Overview
- Lashinger, E.S. et al. (2008) Am. J. Renal Physiol. 295, F803.
Alomone Labs AMTB hydrochloride inhibits TRPM8 channels expressed in HEK-293 cells.Dose-response curve of TRPM8 inhibition by AMTB hydrochloride (#A-305), showing complete inhibition at 100 µM (pIC50 = 5.11). Cells were loaded with Calcium-5 dye, incubated for 10 min with increasing concentrations of AMTB hydrochloride, and activated by 30 nM icilin. Changes in intracellular Ca2+ following agonist application were detected as changes in 485 nm/525 nm fluorescence (RFU).
AMTB hydrochloride is a TRPM8 channel blocker, able to inhibit icilin-induced human TRPM8 channel activation. The compound shows very little affinity for TRPV1 and TRPV4 channels and is being used as a tool to evaluate the role of TRPM8 channels in different animal models1. TRPM8 channel blockers may provide a new therapeutic treatment for overactive and painful bladder syndrome1,2.
TRPM8 channel is a member of the TRP channel superfamily. TRPM8 is a Ca2+-permeable, nonselective cation channel that is activated by temperatures in the range of 8–28°C and by chemical agonists such as menthol and icilin. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons. It’s expression is up-regulated in prostate cancer and other malignancies3,4.
