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Submit ReviewSR 144528 is a high affinity and selective CB2 inverse agonist (Ki = 0.6 nM). Exhibits >700-fold selectivity for CB2 over CB1 receptors. Blocks the effects of CP 55,940 (Cat. No. 0949) on forskolin-sensitive adenylyl cyclase activity and MAPK in CHO cells expressing CB2 receptors. Also blocks CP 55,940-induced B-cell activation. Orally bioavailable.
分子量 | 476.05 |
公式 | C29H34ClN3O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 192703-06-3 |
PubChem ID | 3081355 |
InChI Key | SUGVYNSRNKFXQM-XRHWURSXSA-N |
Smiles | C[C@]1(C2)[C@H](NC(C3=NN(CC4=CC=C(C)C=C4)C(C5=CC=C(Cl)C(C)=C5)=C3)=O)C(C)(C)[C@@H]2CC1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Rinaldi-Carmona et al (1998) SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J.Pharmacol.Exp.Ther. 284 644 PMID: 9454810
Kotsikorou et al (2013) The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimeth J.Med.Chem. 56 6593 PMID: 23855811
Bouaboula et al (1999) Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation. Mol.Pharmacol. 55 473 PMID: 10051530
关键词: SR 144528, SR 144528 supplier, SR144528, high, affinity, selective, cannabinoid, receptors, CB2, inverse, agonists, orally, bioavailable, immunology, Receptors, 5039, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SR 144528 的部分引用包括:
Shang et al (2016) Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors Biochemical Pharmacology PMID: 27641813
Cecconi et al (2019) Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation. Int J Mol Sci 20 PMID: 31212770
Alharris et al (2019) Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget 10 45 PMID: 30713602
Capozzi et al (2021) Anti-Inflammatory Activity of a CB2 Selective Cannabinoid Receptor Agonist: Signaling and Cytokines Release in Blood Mononuclear Cells. Molecules 27 64 PMID: 35011295
Fu (2017) Activation of cannabinoid receptor type 2 by JWH133 alleviates bleomycin-induced pulmonary fibrosis in mice. Oncotarget 8 103486 PMID: 29262578
Mitzi et al (2021) Cannabinoid Receptor Activation on Haematopoietic Cells and Enterocytes Protects against Colitis. J Crohns Colitis 15 1032-1048 PMID: 33331878
Acevedo-Canabal et al (2019) Altered Swimming Behaviors in Zebrafish Larvae Lacking Cannabinoid Receptor 2. Cannabis Cannabinoid Res 4 88 PMID: 31236475
Woong-Ki et al (2022) Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation. Respir Res 23 326 PMID: 36463179
Neta et al (2010) Cannabinoids Delta(9)-tetrahydrocannabinol and cannabidiol differentially inhibit the lipopolysaccharide-activated NF-kappaB and interferon-beta/STAT proinflammatory pathways in BV-2 microglial cells. J Biol Chem 285 1616-26 PMID: 19910459
Presley et al (2015) Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist. J Neurosci 3 e00159 PMID: 26196013
Manuela et al (2020) Positive Allosteric Modulation of CB1 and CB2 Cannabinoid Receptors Enhances the Neuroprotective Activity of a Dual CB1R/CB2R Orthosteric Agonist. Life (Basel) 10 PMID: 33302569
Miriam et al (2020) 2-arachidonoylglycerol reduces chondroitin sulphate proteoglycan production by astrocytes and enhances oligodendrocyte differentiation under inhibitory conditions. Glia 68 1255-1273 PMID: 31894889
Mohammed et al (2020) Administration of Δ9-Tetrahydrocannabinol (THC) Post-Staphylococcal Enterotoxin B Exposure Protects Mice From Acute Respiratory Distress Syndrome and Toxicity. Front Pharmacol 11 PMID: 32612530
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