Cuypers E, Dabrowski M, Horoszok L, Terp G E, Tytgat J
Lab of Toxicology, Campus Gasthuisberg, O&N2, Herestraat 49, Leuven, Belgium.
CNS Neurol Disord Drug Targets. 2008 Apr;7(2):159-71. doi: 10.2174/187152708784083803.
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 capsaicin's 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.
在过去几年里，瞬时受体电位香草酸亚型1（TRPV1）通道一直是离子通道研究中的热门话题。由于这个研究领域仍然相当新，关于TRPV1及其配体的工作机制所知甚少。然而，其重要的生理作用和治疗潜力前景广阔。因此，相关的广泛研究正在进行，并且已经描述了许多天然和合成化合物。在这篇综述中，我们简要概述了辣椒素的历史以及目前对其作用机制和生理作用的认识。我们讨论了作用于TRPV1的最知名植物分子，并重点介绍了TRPV1研究中的最新发现：作用于TRPV1通道的动物毒液和毒素。为了全面呈现目前已知的TRPV1配体，我们展示了最有前景的合成化合物。最后，我们提出了一个描述假定配体结合域的新型药效团模型。
