AMTB hydrochloride

Names

[ Name ]:
AMTB hydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Cancer

Research Areas >> Neurological Disease

[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].

[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].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₇ClN₂O₂S

[ Molecular Weight ]:
430.99100

[ Exact Mass ]:
430.14800

[ PSA ]:
83.80000

[ LogP ]:
6.12900

MSDS

Click to get detail MSDS

Related Compounds

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