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Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels |
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| Authors: | Yamamoto Takashi Niwa Seiji Ohno Seiji Onishi Tomoyuki Matsueda Hiroyuki Koganei Hajime Uneyama Hisayuki Fujita Shin-ichi Takeda Tomoko Kito Morikazu Ono Yukitsugu Saitou Yuki Takahara Akira Iwata Seinosuke Shoji Masataka |
| Institution: | Pharmaceutical Research Laboratory, Ajinomoto company Inc., Kawasaki-ku, Kawasaki-shi, Japan. |
| 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. |
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