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电压门控钙通道的药理学调节剂及其治疗应用。

Pharmacological modulators of voltage-gated calcium channels and their therapeutical application.

作者信息

Kochegarov Andrei A

机构信息

Department of Neurology, UCLA, 695 Charles E. Young Dr. 50, GONDA 5524, Los Angeles, CA 90095, USA.

出版信息

Cell Calcium. 2003 Mar;33(3):145-62. doi: 10.1016/s0143-4160(02)00239-7.


DOI:10.1016/s0143-4160(02)00239-7
PMID:12600802
Abstract

Calcium channels (CCs) play an important role in the transduction of action potential to the cytosol. An influx of Ca(2+) is essential for muscle contraction, neurotransmitter, and hormonal release. Level of cytosolic Ca(2+) controls activities of many enzymes and regulatory proteins. Voltage-gated calcium channels (VGCCs) serve as sensors for membrane depolarization. Blood pressure reduction is due to relaxation of actomyosine filaments in vascular smooth muscles. Calcium channel blockers (CCBs) are traditionally used for treatment of cardiovascular diseases. Neurotransmitter release from presynaptic neurons is triggered by Ca(2+) influx. Blockers of neuronal CCs may be applied for pain treatment. Overload of neurons by Ca(2+) is toxic. CCBs may be applied for prevention of some neurodegenerative disorders.

摘要

钙通道(CCs)在动作电位向细胞质的转导过程中发挥着重要作用。钙离子(Ca²⁺)的内流对于肌肉收缩、神经递质释放和激素分泌至关重要。细胞质中Ca²⁺的水平控制着许多酶和调节蛋白的活性。电压门控钙通道(VGCCs)作为膜去极化的传感器。血压降低是由于血管平滑肌中肌动球蛋白丝的松弛。钙通道阻滞剂(CCBs)传统上用于治疗心血管疾病。突触前神经元释放神经递质是由Ca²⁺内流触发的。神经元CCs的阻滞剂可用于疼痛治疗。Ca²⁺使神经元过载具有毒性。CCBs可用于预防某些神经退行性疾病。

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