Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain

A series of compounds was designed as dual inhibitors of the H(3) receptor and the norepinephrine transporter. Compound 5 (rNET K(i) = 14 nM; rH(3)R K(i) = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 2010-11, Vol.53 (21), p.7869-7873
Hauptverfasser:	Altenbach, Robert J, Black, Lawrence A, Strakhova, Marina I, Manelli, Arlene M, Carr, Tracy L, Marsh, Kennan C, Wetter, Jill M, Wensink, Erica J, Hsieh, Gin C, Honore, Prisca, Garrison, Tiffany Runyan, Brioni, Jorge D, Cowart, Marlon D
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Histamine H3 Antagonists - chemical synthesis Histamine H3 Antagonists - pharmacokinetics Histamine H3 Antagonists - pharmacology Naphthols - chemical synthesis Naphthols - pharmacokinetics Naphthols - pharmacology Norepinephrine Plasma Membrane Transport Proteins - antagonists & inhibitors Osteoarthritis - drug therapy Pain - drug therapy Pyrrolidines - chemical synthesis Pyrrolidines - pharmacokinetics Pyrrolidines - pharmacology Rats Rats, Sprague-Dawley Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A series of compounds was designed as dual inhibitors of the H(3) receptor and the norepinephrine transporter. Compound 5 (rNET K(i) = 14 nM; rH(3)R K(i) = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.
ISSN:	1520-4804
DOI:	10.1021/jm100666w