Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca2+-activated K+ channel blockers

In parallel to the development of N-methyl-laudanosine derivatives, a chiral and bis-tertiary amine, AG525E1, shows an approximately 100-fold increase in affinity for apamin-sensitive sites than laudanosine. Physicochemical parameters support its ability to reach CNS targets.