Bioactivity | AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC50 of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (NaV)[1][2]. |
Invitro | 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]. |
In Vivo | 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]. |
Name | AMTB hydrochloride |
CAS | 926023-82-7 |
Formula | C23H27ClN2O2S |
Molar Mass | 430.99 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
Reference | [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. |