Research ArticleDrug Discovery and Translational Medicine
Pharmacology of Basimglurant (RO4917523, RG7090), a Unique Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator in Clinical Development for Depression
Lothar Lindemann, Richard H. Porter, Sebastian H. Scharf, Basil Kuennecke, Andreas Bruns, Markus von Kienlin, Anthony C. Harrison, Axel Paehler, Christoph Funk, Andreas Gloge, Manfred Schneider, Neil J. Parrott, Liudmila Polonchuk, Urs Niederhauser, Stephen R. Morairty, Thomas S. Kilduff, Eric Vieira, Sabine Kolczewski, Juergen Wichmann, Thomas Hartung, Michael Honer, Edilio Borroni, Jean-Luc Moreau, Eric Prinssen, Will Spooren, Joseph G. Wettstein and Georg Jaeschke
Journal of Pharmacology and Experimental Therapeutics April 2015, 353 (1) 213-233; DOI: https://doi.org/10.1124/jpet.114.222463
Lothar Lindemann
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Richard H. Porter
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Sebastian H. Scharf
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Basil Kuennecke
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Andreas Bruns
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Markus von Kienlin
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Anthony C. Harrison
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Axel Paehler
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Christoph Funk
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Andreas Gloge
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Manfred Schneider
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Neil J. Parrott
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Liudmila Polonchuk
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Urs Niederhauser
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Stephen R. Morairty
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Thomas S. Kilduff
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Eric Vieira
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Sabine Kolczewski
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Juergen Wichmann
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Thomas Hartung
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Michael Honer
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Edilio Borroni
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Jean-Luc Moreau
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Eric Prinssen
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Will Spooren
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Joseph G. Wettstein
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
Georg Jaeschke
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases (L.L., S.H.S., B.K., A.B., M.v.K., M.H., E.B., E.P., W.S., J.G.W.), Discovery Chemistry (E.V., S.K., J.W., G.J.), Operations for Neuroscience, Ophthalmology, and Rare Diseases (R.H.P., J.-L.M.), Pharmaceutical Sciences (A.C.H., A.P., C.F., A.G., M.S., N.J.P., L.P., U.N.), and Small Molecules Process Research and Synthesis (T.H.), Roche Innovation Center Basel, Basel, Switzerland; and Center for Neuroscience, Biosciences Division, SRI International, Menlo Park, California (S.R.M., T.S.K.)
JPET articles become freely available 12 months after publication, and remain freely available for 5 years.Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page.
|
Log in using your username and password
Purchase access
You may purchase access to this article. This will require you to create an account if you don't already have one.
In this issue
Research ArticleDrug Discovery and Translational Medicine
Basimglurant, an mGlu5 NAM in Development for Depression
Lothar Lindemann, Richard H. Porter, Sebastian H. Scharf, Basil Kuennecke, Andreas Bruns, Markus von Kienlin, Anthony C. Harrison, Axel Paehler, Christoph Funk, Andreas Gloge, Manfred Schneider, Neil J. Parrott, Liudmila Polonchuk, Urs Niederhauser, Stephen R. Morairty, Thomas S. Kilduff, Eric Vieira, Sabine Kolczewski, Juergen Wichmann, Thomas Hartung, Michael Honer, Edilio Borroni, Jean-Luc Moreau, Eric Prinssen, Will Spooren, Joseph G. Wettstein and Georg Jaeschke
Journal of Pharmacology and Experimental Therapeutics April 1, 2015, 353 (1) 213-233; DOI: https://doi.org/10.1124/jpet.114.222463
Research ArticleDrug Discovery and Translational Medicine
Basimglurant, an mGlu5 NAM in Development for Depression
Lothar Lindemann, Richard H. Porter, Sebastian H. Scharf, Basil Kuennecke, Andreas Bruns, Markus von Kienlin, Anthony C. Harrison, Axel Paehler, Christoph Funk, Andreas Gloge, Manfred Schneider, Neil J. Parrott, Liudmila Polonchuk, Urs Niederhauser, Stephen R. Morairty, Thomas S. Kilduff, Eric Vieira, Sabine Kolczewski, Juergen Wichmann, Thomas Hartung, Michael Honer, Edilio Borroni, Jean-Luc Moreau, Eric Prinssen, Will Spooren, Joseph G. Wettstein and Georg Jaeschke
Journal of Pharmacology and Experimental Therapeutics April 1, 2015, 353 (1) 213-233; DOI: https://doi.org/10.1124/jpet.114.222463
Jump to section
Related Articles
Cited By...
More in this TOC Section
Similar Articles
Advertisement