SYNTHESIS AND IN-VITRO PHARMACOLOGY OF NEW 1,4-DIHYDROPYRIDINES .1. -(OMEGA-AMINOALKYLTHIOMETHYL)-1,4-DIHYDROPYRIDINES AS POTENT CALCIUM-CHANNEL BLOCKERS

The synthesis and in vitro calcium channel blocking activities and bin ding of ethyl)-4-(substituted)phenyl-1,4-dihydropyridines, by determin ation of the displacement of [H-3]nitrendipine from the calcium channe l binding sites on rat cortex have been discussed. It has been shown t hat increasing the alkyl chain length on the 2-position of the 1,4-dih ydropyridine ring from ethyl to pentyl does not affect the calcium cha nnel blocking activity of 3-nitrophenyl substituted dihydropyridines, measured on K+-depolarisation induced contractile responses in rat aor ta strips. It did not seem to be important whether the 1,4-dihydropyri dines bore 2 identical or different ester moieties on the 3- and 5-pos ition of the 1,4-dihydropyridine ring.