215119-89-4Relevant academic research and scientific papers
The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels
Yamamoto, Takashi,Niwa, Seiji,Ohno, Seiji,Tokumasu, Munetaka,Masuzawa, Yoko,Nakanishi, Chika,Nakajo, Akira,Onishi, Tomoyuki,Koganei, Hajime,Fujita, Shin-ichi,Takeda, Tomoko,Kito, Morikazu,Ono, Yukitsugu,Saitou, Yuki,Takahara, Akira,Iwata, Seinosuke,Shoji, Masataka
, p. 4813 - 4816 (2008)
In order to find an injectable and selective N-type calcium channel blocker, we have performed the structure-activity relationship (SAR) study on the 2-, 5-, and 6-position of 1,4-dihydropyridine-3-carboxylate derivative APJ2708 (2), which is a derivative of Cilnidipine and has L/N-type calcium channel dual inhibitory activities. As a consequence of the optimization, 6-dimethylacetal derivative 7 was found to have an effective inhibitory activity against N-type calcium channels with more than 170-fold lower activity for L-type channel compared to that of APJ2708.
