• Acs Med Chem Lett · Aug 2014

    Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.

    • Stefan Schunk, Klaus Linz, Claudia Hinze, Sven Frormann, Stefan Oberbörsch, Bernd Sundermann, Saskia Zemolka, Werner Englberger, Tieno Germann, Thomas Christoph, Babette-Y Kögel, Wolfgang Schröder, Stephanie Harlfinger, Derek Saunders, Achim Kless, Hans Schick, and Helmut Sonnenschein.
    • Departments of Medicinal Chemistry, Preclinical Drug Safety, Molecular Pharmacology, Pain Pharmacology, Pharmacokinetics, and Discovery Informatics, Global Drug Discovery, Grünenthal Innovation, Grünenthal GmbH , D-52099 Aachen, Germany.
    • Acs Med Chem Lett. 2014 Aug 14;5(8):857-62.

    AbstractIn a previous communication, our efforts leading from 1 to the identification of spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amine 2a as analgesic NOP and opioid receptor agonist were disclosed and their favorable in vitro and in vivo pharmacological properties revealed. We herein report our efforts to further optimize lead 2a, toward trans-6'-fluoro-4',9'-dihydro-N,N-dimethyl-4-phenyl-spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-b]indol]-4-amine (cebranopadol, 3a), which is currently in clinical development for the treatment of severe chronic nociceptive and neuropathic pain.

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