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目的:研究去甲肾上腺素(NE)介导大鼠肠系膜血管床(MVB)收缩的α1肾上腺素受体(α1AR)亚型.方法:用灌流大鼠MVB标本收缩功能实验和克隆细胞放射配体结合实验测定α1AR亚型选择性拮抗剂pA2和pKi,并作相关分析.结果:α1AAR选择性拮抗剂RS17053、WB4101、5MU及α1DAR选择性拮抗剂BMY7378的pA2分别为898±028,916±020,8.69±002和603±026,Schild作图斜率值与10差别无显著性.其pA2值与α1AAR的pKi相关系数为097,与α1B和α1DAR的相关系数分别为052和004.结论:介导外源性NE收缩大鼠MVB的功能性受体为α1AAR
Objective: To investigate the effect of norepinephrine (NE) on α1adrenoceptor (α1AR) subtype in rat mesenteric vascular bed (MVB). METHODS: The α1AR subtype selective antagonists pA2 and pKi were determined by the contractile function of MVB specimens and the radioligand binding assay of the cloned cells. The correlation analysis was performed. Results: The pA2 of α1AAR selective antagonist RS17053, WB4101,5MU andα1DAR selective antagonist BMY7378 were898 ± 0.28,916 ± 0.20,8.69 ± 002 and 603 ± 026, Schild plot slope value and 1 0 difference was not significant. The pA2 value of pA2 and α1AAR were 0.97 for pKi and 052 and 0.04 for α1Band α1DAR, respectively. CONCLUSIONS: The functional receptor mediating MVB in exogenous NE-contracted rats is α1AAR