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Research ArticleNeuropharmacology

Cebranopadol: A Novel Potent Analgesic Nociceptin/Orphanin FQ Peptide and Opioid Receptor Agonist

Klaus Linz, Thomas Christoph, Thomas M. Tzschentke, Thomas Koch, Klaus Schiene, Michael Gautrois, Wolfgang Schröder, Babette Y. Kögel, Horst Beier, Werner Englberger, Stefan Schunk, Jean De Vry, Ulrich Jahnel and Stefanie Frosch
Journal of Pharmacology and Experimental Therapeutics June 2014, 349 (3) 535-548; DOI: https://doi.org/10.1124/jpet.114.213694
Klaus Linz
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Thomas Christoph
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Thomas M. Tzschentke
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Thomas Koch
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Klaus Schiene
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Michael Gautrois
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Wolfgang Schröder
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Babette Y. Kögel
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Horst Beier
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Werner Englberger
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Stefan Schunk
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Jean De Vry
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Ulrich Jahnel
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Stefanie Frosch
Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
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Article Information

vol. 349 no. 3 535-548
DOI 
https://doi.org/10.1124/jpet.114.213694
PubMed 
24713140

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0022-3565
Online ISSN 
1521-0103
History 
  • Received February 23, 2014
  • Accepted April 7, 2014
  • Published online May 8, 2014.

Article Versions

  • Earlier version (April 8, 2014 - 12:30).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Klaus Linz,
  2. Thomas Christoph,
  3. Thomas M. Tzschentke,
  4. Thomas Koch,
  5. Klaus Schiene,
  6. Michael Gautrois,
  7. Wolfgang Schröder,
  8. Babette Y. Kögel,
  9. Horst Beier,
  10. Werner Englberger,
  11. Stefan Schunk,
  12. Jean De Vry,
  13. Ulrich Jahnel, and
  14. Stefanie Frosch
  1. Departments of Preclinical Drug Safety (K.L.), Global Preclinical Drug Development (S.F.), Global Preclinical Research and Development (U.J.), Pain Pharmacology (T.C., T.M.T., K.S., B.Y.K., J.D.V.), Molecular Pharmacology (T.K., W.E.), Translational Science (W.S.), Pharmacokinetics (M.G., H.B.), and Medicinal Chemistry (S.S.), Grünenthal GmbH, Aachen, Germany
  1. Address correspondence to:
    Dr. Klaus Linz, Grünenthal GmbH, Preclinical Research and Development, Department of Preclinical Drug Safety, Zieglerstrasse 6, 52078 Aachen, Germany. E-mail: Klaus.Linz{at}grunenthal.com
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Journal of Pharmacology and Experimental Therapeutics: 349 (3)
Journal of Pharmacology and Experimental Therapeutics
Vol. 349, Issue 3
1 Jun 2014
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Research ArticleNeuropharmacology

Cebranopadol: A Potent NOP/Opioid Receptor Agonist Analgesic

Klaus Linz, Thomas Christoph, Thomas M. Tzschentke, Thomas Koch, Klaus Schiene, Michael Gautrois, Wolfgang Schröder, Babette Y. Kögel, Horst Beier, Werner Englberger, Stefan Schunk, Jean De Vry, Ulrich Jahnel and Stefanie Frosch
Journal of Pharmacology and Experimental Therapeutics June 1, 2014, 349 (3) 535-548; DOI: https://doi.org/10.1124/jpet.114.213694

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Research ArticleNeuropharmacology

Cebranopadol: A Potent NOP/Opioid Receptor Agonist Analgesic

Klaus Linz, Thomas Christoph, Thomas M. Tzschentke, Thomas Koch, Klaus Schiene, Michael Gautrois, Wolfgang Schröder, Babette Y. Kögel, Horst Beier, Werner Englberger, Stefan Schunk, Jean De Vry, Ulrich Jahnel and Stefanie Frosch
Journal of Pharmacology and Experimental Therapeutics June 1, 2014, 349 (3) 535-548; DOI: https://doi.org/10.1124/jpet.114.213694
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