Catalog Number: 1120
Chemical Name: 6-Iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl)methanone
Biological Activity
CB2 antagonist/inverse agonist (Ki = 31.2 nM) that displays 165-fold selectivity over CB1 receptors. Behaves as a weak partial/inverse agonist at CB1 receptors.
Technical Data
  • M.Wt:
    504.37
  • Formula:
    C23H25IN2O3
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    164178-33-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630.
    Ross et al.
    Br.J.Pharmacol., 1999;126:665
  2. AM630 antagonism of cannabinoid-stimulated [35S]GTPγS binding in the mouse brain.
    Hosohata et al.
    Eur.J.Pharmacol., 1997;321:R1
  3. AM630 is a competitive cannabinoid receptor antagonist in the guinea pig brain.
    Hosohata et al.
    Life Sci., 1997;61:PL115
  4. AM630 is an inverse agonist at the human cannabinoid CB1 receptor.
    Landsman et al.
    Life Sci., 1998;62:PL109
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AM 630 include:

68 Citations: Showing 1 - 10
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  1. Expression and function of cannabinoid receptors CB1 and CB2 and their cognate cannabinoid ligands in murine embryonic stem cells.
    Authors: Jiang Et al.
    PLoS One ;2:e641
  2. 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
  3. Cannabinoid receptor subtype 2 (CB2R) agonist, GW405833 reduces agonist-induced Ca2+ oscillations in mouse pancreatic acinar cells
    Authors: Huang Et al.
    Scientific Reports 2016;6:29757
  4. CB2 Cannabinoid Receptor Knockout in Mice Impairs Contextual Long-Term Memory and Enhances Spatial Working Memory.
    Authors: Li and Kim
    Mol Pharmacol 2016;2016:9817089
  5. Correlations between the Memory-Related Behavior and the Level of Oxidative Stress Biomarkers in the Mice Brain, Provoked by an Acute Administration of CB Receptor Ligands.
    Authors: Kruk-Slomka Et al.
    Neural Plast 2016;2016:9815092
  6. The endocannabinoid anandamide impairs in vitro decidualization of human cells.
    Authors: Almada Et al.
    Reproduction 2016;152:351
  7. Cannabinoid 2 receptor is a novel anti-inflammatory target in experimental proliferative vitreoretinopathy
    Authors: Szczesniak Et al.
    Neuropharmacology 2016;
  8. CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion.
    Authors: Zhang Et al.
    Mediators Inflamm 2015;8:3491
  9. Differential immune mechanism to HIV-1 Tat variants and its regulation by AEA [corrected].
    Authors: Krishnan and Chatterjee
    PLoS One 2015;5:9887
  10. Cannabinoid receptor CB2 is involved in tetrahydrocannabinol-induced anti-inflammation against lipopolysaccharide in MG-63 cells.
    Authors: Yang Et al.
    PLoS One 2015;2015:362126
  11. Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures.
    Authors: Malek Et al.
    Neural Plast 2015;2015:130639
  12. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
    Authors: Borrelli Et al.
    Sci Rep 2015;172:142
  13. Anti-Obesity Effect of the CB2 Receptor Agonist JWH-015 in Diet-Induced Obese Mice.
    Authors: Verty Et al.
    PLoS One 2015;10:e0140592
  14. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    Neural Plast 2015;10:e0136546
  15. Cannabinoid CB2 Receptors in a Mouse Model of Aβ Amyloidosis: Immunohistochemical Analysis and Suitability as a PET Biomarker of Neuroinflammation.
    Authors: Savonenko Et al.
    PLoS One 2015;10:e0129618
  16. High-fat diet-induced insulin resistance does not increase plasma anandamide levels or potentiate anandamide insulinotropic effect in isolated canine islets.
    Authors: Woolcott Et al.
    Br J Pharmacol 2015;10:e0123558
  17. Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
    Authors: Stanley Et al.
    Sleep 2015;107:568
  18. Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
    Authors: Alpár Et al.
    Pharmacol Res 2014;5:4421
  19. Experimental cannabinoid 2 receptor-mediated immune modulation in sepsis.
    Authors: Sardinha Et al.
