Recent advances in the development of T-type calcium channel blockers for pain intervention

Br J Pharmacol. 2018 Jun;175(12):2375-2383. doi: 10.1111/bph.13906. Epub 2017 Jul 12.

Abstract

Cav 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 Cav 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.

Linked articles: This article is part of a themed section on Recent Advances in Targeting Ion Channels to Treat Chronic Pain. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v175.12/issuetoc.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Calcium Channel Blockers / chemistry
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, T-Type / metabolism*
  • Humans
  • Pain / drug therapy*
  • Pain Management*

Substances

  • Calcium Channel Blockers
  • Calcium Channels, T-Type

Grant support