Document Report Card

ID: ALA1141076

Journal: J Med Chem

Title: Modifications to the tetracaine scaffold produce cyclic nucleotide-gated channel blockers with widely varying efficacies.

Authors: Strassmaier T, Uma R, Ghatpande AS, Bandyopadhyay T, Schaffer M, Witte J, McDougal PG, Brown RL, Karpen JW.

Abstract: Five new tetracaine analogues were synthesized and evaluated for potency of blockade of cyclic nucleotide-gated channels relative to a multiply charged tetracaine analogue described previously. Increased positive charge at the tertiary amine end of tetracaine results in higher potency and voltage dependence of block. Modifications that reduce the hydrophobic character at the butyl tail are deleterious to block. The tetracaine analogues described here have apparent affinities for CNGA1 channels that vary over nearly 8 orders of magnitude.

CiteXplore: 16134947

DOI: 10.1021/jm0502485