Pharmacology of transient receptor potential melastatin channels in the vasculature


  • Standard abbreviations conform to BJP's Guide to Receptors & Channels (Alexander et al., 2008) and to the IUPHAR guidelines, as published in Pharmacological Reviews.

Alexander Zholos, Centre for Vision & Vascular Science, School of Medicine, Dentistry and Biomedical Sciences, Medical Biology Centre, Queen's University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK. E-mail:


Mammalian transient receptor potential melastatin (TRPM) non-selective cation channels, the largest TRP subfamily, are widely expressed in excitable and non-excitable cells where they perform diverse functions ranging from detection of cold, taste, osmolarity, redox state and pH to control of Mg2+ homeostasis and cell proliferation or death. Recently, TRPM gene expression has been identified in vascular smooth muscles with dominance of the TRPM8 channel. There has been in parallel considerable progress in decoding the functional roles of several TRPMs in the vasculature. This research on native cells is aided by the knowledge of the activation mechanisms and pharmacological properties of heterologously expressed TRPM subtypes. This paper summarizes the present state of knowledge of vascular TRPM channels and outlines several anticipated directions of future research in this area.