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

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.