Pharmacological profile of the NOP agonist and cough suppressing agent SCH 486757 (8-[Bis(2-Chlorophenyl)Methyl]-3-(2-Pyrimidinyl)-8-Azabicyclo[3.2.1]Octan-3-Ol) in preclinical models

We describe the pharmacological and pharmacokinetic profiles of SCH 486757, a nociceptin/orphanin FQ peptide (NOP) receptor agonist that has recently entered human clinical trials for cough. SCH 486757 selectively binds human NOP receptor (K(i) = 4.6 ± 0.61 nM) over classical opioid receptors. In a...

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Hauptverfasser: McLeod, Robbie L., Tulshian, Deen B., Bolser, Donald C., Varty, Geoffrey B., Baptista, Marco, Fernandez, Xiomara, Parra, Leonard E., Zimmer, Jennifer C., Erickson, Christine H., Ho, Ginny D., Jia, Yanlin, Ng, Fay W., Korfmacher, Walter, Xu, Xiaoying, Veals, John, Smith-Torhan, April, Wainhaus, Samuel, Fawzi, Ahmad B., Austin, Theodore M., van Heek, Margaret, Hey, John A.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2009
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC2922759/
https://ncbi.nlm.nih.gov/pubmed/20006596
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.ejphar.2009.12.003
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