Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties

Pyridineethanolamine derivatives containing cyanoguanidine or nitroethylenediamine moieties were examined as human beta3 adrenergic receptor (AR) agonists. Notably, indoline derivatives 6a and 11 were potent beta3 AR agonists (beta3 EC50 = 13 and 19 nM, respectively), which showed good selectivity o...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-02, Vol.11 (3), p.379
Hauptverfasser:	Brockunier, L L, Candelore, M R, Cascieri, M A, Liu, Y, Tota, L, Wyvratt, M J, Fisher, M H, Weber, A E, Parmee, E R
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenylyl Cyclases - drug effects Adenylyl Cyclases - metabolism Adrenergic beta-3 Receptor Agonists Adrenergic beta-Agonists - chemical synthesis Adrenergic beta-Agonists - chemistry Adrenergic beta-Agonists - pharmacology Animals Cell Membrane - chemistry CHO Cells Combinatorial Chemistry Techniques Cricetinae Diamines - chemistry Ethane - analogs & derivatives Ethane - chemistry Guanidines - chemistry Humans Inhibitory Concentration 50 Nitroparaffins - chemistry Radioligand Assay Receptors, Adrenergic, beta - metabolism Receptors, Adrenergic, beta-3 - metabolism Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	Pyridineethanolamine derivatives containing cyanoguanidine or nitroethylenediamine moieties were examined as human beta3 adrenergic receptor (AR) agonists. Notably, indoline derivatives 6a and 11 were potent beta3 AR agonists (beta3 EC50 = 13 and 19 nM, respectively), which showed good selectivity over binding to and minimal activation of the beta1 and beta2 ARs.
ISSN:	0960-894X