Functional α1-adrenergic receptor subtypes in human right gastroepiploic artery  

作　　者：HANJiang-Li ZHANGYou-Yi 

机构地区：[1]DepartmentofCardiovasology [2]InstituteofVascularMedicine

出　　处：《Acta Pharmacologica Sinica》2003年第4期327-331,共5页中国药理学报（英文版）

摘　　要：AIM：To study the functionalα1-adrenergic receptor(α1-AR)subtypes in human right gastroepiploic artery(RGA).METHODS:The effects of α2-AR,α1-AR,and α1-AR subtype selective antagonists on norepinephrine(NE)-induced vasoconstriction in isolated human RGA were observed by contractile function experiment,RESULTS: Cumulative concentration-response curves for NE were competitively antagonized in RGA by α2-AR selective antagonist yohimbine(pA26.820.28,slope 1.12±0.40),α1-AR selective antagonist praxosin(pA29.77±0.22,slope 0.90±0.22),α1A-AR selective antagonists RS17053(pA8.42±0.20,solpe 0.93±0.20)and 5-MU(pA2 8.42±0.22,slope 0.88±0.18),α1D-AR selective antagonist BMY7378(pA26.84±0.32,slope 1.05±0.17),and α1A-,α1B-AR selective antagonist WB4104(pA28.88±0.20,slope 1.15±0.16).The correlation coefficients between these pA2 values of α1-AR selective antagonists with pKi values of which obtained from α1A-,α1B-and α1D-AR cloned cells are 0.95,0.82,and 0.42.After the vessels were pretreated by chlorethylclonidine(CEC),an α1B-and α1D-AR irreversible alkylating agent,the pD2 values were changed from 5.9±0.5 to 5.6±0.6 and the maximal contraction was changed from(8.9±3.2)g to(8.0±3.2)g,respectively.The difference was not significant.CONCLUSION:In human RGA,the contraction response is mainly mediated by α1-AR，of which α1A-AR plays an important role,whereas α1B-AR are not involved in the contraction response.

关 键 词：α1肾上腺素能受体亚型 血管收缩 人右胃网膜动脉 肾上腺素α受体拮抗剂 

分 类 号：R972[医药卫生—药品] R962[医药卫生—药学]