2-Aminoethoxydiphenyl Borate as a Common Activator of TRPV1, TRPV2, and TRPV3 Channels
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.
Keywords2APB Transient receptor potential TRPC Store-operated channel Thermosensitive channel
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- Nöth H (1970) Some recent developments in boron-nitrogen chemistry. In: Brotherton RJ, Steinberg H (eds) Progress in boron chemistry. Pergamon Press, New York, pp 211–311Google Scholar
- Schindl R, Kahr H, Graz I, Groschner K, Romanin C (2002) Store depletion-activated CaT1 currents in rat basophilic leukemia mast cells are inhibited by 2-aminoethoxydiphenyl borate. Evidence for a regulatory component that controls activation of both CaT1 and CRAC (Ca2+ release-activated Ca2+ channel) channels. J Biol Chem 277:26950–26958PubMedCrossRefGoogle Scholar