AM 630

  ( 86 citations )    
Product Datasheet
Catalog Number:1120
Chemical Name:6-Iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl)methanone
Product Details
Citations (86)
Supplemental Products
Reviews
Biological Activity
CB2 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.
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Citations:

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

86 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. Abnormal cannabidiol attenuates experimental colitis in mice, promotes wound healing and inhibits neutrophil recruitment.
    Authors: Krohn Et al.
    J Inflamm (Lond)  2016;13:21
  8. Impaired Excitatory Neurotransmission in the Urinary Bladder from the Obese Zucker Rat: Role of Cannabinoid Receptors.
    Authors: Blaha Et al.
    PLoS One  2016;11:e0157424
  9. Cannabinoid 2 receptor is a novel anti-inflammatory target in experimental proliferative vitreoretinopathy
    Authors: Szczesniak Et al.
    Neuropharmacology  2016;
  10. CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion.
    Authors: Zhang Et al.
    Mediators Inflamm  2015;8:3491
  11. Differential immune mechanism to HIV-1 Tat variants and its regulation by AEA [corrected].
    Authors: Krishnan and Chatterjee
    PLoS One  2015;5:9887
  12. 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
  13. Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures.
    Authors: Malek Et al.
    Neural Plast  2015;2015:130639
  14. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
    Authors: Borrelli Et al.
    Sci Rep  2015;172:142
  15. Anti-Obesity Effect of the CB2 Receptor Agonist JWH-015 in Diet-Induced Obese Mice.
    Authors: Verty Et al.
    PLoS One  2015;10:e0140592
  16. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    Neural Plast  2015;10:e0136546
  17. 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
  18. 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
  19. Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
    Authors: Stanley Et al.
    Sleep  2015;107:568
  20. Permanent suppression of cortical oscillations in mice after adolescent exposure to cannabinoids: receptor mechanisms.
    Authors: Raver and Keller
    Neuropharmacology  2014;86:161
  21. Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
    Authors: Alpár Et al.
    Pharmacol Res  2014;5:4421
  22. Experimental cannabinoid 2 receptor-mediated immune modulation in sepsis.
    Authors: Sardinha Et al.
    Pain  2014;2014:978678
  23. Treatment with a cannabinoid receptor 2 agonist decreases severity of established cystitis.
    Authors: Wang Et al.
    Br J Pharmacol  2014;191:1153
  24. Peripheral interactions between cannabinoid and opioid systems contribute to the antinociceptive effect of crotalphine.
    Authors: Machado Et al.
    Br J Pharmacol  2014;171:961
  25. Effects of the endogenous cannabinoid anandamide on voltage-dependent sodium and calcium channels in rat ventricular myocytes.
    Authors: Kury Et al.
    Br J Pharmacol  2014;171:3485
  26. Anti-inflammatory effects of cannabinoid CB(2) receptor activation in endotoxin-induced uveitis.
    Authors: Toguri Et al.
    PLoS One  2014;171:1448
  27. 2-arachidonoylglycerol effects in cytotrophoblasts: metabolic enzymes expression and apoptosis in BeWo cells.
    Authors: Costa Et al.
    Reproduction  2014;147:301
  28. Monoacylglycerol lipase (MAGL) inhibition attenuates acute lung injury in mice.
    Authors: Costola-de-Souza Et al.
    PLoS One  2013;8:e77706
  29. Deriving dopaminergic neurons for clinical use. A practical approach.
    Authors: Gonzalez Et al.
    Sci Rep  2013;3:1463
  30. 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
  31. Activation of cannabinoid receptor 2 inhibits experimental cystitis.
    Authors: Wang Et al.
    Br J Pharmacol  2013;304:R846
  32. 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
  33. Inhibition of fatty acid amide hydrolase activates Nrf2 signalling and induces heme oxygenase 1 transcription in breast cancer cells.
    Authors: Li Et al.
    Br J Pharmacol  2013;170:489
  34. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors.
    Authors: Marini Et al.
    Br J Pharmacol  2013;169:887
  35. 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
  36. Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection.
    Authors: Guida Et al.
    Mol Pain  2012;8:60
  37. 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
  38. Regulation of MMP-9 by a WIN-binding site in the monocyte-macrophage system independent from cannabinoid receptors.
    Authors: Tauber Et al.
    PLoS One  2012;7:e48272
  39. 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
  40. 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
  41. 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
  42. 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
