AM 630

Cat. No. 1120

AM 630 C23H25IN2O3 [164178-33-0]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
Select another batch:

Ross et al (1999) Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. Br.J.Pharmacol. 126 665. PMID: 10188977.

Landsman et al (1998) AM630 is an inverse agonist at the human cannabinoid CB1 receptor. Life Sci. 62 PL109. PMID: 9496703.

Hosohata et al (1997) AM630 is a competitive cannabinoid receptor antagonist in the guinea pig brain. Life Sci. 61 PL115. PMID: 9284087.

Hosohata et al (1997) AM630 antagonism of cannabinoid-stimulated [35S]GTPγS binding in the mouse brain. Eur.J.Pharmacol. 321 R1. PMID: 9083796.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for AM 630 include:

Almada et al (2016) The endocannabinoid anandamide impairs in vitro decidualization of human cells. Reproduction 152 351. PMID: 27568210.

Huang et al (2016) Cannabinoid receptor subtype 2 (CB2R) agonist, GW405833 reduces agonist-induced Ca2+ oscillations in mouse pancreatic acinar cells Scientific Reports 6 29757. PMID: 27432473.

Kruk-Slomka et al (2016) 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. Neural Plast 2016 9815092. PMID: 26839719.

Li and Kim (2016) CB2 Cannabinoid Receptor Knockout in Mice Impairs Contextual Long-Term Memory and Enhances Spatial Working Memory. Mol Pharmacol 2016 9817089. PMID: 26819779.

Szczesniak et al (2016) Cannabinoid 2 receptor is a novel anti-inflammatory target in experimental proliferative vitreoretinopathy Neuropharmacology. PMID: 27569993.

Borrelli et al (2015) Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. Sci Rep 172 142. PMID: 25205418.

Krishnan and Chatterjee (2015) Differential immune mechanism to HIV-1 Tat variants and its regulation by AEA [corrected]. PLoS One 5 9887. PMID: 25943894.

Malek et al (2015) Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures. Neural Plast 2015 130639. PMID: 26090232.

Savonenko et al (2015) Cannabinoid CB2 Receptors in a Mouse Model of Aβ Amyloidosis: Immunohistochemical Analysis and Suitability as a PET Biomarker of Neuroinflammation. PLoS One 10 e0129618. PMID: 26086915.

Smith et al (2015) The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation. Neural Plast 10 e0136546. PMID: 26414859.

Stanley et al (2015) Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation. Sleep 107 568. PMID: 26092099.

Verty et al (2015) Anti-Obesity Effect of the CB2 Receptor Agonist JWH-015 in Diet-Induced Obese Mice. PLoS One 10 e0140592. PMID: 26588700.

Woolcott et al (2015) High-fat diet-induced insulin resistance does not increase plasma anandamide levels or potentiate anandamide insulinotropic effect in isolated canine islets. Br J Pharmacol 10 e0123558. PMID: 25855974.

Yang et al (2015) Cannabinoid receptor CB2 is involved in tetrahydrocannabinol-induced anti-inflammation against lipopolysaccharide in MG-63 cells. PLoS One 2015 362126. PMID: 25653478.

Zhang et al (2015) CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion. Mediators Inflamm 8 3491. PMID: 26097533.

Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. Pharmacol Res 5 4421. PMID: 25030704.

Sardinha et al (2014) Experimental cannabinoid 2 receptor-mediated immune modulation in sepsis. Pain 2014 978678. PMID: 24803745.

Toguri et al (2014) Anti-inflammatory effects of cannabinoid CB(2) receptor activation in endotoxin-induced uveitis. PLoS One 171 1448. PMID: 24308861.

Wang et al (2014) Treatment with a cannabinoid receptor 2 agonist decreases severity of established cystitis. Br J Pharmacol 191 1153. PMID: 24184363.

Costola-de-Souza et al (2013) Monoacylglycerol lipase (MAGL) inhibition attenuates acute lung injury in mice. PLoS One 8 e77706. PMID: 24204926.

Gonzalez et al (2013) Deriving dopaminergic neurons for clinical use. A practical approach. Sci Rep 3 1463. PMID: 23492920.

Marini et al (2013) Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol 169 887. PMID: 23711022.

