Author/Authors :
Takashi Yamamoto، نويسنده , , Seiji Niwa، نويسنده , , Seiji Ohno، نويسنده , , Tomoyuki Onishi، نويسنده , , Hiroyuki Matsueda، نويسنده , , Hajime Koganei، نويسنده , , Hisayuki Uneyama، نويسنده , , Shin-ichi Fujita، نويسنده , , Tomoko Takeda، نويسنده , , Morikazu Kito، نويسنده , , Yukitsugu Ono، نويسنده , , Yuki Saitou، نويسنده , , Akira Takahara، نويسنده , , Seinosuke Iwata، نويسنده , , Masataka Shoji، نويسنده ,
Abstract :
Cilnidipine is a 1,4-dihydropyridine derived L/N-type calcium channel dual blocker possessing neuroprotective and analgesic effects which are related to its N-type calcium channel inhibitory activity. In order to find specific N-type calcium channel blockers with the least effects on cardiovascular system, we performed structure–activity relationship study on APJ2708, which is a derivative of cilnidipine, and found a promising N-type calcium channel blocker 21b possessing analgesic effect in vivo with a 1600-fold lower activity against L-type calcium channels than that of cilnidipine.
Keywords :
Cilnidipine , Structure–activity relationship study , N-type calcium channels blocker , 4-dihydropyridine , analgesic , 1
