta mercapto-(beta, beta'-cyclopentamethylene propionic acid)]-L-arginine vasopressin, a selective vasopressor (V1) antagonist. 1-Desamino-8-D-arginine-vasopressin, a selective anti-diuretic (V2) agonist failed to induce aggregation and acted as a weak antagonist. Vasopressin analogues which lacked the N-terminal amino group or which contained an uncharged amino acid residue at position 8 acted as partial agonists for the human platelet. The response to such partial agonists could be enhanced by increasing the cytosolic Ca2+ concentration but not by altering the level of cyclic-3', 5'-AMP. These observations provide further evidence indicating that the platelet vasopressin receptor is of the V1 sub-type.
一种选择性血管升压素(V1)拮抗剂1-[β-巯基-(β,β'-环戊亚甲基丙酸)]-L-精氨酸血管加压素可有效抑制血管加压素引起的人血小板聚集。一种选择性抗利尿(V2)激动剂1-去氨基-8-D-精氨酸血管加压素未能诱导聚集,且表现为弱拮抗剂。缺乏N端氨基或在第8位含有不带电荷氨基酸残基的血管加压素类似物可作为人血小板的部分激动剂。通过增加胞质Ca2+浓度而非改变环-3',5'-AMP水平,可增强对这类部分激动剂的反应。这些观察结果提供了进一步证据,表明血小板血管加压素受体属于V1亚型。