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Drug design and development through the vanilloid receptor.
Rosa Planells-Cases11, Antonio Ferrer-Montiel
1Centro de Investigación Príncipe Felipe, Valencia, Spain.
Expert Opinion on Drug Discovery
|March 15, 2013
Summary
The vanilloid receptor (TRPV1) shows promise for pain relief but has limited clinical success. New research suggests preserving TRPV1
Area of Science:
- Pharmacology
- Neuroscience
- Pain Research
Background:
- The vanilloid receptor (TRPV1) is a key target for chronic inflammatory pain therapeutics.
- Numerous TRPV1 agonists and antagonists have been developed, but few advanced to clinical trials for pain management.
- Limited clinical success suggests an incomplete understanding of TRPV1's role in pain and physiology.
Purpose of the Study:
- To investigate the complex role of the vanilloid receptor (TRPV1) beyond pain signaling.
- To explore the physiological functions of TRPV1 and its implications for drug development.
- To address the challenge of developing TRPV1 modulators that balance therapeutic effects with physiological preservation.
Main Methods:
- Review of existing literature on TRPV1 function and pharmacology.
- Analysis of preclinical data regarding TRPV1 modulation in pain models.
- Examination of findings on TRPV1's tonic activity and effects of blockade or abrogation.
Main Results:
- TRPV1 is widely distributed, indicating roles beyond pain, including physiological functions.
- TRPV1 exhibits tonic activity under physiological conditions.
- Pharmacological blockade of TRPV1 can lead to hyperthermia.
- Complete TRPV1 absence in some chronic pain models exacerbates pain.
Conclusions:
- Developing effective TRPV1-targeting drugs requires preserving physiological TRPV1 activity.
- Strategies must differentiate between modulating overactive receptors and inhibiting normal function.
- Future drug development should aim to selectively downregulate aberrant TRPV1 signaling while maintaining essential physiological roles.
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