NEW PRENYLAMINE-ANALOGS - INVESTIGATIONS OF THEIR INFLUENCE ON CALCIUM-DEPENDENT BIOLOGICAL-SYSTEMS

Chemically, prenylamine belongs to the diphenylalkylamine class. Compo unds of this class are calcium antagonists with a broad spectrum of ac tivities due to their influence on both extracellular and intracellula r sites. In the present study the calcium antagonistic profile of a re cently developed new series of prenylamine analogues has been investig ated using different in vitro systems. The inhibiting concentrations f or the most active compound are almost-equal-to 1.5 muM; several deriv atives are inactive up to a concentration of 10 muM. Structural modifi cations towards an increase of lipophilicity make these molecules inte ract (inhibition) with the intracellular calcium-binding protein calmo dulin; for the series no correlation between calcium-blocking and calm odulin antagonistic effects has been found.