2002
DOI: 10.1021/bi027031m
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A Multiply Charged Tetracaine Derivative Blocks Cyclic Nucleotide-Gated Channels at Subnanomolar Concentrations

Abstract: Cyclic nucleotide-gated (CNG) ion channels are central participants in sensory transduction, generating the electrical response to light in retinal photoreceptors and to odorants in olfactory receptors. They are expressed in many other tissues where their specific roles in signaling remain unclear. As is true for many other ion channels, there is a paucity of specific blockers needed to dissect the contributions of these channels to cell signaling. CNG channels are members of the superfamily of voltage-gated i… Show more

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Cited by 12 publications
(20 citation statements)
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“…The reduction of polyamine-evoked CP responses obtained with tetracaine is consistent with the existence of a signaling pathway that involves membrane ionic fluxes. As tetracaine is a general membrane cation channel blocker, with moderate affinity for CNG channels [59,60], we further confirmed our results with L-cis-diltiazem, which specifically blocks CNG channels [30]. The CNG inhibition of CP responses, obtained for all polyamines, corroborates the aforementioned adenylate cyclase results (SQ22536), indicating that the cAMP pathway, and therefore the CNG channel, is involved in all polyamine actions.…”
Section: Discussionsupporting
confidence: 88%
“…The reduction of polyamine-evoked CP responses obtained with tetracaine is consistent with the existence of a signaling pathway that involves membrane ionic fluxes. As tetracaine is a general membrane cation channel blocker, with moderate affinity for CNG channels [59,60], we further confirmed our results with L-cis-diltiazem, which specifically blocks CNG channels [30]. The CNG inhibition of CP responses, obtained for all polyamines, corroborates the aforementioned adenylate cyclase results (SQ22536), indicating that the cAMP pathway, and therefore the CNG channel, is involved in all polyamine actions.…”
Section: Discussionsupporting
confidence: 88%
“…23 We isolated a related derivative (3) with a single added propylamino group. Under physiological conditions 1, 3, and 4 will bear one, two, and three positive charges, respectively.…”
Section: Resultsmentioning
confidence: 99%
“…3840 Compound 1 is clinically approved for temporary anesthesia in various surgical procedures, including those involving the eye. 41,42 Its effects are localized and shortlived due to its rapid degradation by esterases.…”
Section: Introductionmentioning
confidence: 99%