Description

AM-251 is an inverse agonist at the CB₁ cannabinoid receptor. AM-251 is structurally very close to rimonabant; 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 (with a K_i value of 7.5 nM) than rimonabant, which has a K_i value of 11.5 nM, AM-251 is, however, about two-fold more selective for the CB₁ receptor when compared to rimonabant.^[1] Like rimonabant, it is additionally a μ-opioid receptor antagonist contact us

AM251

• Molecular Formula C₂₂H₂₁Cl₂IN₄O
• Average mass 555.239 Da
• Monoisotopic mass 554.013672 Da
• ChemSpider ID 2040
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