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 |
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