AM-251

BML-CR108

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Cannabinoid receptor ligand

Cannabinoid CB₁ receptor antagonist (K_i=7.5 nM). Displays a high level of selectivity (306-fold) for CB₁ over CB₂ receptors. Structurally related to the cannabinoid receptor (CB) antagonist SR 141716A.

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Product Details

Appearance	White to Off White
CAS	183232-66-8
Couple Target	Cannabinoid receptor
Couple Type	Ligand
Formula	C₂₂H₂₁Cl₂IN₄O
Identity	Determined by 1H-NMR.
MW	555.2
Purity	≥98% (HPLC)
Solubility	Soluble in DMSO, 100% ethanol or dimethyl formamide.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store, as supplied, at room temperature for up to 1 year. Store solutions at -20°C for up to 3 months.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Glucose concentration in culture medium affects mRNA expression of TRPV1 and CB1 receptors and changes capsaicin toxicity in PC12 cells: Mohammadi-Farani, A., Ghazi-Khansari, M., et al.; Iran J. Basic. Med. Sci. 17, 673 (2014), Abstract
Endogenous anandamide and cannabinoid receptor-2 contribute to electroacupuncture analgesia in rats: Chen, L., Zhang, J., et al.; J. Pain 10, 732 (2009), Abstract
AM 251 produces sustained reductions in food intake and body weight that are resistant to tolerance and conditioned taste aversion: A.P. Chambers et al.; Br. J. Pharmacol. 147, 109 (2006), Abstract
The cannabinoid CB1 antagonist AM 251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats: P.J. McLaughlin et al.; Psychopharmacology (Berl) 180, 286 (2005), Abstract
The cannabinoid 1 receptor antagonist, AM251, prolongs the survival of rats with severe acute pancreatitis: K. Matsuda et al.; Tohoku. J. Exp. Med. 207, 99 (2005), Abstract
Anxiogenic profile of AM-251, a selective cannabinoid CB1 receptor antagonist, in plus-maze-naive and plus-maze-experienced mice: R.J. Rodgers et al.; Behav. Pharmacol. 16, 405 (2005), Abstract
Inhibition of voltage-sensitive sodium channels by the cannabinoid 1 receptor antagonist AM 251 in mammalian brain: C. Liao et al.; Basic Clin. Pharmacol. Toxicol. 94, 73 (2004), Abstract
Cannabinoid (CB)1 receptor antagonist, AM 251, causes a sustained reduction of daily food intake in the rat: A.P. Chambers et al.; Physiol. Behav. 82, 863 (2004), Abstract
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists: R. Lan et al.; J. Med. Chem. 42, 769 (1999), Abstract
Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors: S. J. Gatley et al.; Life. Sci. 61, PL 191-7 (1997), Abstract

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AM-251

BML-CR108

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