In the anesthetized rat, AMTB (3 mg/kg; intravenous) hydrochloride decreases the frequency of volume-induced bladder contractions, without reducing the amplitude of contraction[1].
In Vitro
AMTB hydrochloride blocks veratridine-induced membrane potential changes at each NaV1 isoform (pIC50s ranging 4.83-5.69 for NaV1.1- NaV1.8)[2]. AMTB hydrochloride decreases viable cell number in MDA-MB-231 and SK-BR-3 breast cancer cell lines (30 and 100 μM), and also reduces the migration of MDA-MB-231 cells (30 μM)[2].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Lashinger ES, et al. AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome. Am J Physiol Renal Physiol. 2008;295(3):F803-F810.
[2]. Yapa KTDS, et al. Assessment of the TRPM8 inhibitor AMTB in breast cancer cells and its identification as an inhibitor of voltage gated sodium channels. Life Sci. 2018;198:128-135.
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