Author/Authors :
N. Laxma Reddy، نويسنده , , Sonia Connaughton، نويسنده , , Deborah Daly، نويسنده , , James B. Fischer، نويسنده , , Stanley M. Goldin، نويسنده , , Lain-Yen Hu، نويسنده , , Katragadda Subbarao، نويسنده , , Graham J. Durant، نويسنده ,
Abstract :
Structure-activity relationship (SAR) studies of N,Nʹ-diarylguanidines as glutamate release inhibitors led to the synthesis of N-(acenaphth-5-yl)-Nʹ-(4-methoxynaphth-1-yl)guanidine (6). Compound 6, with IC50 values of 1.3 and 2.2 μM in 14C-guanidine flux and 45Ca2+- flux assays respectively, effectively inhibited both veratridine and K+-evoked glutamate release in rat brain synaptosomal preparations
