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Molecular Pharmacology

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Research ArticleArticle

Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-Bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-Selective Negative Allosteric Modulators

Christina Mølck, Kasper Harpsøe, David E. Gloriam, Rasmus P. Clausen, Ulf Madsen, Lars Ø. Pedersen, Hermogenes N. Jimenez, Søren M. Nielsen, Jesper M. Mathiesen and Hans Bräuner-Osborne
Molecular Pharmacology November 2012, 82 (5) 929-937; DOI: https://doi.org/10.1124/mol.112.078808
Christina Mølck
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Kasper Harpsøe
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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David E. Gloriam
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Rasmus P. Clausen
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Ulf Madsen
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Lars Ø. Pedersen
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Hermogenes N. Jimenez
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Søren M. Nielsen
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Jesper M. Mathiesen
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Hans Bräuner-Osborne
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
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Article Information

vol. 82 no. 5 929-937
DOI 
https://doi.org/10.1124/mol.112.078808
PubMed 
22899869

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0026-895X
Online ISSN 
1521-0111
History 
  • Received March 31, 2012
  • Accepted August 16, 2012
  • Published online October 18, 2012.

Article Versions

  • Earlier version (August 16, 2012 - 07:19).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2012 The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Christina Mølck,
  2. Kasper Harpsøe,
  3. David E. Gloriam,
  4. Rasmus P. Clausen,
  5. Ulf Madsen,
  6. Lars Ø. Pedersen,
  7. Hermogenes N. Jimenez,
  8. Søren M. Nielsen,
  9. Jesper M. Mathiesen, and
  10. Hans Bräuner-Osborne
  1. Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (C.M., D.E.G., R.P.C., U.M., J.M.M., H.B.-O.); NNF Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (K.H.); Department for Biologics (L.Ø.P.) and Department of Molecular Pharmacology (S.M.N.), H. Lundbeck A/S, Valby, Denmark; and Department of Chemical and Pharmacokinetic Science, Lundbeck Research USA, Paramus, New Jersey (H.N.J.)
  1. Address correspondence to:
    Dr. Hans Bräuner-Osborne, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Fruebjergvej 3, DK-2100 Copenhagen. E-mail: hbo{at}sund.ku.dk
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Molecular Pharmacology: 82 (5)
Molecular Pharmacology
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1 Nov 2012
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Research ArticleArticle

Binding Site Characterization of Novel NAMs on mGluR5

Christina Mølck, Kasper Harpsøe, David E. Gloriam, Rasmus P. Clausen, Ulf Madsen, Lars Ø. Pedersen, Hermogenes N. Jimenez, Søren M. Nielsen, Jesper M. Mathiesen and Hans Bräuner-Osborne
Molecular Pharmacology November 1, 2012, 82 (5) 929-937; DOI: https://doi.org/10.1124/mol.112.078808

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Research ArticleArticle

Binding Site Characterization of Novel NAMs on mGluR5

Christina Mølck, Kasper Harpsøe, David E. Gloriam, Rasmus P. Clausen, Ulf Madsen, Lars Ø. Pedersen, Hermogenes N. Jimenez, Søren M. Nielsen, Jesper M. Mathiesen and Hans Bräuner-Osborne
Molecular Pharmacology November 1, 2012, 82 (5) 929-937; DOI: https://doi.org/10.1124/mol.112.078808
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