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2912170 
Journal Article 
Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol 
Schunk, S; Linz, K; Hinze, C; Frormann, S; Oberboersch, S; Sundermann, B; Zemolka, S; Englberger, W; Germann, T; Christoph, T; Koegel, BY; Schroeder, W; Harlfinger, S; Saunders, D; Kless, A; Schick, H; Sonnenschein, H 
2014 
Yes 
ACS Medicinal Chemistry Letters
ISSN: 1948-5875 
5 
8 
857-862 
English 
25147603 
WOS:000340439300007 
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. 
NOP receptor agonists; MOP receptor agonists; cebranopadol; analgesics