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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Cattle
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Cyclic Nucleotide-Gated Cation Channels
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In Vitro Techniques
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Ion Channel Gating
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Ion Channels / antagonists & inhibitors*
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Ion Channels / genetics
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Ion Channels / physiology
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Membrane Potentials / drug effects
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Oocytes / drug effects
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Oocytes / physiology
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Patch-Clamp Techniques
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Retinal Rod Photoreceptor Cells / metabolism
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Structure-Activity Relationship
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Tetracaine / analogs & derivatives*
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Tetracaine / chemical synthesis*
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Tetracaine / pharmacology
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Xenopus
Substances
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Cyclic Nucleotide-Gated Cation Channels
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Ion Channels
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Tetracaine