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.
Article Details
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Altenbach RJ, Black LA, Strakhova MI, Manelli AM, Carr TL, Marsh KC, Wetter JM, Wensink EJ, Hsieh GC, Honore P, Garrison TR, Brioni JD, Cowart MD
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.
J Med Chem. 2010 Nov 11;53(21):7869-73. doi: 10.1021/jm100666w.
- PubMed ID
- 20945906 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Desipramine Sodium-dependent noradrenaline transporter Kd (nM) 0.83 N/A N/A Details Desipramine Sodium-dependent serotonin transporter Ki (nM) 20 N/A N/A Details Protriptyline Sodium-dependent noradrenaline transporter Kd (nM) 1.4 N/A N/A Details