    Pain 2014;2014:978678
  20. Treatment with a cannabinoid receptor 2 agonist decreases severity of established cystitis.
    Authors: Wang Et al.
    Br J Pharmacol 2014;191:1153
  21. Anti-inflammatory effects of cannabinoid CB(2) receptor activation in endotoxin-induced uveitis.
    Authors: Toguri Et al.
    PLoS One 2014;171:1448
  22. Monoacylglycerol lipase (MAGL) inhibition attenuates acute lung injury in mice.
    Authors: Costola-de-Souza Et al.
    PLoS One 2013;8:e77706
  23. Deriving dopaminergic neurons for clinical use. A practical approach.
    Authors: Gonzalez Et al.
    Sci Rep 2013;3:1463
  24. 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
  25. Activation of cannabinoid receptor 2 inhibits experimental cystitis.
    Authors: Wang Et al.
    Br J Pharmacol 2013;304:R846
  26. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors.
    Authors: Marini Et al.
    Br J Pharmacol 2013;169:887
  27. The cannabinoid WIN 55,212-2 decreases specificity protein transcription factors and the oncogenic cap protein eIF4E in colon cancer cells.
    Authors: Sreevalsan and Safe
    Mol Cancer Ther 2013;12:2483
  28. Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection.
    Authors: Guida Et al.
    Mol Pain 2012;8:60
  29. 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
  30. Tricyclic Pyrazoles. Part 5. Novel 1,4-Dihydroindeno[1,2-c]pyrazole CB2 Ligands Using Molecular Hybridization Based on Scaffold Hopping.
    Authors: Murineddu Et al.
    Open Med Chem J 2012;6:1
  31. Repeated morphine treatment-mediated hyperalgesia, allodynia and spinal glial activation are blocked by co-administration of a selective cannabinoid receptor type-2 agonist.
    Authors: Tumati Et al.
    J Neuroimmunol 2012;244:23
  32. A dysregulated endocannabinoid-eicosanoid network supports pathogenesis in a mouse model of Alzheimer's disease.
    Authors: Piro Et al.
    Eur J Pharmacol 2012;1:617
  33. Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABA(A) receptors.
    Authors: García-Gutiérrez Et al.
    Br J Pharmacol 2012;165:951
  34. AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor.
    Authors: Bolognini Et al.
    Br J Pharmacol 2012;165:2561
  35. Effects of gonadal hormones on the peripheral cannabinoid receptor 1 (CB1R) system under a myositis condition in rats.
    Authors: Niu Et al.
    Br J Pharmacol 2012;153:2283
  36. Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer.
    Authors: Liu Et al.
    Mol Cancer Ther 2012;11:1421
  37. Increasing 2-arachidonoyl glycerol signaling in the periphery attenuates mechanical hyperalgesia in a model of bone cancer pain.
    Authors: Khasabova Et al.
    FASEB J 2011;64:60
  38. Protective role of cannabinoid receptor type 2 in a mouse model of diabetic nephropathy.
    Authors: Barutta Et al.
    Diabetes 2011;60:2386
  39. Perinatal exposure to δ9-tetrahydrocannabinol triggers profound defects in T cell differentiation and function in fetal and postnatal stages of life, including decreased responsiveness to HIV antigens.
    Authors: Lombard Et al.
    J Pharmacol Exp Ther 2011;339:607
  40. β-Caryophyllene inhibits dextran sulfate sodium-induced colitis in mice through CB2 receptor activation and PPARγ pathway.
    Authors: Bento Et al.
    Am J Pathol 2011;178:1153
  41. 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
  42. The cannabinoid WIN55,212-2 protects against oxidized LDL-induced inflammatory response in murine macrophages.
    Authors: Hao Et al.
    J Leukoc Biol 2010;51:2181
  43. A putative 'pre-nervous' endocannabinoid system in early echinoderm development.
    Authors: Buznikov Et al.
    Neurobiol Dis 2010;32:43101
  44. Cannabinoid receptor-dependent and -independent anti-proliferative effects of omega-3 ethanolamides in androgen receptor-positive and -negative prostate cancer cell lines.
    Authors: Brown Et al.
