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Recent advances in the development of T-type calcium channel blockers for pain intervention
Terrance P Snutch1, Gerald W Zamponi2
1Michael Smith Laboratories and Djavad Mowafaghian Centre for Brain Health, University of British Columbia, Vancouver, BC, Canada.
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.
Insights
Novel T-type calcium channel blockers show promise for chronic pain relief. Research focuses on inhibiting Cav 3.2 channels in the nervous system, with recent developments in drug discovery and clinical trials.
Area of Science:
- Neuroscience
- Pharmacology
- Pain Research
Background:
- Cav 3.2 T-type calcium channels regulate pain signaling in the afferent pain pathway.
- Channel activity is altered in chronic pain conditions.
- Targeting these channels offers a potential strategy for pain management.
Purpose of the Study:
- To review recent advancements in the discovery of novel T-type calcium channel blockers.
- To discuss their analgesic effects observed in preclinical pain models and human clinical trials.
Main Methods:
- Review of pharmacological studies on T-type channel blockers.
- Analysis of siRNA-mediated Cav 3.2 channel depletion studies.
- Examination of recent drug discovery efforts for novel blockers.
- Evaluation of preclinical and clinical trial data for analgesic efficacy.
Main Results:
- Early studies with blockers like ethosuximide demonstrated analgesic potential.
- siRNA depletion of Cav 3.2 channels confirmed their role in pain.
- Significant progress has been made in identifying new classes of T-type calcium channel blockers over the last five years.
- These novel blockers have shown analgesic effects in animal models and are being investigated in clinical trials.
Conclusions:
- Inhibiting Cav 3.2 T-type calcium channels in the dorsal root ganglion and spinal dorsal horn is a viable therapeutic target for chronic pain.
- Recent drug discovery efforts have yielded promising novel blockers.
- Further research and clinical trials are essential to translate these findings into effective pain treatments.
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