Colton C K, Zhu M X
Department of Neuroscience, Center for Molecular Neurobiology, The Ohio State University, Columbus, OH 43210, USA.
Handb Exp Pharmacol. 2007(179):173-87. doi: 10.1007/978-3-540-34891-7_10.
2-Aminoethoxydiphenyl borate (2APB) had been depicted as a universal blocker of transient receptor potential (TRP) channels. While evidence has accumulated showing that some TRP channels are indeed inhibited by 2APB, especially in heterologous expression systems, there are other TRP channels that are unaffected or affected very little by this compound. More interestingly, the thermosensitive TRPV1, TRPV2, and TRPV3 channels are activated by 2APB. This has been demonstrated both in heterologous systems and in native tissues that express these channels. A number of 2APB analogs have been examined for their effects on native store-operated channels and heterologously expressed TRPV3. These studies revealed a complex mechanism of action for 2APB and its analogs on ion channels. In this review, we have summarized the current results on 2APB-induced activation of TRPV1-3 and discussed the potential mechanisms by which 2APB may regulate TRP channels.
2-氨基乙氧基二苯硼酸（2APB）曾被描述为瞬时受体电位（TRP）通道的通用阻滞剂。虽然已有越来越多的证据表明，一些TRP通道确实会被2APB抑制，尤其是在异源表达系统中，但也有其他TRP通道不受该化合物影响或受影响极小。更有趣的是，热敏性TRPV1、TRPV2和TRPV3通道会被2APB激活。这在异源系统以及表达这些通道的天然组织中均已得到证实。人们已对多种2APB类似物对天然储存操纵性通道和异源表达的TRPV3的影响进行了研究。这些研究揭示了2APB及其类似物对离子通道的复杂作用机制。在本综述中，我们总结了目前关于2APB诱导TRPV1 - 3激活的研究结果，并讨论了2APB调节TRP通道的潜在机制。
