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1: Bioorg Med Chem Lett. 2006 Feb 15;16(4):798-802. Epub 2005 Nov 23.Click here to read Links

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

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]