Overview
- Almeida, M.C. et al. (2012) J. Neurosci. 32, 2086.
Alomone Labs M8-B hydrochloride inhibits TRPM8 channels expressed in HEK-293 cells.Dose response curve of TRPM8 inhibition by M8-B hydrochloride (#M-220). Cells were loaded with Calcium-5 dye, incubated for 10 min with increasing concentrations of M8-B hydrochloride, and activated by 30 nM Icilin. Changes in intracellular Ca2+ following agonist application were detected as changes in 485nm/525nm fluorescence (RFU). IC50 was determined at 20 nM.
- Almeida, M.C. et al. (2012) J. Neurosci. 32, 2086.
- Tsumura, M. et al. (2013) PLoS ONE 8, e82233.
- Behrendt, H.J. et al. (2004) Br. J. Pharmacol. 141, 737.
M8-B hydrochloride is a potent and selective antagonist of the transient receptor potential melastatin-8 (TRPM8) channel1. It inhibits rat and human TRPM8 channels by cold, by icilin and by menthol and demonstrates IC50 values of 7.8 nM, 26.9 nM, and 64.3 nM, respectively. The compound shows little or no effect on other TRP channels1.
TRPM8 is a Ca2+-permeable channel, a member of the ‘long' or melastatin (M) group of TRP channels and is activated by temperatures range of 8–28°C or by cooling compounds. The TRPM8 gene is up-regulated in prostate cancer and other malignancies. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons2,3.
M8-B hydrochloride (#M-220) is a highly pure, synthetic, and biologically active compound.
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