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AM251

Explanation

AM251: AM-251 is an inverse agonist at the CB₁ cannabinoid receptor. AM-251 is structurally very close to SR141716A; both are biarylpyrazole cannabinoid receptor antagonists. In AM-251 the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group. The resulting compound exhibits slightly better binding affinity for the CB₁ receptor than SR141716A, which has a Kᵢ value of 11.5nM, AM-251 is, however, about two-fold more selective for the CB₁ receptor when compared to SR141716A.

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