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Modulators of voltage-dependent calcium channels for the treatment of nervous system diseases
1Research Resources Center, RIKEN Brain Science Institute, 2-1 Hirosawa, Wako, Saitama, Japan. etakahashi@brain.riken.jp
Abstract:
Voltage-dependent Ca(2+) channels (VDCCs) play important roles in physiological functions and pathological processes of the nervous system. Given that the precise regulation of Ca(2+) signaling is important for neuronal processes such as action potential generation, transmitter release, and synaptic plasticity, alterations in Ca(2+) current through VDCCs affect the functions of neurons and circuits. Central nervous system (CNS) diseases, including pain, epilepsy, seizure, anxiety, depression, dementia, and stroke, are characterized by an altered balance between excitatory and inhibitory neuronal functions. An efficient way of controlling such diseases is to block or modulate VDCC function. An effective strategy to reduce the likelihood of adverse effects is to develop agents that selectively control the VDCC isoform/subunit involved in the mechanism of the disease in question. This review provides an overview of knowledge on VDCCs, traditional and newly developed therapeutic fields, clinical fields, and the diverse medicinal chemistry of traditional and newly developed VDCC blockers in the CNS based on the scientific and patent literature.
Insights
Voltage-dependent calcium channels (VDCCs) are crucial for nervous system function. Modulating VDCCs offers a promising therapeutic strategy for various central nervous system diseases by targeting specific channel types.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- Voltage-dependent calcium channels (VDCCs) regulate critical neuronal processes like action potential generation and neurotransmitter release.
- Dysregulation of calcium signaling through VDCCs is implicated in central nervous system (CNS) disorders such as pain, epilepsy, anxiety, and dementia.
Purpose of the Study:
- To provide a comprehensive overview of VDCCs in the context of CNS diseases.
- To review traditional and novel therapeutic strategies targeting VDCCs.
- To explore the medicinal chemistry of VDCC blockers.
Main Methods:
- Literature review of scientific and patent databases.
- Analysis of traditional and emerging therapeutic fields related to VDCCs.
- Examination of the medicinal chemistry of VDCC modulators.
Main Results:
- VDCCs are key players in both normal neuronal function and the pathophysiology of CNS diseases.
- Targeting specific VDCC isoforms offers a strategy to minimize adverse effects.
- A diverse range of traditional and novel VDCC blockers are being developed.
Conclusions:
- Modulation of VDCCs presents a viable therapeutic avenue for a spectrum of CNS disorders.
- Selective targeting of disease-relevant VDCC subtypes is essential for effective and safe treatment.
- Continued research into VDCC medicinal chemistry holds promise for future drug development.
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