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
Journal of Medicinal Chemistry2010Vol. 53(21), pp. 7869–7873
Citations Over Time
Robert J. Altenbach, Lawrence A. Black, Marina I. Strakhova, Arlene M. Manelli, Tracy L. Carr, Kennan C. Marsh, Jill M. Wetter, Erica J. Wensink, Gin C. Hsieh, Prisca Honoré, Tiffany Runyan Garrison, Jorge D. Brioni, Marlon Cowart
Abstract
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.
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