Title of article
tris-Azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release
Author/Authors
Guangrong Zheng، نويسنده , , Sangeetha P. Sumithran، نويسنده , , Agripina G. Deaciuc، نويسنده , , Linda P. Dwoskin، نويسنده , , Peter A. Crooks، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
6701
To page
6706
Abstract
A series of tris-azaaromatic quaternary ammonium salts has been synthesized and evaluated for their ability to inhibit neuronal nicotinic acetylcholine receptors (nAChRs) mediating nicotine-evoked [3H]dopamine release from superfused rat striatal slices and for inhibition of [3H]nicotine and [3H]methyllycaconitine binding to whole rat brain membranes. The 3-picolinium compound 1,3,5-tri-{5-[1-(3-picolinium)]-pent-1-ynyl}benzene tribromide (tPy3PiB), 3b, exhibited high potency and selectivity for nAChR subtypes mediating nicotine-evoked [3H]dopamine release with an IC50 of 0.2 nM and Imax of 67%.
Keywords
Nicotinic acetylcholine receptor , tris-Azaaromatic quaternary ammonium , Nicotine , Dopamine release
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798871
Link To Document