mGlu5 receptor antagonists and their therapeutic potential

Bibliography

• Brauner-Osborne H, Wellendorph P, Jensen AA. Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors. Curr Drug Targets 2007;8:169-84
   PubMed Web of Science ®Google Scholar
• Nakanishi S. Molecular diversity of glutamate receptors and implications for brain function. Science 1992;258:597-603
   PubMed Web of Science ®Google Scholar
• Schoepp DD, Conn PJ. Metabotropic glutamate receptors in brain function and pathology. Trends Pharmacol Sci 1993;14:13-20
   PubMed Web of Science ®Google Scholar
• Parsons CG, Danysz W, Quack G. Glutamate in CNS disorders as a target for drug development: an update. Drug News Perspect 1998;11:523-69
   PubMed Web of Science ®Google Scholar
• Pin JP, Kniazeff J, Liu J, et al. Allosteric functioning of dimeric class C G-protein-coupled receptors. FEBS J 2005;272:2947-55
   PubMed Web of Science ®Google Scholar
• Romano C, Miller JK, Hyrc K, et al. Covalent and noncovalent interactions mediate metabotropic glutamate receptor mGlu5 dimerization. Mol Pharmacol 2001;59:46-53
   PubMed Web of Science ®Google Scholar
• Johnson MP, Nisenbaum ES, Large TH, et al. Allosteric modulators of metabotropic glutamate receptors: lessons learnt from mGlu1, mGlu2 and mGlu5 potentiators and antagonists. Biochem Soc Trans 2004;32:881-7
   PubMedGoogle Scholar
• Pin JP, Goudet C, Hlavackova V, et al. Dimeric GPCRs: what did we learn from the metabotropic glutamate receptors? In: Insights into Receptor Function and New Drug Development Targets. Conn M, Kordon C, Christen Y, editors. Heidelberg, Springer-Verlag; 2006
   Google Scholar
• Spooren W, Ballard T, Gasparini F, et al. Insight into the function of Group I and Group II metabotropic glutamate (mGlu) receptors: behavioural characterization and implications for the treatment of CNS disorders. Behav Pharmacol 2003;14:257-77
   PubMedGoogle Scholar
• Yu M, Tueckmantel W, Wang X, et al. Methoxyphenylethynyl, methoxypyridylethynyl and phenylethynyl derivatives of pyridine: synthesis, radiolabeling and evaluation of new PET ligands for metabotropic glutamate subtype 5 receptors. Nucl Med Biol 2005;32:631-40
   PubMedGoogle Scholar
• Ferraguti F, Shigemoto R. Metabotropic glutamate receptors. Cell Tissue Res 2006;326:483-504
   PubMed Web of Science ®Google Scholar
• Schoepp DD, Jane DE, Monn JA. Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 1999;38:1431-76
   PubMed Web of Science ®Google Scholar
• Varney MA, Cosford NDP, Jachec C, et al. SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J Pharmacol Exp Ther 1999;290:170-81
   PubMed Web of Science ®Google Scholar
• Gasparini F, Lingenhohl K, Stoehr N, et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 1999;38:1493-503
   PubMed Web of Science ®Google Scholar
• Cosford NDP, Tehrani L, Arruda J, et al. 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl) pyridine (MTEP): design and synthesis of a potent and highly selective metabotropic glutamate subtype 5 (Mglu5) receptor antagonist with anxiolytic activity. Neuropharmacology 2002;43:282-3
   Google Scholar
• Porter RHP, Jaeschke G, Spooren W, et al. Fenobam: A clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther 2005;315:711-21
   PubMed Web of Science ®Google Scholar
• Malherbe P, Kratochwil N, Muhlemann A, et al. Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP. J Neurochemistry 2006;98:601-15
   PubMedGoogle Scholar
• Pecknold JC, McClure DJ, Appeltauer L, et al. Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study. J Clin Psychopharmacol 1982;2:129-33
   PubMed Web of Science ®Google Scholar
• Bach P, Isaac M, Slassi A. Metabotropic glutamate receptor 5 modulators. Expert Opin Ther Patents 2007;17:371-84 • A recent review on mGlu5 modulators.