    Carcinogenesis 2010;31:1584
  45. Interaction between anandamide and sphingosine-1-phosphate in mediating vasorelaxation in rat coronary artery.
    Authors: Mair Et al.
    Br J Pharmacol 2010;161:176
  46. Endocannabinoid involvement in endometriosis.
    Authors: Dmitrieva Et al.
    Pain 2010;151:703
  47. CB1 and CB2 cannabinoid receptors differentially regulate the production of reactive oxygen species by macrophages.
    Authors: Han Et al.
    Cardiovasc Res 2009;84:378
  48. Cannabinoid CB2 receptor potentiates obesity-associated inflammation, insulin resistance and hepatic steatosis.
    Authors: Deveaux Et al.
    Am J Physiol Regul Integr Comp Physiol 2009;4:e5844
  49. The neuroprotective impact of the leak potassium channel TASK1 on stroke development in mice.
    Authors: Meuth Et al.
    Am J Physiol Heart Circ Physiol 2009;33:42675
  50. The cannabinoid receptor type 2 promotes cardiac myocyte and fibroblast survival and protects against ischemia/reperfusion-induced cardiomyopathy.
    Authors: Defer Et al.
    PLoS One 2009;23:2120
  51. Endogenous cannabinoids induce fever through the activation of CB1 receptors.
    Authors: Fraga Et al.
    Mediators Inflamm 2009;157:1494
  52. Analysis of promoter regions regulating basal and interleukin-4-inducible expression of the human CB1 receptor gene in T lymphocytes.
    Authors: Börner Et al.
    Br J Pharmacol 2008;73:1013
  53. Modulation of the anti-nociceptive effects of 2-arachidonoyl glycerol by peripherally administered FAAH and MGL inhibitors in a neuropathic pain model.
    Authors: Desroches Et al.
    J Lipid Res 2008;155:913
  54. CB2 cannabinoid receptor agonists attenuate TNF-alpha-induced human vascular smooth muscle cell proliferation and migration.
    Authors: Rajesh Et al.
    Br J Pharmacol 2008;153:347
  55. The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms.
    Authors: Potenzieri Et al.
    Brain Res 2008;1215:69
  56. Cannabinoid-2 receptor agonist HU-308 protects against hepatic ischemia/reperfusion injury by attenuating oxidative stress, inflammatory response, and apoptosis.
    Authors: Rajesh Et al.
    Cardiovasc Res 2007;82:1382
  57. The differential contractile responses to capsaicin and anandamide in muscle strips isolated from the rat urinary bladder.
    Authors: Saitoh Et al.
    J Cell Biol 2007;570:182
  58. Pharmacological inhibition of CB1 cannabinoid receptor protects against doxorubicin-induced cardiotoxicity.
    Authors: Mukhopadhyay Et al.
    J Am Coll Cardiol 2007;50:528
  59. 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 Clin Exp Pathol 2007;293:H909
  60. 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
  61. 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
  62. Role of the nitric oxide pathway and the endocannabinoid system in neurogenic relaxation of corpus cavernosum from biliary cirrhotic rats.
    Authors: Ghasemi Et al.
    Br J Pharmacol 2007;151:591
  63. Cannabinoid receptor type 2 agonists induce transcription of the mu-opioid receptor gene in Jurkat T cells.
    Authors: Börner Et al.
    Cell Rep 2006;69:1486
  64. Anandamide mediates hyperdynamic circulation in cirrhotic rats via CB(1) and VR(1) receptors.
    Authors: Moezi Et al.
    Dev Neurosci 2006;149:898
  65. Role of endocannabinoids in the pathogenesis of cirrhotic cardiomyopathy in bile duct-ligated rats.
    Authors: Gaskari Et al.
    Nat Commun 2005;146:315
  66. Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons.
    Authors: Price Et al.
    Br J Pharmacol 2004;142:257
  67. Effects of cannabinoid receptor-2 activation on accelerated gastrointestinal transit in lipopolysaccharide-treated rats.
    Authors: Mathison Et al.
    Br J Pharmacol 2004;142:1247
  68. The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response.
    Authors: Williams Et al.
    J Urol 2003;160:481
Expand to show all 68 Citations

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