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    Bioorg Med Chem Lett. 2006 Feb 15;16(4):798-802. Epub 2005 Nov 23.

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

    Yamamoto T, Niwa S, Ohno S, Onishi T, Matsueda H, Koganei H, Uneyama H, Fujita S, Takeda T, Kito M, Ono Y, Saitou Y, Takahara A, Iwata S, Shoji M.

    Pharmaceutical Research Laboratory, Ajinomoto company Inc., Kawasaki-ku, Kawasaki-shi, Japan.

    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.

    PMID: 16309909 [PubMed - indexed for MEDLINE]

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