摘要
该文阐述电压依赖性钙通道不同分型与亚型和抗高血压药物的关系。(1)传统的L型电压依赖性钙通道阻断剂舒张肾入球小动脉,但对肾出球小动脉无作用。第3代新的双氢吡啶类钙通道阻断剂(manidipine,nilvadipine,benzin-damine和efonidipine)能同时作用L及T型钙通道,对肾出球小动脉也能舒张,故对肾性高血压有效,并起保护肾脏作用。(2)L型钙通道的主要组成α1c亚基,在高血压时表达增加,使钙通道数量增多,从而加速高血压的发展,故能使α1c亚基数目恢复正常的药物,有望用于临床治疗高血压。
This paper elucidates the relationship among different types and subunits of voltage-gated calcium channels and antihypertensive drugs. ①L-type calcium channels lack of functional expression in renal efferent arterioles, but it has been found recently that T-type calcium channels have had roles in the regulation of renal efferent arteriolar tone. Third generation dihydropyridine, L-type calcium channel antagonists including manidipine, nilvadipine, benzindamine and efonidipine, can dilate both afferent and efferent renal arterioles, then improve glomerular hypertension and provide renoprotection, because the inhibition of both L and T type calcium channels. ②In hypertensive rats, an increased expression of L-type calcium channel α1 c subunits has been shown, and this increased expression of calcium channel etl c subunit associated with the increase of Ca^2＋ influx and elevated arterial tone can be observed. These findings provide a rational basis for designing antihypertension therapy by normalizing Ca^2＋ channel α1 c subunit expression.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2008年第5期569-572,共4页
Chinese Pharmacological Bulletin
关键词
电压依赖性钙通道
分型
亚基
钙通道阻断剂
高血压
voltage-gated calcium channel
type
subunit
calci-um channel antagonist
hypertension
