Author/Authors :
Takuya Seko، نويسنده , , Masashi Kato، نويسنده , , Hiroshi Kohno، نويسنده , , Shizuka Ono، نويسنده , , Kazuya Hashimura، نويسنده , , Hideyuki Takimizu، نويسنده , , Katsuhiko Nakai، نويسنده , , Hitoshi Maegawa، نويسنده , , Nobuo Katsube، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
The synthesis and structure–activity relationship (SAR) study of a novel series of N-type calcium channel blockers are described. -Cysteine derivative 2a was found to be a potent and selective N-type calcium channel blocker with IC50 0.63 μM on IMR-32 assay. Compound 2a showed analgesic efficacy in the rat formalin-induced pain model by intrathecal and oral administration.
