gw-842166x and Multiple-Sclerosis

gw-842166x has been researched along with Multiple-Sclerosis* in 1 studies

Other Studies

1 other study(ies) available for gw-842166x and Multiple-Sclerosis

Article	Year
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor. Journal of medicinal chemistry, 2015, Aug-13, Volume: 58, Issue:15 The cannabinoid type 2 receptors (CB2Rs) play crucial roles in inflammatory diseases. There has been considerable interest in developing potent and selective ligands for CB2R. In this study, quinoline-2,4(1H,3H)-dione analogs have been designed, synthesized, and evaluated for their potencies and binding properties toward the cannabinoid type 1 receptor (CB1R) and CB2R. C5- or C8-substituted quinoline-2,4(1H,3H)-diones demonstrate CB2R agonist activity, while the C6- or C7-substituted analogs are antagonists of CB2R. In addition, oral administration of 21 dose-dependently alleviates the clinical symptoms of experimental autoimmune encephalomyelitis in a mouse model of multiple sclerosis and protects the central nervous system from immune damage. Furthermore, the interaction modes predicted by docking simulations and the 3D-QSAR model generated with CoMFA may offer guidance for further design and modification of CB2R modulators. Topics: Animals; CHO Cells; Cricetinae; Cricetulus; Disease Models, Animal; Encephalomyelitis, Autoimmune, Experimental; Female; Ligands; Mice; Mice, Inbred C57BL; Molecular Docking Simulation; Multiple Sclerosis; Quantitative Structure-Activity Relationship; Quinolines; Receptor, Cannabinoid, CB2	2015

Article

Year

Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.

Journal of medicinal chemistry, 2015, Aug-13, Volume: 58, Issue:15

The cannabinoid type 2 receptors (CB2Rs) play crucial roles in inflammatory diseases. There has been considerable interest in developing potent and selective ligands for CB2R. In this study, quinoline-2,4(1H,3H)-dione analogs have been designed, synthesized, and evaluated for their potencies and binding properties toward the cannabinoid type 1 receptor (CB1R) and CB2R. C5- or C8-substituted quinoline-2,4(1H,3H)-diones demonstrate CB2R agonist activity, while the C6- or C7-substituted analogs are antagonists of CB2R. In addition, oral administration of 21 dose-dependently alleviates the clinical symptoms of experimental autoimmune encephalomyelitis in a mouse model of multiple sclerosis and protects the central nervous system from immune damage. Furthermore, the interaction modes predicted by docking simulations and the 3D-QSAR model generated with CoMFA may offer guidance for further design and modification of CB2R modulators.

Topics: Animals; CHO Cells; Cricetinae; Cricetulus; Disease Models, Animal; Encephalomyelitis, Autoimmune, Experimental; Female; Ligands; Mice; Mice, Inbred C57BL; Molecular Docking Simulation; Multiple Sclerosis; Quantitative Structure-Activity Relationship; Quinolines; Receptor, Cannabinoid, CB2

2015