  43. Cannabinoid CB? receptor-mediated regulation of impulsive-like behaviour in DBA/2 mice.
    Authors: Navarrete Et al.
    Br J Pharmacol  2012;165:260
  44. AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor.
    Authors: Bolognini Et al.
    Br J Pharmacol  2012;165:2561
  45. Cannabinoid CB(2) receptors modulate ERK-1/2 kinase signalling and NO release in microglial cells stimulated with bacterial lipopolysaccharide.
    Authors: Merighi Et al.
    Br J Pharmacol  2012;165:1773
  46. Inhibiting fatty acid amide hydrolase normalizes endotoxin-induced enhanced gastrointestinal motility in mice.
    Authors: Bashashati Et al.
    Br J Pharmacol  2012;165:1556
  47. 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
  48. 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
  49. The antinociceptive effects of JWH-015 in chronic inflammatory pain are produced by nitric oxide-cGMP-PKG-KATP pathway activation mediated by opioids.
    Authors: Negrete Et al.
    PLoS One  2011;6:e26688
  50. 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
  51. Protective role of cannabinoid receptor type 2 in a mouse model of diabetic nephropathy.
    Authors: Barutta Et al.
    Diabetes  2011;60:2386
  52. 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
  53. 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
  54. THC Prevents MDMA Neurotoxicity in Mice.
    Authors: Touriño Et al.
    PLoS One  2010;5:e9143
  55. 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
  56. 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
  57. The role of nitric oxide in the local antiallodynic and antihyperalgesic effects and expression of delta-opioid and cannabinoid-2 receptors during neuropathic pain in mice.
    Authors: Hervera Et al.
    J Pharmacol Exp Ther  2010;334:887
  58. A putative 'pre-nervous' endocannabinoid system in early echinoderm development.
    Authors: Buznikov Et al.
    Neurobiol Dis  2010;32:43101
  59. 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
  60. Paradoxical effects of the cannabinoid CB2 receptor agonist GW405833 on rat osteoarthritic knee joint pain.
    Authors: Schuelert Et al.
    Osteoarthritis Cartilage  2010;18:1536
  61. Interaction between anandamide and sphingosine-1-phosphate in mediating vasorelaxation in rat coronary artery.
    Authors: Mair Et al.
    Br J Pharmacol  2010;161:176
  62. Endocannabinoid involvement in endometriosis.
    Authors: Dmitrieva Et al.
    Pain  2010;151:703
  63. CB1 and CB2 cannabinoid receptors differentially regulate the production of reactive oxygen species by macrophages.
    Authors: Han Et al.
    Cardiovasc Res  2009;84:378
  64. 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
  65. 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
  66. 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
  67. Central antinociception induced by mu-opioid receptor agonist morphine, but not delta- or kappa-, is mediated by cannabinoid CB1 receptor.
    Authors: Pacheco Et al.
    Br J Pharmacol  2009;158:225
  68. Endogenous cannabinoids induce fever through the activation of CB1 receptors.
    Authors: Fraga Et al.
    Mediators Inflamm  2009;157:1494
  69. 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
  70. 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
  71. 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
  72. The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms.
    Authors: Potenzieri Et al.
    Brain Res  2008;1215:69
  73. 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
  74. 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
  75. Pharmacological inhibition of CB1 cannabinoid receptor protects against doxorubicin-induced cardiotoxicity.
    Authors: Mukhopadhyay Et al.
    J Am Coll Cardiol  2007;50:528
  76. 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
  77. 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
  78. 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
  79. 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
  80. 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
  81. Anandamide mediates hyperdynamic circulation in cirrhotic rats via CB(1) and VR(1) receptors.
    Authors: Moezi Et al.
    Dev Neurosci  2006;149:898
  82. Role of endocannabinoids in the pathogenesis of cirrhotic cardiomyopathy in bile duct-ligated rats.
    Authors: Gaskari Et al.
    Nat Commun  2005;146:315
  83. 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
  84. Effects of cannabinoid receptor-2 activation on accelerated gastrointestinal transit in lipopolysaccharide-treated rats.
    Authors: Mathison Et al.
    Br J Pharmacol  2004;142:1247
  85. The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response.
    Authors: Williams Et al.
    J Urol  2003;160:481
  86. 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
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