New prenylamine-analogues: investigations of their influence on calcium-dependent biological systems
摘要:
Chemically, prenylamine belongs to the diphenylalkylamine class. Compounds of this class are calcium antagonists with a broad spectrum of activities due to their influence on both extracellular and intracellular sites. In the present study the calcium antagonistic profile of a recently developed new series of prenylamine analogues has been investigated using different in vitro systems. The inhibiting concentrations for the most active compound are almost-equal-to 1.5 muM; several derivatives are inactive up to a concentration of 10 muM. Structural modifications towards an increase of lipophilicity make these molecules interact (inhibition) with the intracellular calcium-binding protein calmodulin; for the series no correlation between calcium-blocking and calmodulin antagonistic effects has been found.