L-type calcium channels.
L-type calcium channels.
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DOI：
10.2174/138161206775474503
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发表时间：
2006-01
影响因子：
3.1
通讯作者：
D. Triggle
中科院分区：
文献类型：
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作者：
D. Triggle
Ca2+通道阻滞剂代表了一组成功的治疗药物针对心血管目标，包括高血压和心绞痛。这些药物，包括第一代维拉帕米、硝苯地平和地尔硫卓，都是针对电压门控Ca2+通道的一个亚类——l型通道。Ca2+通道的其他亚类存在并且是新适应症的靶标。本文讨论了l型阻滞剂的作用机制，并讨论了其心血管选择性的起源。虽然这类针对高血压的新药可以开发出来，但临床和经济原因都反对这种开发。然而，还有其他可能的靶点来研究l型通道的拮抗剂和激活剂可能有用的地方：这些靶点包括生育、神经元生长、骨形成和癫痫。讨论了这些方法的局限性。
The Ca2+ channel blockers represent a successful group of therapeutic agents directed against cardiovascular targets, including hypertension and angina. These drugs, including the first-generation verapamil, nifedipine and diltiazem are directed against a subclass of voltage-gated Ca2+ channel - the L-type channel. Other subclasses of Ca2+ channel exist and are targets for new indications. The mechanisms of actions of the L-type blockers are discussed and the origins of their cardiovascular selectivity discussed. Although new drugs of this class directed against hypertension could be developed, there are both clinical and economic reasons that argue against such development. However, there are other possible targets to investigate where antagonists and activators of the L-type channel may be useful: such targets include fertility, neuronal growth, bone formation and epilepsy. Limitations to these approaches are discussed.