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Cell-based Calcium Assay for Medium to High Throughput Screening of TRP Channel Functions using FlexStation 3
Published on: August 17, 2011
T-type voltage-gated calcium channels as targets for the development of novel pain therapies
Slobodan M Todorovic1, Vesna Jevtovic-Todorovic
1Department of Anesthesiology and Neuroscience, University of Virginia School of Medicine, Charlottesville, 22908-0710, USA. st9d@virginia.edu
Abstract:
It is well recognized that voltage-gated calcium (Ca(2+)) channels modulate the function of peripheral and central pain pathways by influencing fast synaptic transmission and neuronal excitability. In the past, attention focused on the modulation of different subtypes of high-voltage-activated-type Ca(2+) channels; more recently, the function of low-voltage-activated or transient (T)-type Ca(2+) channels (T-channels) in nociception has been well documented. Currently, available pain therapies remain insufficient for certain forms of pain associated with chronic disorders (e.g. neuropathic pain) and often have serious side effects. Hence, the identification of selective and potent inhibitors and modulators of neuronal T-channels may help greatly in the development of safer, more effective pain therapies. Here, we summarize the available information implicating peripheral and central T-channels in nociception. We also discuss possible future developments aimed at selective modulation of function of these channels, which are highly expressed in nociceptors.
Insights
Transient (T)-type calcium channels (T-channels) play a key role in pain pathways. Targeting these channels may lead to safer and more effective pain therapies for chronic pain conditions.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- Voltage-gated calcium (Ca2+) channels are crucial for pain pathway modulation.
- Recent research highlights the role of low-voltage-activated transient (T)-type Ca2+ channels (T-channels) in nociception.
- Existing pain therapies often have insufficient efficacy and significant side effects, particularly for chronic pain.
Purpose of the Study:
- To review the involvement of peripheral and central T-channels in pain processing.
- To explore the therapeutic potential of T-channel modulators for pain management.
- To discuss future directions in selective T-channel modulation for safer pain therapies.
Main Methods:
- Literature review of studies on T-channels and nociception.
- Analysis of existing data on the expression and function of T-channels in pain pathways.
- Discussion of pharmacological strategies for T-channel modulation.
Main Results:
- T-channels are implicated in both peripheral and central pain signaling.
- T-channels are highly expressed in nociceptors, suggesting a critical role in pain sensation.
- Selective T-channel inhibitors offer a promising avenue for developing novel analgesics.
Conclusions:
- T-channels represent a significant therapeutic target for pain relief.
- Developing selective modulators of neuronal T-channels could overcome limitations of current pain treatments.
- Further research into T-channel function and pharmacology is warranted for improved pain management.
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