Sreevalsan and Safe (2013) The cannabinoid WIN 55,212-2 decreases specificity protein transcription factors and the oncogenic cap protein eIF4E in colon cancer cells. Mol Cancer Ther 12 2483. PMID: 24030632.

Tchantchou and Zhang (2013) 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. J Neurotrauma 30 565. PMID: 23151067.

Wang et al (2013) Activation of cannabinoid receptor 2 inhibits experimental cystitis. Br J Pharmacol 304 R846. PMID: 23515618.

Arévalo-Martín et al (2012) Early endogenous activation of CB1 and CB2 receptors after spinal cord injury is a protective response involved in spontaneous recovery. Mol Pharmacol 7 e49057. PMID: 23152849.

Bolognini et al (2012) AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor. Br J Pharmacol 165 2561. PMID: 21615724.

García-Gutiérrez et al (2012) Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABA(A) receptors. Br J Pharmacol 165 951. PMID: 21838753.

Guida et al (2012) Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection. Mol Pain 8 60. PMID: 22913292.

Liu et al (2012) Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer. Mol Cancer Ther 11 1421. PMID: 22553354.

Murineddu et al (2012) Tricyclic Pyrazoles. Part 5. Novel 1,4-Dihydroindeno[1,2-c]pyrazole CB2 Ligands Using Molecular Hybridization Based on Scaffold Hopping. Open Med Chem J 6 1. PMID: 22876271.

Niu et al (2012) Effects of gonadal hormones on the peripheral cannabinoid receptor 1 (CB1R) system under a myositis condition in rats. Br J Pharmacol 153 2283. PMID: 22940464.

Piro et al (2012) A dysregulated endocannabinoid-eicosanoid network supports pathogenesis in a mouse model of Alzheimer's disease. Eur J Pharmacol 1 617. PMID: 22813736.

Tumati et al (2012) Repeated morphine treatment-mediated hyperalgesia, allodynia and spinal glial activation are blocked by co-administration of a selective cannabinoid receptor type-2 agonist. J Neuroimmunol 244 23. PMID: 22285397.

Barutta et al (2011) Protective role of cannabinoid receptor type 2 in a mouse model of diabetic nephropathy. Diabetes 60 2386. PMID: 21810593.

Bento et al (2011) β-Caryophyllene inhibits dextran sulfate sodium-induced colitis in mice through CB2 receptor activation and PPARγ pathway. Am J Pathol 178 1153. PMID: 21356367.

Khasabova et al (2011) Increasing 2-arachidonoyl glycerol signaling in the periphery attenuates mechanical hyperalgesia in a model of bone cancer pain. FASEB J 64 60. PMID: 21440630.

Lombard et al (2011) 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. J Pharmacol Exp Ther 339 607. PMID: 21831965.

Alkaitis et al (2010) Evidence for a role of endocannabinoids, astrocytes and p38 phosphorylation in the resolution of postoperative pain. PLoS One 5 e10891. PMID: 20531936.

Brown et al (2010) Cannabinoid receptor-dependent and -independent anti-proliferative effects of omega-3 ethanolamides in androgen receptor-positive and -negative prostate cancer cell lines. Carcinogenesis 31 1584. PMID: 20660502.

Buznikov et al (2010) A putative 'pre-nervous' endocannabinoid system in early echinoderm development. Neurobiol Dis 32 43101. PMID: 19907129.

Dmitrieva et al (2010) Endocannabinoid involvement in endometriosis. Pain 151 703. PMID: 20833475.

Hao et al (2010) The cannabinoid WIN55,212-2 protects against oxidized LDL-induced inflammatory response in murine macrophages. J Leukoc Biol 51 2181. PMID: 20305287.

Mair et al (2010) Interaction between anandamide and sphingosine-1-phosphate in mediating vasorelaxation in rat coronary artery. Br J Pharmacol 161 176. PMID: 20718749.

Defer et al (2009) The cannabinoid receptor type 2 promotes cardiac myocyte and fibroblast survival and protects against ischemia/reperfusion-induced cardiomyopathy. PLoS One 23 2120. PMID: 19246487.

