Structure–Activity Studies of Diazabicyclo[3.3.0]octane-Substituted Pyrazines and Pyridines as Potent α4β2 Nicotinic Acetylcholine Receptor Ligands

A series of diazabicyclo[3.3.0]octane substituted pyridines and pyrazines was synthesized and characterized at the α4β2 neuronal nicotinic acetylcholine receptor (nAChR). The compounds were designed to mimic the profile of ABT-089, high affinity binding ligand for the α4β2 nAChR, with limited agonis...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 2011-11, Vol.54 (21), p.7678-7692
Hauptverfasser:	Scanio, Marc J. C, Shi, Lei, Bunnelle, William H, Anderson, David J, Helfrich, Rosalind J, Malysz, John, Thorin-Hagene, Kirsten K, Van Handel, Ceclia E, Marsh, Kennan C, Lee, Chih-Hung, Gopalakrishnan, Murali
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Brain - metabolism Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis Bridged Bicyclo Compounds, Heterocyclic - pharmacokinetics Bridged Bicyclo Compounds, Heterocyclic - pharmacology Cell Line, Tumor Drug Partial Agonism HEK293 Cells Humans In Vitro Techniques Ligands Neurons - metabolism Nicotinic Agonists - chemical synthesis Nicotinic Agonists - pharmacokinetics Nicotinic Agonists - pharmacology Pyrazines - chemical synthesis Pyrazines - pharmacokinetics Pyrazines - pharmacology Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacokinetics Pyridines - pharmacology Pyrrolidines - chemistry Radioligand Assay Rats Receptors, Nicotinic - metabolism Recombinant Proteins - metabolism Stereoisomerism Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!