Smith R D
Fed Proc. 1983 Feb;42(2):201-6.
Calcium entry blockers (CEBs) are of widespread interest because of the primary role of Ca2+ in excitation-contraction coupling in vascular smooth muscle and the probable involvement of Ca2+ in the etiology of hypertension. The role of CEBs in the chronic management of essential hypertension, however, has not been established. Key issues are the definition of CEB, mechanism of vasodilator action(s), tissue selectivity, quality of antihypertensive effects, other effects, and future developments. CEBs may have multiple intracellular and extracellular sites of action and may modify both energy production and excitation-contraction coupling in vascular smooth muscle. CEBs are not unique in their vasodilator-antihypertensive profile. Other effects, e.g., coronary vasodilator or cardioprotective effects, of CEBs and their tissue selectivity may, however, provide a favorable benefit/risk profile for their chronic use in essential hypertension. New CEBs may be called modifiers of calcium metabolism, may actually be curative in hypertension, and will most certainly be of major physiological and pharmacological interest.
由于钙离子在血管平滑肌的兴奋 - 收缩偶联中起主要作用，且钙离子可能参与高血压的发病机制，钙通道阻滞剂（CEBs）受到广泛关注。然而，CEBs在原发性高血压的长期治疗中的作用尚未确立。关键问题包括CEB的定义、血管舒张作用机制、组织选择性、降压效果质量、其他作用以及未来发展。CEBs可能有多个细胞内和细胞外作用位点，并可能改变血管平滑肌中的能量产生和兴奋 - 收缩偶联。CEBs在其血管舒张 - 降压特性方面并非独一无二。然而，CEBs的其他作用，如冠状动脉舒张或心脏保护作用及其组织选择性，可能为其在原发性高血压中的长期使用提供有利的效益/风险概况。新型CEBs可能被称为钙代谢调节剂，可能实际上对高血压具有治愈作用，并且肯定会引起重大的生理和药理学关注。
