Volume 10 Supplement 1

Proceedings of the Seventh Scientific Meeting of The TMJ Association

Open Access

Preclinical and translational studies of fenobam, an mGlu5 NAM, for the treatment of pain

  • Robert W Gereau IV1 and
  • Laura F Cavallone1
Molecular Pain201410(Suppl 1):O3

https://doi.org/10.1186/1744-8069-10-S1-O3

Published: 15 December 2014

Background

Metabotropic glutamate receptor 5 has been suggested by many rodent studies to be a promising target for the development of novel analgesic drugs. The lack of approved compounds has prevented proof-of-concept studies in human subjects. Here we describe preclinical and translational studies of the mGlu5 negative allosteric modulator (NAM), fenobam.

Materials and methods

Fenobam was tested for analgesic efficacy and toxicity in mouse models. We also tested the plasma levels after oral dosing of fenobam in healthy volunteers, and collected any adverse events following oral dosing compared to placebo.

Results

The mGlu5 NAM Fenobam is effective in a wide variety of preclinical pain models in mice with no evidence of the development of analgesic tolerance on daily dosing. No obvious toxicities were observed in mice, or in several studies in healthy human volunteers.

Conclusions

Fenobam has robust analgesic activity and shows a good safety profile. Fenobam therefore represents a useful tool for proof-of-concept studies in human subjects.

Declarations

Acknowledgements

This work was supported by grants from the National Institutes of Health (NS48602) to RG.

Authors’ Affiliations

(1)
Washington University Pain Center and Department of Anesthesiology, Washington University School of Medicine

Copyright

© Gereau IV and Cavallone; licensee BioMed Central Ltd. 2014

This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.

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