萘哌地尔衍生物(BWYJ)对血管平滑肌细胞游离钙浓度的影响  

Effects of Naftopidil' ramification-BWYJ on intracellularlar free Ca^(2+) in smooth cells

作　　者：王会玖[1] 黄燮南[1] 蒋青松[1] 吴芹[1] 孙安盛[1] 石京山[1] 

机构地区：[1]遵义医学院药理学教研室

出　　处：《中国临床药理学与治疗学》2005年第7期772-775,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：贵州省科委基金资助项目(№C-184)

摘　　要：目的:观察萘哌地尔衍生物(BWYJ)对家兔血管平滑肌细胞游离钙浓度的影响,对其血管活性进行机理探讨,进一步明确其作用机制。方法:采用钙荧光指示剂Fura-2/AM负载的培养家兔胸主动脉平滑肌细胞,观察该药对NA、5-HT和高钾所致的[Ca2+]i的升高的影响。结果:Fura-2/AM负载血管平滑肌细胞的实验中,静息时各浓度的BWYJ对[Ca2+]i无明显影响,但其对NA和5-HT所引起的血管平滑肌[Ca2+]i增加均有明显的抑制作用,而不影响高钾所致血管平滑肌[Ca2+]i的增加。结论:BWYJ通过阻断细胞膜上的α1受体或5-HT2A受体,抑制这些受体中介的钙内流,从而抑制细胞内Ca2+的释放,使血管平滑肌[Ca2+]i降低。AIM： To observed the effects of BWYJ （a naftopidil ramification） on intracellularlar free Ca^2＋（ [ Ca^2 ＋ ]i ） in smooth cells （SMCs） in order to further explore its vasodilative mechanisms. METHODS： The[Ca^2＋ ]i was determined with the Fura-2/AM loaded SMCs in aorta of rabbit, and the effects of BWYJ on the elevation induced by NA, and high potassium and 5-HT were observe. RESULT： In the Fura-2/AM loaded SMCs, BWYJ had no effect on the resting [ Ca^2 ＋ ]i, but it reduced the increase of [ Ca^2 ＋ ]i induced by NA and 5-HT, and there was no influence on the increase of [Ca^2＋ ]i induced by high potassium. CONCLUSION： The vasodilative mechanisms of BWYJ may be related to its inhibitive effects on the Ca^2＋ -influx and Ca^2＋ -release mediated by α1- and 5-HT2A receptors. It inhibits the release of intracellular calcium, and the result is it decrease the [Ca^2 ＋ ]i in SMCs.

关 键 词：BWYJ 萘哌地尔 细胞内游离钙 去甲肾上腺素 5-羟色胺 氯化钾 

分 类 号：R972.4[医药卫生—药品]