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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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

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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.

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