Synthesis and in vitro pharmacology of new 1,4-dihydropyridines. 1. 2-(ω-Aminoalkylthiomethyl)-1,4-dihydropyridines as potent calcium channel blockers

JAM Christiaans, AD Windhorst, PM Groenenberg, H. van der Goot, H. Timmerman

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The synthesis and in vitro calcium channel blocking activities and binding of 2-(ω- aminoalkylthiomethyl)-4-(substituted)phenyl-1,4-dihydropyridines, by determination of the displacement of [3H]nitrendipine from the calcium channel binding sites on rat cortex have been discussed. It has been shown that increasing the alkyl chain length on the 2-position of the 1,4-dihydropyridine ring from ethyl to pentyl does not affect the calcium channel blocking activity of 3-nitrophenyl substituted dihydropyridines, measured on K+-depolarisation induced contractile responses in rat aorta strips. It did not seem to be important whether the 1,4-dihydropyridines bore 2 identical or different ester moieties on the 3- and 5-position of the 1,4-dihydropyridine ring.

Original languageEnglish
Pages (from-to)859-867
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Issue number11
Publication statusPublished - 1 Jan 1993


  • 1,4-dihydropyridines
  • calcium channel blocker
  • tiamdipine

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