Quaternary ammonium 3-(aminoethoxy)pyridines as antinociceptive agents
Quaternization via N-methylation of the terminal amines of a series of 3-(dialkylaminoethoxy)pyridines resulted in analogues that displayed up to 50–60-fold enhanced affinity for nicotinic acetylcholinergic (nACh) receptors. Several of these compounds displayed antinociceptive properties in mice usi...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2003-09, Vol.13 (17), p.2917-2920 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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Zusammenfassung: | Quaternization via
N-methylation of the terminal amines of a series of 3-(dialkylaminoethoxy)pyridines resulted in analogues that displayed up to 50–60-fold enhanced affinity for nicotinic acetylcholinergic (nACh) receptors. Several of these compounds displayed antinociceptive properties in mice using the tail-flick assay and serve as possible leads for the development of novel analgesic agents.
Compound
2 (
K
i=0.5 nM) was one of several quaternary amines shown to bind at nicotinic acetylcholinergic receptors with high affinity. Antinociceptive action (mouse tail-flick assay) was evident following either subcutaneous or intrathecal administration of
2. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(03)00585-7 |