Recent advances in the development of T-type calcium channel blockers for pain intervention
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TLDR
Recent developments in the discovery of novel classes of T‐type calcium channel blockers, and their analgesic effects in animal models of pain and in clinical trials are reviewed.Abstract:
Cav3.2 T-type calcium channels are important regulators of pain signals in afferent pain pathway, and their activities are dysregulated during various chronic pain states. Therefore it stands to reason that inhibiting T-type calcium channels in dorsal root ganglion neurons and in the spinal dorsal horn can be targeted for pain relief. This is supported by early pharmacological studies with T-type channel blockers such as ethosuximide, and by analgesic effects of siRNA depletion of Cav3.2 channels. In the past five years, considerable effort has been applied towards identifying novel classes of T-type calcium channel blockers. Here we review recent developments in the discovery of novel classes of T-type calcium channel blockers, and their analgesics effects in animal models of pain and in clinical trials.read more
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Neuropathic Pain: From Mechanisms to Treatment
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T-type calcium channels: From molecule to therapeutic opportunities
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TL;DR: The diversity, molecular structure, and principal electrophysiological properties of T-type channels are introduced and their role in neuronal development, and their pathophysiological role in the nervous system are highlighted.
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[T-type calcium channel blockers].
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