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ACS Med Chem Lett. 2014 Jun 24;5(8):857-62. doi: 10.1021/ml500117c. eCollection 2014 Aug 14.

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

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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.
ASCA GmbH Angewandte Synthesechemie Adlershof , Magnusstr. 11, 12489 Berlin, Germany.


In 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.


MOP receptor agonists; NOP receptor agonists; analgesics; cebranopadol

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