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 :
Synthesis and structure–activity relationship (SAR) studies of -cysteine-based N-type calcium channel blockers are described. In the course of exploring SAR of the N- and C-terminal substituents, the -cysteine derivative 4b was found to be a potent N-type calcium channel blocker with an IC50 value of 0.14 μM on IMR-32 assay. Compound 4b showed 12-fold selectivity for N-type over L-type calcium channels on AtT-20 assay.
