高血压大鼠尾动脉上κ,σ和苯环利定受体激动剂的效应(英文)  

Effects of K a and phencyclidine receptors agonists in rat tail arteries of spontaneously hypertensive rats

作　　者：高骏[1] 包维丽[1] 孙凤艳[1] 张安中[1] 

机构地区：[1]上海医科大学医学神经生物学国家重点实验室

出　　处：《中国药理学报》1994年第2期111-114,共4页Acta Pharmacologica Sinica

基　　金：Project supported by the National Natural Science Foundation of China,№ 38970283.

摘　　要：利用电场刺激引起的大鼠尾动脉收缩模型,研究了κ,(?)和苯环利定(Phe)受体在高血压大鼠(SHR)上的变化,结果,埃托啡和U-50 488H在SHR上的抑制作用显著高于非高血压大鼠(WKY)。(+)-3-PPP的结果与上述相反,DTG的作用很小,Phe,TCP和MK-801的增强作用在两者间无显著差别。提示在SHR上κ受体的敏感性增高,(?)受体相反,而Phe受体的敏感性变化较少。The effects of the kappa receptor agonist trans -4-dichloro-N-methyl-N-( 2-( 1-pyrrolidin ) cyclohexyl )-benzeneacefamide methane sulfonate (U-50 488H)., etorphine, the sigma (a) receptor agonists ( + ) - 3 - ( 3 -hydroxychenyl )-N-( 1-propyl ) piperidine (( + )-3-PPP ), 1, 3-di-o-tolyl-guanidine (DTG), and the phencyclidine (Phe) receptor agonists Phe, N-( l-( 2-thienyl ) cyclohexyl ) piperidine (TCP ) , and dizocilipine maleate (MK-801) on electrically stimulated constriction (ESC) were investigated in the rat tail arteries (RTA) of spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto (WKY) rats. Etorphine and U-50 488H inhibited the response to ESC in SHR more than that in WKY. The effects of U-50 488H were greater than those of etorphine. The IC50 and Kact of U-50 488H in SHR were 2. 5 ± 2. 0 and 0. 43±0. 22 μmol·L-1, respectively, while the corresponding figures in WKY were 23 μ15 and 2.3±1.0 μmol·L-1, respectively (P< 0.05). The inhibitory effects of ( + )-3-PPP on ESC in RTA of SHR were weaker than those in WKY. Its IC50 and Kact, in SHR were 11. 6 ± 5. 4 and 0. 87±0. 30 μmol·L-1, respectively, while the corresponding figures in WKY were 0. 63 ± 0. 16 and 0. 35 ± 0. 18 μmol· L-1, respectively (P<0.05). But the inhibitory effect of DTG was very slight and the difference of Kact between WKY and SHR was not significant. The enhancing effects of Phe, TCP, and MK-801 in SHR were not at all different from those in WKY at each concentration tested. These results suggested that the sensitivity of kappa (K) receptor in peripheral blood vessels of SHR was higher than that of WKY while that of the a receptor was quite the contrary, and that the sensitivity of Phe may have little difference.

关 键 词：苯环利定 受体 高血压 尾动脉 大鼠 

分 类 号：R965.2[医药卫生—药理学]