Deveaux et al (2009) Cannabinoid CB2 receptor potentiates obesity-associated inflammation, insulin resistance and hepatic steatosis. Am J Physiol Regul Integr Comp Physiol 4 e5844. PMID: 19513120.

Fraga et al (2009) Endogenous cannabinoids induce fever through the activation of CB1 receptors. Mediators Inflamm 157 1494. PMID: 19681872.

Han et al (2009) CB1 and CB2 cannabinoid receptors differentially regulate the production of reactive oxygen species by macrophages. Cardiovasc Res 84 378. PMID: 19596672.

Meuth et al (2009) The neuroprotective impact of the leak potassium channel TASK1 on stroke development in mice. Am J Physiol Heart Circ Physiol 33 42675. PMID: 18930826.

Börner et al (2008) Analysis of promoter regions regulating basal and interleukin-4-inducible expression of the human CB1 receptor gene in T lymphocytes. Br J Pharmacol 73 1013. PMID: 18156315.

Desroches et al (2008) Modulation of the anti-nociceptive effects of 2-arachidonoyl glycerol by peripherally administered FAAH and MGL inhibitors in a neuropathic pain model. J Lipid Res 155 913. PMID: 18695638.

Potenzieri et al (2008) The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms. Brain Res 1215 69. PMID: 18486111.

Rajesh et al (2008) CB2 cannabinoid receptor agonists attenuate TNF-alpha-induced human vascular smooth muscle cell proliferation and migration. Br J Pharmacol 153 347. PMID: 17994109.

Bátkai et al (2007) Decreased age-related cardiac dysfunction, myocardial nitrative stress, inflammatory gene expression, and apoptosis in mice lacking fatty acid amide hydrolase. Int J Clin Exp Pathol 293 H909. PMID: 17434980.

Ghasemi et al (2007) Role of the nitric oxide pathway and the endocannabinoid system in neurogenic relaxation of corpus cavernosum from biliary cirrhotic rats. Br J Pharmacol 151 591. PMID: 17486141.

Mukhopadhyay et al (2007) Pharmacological inhibition of CB1 cannabinoid receptor protects against doxorubicin-induced cardiotoxicity. J Am Coll Cardiol 50 528. PMID: 17678736.

Rajesh et al (2007) Cannabidiol attenuates high glucose-induced endothelial cell inflammatory response and barrier disruption. Am J Physiol Heart Circ Physiol 293 H610. PMID: 17384130.

Rajesh et al (2007) CB2-receptor stimulation attenuates TNF-alpha-induced human endothelial cell activation, transendothelial migration of monocytes, and monocyte-endothelial adhesion. Am J Physiol Heart Circ Physiol 293 H2210. PMID: 17660390.

Rajesh et al (2007) Cannabinoid-2 receptor agonist HU-308 protects against hepatic ischemia/reperfusion injury by attenuating oxidative stress, inflammatory response, and apoptosis. Cardiovasc Res 82 1382. PMID: 17652447.

Saitoh et al (2007) The differential contractile responses to capsaicin and anandamide in muscle strips isolated from the rat urinary bladder. J Cell Biol 570 182. PMID: 17586490.

Börner et al (2006) Cannabinoid receptor type 2 agonists induce transcription of the mu-opioid receptor gene in Jurkat T cells. Cell Rep 69 1486. PMID: 16434616.

Moezi et al (2006) Anandamide mediates hyperdynamic circulation in cirrhotic rats via CB(1) and VR(1) receptors. Dev Neurosci 149 898. PMID: 17043671.

Gaskari et al (2005) Role of endocannabinoids in the pathogenesis of cirrhotic cardiomyopathy in bile duct-ligated rats. Nat Commun 146 315. PMID: 16025138.

Mathison et al (2004) Effects of cannabinoid receptor-2 activation on accelerated gastrointestinal transit in lipopolysaccharide-treated rats. Br J Pharmacol 142 1247. PMID: 15249429.

Price et al (2004) Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons. Br J Pharmacol 142 257. PMID: 15155534.

Williams et al (2003) The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response. J Urol 160 481. PMID: 12578907.

Jiang et al Expression and function of cannabinoid receptors CB1 and CB2 and their cognate cannabinoid ligands in murine embryonic stem cells. PLoS One 2 e641. PMID: 17653268.

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