ArticleACS chemical neuroscience2012
Identification of the benzyloxyphenyl pharmacophore: a structural unit that promotes sodium channel slow inactivation.
Article in ACS chemical neuroscience, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 15 citations in OpenAlex.
- Prediction and Prioritisation of Novel Anthelmintic Candidates from Public Databases Using Deep Learning and Available Bioactivity Data Sets.International journal of molecular sciences · 2025Article
- One-pot synthesis of tetrahydropyrimidinecarboxamides enablingRSC advances · 2024Article
- Modulation of sodium channels as pharmacological tool for pain therapy-highlights and gaps.Naunyn-Schmiedeberg's archives of pharmacology · 2018Review
- Chimeric agents derived from the functionalized amino acid, lacosamide, and the α-aminoamide, safinamide: evaluation of their inhibitory actions on voltage-gated sodium channels, and antiseizure and antinociception activities and comparison with lacosamide and safinamide.ACS chemical neuroscience · 2015Article
- Substituted N-(biphenyl-4'-yl)methyl (R)-2-acetamido-3-methoxypropionamides: potent anticonvulsants that affect frequency (use) dependence and slow inactivation of sodium channels.Journal of medicinal chemistry · 2014Article
- CRMP2 protein SUMOylation modulates NaV1.7 channel trafficking.The Journal of biological chemistry · 2013Article
- (Biphenyl-4-yl)methylammonium chlorides: potent anticonvulsants that modulate Na+ currents.Journal of medicinal chemistry · 2013Article
- Discovery of lacosamide affinity bait agents that exhibit potent voltage-gated sodium channel blocking properties.ACS chemical neuroscience · 2013Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
Abstract
Four compounds that contained the N-benzyl 2-amino-3-methoxypropionamide unit were evaluated for their ability to modulate Na(+) currents in catecholamine A differentiated CAD neuronal cells. The compounds differed by the absence or presence of either a terminal N-acetyl group or a (3-fluoro)benzyloxy moiety positioned at the 4'-benzylamide site. Analysis of whole-cell patch-clamp electrophysiology data showed that the incorporation of the (3-fluoro)benzyloxy unit, to give the (3-fluoro)benzyloxyphenyl pharmacophore, dramatically enhanced the magnitude of Na(+) channel slow inactivation. In addition, N-acetylation markedly increased the stereoselectivity for Na(+) channel slow inactivation. Furthermore, we observed that Na(+) channel frequency (use)-dependent block was maintained upon inclusion of this pharmacophore. Confirmation of the importance of the (3-fluoro)benzyloxyphenyl pharmacophore was shown by examining compounds where the N-benzyl 2-amino-3-methoxypropionamide unit was replaced by a N-benzyl 2-amino-3-methylpropionamide moiety, as well as examining a series of compounds that did not contain an amino acid group but retained the pharmacophore unit. Collectively, the data indicated that the (3-fluoro)benzyloxyphenyl unit is a novel pharmacophore for the modulation of Na(+) currents.
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Registered trials
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