Author/Authors :
Dimitrios Galanakis، نويسنده , , Carole A. Davis، نويسنده , , Benedicto Del Rey Herrero، نويسنده , , C. Robin Ganellin، نويسنده , , Philip M. Dunn، نويسنده , , Donald H. Jenkinson، نويسنده ,
Abstract :
Dequalinium (1) is a potent and selective non-peptidic blocker of the SKCa channel. The contribution of the 4-amino group to activity was investigated by replacing it by other groups R4. The size or lipophilicity of R4 was found to be unimportant and a good correlation was obtained between σR for R4 and the blocking potency of the analogues, suggesting that the role of the NH2 group is electronic.