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Xenobiotica
the fate of foreign compounds in biological systems
Volume 47, 2017 - Issue 2
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Clinical Pharmacokinetics and Metabolism

A double-tracer technique to characterize absorption, distribution, metabolism and excretion (ADME) of [14C]-basimglurant and absolute bioavailability after oral administration and concomitant intravenous microdose administration of [13C6]-labeled basimglurant in humans

Elena GueriniRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and Correspondence[email protected]
,
Simone SchadtRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
,
Gerard GreigRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
,
Ruth HaasRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
,
Christophe HusserRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
,
Manfred ZellRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
,
Christoph FunkRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
,
Thomas HartungRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
,
Andreas GlogeRoche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Basel, Switzerland and
&
Navita L. MallalieuRoche Pharmaceutical Research and Early Development, Roche Innovation Center NYC, NY, USA
 show all
Pages 144-153 | Received 01 Feb 2016, Accepted 18 Mar 2016, Published online: 28 Apr 2016

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Kyle A. Emmitte. (2017) mGlu5 negative allosteric modulators: a patent review (2013 - 2016). Expert Opinion on Therapeutic Patents 27:6, pages 691-706.
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Renzo Rossi & Maurizio Ciofalo. (2019) Current Advances in the Synthesis and Biological Evaluation of Pharmacologically Relevant 1,2,4,5-Tetrasubstituted-1H-Imidazole Derivatives. Current Organic Chemistry 23:19, pages 2016-2101.
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Thomas K. David, Nayak K. Prashanth, M. Rajendraswami, Devendrareddy Pallalu, Arlindo L. Castelhano, Michael J. Kates, Anna L. Blobaum, Carrie K. Jones, Kyle A. Emmitte, P. Jeffrey Conn & Craig W. Lindsley. (2017) Development and kilogram-scale synthesis of mGlu5 negative allosteric modulator VU0424238 (auglurant). Tetrahedron Letters 58:36, pages 3554-3558.
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Andrew S. Felts, Alice L. Rodriguez, Anna L. Blobaum, Ryan D. Morrison, Brittney S. Bates, Analisa Thompson Gray, Jerri M. Rook, Mohammed N. Tantawy, Frank W. Byers, Sichen Chang, Daryl F. Venable, Vincent B. Luscombe, Gilles D. Tamagnan, Colleen M. Niswender, J. Scott Daniels, Carrie K. Jones, P. Jeffrey Conn, Craig W. Lindsley & Kyle A. Emmitte. (2017) Discovery of N -(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation . Journal of Medicinal Chemistry 60:12, pages 5072-5085.
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Stephen Fowler, Elena Guerini, NaHong Qiu, Yumi Cleary, Neil Parrott, Gerard Greig & Navita L. Mallalieu. (2017) Low Potential of Basimglurant to Be Involved in Drug-Drug Interactions: Influence of Non–Michaelis-Menten P450 Kinetics on Fraction Metabolized. Journal of Pharmacology and Experimental Therapeutics 360:1, pages 164-173.
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