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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Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2009
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Article
On-line přístup: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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