AM 281

Discontinued Product

1115 has been discontinued.
View all Cannabinoid R1 / CB1 Inverse Agonists products.
AM 281 | CAS No. 202463-68-1 | Cannabinoid R1 / CB1 Inverse Agonists
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Description: Potent and selective CB1 inverse agonist

Chemical Name: 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide

Purity: ≥99%

Product Details
Citations (40)

Biological Activity

AM 281 is a potent, selective CB1 cannabinoid receptor antagonist/inverse agonist (Ki values are 12 and 4200 nM for CB1 and CB2 receptors respectively). Increases locomotor activity following systemic administration in vivo. Analog of SR141716A (Ki = 14 nM).

Technical Data

Soluble to 75 mM in DMSO with gentle warming
Desiccate at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of the University of Connecticut

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Citations for AM 281

The citations listed below are publications that use Tocris products. Selected citations for AM 281 include:

40 Citations: Showing 1 - 10

  1. On the influence of cannabinoids on cell morphology and motility of glioblastoma cells.
    Authors: Hohmann Et al.
    PLoS One  2019;14:e0212037
  2. Synthetic Cannabinoids Influence the Invasion of Glioblastoma Cell Lines in a Cell- and Receptor-Dependent Manner.
    Authors: Hohmann Et al.
    Cancers (Basel)  2019;11
  3. Coordination of ENT2-dependent adenosine transport and signaling dampens mucosal inflammation.
    Authors: Aherne Et al.
    JCI Insight  2018;3
  4. A novel crosstalk within the endocannabinoid system controls GABA transmission in the striatum.
    Authors: Musella
    Sci Rep  2017;7(1):7363
  5. The synthetic cannabinoid WIN-55,212-55,212 induced-apoptosis in cytotrophoblasts cells by a mechanism dependent on CB1 receptor.
    Authors: Almada
    Toxicology  2017;385:67
  6. Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
    Authors: Han
    Brain Res  2017;1663:132
  7. Cannabinoid receptor agonist WIN55,212-2 and fatty acid amide hydrolase inhibitor URB597 may protect against cognitive impairment in rats of chronic cerebral hypoperfusion via PI3K/AKT signaling
    Authors: Shao-Hua Su Et al.
    Behavioural Brain Research  2016;313:334
  8. Lack of Hypophagia in CB1 Null Mice is Associated to Decreased Hypothalamic POMC and CART Expression.
    Authors: Lage Et al.
    Mol Pharmacol  2015;18
  9. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    Int J Neuropsychopharmacol  2015;16:5555
  10. Selective inhibition of alpha/beta-hydrolase domain 6 attenuates neurodegeneration, alleviates blood brain barrier breakdown, and improves functional recovery in a mouse model of traumatic brain injury.
    Authors: Tchantchou and Zhang
    J Neurotrauma  2013;30:565
  11. The non-selective cannabinoid receptor agonist WIN 55,212-2 attenuates responses of C-fiber nociceptors in a murine model of cancer pain.
    Authors: Uhelski Et al.
    Neuroscience  2013;247:84
  12. Early endogenous activation of CB1 and CB2 receptors after spinal cord injury is a protective response involved in spontaneous recovery.
    Authors: Arévalo-Martín Et al.
    Mol Pharmacol  2012;7:e49057
  13. Increasing 2-arachidonoyl glycerol signaling in the periphery attenuates mechanical hyperalgesia in a model of bone cancer pain.
    Authors: Khasabova Et al.
    Cereb Cortex  2011;64:60
  14. Effects of drugs of abuse on putative rostromedial tegmental neurons, inhibitory afferents to midbrain DA cells.
    Authors: Lecca Et al.
    Neuropsychopharmacology  2011;36:589
  15. Evidence for a role of endocannabinoids, astrocytes and p38 phosphorylation in the resolution of postoperative pain.
    Authors: Alkaitis Et al.
    PLoS One  2010;5:e10891
  16. Cannabinoid CB1 receptor facilitation of substance P release in the rat spinal cord, measured as neurokinin 1 receptor internalization.
    Authors: Zhang Et al.
    Eur J Neurosci  2010;31:225
  17. Expression of cannabinoid CB1 receptors by vagal afferent neurons: kinetics and role in influencing neurochemical phenotype.
    Authors: Burdyga Et al.
    Am J Physiol Gastrointest Liver Physiol  2010;299:G63
