2-Aminoethoxydiphenyl borate as a common activator of TRPV1, TRPV2, and TRPV3 channels.

ABSTRACT: 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,

SUBMITTER: Colton CK 

PROVIDER: S-EPMC4458144 | biostudies-literature | 2007

REPOSITORIES: biostudies-literature