Title of article :
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: Discovery of CB2 receptor selective compounds
Author/Authors :
Hiroyuki Kai، نويسنده , , Yasuhide Morioka، نويسنده , , Takami Murashi، نويسنده , , Koichi Morita، نويسنده , , Satomi Shinonome، نويسنده , , Hitoshi Nakazato، نويسنده , , Keiko Kawamoto، نويسنده , , Kohji Hanasaki، نويسنده , , Fumiyo Takahashi، نويسنده , , Shin-ichi Mihara، نويسنده , , Tohko Arai، نويسنده , , Kohji Abe، نويسنده , , Hiroshi Okabe، نويسنده , , Takahiko Baba، نويسنده , , Takayoshi Yoshikawa، نويسنده , , Hideyuki Takenaka، نويسنده ,
Abstract :
2-Arylimino-5,6-dihydro-4H-1,3-thiazines have been identified as a novel class of cannabinoid agonists. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure–activity relationships led to the discovery of potent agonists of CB2 receptor. The most potent compound 13 displays Ki values of >5000 and 9 nM to CB1 and CB2 receptors, respectively.
Keywords :
Cannabinoid receptor agonist , CB1 , CB2 , CB2 receptor selective , structure–activity relationship , pain , 1 , 3-Thiazine
