Home / Cannabinoid R2 / CB2 Inverse Agonists / AM 630

AM 630

Catalog #: 1120
100 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1120/10
1120/50
AM 630 | CAS No. 164178-33-0 | Cannabinoid R2 / CB2 Inverse Agonists
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Description: Selective CB2 inverse agonist

Chemical Name: 6-Iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl)methanone

Purity: ≥98%

Product Details
Citations (100)
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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

AM 630 is a CB 2 inverse agonist (K i = 31.2 nM) that displays 165-fold selectivity over CB 1 receptors. Behaves as a weak partial/inverse agonist at CB 1 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for AM 630

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

100 Citations: Showing 1 - 10

  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. Altered Swimming Behaviors in Zebrafish Larvae Lacking Cannabinoid Receptor 2.
    Authors: Acevedo-Canabal Et al.
    Cannabis Cannabinoid Res  2019;4:88
  3. On the influence of cannabinoids on cell morphology and motility of glioblastoma cells.
    Authors: Hohmann Et al.
    PLoS One  2019;14:e0212037
  4. Synthetic Cannabinoids Influence the Invasion of Glioblastoma Cell Lines in a Cell- and Receptor-Dependent Manner.
    Authors: Hohmann Et al.
    Cancers (Basel)  2019;11
  5. Ca2+ Signaling and IL-8 Secretion in Human Testicular Peritubular Cells Involve the Cation Channel TRPV2.
    Authors: Eubler Et al.
    Int J Mol Sci  2018;19
  6. Involvement of the CB2 cannabinoid receptor in cell growth inhibition and G0/G1 cell cycle arrest via the cannabinoid agonist WIN 55,212-2 in renal cell carcinoma.
    Authors: Khan Et al.
    BMC Cancer  2018;18:583
  7. The Endocannabinoid/Cannabinoid Receptor 2 System Protects Against Cisplatin-Induced Hearing Loss.
    Authors: Ghosh Et al.
    Front Cell Neurosci  2018;12:271
  8. 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
  9. Up-regulation of immunomodulatory effects of mouse bone-marrow derived mesenchymal stem cells by tetrahydrocannabinol pre-treatment involving cannabinoid receptor CB2.
    Authors: Xie Et al.
    Oncotarget  2016;7:6436
  10. 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
  11. 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
  12. 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
  13. The endocannabinoid anandamide impairs in vitro decidualization of human cells.
    Authors: Almada Et al.
    Reproduction  2016;152:351
  14. Abnormal cannabidiol attenuates experimental colitis in mice, promotes wound healing and inhibits neutrophil recruitment.
    Authors: Krohn Et al.
    J Inflamm (Lond)  2016;13:21
  15. 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
  16. Cannabinoid 2 receptor is a novel anti-inflammatory target in experimental proliferative vitreoretinopathy
    Authors: Szczesniak Et al.
    Neuropharmacology  2016;
  17. CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion.
    Authors: Zhang Et al.
    Mediators Inflamm  2015;8:3491
  18. Differential immune mechanism to HIV-1 Tat variants and its regulation by AEA [corrected].
    Authors: Krishnan and Chatterjee
    PLoS One  2015;5:9887
  19. 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
  20. Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures.
    Authors: Malek Et al.
    Neural Plast  2015;2015:130639
  21. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
    Authors: Borrelli Et al.
    Sci Rep  2015;172:142
  22. Anti-Obesity Effect of the CB2 Receptor Agonist JWH-015 in Diet-Induced Obese Mice.
    Authors: Verty Et al.
    PLoS One  2015;10:e0140592
  23. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    Neural Plast  2015;10:e0136546
  24. 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
  25. High-fat diet-induced Ins resistance does not increase plasma anandamide levels or potentiate anandamide Insotropic effect in isolated canine islets.
    Authors: Woolcott Et al.
    Br J Pharmacol  2015;10:e0123558
  26. Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
    Authors: Stanley Et al.
    Sleep  2015;107:568
  27. Permanent suppression of cortical oscillations in mice after adolescent exposure to cannabinoids: receptor mechanisms.
    Authors: Raver and Keller
    Neuropharmacology  2014;86:161
  28. Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
    Authors: Alpár Et al.
    Pharmacol Res  2014;5:4421
  29. Experimental cannabinoid 2 receptor-mediated immune modulation in sepsis.
    Authors: Sardinha Et al.
    Pain  2014;2014:978678
  30. Treatment with a cannabinoid receptor 2 agonist decreases severity of established cystitis.
    Authors: Wang Et al.
    Br J Pharmacol  2014;191:1153
  31. Peripheral interactions between cannabinoid and opioid systems contribute to the antinociceptive effect of crotalphine.
    Authors: Machado Et al.
    Br J Pharmacol  2014;171:961
  32. 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
  33. Anti-inflammatory effects of cannabinoid CB(2) receptor activation in endotoxin-induced uveitis.
    Authors: Toguri Et al.
    PLoS One  2014;171:1448
  34. 2-arachidonoylglycerol effects in cytotrophoblasts: metabolic enzymes expression and apoptosis in BeWo cells.
    Authors: Costa Et al.
    Reproduction  2014;147:301
  35. The cannabinoid receptor type 2 as mediator of mesenchymal stromal cell immunosuppressive properties.
    Authors: Rossi Et al.
    PLoS One  2013;8:e80022
  36. Monoacylglycerol lipase (MAGL) inhibition attenuates acute lung injury in mice.
    Authors: Costola-de-Souza Et al.
    PLoS One  2013;8:e77706
  37. Deriving DArgic neurons for clinical use. A practical approach.
    Authors: Gonzalez Et al.
    Sci Rep  2013;3:1463
  38. 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
  39. Activation of cannabinoid receptor 2 inhibits experimental cystitis.
    Authors: Wang Et al.
    Br J Pharmacol  2013;304:R846
  40. 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
  41. 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
