Diaryldiamines with Dual Inhibition of the Histamine H<sub>3</sub> 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 - Concepedia

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Diaryldiamines with Dual Inhibition of the Histamine H<sub>3</sub> 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

DOI Full Paper Access

19

Citations

20

References

2010

Year

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,

Journal of Medicinal Chemistry

Pain TherapyPain DisordersPain MedicineNeuropathic PainMolecular PainPharmacotherapyExperimental PharmacologyRat ModelMolecular PharmacologyMedicinal ChemistryOsteoarthritisPain ManagementAnalgesicsHealth SciencesBiochemistryDual InhibitorsMechanism Of ActionPharmacological AgentNeuropharmacologyPharmacologyPain ResearchDual InhibitionPhysiologyPain MechanismMedicineNorepinephrine TransporterDrug DiscoveryAnesthesiology

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.

References

	Year	Citations

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