Pharmacology of Basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression

Journal of Pharmacology and Experimental Therapeutics

Volumn 353, Issue 1, 2015, Pages 213-233

  Lindemann, Lothar ^a   Porter, Richard H ^c   Scharf, Sebastian H ^a   Kuennecke, Basil ^a   Bruns, Andreas ^a   Von Kienlin, Markus ^a   Harrison, Anthony C ^d   Paehler, Axel ^d   Funk, Christoph ^d   Gloge, Andreas ^d   Schneider, Manfred ^d   Parrott, Neil J ^d   Polonchuk, Liudmila ^d   Niederhauser, Urs ^d   Morairty, Stephen R ^a,f   Kilduff, Thomas S ^a,f   Vieira, Eric ^b   Kolczewski, Sabine ^b   Wichmann, Juergen ^b   Hartung, Thomas ^e   Honer, Michael ^a   Borroni, Edilio ^a   Moreau, Jean Luc ^c   Prinssen, Eric ^a   Spooren, Will ^a   Wettstein, Joseph G ^a   Jaeschke, Georg ^b   more..

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b Metabolism and Pharmacokinetics   (Switzerland)

^c and Rare Diseases   (Switzerland)

^d Pharmaceutical Sciences ^*  (Switzerland)

^e Small Molecules Process Research and Synthesis   (Switzerland)

^f SRI INTERNATIONAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 CHLORO 4 [[2,5 DIMETHYL 1 [4 (TRIFLUOROMETHOXY)PHENYL] 1H IMIDAZOL 4 YL]ETHYNYL]PYRIDINE; 2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; 3 [(2 METHYL 4 THIAZOLYL)ETHYNYL]PYRIDINE; BASIMGLURANT; CAFFEINE; DIAZEPAM; DOPAMINE; DULOXETINE; FENOBAM; FLUOXETINE; METABOTROPIC RECEPTOR 5; METABOTROPIC RECEPTOR ANTAGONIST; MONOAMINE; MORPHINE; PAROXETINE; UNCLASSIFIED DRUG; VESICULAR MONOAMINE TRANSPORTER; 2-CHLORO-4-(1-(4-FLUOROPHENYL)-2,5-DIMETHYL-1H-IMIDAZOL-4-YLETHYNYL)PYRIDINE; ANTIDEPRESSANT AGENT; ANXIOLYTIC AGENT; BIOGENIC AMINE; IMIDAZOLE DERIVATIVE; PYRIDINE DERIVATIVE;

ADULT; ALLODYNIA; ANHEDONIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIDEPRESSANT ACTIVITY; ANTINOCICEPTION; ANXIETY; APATHY; ARTICLE; COMORBIDITY; CONTROLLED STUDY; DAYTIME SOMNOLENCE; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG MEGADOSE; DRUG PENETRATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ELECTROENCEPHALOGRAPHY; FEMALE; FRONTAL CORTEX; FUNCTIONAL MAGNETIC RESONANCE IMAGING; HUMAN; HUMAN CELL; HUMAN TISSUE; IN VITRO STUDY; IN VIVO STUDY; LETHARGY; MAJOR DEPRESSION; MALE; MOUSE; NONHUMAN; NONREM SLEEP; NUCLEUS ACCUMBENS; OVERACTIVE BLADDER; PAIN; PRIORITY JOURNAL; RAT; SINGLE DRUG DOSE; TRANQUILIZING ACTIVITY; WAKEFULNESS; ALLOSTERISM; ANIMAL; ANTAGONISTS AND INHIBITORS; BRAIN; CELL CULTURE; CRICETULUS; DEPRESSION; INVERSE AGONISM; MACACA FASCICULARIS; METABOLISM; PATHOPHYSIOLOGY; PSYCHOLOGY; RADIOASSAY; SPRAGUE DAWLEY RAT; URINARY BLADDER, OVERACTIVE; WISTAR RAT;

ALLOSTERIC REGULATION; ANIMALS; ANTI-ANXIETY AGENTS; ANTIDEPRESSIVE AGENTS; BIOGENIC MONOAMINES; BRAIN; CELLS, CULTURED; CRICETULUS; DEPRESSION; DRUG INVERSE AGONISM; ELECTROENCEPHALOGRAPHY; FEMALE; IMIDAZOLES; MACACA FASCICULARIS; MALE; MICE; PAIN; PYRIDINES; RADIOLIGAND ASSAY; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; RECEPTOR, METABOTROPIC GLUTAMATE 5; URINARY BLADDER, OVERACTIVE;

EID: 84928926411     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.114.222463     Document Type: Article

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