   Web of Science ®Google Scholar
• Rodriguez AL, Williams R. Recent progress in the development of allosteric modulators of mGluR5. Curr Opin Drug Discov Dev 2007;10:715-22
   PubMedGoogle Scholar
• Movsesyan VA, O'Leary DM, Fan L, et al. mGluR5 antagonists 2-methyl-6-(phenylethynyl)-pyridine and (E)-2-methyl-6-(2-phenylethenyl)-pyridine reduce traumatic neuronal injury in vitro and in vivo by antagonizing N-methyl-D-aspartate receptors. J Pharmacol Exp Ther 2001;296:41-7
   PubMed Web of Science ®Google Scholar
• Smith ND, Poon SF, Huang D, et al. Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. Bioorg Med Chem Lett 2004;14:5481-4
   PubMedGoogle Scholar
• Milbank JBJ, Knauer CS, Augelli-Szafran CE, et al. Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett 2007;17:4415-8
   PubMedGoogle Scholar
• Bolea C, Mutel V, Rocher J-P, et al. Addex Pharmaceuticals, Switzerland. Preparation of novel aminopyridine derivatives as mGluR5 antagonists. WO2004078728 (2004)
   Google Scholar
• Bessis A-S, Bolea C, Bonnet B, et al. Addex Pharmaceuticals, Switzerland. Preparation of heterocycle-containing alkynyl derivatives as modulators of metabotropic glutamate receptors. WO2005123703 (2005)
   Google Scholar
• Gasparini F, Auberson Y, Ofner S. Novartis, Switzerland. Preparation of acetylene derivatives having mGluR 5 antagonistic activity. WO2003047581 (2003)
   Google Scholar
• Rouzade-Dominguez M-L, Pfannkuche H-J, Gasparini F. Novartis, Switzerland. Use of phenylethynyl derivative metabotropic glutamate receptor 5 (mGluR5) antagonists for the treatment of gastrointestinal tract, urinary tract, and post-operative disorders and associated pain. WO2007006530 (2007)
   Google Scholar
• Glatthar R, Troxler TJ. Novartis, Switzerland. Phenylacetylene derivatives having mGluR5 receptor affinity and their preparation, pharmaceutical compositions and use in the treatment of CNS disorders. WO2006114260 (2006)
   Google Scholar
• Glatthar R, Troxler TJ, Zoller T, et al. Novartis, Switzerland. Arylacetylene derivatives as mGluR5 modulators and their preparation, pharmaceutical compositions and their use in the treatment of CNS disorders. WO2006114262 (2006)
   Google Scholar
• Glatthar R, Troxler TJ. Novartis, Switzerland. Phenylacetylene derivatives as mGluR5 modulators and their preparation, pharmaceutical compositions and use in the treatment of CNS disorders. WO2006114264 (2006)
   Google Scholar
• Glatthar R, Troxler TJ, Zoller T, et al. Novartis, Switzerland. Preparation of pyrrolidine and piperidine acetylene derivatives for use as mGluR5 antagonists. WO2006089700 (2006)
   Google Scholar
• Hintermann S, Vranesic I, Allgeier H, et al. ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies. Bioorg Med Chem 2007;15:903-14
   PubMed Web of Science ®Google Scholar
• Ametamey SM, Kessler LJ, Honer M, et al. Radiosynthesis and preclinical evaluation of 11C-ABP688 as a probe for imaging the metabotropic glutamate receptor subtype 5. J Nucl Med 2006;47:698-705
   PubMed Web of Science ®Google Scholar
• Ametamey SM, Treyer V, Streffer J, et al. Human PET studies of metabotropic glutamate receptor subtype 5 with 11C-ABP688. J Nucl Med 2007;48:247-52
   PubMed Web of Science ®Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. Preparation of (1H-imidazol-4-yl)ethynylpyridines as metabotropic glutamate 5 receptor antagonists for treating neurodegenerative diseases, in particular anxiety. WO2004080998 (2004)
   Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. A preparation of (pyridin-4-ylethynyl)imidazole derivatives, useful for the treatment of mGluR5 receptor mediated disorders. WO2004108701 (2004)
   Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. Preparation of heteroarylphenylethynylimidazoles for treatment of mGluR5 receptor mediated disorders. WO2004111040 (2004)
   Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. A preparation of 4-(imidazol-4-ylethynyl)pyridine derivatives, useful as mGluR5 receptor antagonists. WO2005003117 (2005)
   Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. Preparation of aralkynylimidazoles as metabotropic glutamate mGluR5 receptor antagonists for treatment of neurological disorders. WO2005023795 (2005)
   Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. A preparation of (pyridin-4-ylethynyl)imidazole derivatives, useful for the treatment of mGluR5 receptor mediated disorders. US2005143375 (2005)
   Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. Preparation of pyridin-4-ylethynylimidazoles and -pyrazoles as mGluR5a receptor antagonists. WO2005118568 (2005)
   Google Scholar
• Cosford NDP, McDonald IA, Bleicher LS, et al. Merck & Co., USA. Preparation of heterocyclic compounds as metabotropic glutamate receptor 5 (mGluR5) modulators. WO2001016121 (2001)
   Google Scholar
• Roppe JR, Wang B, Huang D, et al. 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3′-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. Bioorg Med Chem Lett 2004;14:3993-6
   PubMedGoogle Scholar
• Cosford ND, Kamenecka T, Roppe JR. Merck & Co., USA. A preparation of imidazolyl- and pyrazolyl-ethyne derivatives, useful as modulators of receptors in the nervous system. US2005085523 (2005)
   Google Scholar
• Cosford ND, Roppe JR, Tehrani LR, et al. Merck & Co., USA. Preparation of pyridazine, pyrimidine and pyrazine ethyne compounds. US2005043307 (2005)
   Google Scholar
• Cosford ND, Seiders TJ, Payne J, et al. Merck & Co., USA. Thiazolyl derivatives as mGluR5 antagonists and their preparation and methods for their use. WO2007050050 (2007)
   Google Scholar
• Bach P, Nilsson K, Svensson T, et al. Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5). Bioorg Med Chem Lett 2006;16:4788-91
   PubMedGoogle Scholar
• Bach P, Nilsson K, Wallberg A, et al. A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5). Bioorg Med Chem Lett 2006;16:4792-5
   PubMedGoogle Scholar
• Bach P, Bauer U, Nilsson K, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of phenylthioalkyl or phenylaminoalkyl pyridinylalkynes for treating gestroesophageal reflux disease. WO2005044267 (2005)
   Google Scholar
• Bach P, Bauer U, Nilsson K, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of phenylalkyl pyridinyl alkynes for treating gestroesophageal reflux disease. WO2005044266 (2005)
   Google Scholar
• Bach P, Bauer U, Nilsson K, et al. Astrazeneca AB, Sweden; NPS Pharmaceuticals, USA. Preparation of phenoxyalkyl pyridinyl alkynes for treating gestroesophageal reflux disease. WO2005044265 (2005)
   Google Scholar
• Bryan C, Isaac M, Stefanac T. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of substituted alkynyl piperazines as metabotropic glutamate receptor antagonists. WO2005080363 (2005)
   Google Scholar
• Agejas-Chicharro FJ, Dressman BA, Gutierrez Sanfeliciano S, et al. Eli Lilly, USA. Preparation of pyridines as mGlu5 receptor antagonists. WO2005094822 (2005)
   Google Scholar
• Gharagozloo P, Islam K, Kyle DJ, et al. Euro-Celtique, Luxembourg. Preparation of 1-(pyrid-2-yl)piperazines as metabotropic glutamate receptor inhibitor. WO2003093236 (2003)
   Google Scholar
• Chen Z, Tafesse L. Euro-Celtique, Luxembourg. Preparation of alkynylpiperazinylpyrimidines as mGluR5 receptor function inhibitors for treatment of pain, addiction, Parkinson's disease, etc. WO2004029044 (2004)
