Channel name | TRPM81,2,3,4,5 |
Description | Cooling and menthol-sensing TRP channel |
Other names | CMR1 (cold and menthol receptor), Trp-p8 |
Molecular information | Human unigene: Hs0.366053, chr. 2q37.1 |
Mouse unigene: Mm0.218753, chr. 1 D | |
Associated subunits | Not established |
Functional assays | Patch-clamp, calcium imaging |
Current | Steeply outwardly rectifying >0 mV |
Conductance | 83pS (slope conductance) |
Ion selectivity | PNa/PCa = 0.3, nonselective cation channel |
Activation | 8–26°C |
Inactivation | Warming >28°C |
Activators | Cooling below 22–26°C, cooling agents such as menthol (EC50 = 70 μM) and icilin (EC50 = 360 nM); less potent: linalool, geraniol, hydroxycitronella |
Gating inhibitors | None |
Blockers | BCTC, thio-BCTC, capsazepine |
Radioligands | None |
Channel distribution | Small sensory neurons of trigeminal ganglion and dorsal root ganglia, prostate epithelium |
Physiological functions | Cold sensation |
Mutations and pathophysiology | Not established |
Pharmacological significance | Putative menthol receptor |
Comments | The neuronal colocalization and potential coassembly of TRPV1, TRPV2, TRPV3, and TRPM8 are under study |
chr., chromosome.
↵1. McKemy DD, Neuhausser WM, and Julius D (2002) Identification of a cold receptor reveals a general role for TRP channels in thermosensation. Nature (Lond) 416:52-58
↵2. Peir AM, Moqrich A, Hergarden AC, Reeve AJ, Andersson DA, Story GM, Earley TJ, Dragoni I, McIntyre P, Bevan S, et al. (2002) A TRP channel that senses cold stimuli and menthol. Cell 108:705-715
↵3. Voets T, Droogmans G, Wissenbach U, Janssens A, Flockerzi V, and Nilius B (2004) The principle of temperature-dependent gating in cold- and heat-sensitive TRP channels. Nature (Lond) 430:748-754
↵4. Brauchi S, Orio P, and Latorre R (2004) Clues to understanding cold sensation: thermodynamics and electrophysiological analysis of the cold receptor TRPM8. Proc Natl Acad Sci USA 101:15494-15499
↵5. Behrendt HJ, Germann T, Gillen C, Hatt H, and Jostock R (2004) Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay. Br J Pharmacol 141:737-745