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Recent advances in the development of T‐type calcium channel blockers for pain intervention
Author(s) -
Snutch Terrance P,
Zamponi Gerald W
Publication year - 2018
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.13906
Subject(s) - ethosuximide , calcium channel , t type calcium channel , analgesic , dorsal root ganglion , medicine , neuroscience , voltage dependent calcium channel , chronic pain , nociception , pharmacology , calcium , receptor , dorsum , psychology , anatomy , epilepsy , carbamazepine
Ca v 3.2 T-type calcium channels are important regulators of pain signals in the afferent pain pathway, and their activities are dysregulated during various chronic pain states. Therefore, it is reasonable to predict 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 Ca v 3.2 channels. In the past 5 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 analgesic effects in animal models of pain and in clinical trials.