Novel bis-, tris-, and tetrakis-tertiary amino analogs as antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release
Graphical abstract
A series of tertiary amine analogs derived from lead azaaromatic quaternary ammonium salts has been designed and synthesized. The bis-tertiary amine analog 7 exhibited an IC50 of 0.95 nM, while the tris-tertiary amine analog 19 had an IC50 of 0.35 nM at nAChRs mediating nicotine-evoked dopamine release.
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Acknowledgment
This work was supported by NIH. (Grant U19DA017548)
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