AM251

AM251 is a compound that, like the closely related AM2201, acts as a selective antagonist at the cannabinoid receptor CB1. AM251 is structurally very close to SR141716A (rimonabant), which is also a CB1 antagonist. AM251 has been used in research to explore the role of the CB1 receptor in the regulation of food intake, memory and anxiety, and in the potential treatment of obesity and drug addiction.

Chemistry

AM251 is a derivative of 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide. It is a member of the 1H-pyrazole class of drugs and is structurally related to the cannabinoid antagonist SR141716A.

Pharmacology

AM251 acts as a selective antagonist at the cannabinoid receptor CB1. It has a Ki value of 7.49nM at this receptor, and over 400 times selectivity over the related CB2 receptor. AM251 is an inverse agonist at the CB1 receptor, meaning it produces the opposite effect to the typical agonist of this receptor, THC.

Research

AM251 has been used in research to explore the role of the CB1 receptor in various physiological processes. Studies have shown that AM251 can reduce food intake in animals, suggesting a role for the CB1 receptor in the regulation of appetite. Other studies have shown that AM251 can improve memory in animal models, suggesting a role for the CB1 receptor in cognitive function. AM251 has also been used in research into the potential treatment of obesity and drug addiction.

See also

• Cannabinoid receptor antagonist
• AM2201
• SR141716A