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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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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Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories,
100 Abbott Park Road, Abbott Park, Illinois 60064-6100, United States. robert.j.altenbach@abbott.com