钙通道不同分型与亚基和抗高血压药物的关系

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。

Relationship among different types and subunits of calcium channels and antihypertensive drugs

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.② In hypertensive rats,an increased expression of L-type calcium channel α1c subunits has been shown.and this increased expression of calcium channel α1c subunit associated with the increase of Ca2+ influx and elevated arterial tone can be observed.These findings provide a rational basis for designing antihypertension therapy by normalizing Ca2+ channel α1c subunit expression.