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

T Strassmaier, R Uma, AS Ghatpande…

文献索引：Strassmaier, Timothy; Uma, Ramalinga; Ghatpande, Ambarish S.; Bandyopadhyay, Tapasree; Schaffer, Michelle; Witte, John; McDougal, Patrick G.; Brown, R. Lane; Karpen, Jeffrey W. Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5805 - 5812

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被引用次数: 11

摘要

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 (4). 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 ...