2. Academic Validation
  3. Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels

Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels

  • Bioorg Med Chem Lett. 2006 Feb 15;16(4):798-802. doi: 10.1016/j.bmcl.2005.11.021.
Takashi Yamamoto 1,  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
Affiliations

Affiliation

  • 1 Pharmaceutical Research Laboratory, Ajinomoto company Inc., Kawasaki-ku, Kawasaki-shi, Japan.
PMID: 16309909 DOI: 10.1016/j.bmcl.2005.11.021
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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