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AMTB is an antagonist of transient receptor potential melastatin 8 (TRPM8).1 It inhibits calcium influx induced by the TRPM8 agonist icilin (Item No. 10137) with an IC50 value of 0.58 µM. AMTB (3 mg/kg) decreases the number of volume-induced bladder contractions in a rat model of noxious bladder distension. It also decreases the visceromotor reflex response to urinary bladder distension (ID50 = 2.42 mg/kg), indicating antinociceptive activity. AMTB inhibits the sodium channel (Nav) isoforms Nav1.1-1.8 (IC50s = 2-14.8 µM) and decreases viability of MDA-MB-231 and SK-BR-3 breast cancer cells (IC50s = ~23.7 and 17.3 µM, respectively) in a TRPM8-independent manner.2
WARNING This product is not for human or veterinary use.
1. AMTB, a TRPM8 channel blocker: Evidence in rats for activity in overactive bladder and painful bladder syndrome. Am. J. Physiol. Renal Physiol. 295(3), F803-F810 (2008).
2. Assessment of the TRPM8 inhibitor AMTB in breast cancer cells and its identification as an inhibitor of voltage gated sodium channels. Life Sci. 198, 128-135 (2018).