Date published: 2025-10-19

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AM-251 (CAS 183232-66-8)

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Alternate Names:
AM-251 is known as a CB1 receptor antagonist.
Application:
AM-251 is an iodine-123 radiolabelled inverse agonist of the CB1 receptor, potentially able to reduce fasting-induced food intake and body weight gain in mice.
CAS Number:
183232-66-8
Purity:
≥98%
Molecular Weight:
555.24
Molecular Formula:
C22H21Cl2IN4O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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AM-251 is a compound known for its role as a selective antagonist of the CB1 cannabinoid receptor and is widely used in research to understand the endocannabinoid system. Its ability to bind to the CB1 receptor without activating it provides insight into the physiological processes influenced by cannabinoid receptors, such as appetite control, pain regulation, and mood. In neuroscientific research, AM-251 has been utilized to explore the effects of endocannabinoid signaling on cognitive functions and memory. Additionally, it has been instrumental in studies assessing the role of the endocannabinoid system in energy homeostasis and metabolic regulation.


AM-251 (CAS 183232-66-8) References

  1. Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.  |  Lan, R., et al. 1999. J Med Chem. 42: 769-76. PMID: 10052983
  2. Inhibition of methamphetamine self-administration in rats by cannabinoid receptor antagonist AM 251.  |  Vinklerová, J., et al. 2002. J Psychopharmacol. 16: 139-43. PMID: 12095072
  3. The cannabinoid CB1 antagonists SR 141716A and AM 251 suppress food intake and food-reinforced behavior in a variety of tasks in rats.  |  McLaughlin, PJ., et al. 2003. Behav Pharmacol. 14: 583-8. PMID: 14665975
  4. Cannabinoid (CB)1 receptor antagonist, AM 251, causes a sustained reduction of daily food intake in the rat.  |  Chambers, AP., et al. 2004. Physiol Behav. 82: 863-9. PMID: 15451651
  5. The cannabinoid CB1 antagonist AM 251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats.  |  McLaughlin, PJ., et al. 2005. Psychopharmacology (Berl). 180: 286-93. PMID: 15948012
  6. Anxiogenic profile of AM-251, a selective cannabinoid CB1 receptor antagonist, in plus-maze-naïve and plus-maze-experienced mice.  |  Rodgers, RJ., et al. 2005. Behav Pharmacol. 16: 405-13. PMID: 16148445
  7. AM 251 produces sustained reductions in food intake and body weight that are resistant to tolerance and conditioned taste aversion.  |  Chambers, AP., et al. 2006. Br J Pharmacol. 147: 109-16. PMID: 16258524
  8. The cannabinoid CB1 receptor inverse agonist AM 251 and antagonist AM 4113 produce similar effects on the behavioral satiety sequence in rats.  |  Hodge, J., et al. 2008. Behav Brain Res. 193: 298-305. PMID: 18602425
  9. The effects of intracerebroventricular AM-251, a CB1-receptor antagonist, and ACEA, a CB1-receptor agonist, on penicillin-induced epileptiform activity in rats.  |  Kozan, R., et al. 2009. Epilepsia. 50: 1760-7. PMID: 19453709
  10. Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action and unanswered questions.  |  Fong, TM. and Heymsfield, SB. 2009. Int J Obes (Lond). 33: 947-55. PMID: 19597516
  11. AM 251 differentially effects food-maintained responding depending on food palatability.  |  Droste, SM., et al. 2010. Pharmacol Biochem Behav. 95: 443-8. PMID: 20331999
  12. AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies.  |  Seely, KA., et al. 2012. Neuropharmacology. 63: 905-15. PMID: 22771770
  13. The effects of leptin in combination with a cannabinoid receptor 1 antagonist, AM 251, or cannabidiol on food intake and body weight in rats fed a high-fat or a free-choice high sugar diet.  |  Wierucka-Rybak, M., et al. 2014. J Physiol Pharmacol. 65: 487-96. PMID: 25179081
  14. Involvement of opioid system in antidepressant-like effect of the cannabinoid CB1 receptor inverse agonist AM-251 after physical stress in mice.  |  Ostadhadi, S., et al. 2016. Clin Exp Pharmacol Physiol. 43: 203-12. PMID: 26609670
  15. Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors.  |  Gatley, SJ., et al. 1997. Life Sci. 61: PL 191-7. PMID: 9335234

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AM-251, 5 mg

sc-200366A
5 mg
$71.00

AM-251, 10 mg

sc-200366
10 mg
$143.00

AM-251, 50 mg

sc-200366B
50 mg
$612.00

AM-251, 100 mg

sc-200366C
100 mg
$847.00