Diaryldiamines with Dual Inhibition of the Histamine H3 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

Diaryldiamines with Dual Inhibition of the Histamine H3 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 H3 receptor and the norepinephrine transporter. Compound 5 (rNET K i = 14 nM; rH3R K i = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.

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Bibliographic Details
Published in:Journal of medicinal chemistry Vol. 53; no. 21; pp. 7869 - 7873
Main Authors: 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: Journal Article
Language:English
Published: American Chemical Society 11-11-2010
Online Access:Get full text
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Description
Summary:A series of compounds was designed as dual inhibitors of the H3 receptor and the norepinephrine transporter. Compound 5 (rNET K i = 14 nM; rH3R K i = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm100666w