Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter.
A series of bis-azaaromatic quaternary ammonium compounds containing flexible polymethylenic linkers as well as conformationally restricted linkers were evaluated for their affinity for the blood-brain barrier choline transporter (BBB-ChT). The preliminary structure-activity relationships obtained from this study suggest that incorporating a linear, conformationally restricted linker into the molecule improves affinity for the BBB-ChT.
Zheng
Guangrong
G
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA.
Zhang
Zhenfa
Z
Lockman
Paul R
PR
Geldenhuys
Werner J
WJ
Allen
David D
DD
Dwoskin
Linda P
LP
Crooks
Peter A
PA
D000818:Animals; D001812:Blood-Brain Barrier; D008024:Ligands; D026901:Membrane Transport Proteins / Q000378:metabolism*; D000644:Quaternary Ammonium Compounds / Q000378:metabolism*; D012492:Salts; D013329:Structure-Activity Relationship
D008024:Ligands; D026901:Membrane Transport Proteins; D000644:Quaternary Ammonium Compounds; D012492:Salts; C065637:choline transporter
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