Functional α_1-adrenergic receptor subtypes in human right gastroepiploic artery  

人右胃网膜动脉的功能性α_1-肾上腺素受体亚型(英文)

作　　者：韩江莉[1] 张幼怡[2] 吕志珍[2] 毛节明[1] 陈明哲[1] 韩启德 

机构地区：[1]北京大学第三医院心血管内科 [2]北京大学第三医院血管医学研究所

出　　处：《Acta Pharmacologica Sinica》2003年第4期41-45,97,共6页中国药理学报（英文版）

基　　金：Project supported by the Major State Basic Research Development Program of People's Republic of China (G2000056906) ;the National Natural Science Foundation of China (№ 30070872, 30171083).

摘　　要：AIM: To study the functional α₁-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 （pA₂ 6.82±0.28, slope 1.12±0.40）, α₁-AR selective antagonist prazosin （pA₂ 9.77±0.22, slope 0.90±0.22）, α_1A-AR selective antagonists RS17053 （pA₂ 8.42±0.20, slope 0.93±0.20） and 5-MU （pA₂ 8.42±0.22, slope 0.88±0.18）, α_1D-AR selective antagonist BMY7378 （pA₂ 6.84±0.32, slope 1.05±0.17）, and α_1A-, α_1B-AR selective antagonist WB4101 （pA₂ 8.88±0.20, slope 1.15±0.16）. The correlation coefficients between these pA₂ values of α₁-AR selective antagonists with pK_i values of which obtained from α_1A-, α_1B- and α_1D-AR cloned cells are 0.95, 0.82, and 0.42. After the vessels were pretreated by chlorethylclonidine （CEC）, an α_1B- and α_1D-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 α_1A-AR plays an important role, whereas α_1B- and α_1D-AR are not involved in the contraction response.目的:研究人右胃网膜动脉(RGA)中介导收缩的功能性α_1-肾上腺素受体(α_1-AR)亚型。方法:离体血管收缩功能实验。结果:在RGA中α_2-AR选择性拮抗剂育亨宾、α_1-AR选择性拮抗剂哌唑嗪及α_(1A)-AR选择性拮抗剂RS17053和5-MU,α_(1D)-AR选择性拮抗剂BMY7378和α_(1A)-与α_(1B)-AR选择性拮抗剂WB4101拮抗NE引起收缩效应的pA_2值分别为6.82±0.28、9.77±0.22、8.42±0.22、8.42±0.22、6.84±0.32和8.88±0.20,斜率分别为1.12±0.40、0.90±0.22、0.93±0.22、0.88±0.18、1.05±0.17、1.15±0.16。α_1-AR选择性拮抗剂的pA_2值与这些拮抗剂在表达α_(1A)-、α_(1B)-、α_(1D)-AR的细胞株上得出的pK_i值之间的相关系数分别为0.95、0.82和0.42。用α_(1B)-、α_(1D)-AR的不可逆选择性拮抗剂氯乙基可乐定(CEC)预处理RGA前后,NE的pD_2值分别为5.9±0.5和5.6±0.6,最大收缩分别为(8.9±3.2)g和(8.0±3.2)g,差异无显著性。结论:在RGA中NE引起的收缩效应主要由α_(1A)-AR介导,而α_(1B)-AR和α^(1D)-AR均不参与收缩效应。

关 键 词：alpha-1 adrenergic receptors right gastroepiploic artery VASOCONSTRICTION adrenergic alphaantagonists RS17053 5-MU BMY7378 WB4101 chlorethylclonidine 

分 类 号：R33[医药卫生—人体生理学]