| Literature DB >> 16309909 |
Takashi Yamamoto1, Seiji Niwa, Seiji Ohno, Tomoyuki Onishi, Hiroyuki Matsueda, Hajime Koganei, Hisayuki Uneyama, Shin-ichi Fujita, Tomoko Takeda, Morikazu Kito, Yukitsugu Ono, Yuki Saitou, Akira Takahara, Seinosuke Iwata, Masataka Shoji.
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.Entities:
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Year: 2005 PMID: 16309909 DOI: 10.1016/j.bmcl.2005.11.021
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823