A CB1 receptor antagonist; binds to CB1 receptors in rat forebrain membrane preparations (Ki = 7.5 nM); selective over CB2 receptors (Ki = 2

AM251 – 100 mg

Brand:
Cayman
CAS:
183232-66-8
Storage:
-20
UN-No:
Non-Hazardous - /

AM251 is a cannabinoid (CB) receptor 1 antagonist.{9721} It binds to CB1 receptors in rat forebrain membrane preparations (Ki = 7.5 nM) and is selective over CB2 receptors in mouse spleen preparations (Ki = 2,290 nM) in radioligand binding assays. AM251 inhibits GTPγS binding induced by the CB receptor agonist CP 55,940 in HEK293 cells expressing human CB1 receptors (EC50 = 8 nM).{17583} AM251 (10 mg/kg) decreases immobility time in the forced swim test in wild-type but not CB1 receptor-deficient mice.{38334} It reduces fasting-induced food intake and body weight gain in mice when administered at a dose of 30 mg/kg. AM251 also induces GTPγS binding in HEK293 cells expressing the orphan receptor GPR55 (EC50 = 39 nM) and potentiates GABA-induced GABAA receptor currents (EC50 = 0.4 µM).{17583,38332} It prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT), inhibits SMAD2/3 and p38 MAPK activation, and reduces the expression of EMT-related transcription factors in HK-2 renal tubule epithelial cells.{38335} AM251 induces cell cycle arrest at the G2/M phase and apoptosis in A375 human melanoma cells.{38333}  

 

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Description

A CB1 receptor antagonist; binds to CB1 receptors in rat forebrain membrane preparations (Ki = 7.5 nM); selective over CB2 receptors (Ki = 2,290 nM for mouse spleen membrane preparations); inhibits CP 55,940-induced GTPγS binding in HEK293 cells expressing human CB1 receptors (EC50 = 8 nM); decreases immobility time in the forced swim test in wild-type but not CB1 receptor-deficient mice at 10 mg/kg; reduces fasting-induced food intake and body weight gain in mice at 30 mg/kg; induces GTPγS binding in HEK293 cells expressing the orphan receptor GPR55 (EC50 = 39 nM); potentiates GABA-induced GABAA receptor currents (EC50 = 0.4 µM); prevents TGF-β1-induced EMT, inhibits SMAD2/3 and p38 MAPK activation, and reduces the expression of EMT-related transcription factors in HK-2 renal tubule epithelial cells; induces cell cycle arrest at the G2/M phase and apoptosis in A375 human melanoma cells

Formal name: 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide

Synonyms: 

Molecular weight: 555.2

CAS: 183232-66-8

Purity: ≥98%

Formulation: A crystalline solid

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