2-Aminoethoxydiphenyl Borate as a Common Activator of TRPV1, TRPV2, and TRPV3 Channels

  • C. K. Colton
  • M. X. Zhu
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 179)


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.


2APB Transient receptor potential TRPC Store-operated channel Thermosensitive channel 


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Copyright information

© Springer-Verlag Berlin Heidelberg 2007

Authors and Affiliations

  • C. K. Colton
    • 1
  • M. X. Zhu
    • 1
  1. 1.Department of Neuroscience and Center for Molecular NeurobiologyThe Ohio State UniversityColumbusUSA

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