کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1374991 | 981929 | 2008 | 5 صفحه PDF | دانلود رایگان |
A series of tetrakis-azaaromatic quaternary ammonium salts was synthesized to identify compounds with higher affinity and selectivity as antagonists at neuronal nicotinic receptor subtypes (nAChR) that mediate nicotine-evoked DA release. A high hit rate was achieved in identifying potent analogs that inhibit these nAChRs. Three tetrakis analogs, 11j, 11f, and 11g, were identified as potent (IC50 = 3, 28 and 56 nM, respectively) antagonists at these receptors. These compounds represent a novel structural class of nicotinic receptor antagonists.
Tetrakis-azaaromatic quaternary ammonium salts were identified as antagonists with high affinity and selectivity at nAChR subtypes (nAChR) that mediate nicotine-evoked DA release. Analog 11j (IC50 = 3 nM), is a representative member of this novel structural class of selective nicotinic receptor antagonists.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 21, 1 November 2008, Pages 5753–5757