1070877-57-4Relevant articles and documents
Discovery and evaluation of selective N-type calcium channel blockers: 6-Unsubstituted-1,4-dihydropyridine-5-carboxylic acid derivatives
Yamamoto, Takashi,Niwa, Seiji,Tokumasu, Munetaka,Onishi, Tomoyuki,Ohno, Seiji,Hagihara, Masako,Koganei, Hajime,Fujita, Shin-Ichi,Takeda, Tomoko,Saitou, Yuki,Iwayama, Satoshi,Takahara, Akira,Iwata, Seinosuke,Shoji, Masataka
scheme or table, p. 3639 - 3642 (2012/07/17)
A structure-activity relationship study of 6-unsubstituted-1,4- dihydropyridine and 2,6-unsubstituted-1,4-dihydropyridine derivatives was conducted in an attempt to discover N-type calcium channel blockers that were highly selective over L-type calcium channel blockers. Among the tested compounds, (+)-4-(3,5-dichloro-4-methoxy-phenyl)-1,4-dihydro-pyridine-3,5- dicarboxylic acid 3-cinnamyl ester was found to be an effective and selective N-type calcium channel blocker with oral analgesic potential.
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
body text, p. 4813 - 4816 (2009/06/06)
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.