  18. Cannabinoid-1 receptor activation induces reactive oxygen species-dependent and -independent mitogen-activated protein kinase activation and cell death in human coronary artery endothelial cells.
    Authors: Rajesh Et al.
    Front Pharmacol  2010;160:688
  19. GPR55 ligands promote receptor coupling to multiple signalling pathways.
    Authors: Henstridge Et al.
    Br J Pharmacol  2010;160:604
  20. Regulation of the hypothalamic-pituitary-adrenal axis circadian rhythm by endocannabinoids is sexually diergic.
    Authors: Atkinson Et al.
    Endocrinology  2010;151:3720
  21. Effects of cannabinoids on caffeine contractures in slow and fast skeletal muscle fibers of the frog.
    Authors: Huerta Et al.
    J Membr Biol  2009;229:91
  22. Analysis of promoter regions regulating basal and interleukin-4-inducible expression of the human CB1 receptor gene in T lymphocytes.
    Authors: Börner Et al.
    Pharmacol Res  2008;73:1013
  23. Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors.
    Authors: Melis Et al.
    J Neurosci  2008;28:13985
  24. Pharmacological inhibition of CB1 cannabinoid receptor protects against doxorubicin-induced cardiotoxicity.
    Authors: Mukhopadhyay Et al.
    J Am Coll Cardiol  2007;50:528
  25. N-arachidonoyl-DA tunes synaptic transmission onto DArgic neurons by activating both cannabinoid and vanilloid receptors.
    Authors: Marinelli Et al.
    Neuropsychopharmacology  2007;32:298
  26. Decreased age-related cardiac dysfunction, myocardial nitrative stress, inflammatory gene expression, and apoptosis in mice lacking fatty acid amide hydrolase.
    Authors: Bátkai Et al.
    Int J Mol Sci  2007;293:H909
  27. Cannabidiol attenuates high glucose-induced endothelial cell inflammatory response and barrier disruption.
    Authors: Rajesh Et al.
    Am J Physiol Heart Circ Physiol  2007;293:H610
  28. CB2-receptor stimulation attenuates TNF-alpha-induced human endothelial cell activation, transendothelial migration of monocytes, and monocyte-endothelial adhesion.
    Authors: Rajesh Et al.
    Am J Physiol Heart Circ Physiol  2007;293:H2210
  29. Tonic enhancement of endocannabinoid-mediated retrograde suppression of inhibition by cholinergic interneuron activity in the striatum.
    Authors: Narushima Et al.
    J Cell Biol  2007;27:496
  30. Presynaptic monoacylglycerol lipase activity determines basal endocannabinoid tone and terminates retrograde endocannabinoid signaling in the hippocampus.
    Authors: Hashimotodani Et al.
    J Neurosci  2007;27:1211
  31. Endocannabinoids mediate muscarine-induced synaptic depression at the vertebrate neuromuscular junction.
    Authors: Newman Et al.
    Eur J Neurosci  2007;25:1619
  32. Cannabinoid action in the olfactory epithelium.
    Authors: Czesnik Et al.
    Proc Natl Acad Sci U S A  2007;104:2967
  33. Cannabinoid receptor type 2 agonists induce transcription of the mu-opioid receptor gene in Jurkat T cells.
    Authors: Börner Et al.
    J Neurosci  2006;69:1486
  34. Anti-inflammatory potential of CB1-mediated cAMP elevation in mast cells.
    Authors: Small-Howard Et al.
    Biochem J  2005;388:465
  35. BDNF locally potentiates GABAergic presynaptic machineries: target-selective circuit inhibition.
    Authors: Ohba Et al.
    PLoS One  2005;15:291
  36. Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in DA neurons.
    Authors: Melis Et al.
    J Neurosci  2004;24:10707
  37. The cannabinomimetic arachidonyl-2-chloroethylamide (ACEA) acts on capsaicin-sensitive TRPV1 receptors but not cannabinoid receptors in rat joints.
    Authors: Baker
    Br J Pharmacol  2004;142:1361
  38. The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response.
    Authors: Williams Et al.
    Br J Pharmacol  2003;160:481
  39. Evidence of a novel site mediating anandamide-induced negative inotropic and coronary vasodilatator responses in rat isolated hearts.
    Authors: Ford Et al.
    Br J Pharmacol  2002;135:1191
  40. Cannabinoid receptor mediated inhibition of excitatory synaptic transmission in the rat hippocampal slice is developmentally regulated.
    Authors: Al-Hayani and Davies
    Br J Pharmacol  2000;131:663


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