SR 144528 is a selective peripheral CB2 (cannabinoid) receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors. SR 144528 antagonizes the inhibitory effects of CP 55,940 on forskolin-induced adenylyl cyclase activity in CHO cells expressing hCB2. SR 144528 has also been used to investigate the contribution of the CB2 receptor in the control of pain initiation as well as suppression of inflammation and immune activation.
1 Rinaldi-Carmona, M., Barth, F., Millan, J., et al. SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J Pharmacol Exp Ther 284(2) 644-650 (1998). 2 Portier, M., Rinaldi-Carmona, M., Pecceu, F., et al. SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist. J Pharmacol Exp Ther 288(2) 582-589 (1999). 3 Barth, F., Rinaldi-Carmona, M. The development of cannabinoid antagonists. Current Medicinal Chemistry 6 745-755 (1999). 4 Di Marzo, V. Targeting the endocannabinoid system: To enhance or reduce?. Nature Reviews Drug Discovery 7 438-455 (2008). 5 Iwamura, H., Suzuki, H., Ueda, Y., et al. In vitro and in vivo pharmacological characterization of JTE-907, a novel selection ligand for cannabinoid CB2 receptor. J Pharmacol Exp Ther 296(2) 420-425 (2001). 6 Wright, K.L., Duncan, M., Sharkey, K.A. Cannabinoid CB2 receptors in the gastrointestinal tract: A regulatory system in states of inflammation. Br J Pharmacol 153 263-270 (2008).
See how others have used SR 144528. Click on the entry to view the PubMed entry .
PMID: # 26890113 Deiana, V. et al. 2016. Eur J Med Chem. 112: 66-80.
PMID: # 26209834 Ragusa, G. et al. 2015. Eur J Med Chem. 101: 651-67.
PMID: # 26376816 Li, L. et al. 2015. Transl Stroke Res. 6: 467-77.
PMID: # 22595113 Miyashita, K. et al. 2012. J Endod. 38: 786-90.
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