Synthesis and characterization of N-(acenaphth-5-yl)-N'-(4-methoxynaphth-1-yl)guanidine as a glutamate release inhibitor and potential anti-ischemic agent

Abstract

Structure-activity relationship (SAR) studies of N,N'-diarylguanidines as glutamate release inhibitors led to the synthesis of N-(acenaphth-5-yl)-N'-(4-methoxynaphth-1-yl)guanidine ( 6). Compound 6, with IC 50 values of 1.3 and 2.2 μM in 14C-guanidine flux and 45Ca 2+- flux assays respectively, effectively inhibited both veratridine and K +-evoked glutamate release in rat brain synaptosomal preparations.