TM 38837

Names

[ Name ]:
TM 38837

[Synonym ]:
1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-4-ethyl-N-1-piperidinyl-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-
1-(2,4-Dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-5-(5-{[4-(trifluoromethyl)phenyl]ethynyl}-2-thienyl)-1H-pyrazole-3-carboxamide
TM-38837

Biological Activity

[Description]:

TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects[1][2].

[Related Catalog]:

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

[Target]

CB1

[In Vivo]

TM38837 (10-100 mg/kg; p.o.) induces a significant increase in freezing behavior at 100 mg/kg[1]. Animal Model: 7-8 weeks old male C57BL/6 N mice (B6N)[1] Dosage: 10, 30, or 100 mg/kg Administration: p.o. Result: High dose (100 mg/kg) induced a significant increase in freezing behavior.

[References]

[1]. Micale V, et al. The Cannabinoid CB1 Antagonist TM38837 With Limited Penetrance to the Brain Shows ReducedFear-Promoting Effects in Mice. Front Pharmacol. 2019 Mar 20;10:207.

[2]. Klumpers LE, et al. Peripheral selectivity of the novel cannabinoid receptor antagonist TM38837 in healthy subjects. Br J Clin Pharmacol. 2013 Dec;76(6):846-57.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₃₀H₂₅Cl₂F₃N₄OS

[ Molecular Weight ]:
617.512

[ Exact Mass ]:
616.107849

[ LogP ]:
8.91

[ Index of Refraction ]:
1.635

Related Compounds

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