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Products
Pharmacology
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AM 251
Cat. No. CB-010
Structure:
N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
Activity:
CB1 receptor inverse agonist
AM 251 is a potent CB1 receptor inverse agonist, with an IC50 of 8 nM at CB1 and 306-fold selectivity over CB2 receptors. AM 251 is also a GPR55 agonist with an EC50 of 39 nM and a μ-opioid receptor antagonist with a Ki of 251 nM. AM251 displays anorectic, antidepressant-like and analgesic effects in animals. AM251 can attenuate or reverse the nociceptive - hyperalgesia and allodynia - behaviours induced by burn injury.
Lan et al (1999) Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J Med Chem. 42(4) 769 PMID: 10052983
Shearman et al (2003) Antidepressant-like and anorectic effects of the cannabinoid CB1 receptor inverse agonist AM251 in mice. Behav Pharmacol. 4(8) 573 PMID: 14665974
Seely et al (2012) AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies. Neuropharmacology 63(5) 905 PMID: 22771770
Ueda et al (2014) Cannabinoid receptor type 1 antagonist, AM251, attenuates mechanical allodynia and thermal hyperalgesia after burn injury. Anesthesiology 21(6) 1311 PMID: 25188001
Related areas
All small molecules >
All cannabinoid receptor modulators >
All μ opioid receptor modulators >
All pain research categories >
All neuroscience research categories >
Technical Data
| Structure | N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide |
| CAS Number | 183232-66-8 |
| Molecular Weight | 555.24 |
| Formula | C22H21Cl2IN4O |
Solubility and Storage
| Solubility | Soluble in DMSO to 50 mg/ml or ethanol to 13 mg/ml |
| Appearance | Off-white solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | 98% by TLC , NMR conforms |
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