Quaternary Ammonium Derivative of Lidocaine as a Long-acting Local Anesthetic
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Background: Use of long-acting local anesthetics that elicit complete neural blockade for more than 3 h often is desirable in pain management. Unfortunately, clinically available local anesthetics are in general not suitable for prolonged analgesia. This report describes the organic synthesis and functional testing of a lidocaine derivative that appears to fulfill the criteria of long-acting local anesthetics.
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Quaternary amines with substantial hydrophobic substituents display detectable membrane permeability.
“Quaternary amines with substantial hydrophobic substituents also display detectable membrane permeability; this is revealed in the literature on blockers of voltage-gated ion channels.”
From Nicotine is a selective pharmacological chaperone of acetylcholine receptor number and stoichiometry. Implications for drug discovery (2009) · cites this paper as [42]
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- Authors
- Wang, G. K., Quan, C., Vladimirov, M., Mok, W. M., & Thalhammer, J. G.
- Affiliations
- Harvard University (US)
- Venue
- Anesthesiology
- Published
- 1995-12-01
- Volume
- 83
- Issue
- 6
- Pages
- 1293-1301
- ISSN
- 0003-3022 (ISSN-L)
- OpenAlex
- W2114605607
- Cited by
- 53
- References
- 18
- Citations by year
- 2026: 1 · 2025: 1 · 2022: 1 · 2017: 1 · 2015: 1 · 2013: 5
- FWCI
- 3.44
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Anesthesiology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (5r01gm035401-16)
- National Institute of General Medical Sciences (GM-48090, GM35401, R01GM048090)
- Topics
- Health Sciences › Medicine › Surgery › Anesthesia and Pain Management
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Health Sciences › Dentistry › Oral Surgery › Dental Anxiety and Anesthesia Techniques
- Keywords
- lidocaine derivatives, quaternary ammonium compounds, long-acting local anesthetics, sodium channel blockade, sciatic nerve block, sensory and motor blockade, pain management, organic synthesis, use-dependent block
- MeSH terms
- Quaternary Ammonium Compounds, Anesthetics, Local, Animals, Cells, Cultured, Lidocaine, Motor Neurons, Neurons, Afferent, Sodium, Structure-Activity Relationship, Time Factors, Sodium Channels, Ion Channel Gating, Patch-Clamp Techniques, Rats
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