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AM251 | Cannabinoid CB1 antagonist

AM251 (183232-66-8) is a potent cannabinoid CB1 receptor antagonist with selectivity over CB2 receptors (306-fold).1-3 Displays anorectic effects and antidepressant-like effects in mice.4 Behaves as an agonist at GPR55, EC50=39nM.5 Active in vivo.


1) Gatley et al. (1996), 123I-labeled AM251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors; Eur. J. Pharmacol., 307 331
2) Gatley et al. (1997), Binding of the non-classical cannabinoid CP 55,940 and the diarylpyrazole AM251 to rodent brain cannabinoid receptors; Life Sci., 61 191
3) Pertwee et al. (2005), Inverse agonism and neutral antagonism at cannabinoid CB1 receptors; Life Sci., 76 1307
4) Shearman et al. (2003), Antidepressant-like and anorectic effects of the cannabinoid CB1 receptor inverse agonist AM251 in mice; behave. Pharmacol., 14 573
5) Ryberg et al. (2007), The orphan receptor GPR55 is a novel cannabinoid receptor; Br. J. Pharmacol., 152 1092

Focus Biomolecules cell signaling reagent supplier, chemical structure AM251 | Cannabinoid CB1 antagonist | CAS 183232-66-8

Catalog#  10-2007-0010

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Catalog Number:
Cannabinoid CB1 receptor antagonist
Chemical Name:
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 13 mg/ml)
Physical Properties:
Off-white solid
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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