Date published: 2025-11-24

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AM 281 (CAS 202463-68-1)

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Alternate Names:
1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide
Application:
AM 281 is a potent CB1 receptor antagonist/inverse agonist
CAS Number:
202463-68-1
Purity:
≥98% (HPLC)
Molecular Weight:
557.21
Molecular Formula:
C21H19Cl2IN4O2
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
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 281 is an inverse agonist for the cannabinoid receptor CB1, used in research to study the endocannabinoid system and its role in regulating various physiological processes. In neuroscience research, AM 281 has been utilized to investigate the modulation of appetite, memory, and pain sensation, as it helps in understanding how CB1 receptor antagonism affects these functions. Additionally, AM 281 is instrumental in exploring the mechanisms of cannabinoid receptor desensitization and down-regulation, providing insights into how prolonged exposure to cannabinoids can alter receptor function. In metabolic studies, researchers employ AM 281 to examine the impact of CB1 receptor activity on energy balance and glucose metabolism. The compound has also been used in the development of imaging agents for the purpose of visualizing the distribution of CB1 receptors in the brain using positron emission tomography (PET) scans.


AM 281 (CAS 202463-68-1) References

  1. Effects of the cannabinoid antagonists AM281 and AM630 on deprivation-induced intake in Lewis rats.  |  Werner, NA. and Koch, JE. 2003. Brain Res. 967: 290-2. PMID: 12650991
  2. Inverse agonism and neutral antagonism at cannabinoid CB1 receptors.  |  Pertwee, RG. 2005. Life Sci. 76: 1307-24. PMID: 15670612
  3. Effects of AM281, a cannabinoid antagonist, on systemic haemodynamics, internal carotid artery blood flow and mortality in septic shock in rats.  |  Kadoi, Y., et al. 2005. Br J Anaesth. 94: 563-8. PMID: 15734782
  4. Cannabinoid antagonist AM 281 reduces mortality rate and neurologic dysfunction after cecal ligation and puncture in rats.  |  Kadoi, Y., et al. 2005. Crit Care Med. 33: 2629-36. PMID: 16276190
  5. Effects of cannabinoids on the anxiety-like response in mice.  |  Rutkowska, M., et al. 2006. Pharmacol Rep. 58: 200-6. PMID: 16702621
  6. Cannabinoids alter spontaneous firing, bursting, and cell synchrony of hippocampal principal cells.  |  Goonawardena, AV., et al. 2011. Hippocampus. 21: 520-31. PMID: 20101600
  7. 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
  8. Analgesic effect of a mixed T-type channel inhibitor/CB2 receptor agonist.  |  Gadotti, VM., et al. 2013. Mol Pain. 9: 32. PMID: 23815854
  9. The endocannabinoid system and associative learning and memory in zebrafish.  |  Ruhl, T., et al. 2015. Behav Brain Res. 290: 61-9. PMID: 25956869
  10. Quetiapine induces myocardial necroptotic cell death through bidirectional regulation of cannabinoid receptors.  |  Li, X., et al. 2019. Toxicol Lett. 313: 77-90. PMID: 31220554
  11. Imaging the brain marijuana receptor: development of a radioligand that binds to cannabinoid CB1 receptors in vivo.  |  Gatley, SJ., et al. 1998. J Neurochem. 70: 417-23. PMID: 9422389
  12. Effect of the cannabinoid receptor SPECT agent, AM 281, on hippocampal acetylcholine release from rat brain slices.  |  Gifford, AN., et al. 1997. Neurosci Lett. 238: 84-6. PMID: 9464661
  13. Large receptor reserve for cannabinoid actions in the central nervous system.  |  Gifford, AN., et al. 1999. J Pharmacol Exp Ther. 288: 478-83. PMID: 9918548

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AM 281, 1 mg

sc-202050
1 mg
$31.00

AM 281, 5 mg

sc-202050A
5 mg
$82.00