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Possible consequences of blocking transient receptor potential vanilloid
Mahendra Bishnoi1, Louis S Premkumar
1Department of Pharmacology, Southern Illinois University School of Medicine Springfield, IL 62702, USA.
Current Pharmaceutical Biotechnology
|October 12, 2010
Summary
Transient Receptor Potential Vanilloid 1 (TRPV1) antagonists show promise for pain relief but can cause hyperthermia. Further research is needed to understand TRPV1
Area of Science:
- Neuroscience
- Molecular Biology
- Pharmacology
Background:
- The cloning of Transient Receptor Potential Vanilloid 1 (TRPV1) in 1997 revolutionized pain research.
- TRPV1 is primarily expressed in nociceptors and activated by noxious stimuli, playing a role in inflammatory pain hypersensitivity.
Purpose of the Study:
- To review the expression and function of TRPV1 in various organ systems.
- To highlight potential adverse effects of TRPV1 blockade, such as hyperthermia.
Main Methods:
- Literature review of studies on TRPV1 expression, function, and antagonist clinical trials.
- Analysis of gene disruption studies to confirm TRPV1's role in pain pathways.
Main Results:
- TRPV1 gene disruption confirms its role in inflammatory thermal hypersensitivity.
- TRPV1 is also expressed in non-sensory neurons and non-neuronal cells.
- Clinical trials revealed hyperthermia as a significant side effect of TRPV1 antagonists.
Conclusions:
- TRPV1 antagonists offer potential for pain management but carry risks like hyperthermia.
- Understanding TRPV1's broader expression is crucial for mitigating adverse effects.
- Further research is needed to balance therapeutic benefits with safety concerns.
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