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M8 B hydrochloride

Names

[ CAS No. ]:
883976-12-3

[ Name ]:
M8 B hydrochloride

[Synonym ]:
MFCD27978374
N-(2-Aminoethyl)-N-[4-(benzyloxy)-3-methoxybenzyl]-2-thiophenecarboxamide hydrochloride (1:1)
2-Thiophenecarboxamide, N-(2-aminoethyl)-N-[[3-methoxy-4-(phenylmethoxy)phenyl]methyl]-, hydrochloride (1:1)

Biological Activity

[Description]:

M8-B is a potent transient receptor potential melastatin-8 (TRPM8) antagonist. M8-B blocks cold-induced and TRPM8-agonist-induced activation TRPM8 channels. M8-B decreases deep body temperature (Tb)[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Research Areas >> Metabolic Disease

[Target]

TRPM8


[In Vitro]

M8-B (0-100 µM) 以剂量依赖性方式抑制最大 Ca2+ 摄取来抑制 TRPM8 通道活性[1]。

[In Vivo]

M8-B (6 mg/kg; i.v. or i.p.) 降低大鼠和小鼠的深部体温[1]。 Animal Model: Trpm8+/+ rats and mice[1] Dosage: 6 mg/kg Administration: I.v. or i.p. Result: Decreased deep body temperature (T(b)) in Trpm8+/+ rats and mice, but not in Trpm8−/− mice.

[References]

[1]. Almeida MC, et al. Pharmacological blockade of the cold receptor TRPM8 attenuates autonomic and behavioral cold defenses and decreases deep body temperature. J Neurosci. 2012 Feb 8;32(6):2086-99.  

Chemical & Physical Properties

[ Molecular Formula ]:
C22H25ClN2O3S

[ Molecular Weight ]:
432.964

[ Exact Mass ]:
432.127441

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds