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 / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

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:

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.

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

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.

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.

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.

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.

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.

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

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.

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.

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.

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.

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.

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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Keywords: AM 630, supplier, CB2, selective, antagonists, inverse, agonists, Cannabinoids, Receptors, AM630, cb2r, Tocris Bioscience, CB2 Receptor Antagonist products

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