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, 53 (21), 7869-73

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

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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

Robert J Altenbach et al. J Med Chem.

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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