Zhang_2011_Bioorg.Med.Chem.Lett_21_88

Reference

Title : Novel bis-, tris-, and tetrakis-tertiary amino analogs as antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release - Zhang_2011_Bioorg.Med.Chem.Lett_21_88
Author(s) : Zhang Z , Zheng G , Pivavarchyk M , Deaciuc AG , Dwoskin LP , Crooks PA
Ref : Bioorganic & Medicinal Chemistry Lett , 21 :88 , 2011
Abstract :

A series of tertiary amine analogs derived from lead azaaromatic quaternary ammonium salts has been designed and synthesized. The preliminary structure-activity relationships of these new analogs suggest that such tertiary amine analogs, which potently inhibit nicotine-evoked dopamine release from rat striatum, represent drug-like inhibitors of alpha6-containing nicotinic acetylcholine receptors. The bis-tertiary amine analog 7 exhibited an IC(50) of 0.95 nM, while the tris-tertiary amine analog 19 had an IC(50) of 0.35 nM at nAChRs mediating nicotine-evoked dopamine release.

PubMedSearch : Zhang_2011_Bioorg.Med.Chem.Lett_21_88
PubMedID: 21147530

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Citations formats

Zhang Z, Zheng G, Pivavarchyk M, Deaciuc AG, Dwoskin LP, Crooks PA (2011)
Novel bis-, tris-, and tetrakis-tertiary amino analogs as antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release
Bioorganic & Medicinal Chemistry Lett 21 :88

Zhang Z, Zheng G, Pivavarchyk M, Deaciuc AG, Dwoskin LP, Crooks PA (2011)
Bioorganic & Medicinal Chemistry Lett 21 :88