Author/Authors :
Hirofumi Omura، نويسنده , ,
YOSHIHIRO MATSUDA AND MAKOTO KAWAI، نويسنده , , Akiko Shima، نويسنده , , Yasuhiro Iwata، نويسنده , , Fumitaka Ito، نويسنده , , Tsutomu Masuda، نويسنده , , Atsuko Ohta، نويسنده , , Naoya Makita، نويسنده , , Kiyoyuki Omoto، نويسنده , , Hiromi Sugimoto، نويسنده , , Akira Kikuchi، نويسنده , , Hiroshi Iwata، نويسنده , , Kazuo Ando، نويسنده ,
Abstract :
Benzimidazolone derivatives were discovered as novel CB2 selective agonists. Structure Activity Relationship (SAR) studies around them were examined to improve metabolic stability. Compound 39 exhibited excellent metabolic stability in human liver microsomes (HLM) and significant attenuation of the chronic colonic allodynia in the TNBS-treated rats by po administration.
Keywords :
Cannabinoid , Metabolic stability , Benzimidazolone , CB2 agonist