Abstract
Over the last couple of years, transient receptor potential vanilloid 1(TRPV1) channels have been a hot topic in ion channel research. Since this research field is still rather new, there is not much known about the working mechanism of TRPV1 and its ligands. Nevertheless, the important physiological role and therapeutic potential are promising. Therefore, extensive research is going on and a lot of natural as well as synthetic compounds are already described. In this review, we briefly give an overview of capsaicins history and the current knowledge of its working mechanism and physiological role. We discuss the best known plant molecules acting on TRPV1 and highlight the latest discovery in TRPV1 research: animal venoms and toxins acting on TRPV1 channels. In an effort to give the complete image of TRPV1 ligands known today, the most promising synthetic compounds are presented. Finally, we present a novel pharmacophore model describing putative ligand binding domains.
Keywords: TRPV1, plant molecules, animal venoms, animal toxins, synthetic molecules
CNS & Neurological Disorders - Drug Targets
Title: Transient Receptor Potential Vanilloid 1 and Xenobiotics
Volume: 7 Issue: 2
Author(s): E. Cuypers, M. Dabrowski, L. Horoszok, G. E. Terp and J. Tytgat
Affiliation:
Keywords: TRPV1, plant molecules, animal venoms, animal toxins, synthetic molecules
Abstract: Over the last couple of years, transient receptor potential vanilloid 1(TRPV1) channels have been a hot topic in ion channel research. Since this research field is still rather new, there is not much known about the working mechanism of TRPV1 and its ligands. Nevertheless, the important physiological role and therapeutic potential are promising. Therefore, extensive research is going on and a lot of natural as well as synthetic compounds are already described. In this review, we briefly give an overview of capsaicins history and the current knowledge of its working mechanism and physiological role. We discuss the best known plant molecules acting on TRPV1 and highlight the latest discovery in TRPV1 research: animal venoms and toxins acting on TRPV1 channels. In an effort to give the complete image of TRPV1 ligands known today, the most promising synthetic compounds are presented. Finally, we present a novel pharmacophore model describing putative ligand binding domains.
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Cuypers E., Dabrowski M., Horoszok L., Terp E. G. and Tytgat J., Transient Receptor Potential Vanilloid 1 and Xenobiotics, CNS & Neurological Disorders - Drug Targets 2008; 7 (2) . https://dx.doi.org/10.2174/187152708784083803
DOI https://dx.doi.org/10.2174/187152708784083803 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
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