SYNTHESIS AND IN-VITRO PHARMACOLOGY OF A SERIES OF HYBRID MOLECULES POSSESSING 1,4-DIHYDROPYRIDINE CALCIUM-CHANNEL BLOCKING ACTIVITY AND HISTAMINE H-2-AGONISTIC PROPERTIES

The synthesis and in vitro pharmacology of a series of new cardiovascu lar hybrid molecules, which could be useful for the treatment of certa in types of hypertension and at the same time for the treatment of car diac ischemic disease, are discussed. Two types of 1,4-dihydropyridine Ca2+-channel blockers have been studied. In general, hybrid molecules possessing a diethyl 2-(omega aminoalkylthio)methyl-2 tuted)phenyl]-1 ,4-dihydropyridine-3,5-dicarboxylic structural moiety and a histamine H-2-agonistic structural moiety are more potent L-type calcium-channel blockers and histamine H-2-agonists than hybrid molecules containing a diethyl -2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic structura l moiety.