Overview
- Behrendt, H.J. et al. (2004) Br. J. Pharmacol. 141, 737.
Alomone Labs Icilin activates TRPM8 channels expressed in HEK-293 cells.Dose response curve of human TRPM8 activation by increasing concentrations of Icilin (#I-145). EC50 was determined at 27 nM. hTRPM8/HEK-293 cells were loaded with Calcium-5 dye. Increase in intracellular Ca2+ levels following Icilin application was detected as a rise in 485 nm/525 nm fluorescence (RFU).
Icilin is a synthetic cooling substance that acts as a potent TRPM8 channel activator with an EC50 value of 0.2 ± 0.1μM1. This compound also shown to activate TRPA1 ion channel but at higher concentrations. Activation of TRPM8 channel by icilin produces Na+ and Ca2+ ion influx that results in cellular depolarization and the feeling of cold. Icilin has the ability to produce behavioral activation in rats and mice1-3.
TRPM8 is a Ca2+-permeable channel, a member of the ‘long' or melastatin (M) group of TRP channels and is activated by temperatures in the range of 8-28°C or by cooling compounds such as icilin. The TRPM8 gene is expressed and up-regulated in prostate cancer and other malignancies. TRPM8 channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons1,4.