  42. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors.
    Authors: Marini Et al.
    Br J Pharmacol  2013;169:887
  43. 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
  44. Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection.
    Authors: Guida Et al.
    Mol Pain  2012;8:60
  45. 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
  46. 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
  47. 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
  48. Repeated mor. 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
  49. 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
  50. Cannabinoid CB(2) receptor attenuates morphine-induced inflammatory responses in activated microglial cells.
    Authors: Merighi Et al.
    Br J Pharmacol  2012;166:2371
  51. 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
  52. Cannabinoid CB? receptor-mediated regulation of impulsive-like behaviour in DBA/2 mice.
    Authors: Navarrete Et al.
    Br J Pharmacol  2012;165:260
  53. AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor.
    Authors: Bolognini Et al.
    Br J Pharmacol  2012;165:2561
  54. 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
  55. Inhibiting fatty acid amide hydrolase normalizes endotoxin-induced enhanced gastrointestinal motility in mice.
    Authors: Bashashati Et al.
    Br J Pharmacol  2012;165:1556
  56. 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
  57. Spinal cannabinoid receptor type 2 agonist reduces mechanical allodynia and induces mitogen-activated protein kinase phosphatases in a rat model of neuropathic pain.
    Authors: Landry Et al.
    J Pain  2012;13:836
  58. 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
  59. 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
  60. 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
  61. Protective role of cannabinoid receptor type 2 in a mouse model of diabetic nephropathy.
    Authors: Barutta Et al.
    Diabetes  2011;60:2386
  62. 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
  63. 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
  64. THC Prevents MDMA Neurotoxicity in Mice.
    Authors: Touriño Et al.
    PLoS One  2010;5:e9143
  65. 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
  66. 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
  67. 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
  68. A putative 'pre-nervous' endocannabinoid system in early echinoderm development.
    Authors: Buznikov Et al.
    Neurobiol Dis  2010;32:43101
  69. 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
  70. Paradoxical effects of the cannabinoid CB2 receptor agonist GW405833 on rat osteoarthritic knee joint pain.
    Authors: Schuelert Et al.
    Osteoarthritis Cartilage  2010;18:1536
  71. Interaction between anandamide and sphingosine-1-phosphate in mediating vasorelaxation in rat coronary artery.
    Authors: Mair Et al.
    Br J Pharmacol  2010;161:176
  72. Endocannabinoid involvement in endometriosis.
    Authors: Dmitrieva Et al.
    Pain  2010;151:703
  73. CB1 and CB2 cannabinoid receptors differentially regulate the production of reactive oxygen species by macrophages.
    Authors: Han Et al.
    Cardiovasc Res  2009;84:378
  74. Cannabinoid CB2 receptor potentiates obesity-associated inflammation, Ins resistance and hepatic steatosis.
    Authors: Deveaux Et al.
    Am J Physiol Regul Integr Comp Physiol  2009;4:e5844
  75. 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
  76. 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
  77. 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
  78. Endogenous cannabinoids induce fever through the activation of CB1 receptors.
    Authors: Fraga Et al.
    Mediators Inflamm  2009;157:1494
  79. 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
  80. 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
  81. The mu-opioid receptor agonist morphine, but not agonists at delta- or kappa-opioid receptors, induces peripheral antinociception mediated by cannabinoid receptors.
    Authors: Pacheco Et al.
    Br J Pharmacol  2008;154:1143
  82. 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
  83. The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms.
    Authors: Potenzieri Et al.
    Brain Res  2008;1215:69
  84. 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
  85. 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
  86. Pharmacological inhibition of CB1 cannabinoid receptor protects against doxorubicin-induced cardiotoxicity.
    Authors: Mukhopadhyay Et al.
    J Am Coll Cardiol  2007;50:528
  87. Cannabinoid (CB1) receptor activation inhibits trigeminovascular neurons.
    Authors: Akerman Et al.
    J Pharmacol Exp Ther  2007;320:64
  88. 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
  89. 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
  90. 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
  91. Antinociceptive effect of cannabinoid agonist WIN 55,212-2 in rats with a spinal cord injury.
    Authors: Hama
    Exp Neurol  2007;204:454
  92. 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
  93. 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
  94. Anandamide mediates hyperdynamic circulation in cirrhotic rats via CB(1) and VR(1) receptors.
    Authors: Moezi Et al.
    Dev Neurosci  2006;149:898
  95. Role of endocannabinoids in the pathogenesis of cirrhotic cardiomyopathy in bile duct-ligated rats.
    Authors: Gaskari Et al.
    Nat Commun  2005;146:315
  96. 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
  97. 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
  98. Effects of cannabinoid receptor-2 activation on accelerated gastrointestinal transit in lipopolysaccharide-treated rats.
    Authors: Mathison Et al.
    Br J Pharmacol  2004;142:1247
  99. The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response.
    Authors: Williams Et al.
    J Urol  2003;160:481
  100. 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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