Author/Authors :
Karin Worm، نويسنده , , Q. Jean Zhou، نويسنده , , Christopher T. Saeui، نويسنده , , Rosalyn C. Green، نويسنده , , Joel A. Cassel، نويسنده , , Gabriel J. Stabley، نويسنده , , Robert N. DeHaven، نويسنده , , Nathalie Conway-James، نويسنده , , Christopher J. LaBuda، نويسنده , , Michael Koblish، نويسنده , , Patrick J. Little، نويسنده , , Roland E. Dolle، نويسنده ,
Abstract :
Sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Starting from a screening hit 8 that had modest affinity for the cannabinoid CB2 receptor, a parallel synthesis approach and initial SAR are described, leading to compound 27 with 120-fold functional selectivity for the CB2 receptor. This compound produced robust antiallodynic activity in rodent models of postoperative pain and neuropathic pain without traditional cannabinergic side effects.
Keywords :
Cannabinoid CB2 receptor , parallel synthesis , Sulfamoyl benzamides , Antiallodynic activity , structure–activity relationship
