Worm Karin, Weaver Damian G, Green Rosalyn C, Saeui Christopher T, Dulay Doreen-Marie S, Barker William M, Cassel Joel A, Stabley Gabriel J, DeHaven Robert N, LaBuda Christopher J, Koblish Michael, Brogdon Bernice L, Smith Steven A, Dolle Roland E
Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA.
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5004-8. doi: 10.1016/j.bmcl.2009.07.057. Epub 2009 Jul 12.
Recently sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Replacing the sulfonamide functionality and reversing the original carboxamide bond led to the discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB(2) agonists. Selective CB(2) agonist 31 (K(i)=2.7; CB(1)/CB(2)=190) displayed robust activity in a rodent model of postoperative pain.
最近，磺酰基苯甲酰胺被鉴定为一类新型的大麻素受体配体。取代磺酰胺官能团并反转原来的羧酰胺键，从而发现了N-(3-(吗啉甲基)-苯基)-酰胺作为强效且选择性的CB(2)激动剂。选择性CB(2)激动剂31（K(i)=2.7；CB(1)/CB(2)=190）在术后疼痛的啮齿动物模型中表现出强大的活性。
