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研究大鼠不同血管中α1 肾上腺素受体(α1adrenoceptor,α1AR) 亚型的分布情况及其功能意义。方法:采用离体血管收缩功能实验,测定α1AR 选择性拮抗剂抑制大鼠血管NE收缩反应的功能性亲和常数(pA2) ,与分别表达α1A、α1B和α1DAR的克隆细胞上结合常数(pKi)作相关性分析,以判断血管中的α1AR 亚型分布。结果:哌唑嗪、WB4101 、5MU、BMY7378 和RS17053 分别竞争性地抑制血管对NE 的收缩效应,pA2 值与这些拮抗剂对克隆α1A、α1B、α1DAR 的pKi 值间的决定系数在肺动脉分别为0 .05、0.45、0.77 ;在肠系膜动脉分别为0.02、0.47 、0 .87 ;在尾动脉分别为0 .77 、0 .77 、0 .44 ;在门静脉分别为0 .79 、0 .81、0 .27。结论:大鼠肺动脉、肠系膜动脉的功能性α1AR主要为α1DAR;而尾动脉与门静脉的功能性α1AR主要是α1A和α1B亚型。
To study the distribution of α1-adrenoceptor (α1AR) subtypes in different blood vessels of rats and their functional significance. Methods: The in vitro vasoconstriction function was used to determine the functional affinity constant (pA2) of α1AR selective antagonist to inhibit the NE contraction of blood vessels and the expression of α1A, α1Band α1DAR On the binding constant (pKi) for correlation analysis to determine the vascular α1 AR subtype distribution. RESULTS: Prazosin, WB4101, 5MU, BMY7378 and RS17053 respectively competitively inhibited the contractile effect of NE on blood vessels. The determination of pA2 value and the pKi values of these antagonists on the clones α1A, α1B, α1DAR Coefficients were 0 in the pulmonary artery. 05, 0.45, 0.77; in mesenteric artery, 0.02, 0.47, 0 respectively. 87; respectively 0 in the caudal artery. 77, 0. 77, 0. 44; 0 in portal vein respectively. 79, 0. 81,0. 27. Conclusions: The functional α1AR of pulmonary arteries and mesenteric arteries of rats are mostly α1DAR. The functional α1AR of caudal artery and portal vein are mainly α1A and α1B subtypes.