   Google Scholar
• Gharagozloo, P. Euro-Celtique, Luxembourg. Preparation of pyridine/pyrimidine derivatives as mGluR1 and mGluR5 ligands useful for treating pain. WO2005035500 (2005)
   Google Scholar
• Kuehnert S, Oberboersch S, Haurand M, et al. Gruenenthal GmbH, Germany. Preparation of 1-(1-oxo-2-propynyl)piperazines as mGluR5 receptor modulators for the treatment of pain. WO2006002981 (2006)
   Google Scholar
• Kuehnert S, Oberboersch S, Sundermann C, et al. Gruenenthal GmbH, Germany. Preparation of imidazo[1,2-a]pyridin-3-amines and related compounds as mGlur5 receptor modulators. WO2006029980 (2006)
   Google Scholar
• Kuehnert S, Reich M, Zemolka S, et al. Gruenenthal, Germany. Preparation of thiazoles as mGluR5 receptor inhibitors. WO2007079961 (2007)
   Google Scholar
• Kuehnert S, Reich M, Zemolka S, et al. Gruenenthal, Germany. Preparation of thiazoles as mGluR5 receptor inhibitors. WO2007079960 (2007)
   Google Scholar
• Kuehnert S, Reich M, Zemolka S, et al. Gruenenthal, Germany. Preparation of propiolamides as mGluR5 receptor inhibitors. WO2007079957 (2007)
   Google Scholar
• Kuehnert S, Oberboersch S, Haurand M, et al. Gruenenthal, Germany. Preparation of N-ethylpropiolamides as mGluR5 receptor inhibitors. WO2007079958 (2007)
   Google Scholar
• Jirgensons A, Parsons CGR, Jaunzeme I, et al. Merz, Germany. Tetrahydroquinolones as modulators of metabotropic glutamate receptors, their preparation, pharmaceutical compositions, and use in therapy. US2005288284 (2005)
   Google Scholar
• Van Wagenen BC, Stormann TM, Moe ST, et al. NPS Pharmaceuticals, USA. Preparation of 3-(2-pyridyl)-5-phenyl substituted 1,2,4-oxadiazoles, 1,2-oxazoles and 1,2,4-triazoles as metabotropic glutamate receptor antagonists. WO2001012627 (2001)
   Google Scholar
• Wensbo D, Xin T, Stefanac T, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of [1,2,4]oxadiazole derivatives as mGluR5 receptor inhibitors. WO2004014902 (2004)
   Google Scholar
• McLeod DA, Kers A, Malmberg J, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of heterocyclic compounds having an activity at metabotropic glutamate receptors (mGluRs). WO2004014370 (2004)
   Google Scholar
• Minidis A, Wensbo D, Slassi A, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of 5-(phenylisoxazolylethoxy)triazol-3-yl substituted pyridines for treating neurological, psychiatric or pain disorders. WO2007040982 (2007)
   Google Scholar
• Arora J, Edwards L, Isaac M, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Synthesis of polyheterocyclic compounds as metabotropic glutamate receptor antagonists. WO2005080386 (2005)
   Google Scholar
• Edwards L, Isaac M, Johansson M, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists. US2005272779 (2005)
   Google Scholar
• Johansson M, Minidis A, Staaf K, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of tetrazole compounds and their use as metabotropic glutamate receptor antagonists. WO2005080356 (2005)
   Google Scholar
• Edwards L, Isaac M, Johansson M, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of triazoles as mGluR5 metabotropic glutamate receptor antagonists. WO2005080379 (2005)
   Google Scholar
• Edwards L, Slassi A, Isaac M, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Preparation of substituted piperazines as metabotropic glutamate receptor antagonists. WO2007021573 (2007)
   Google Scholar
• Edwards L, Isaac M, Slassi A, et al. Astrazeneca, Sweden; NPS Pharmaceuticals, USA. Bicyclic piperazines as metabotropic glutamate receptor antagonists. WO2007021574 (2007)
   Google Scholar
• Hammerland LG, Johansson M, Malmstroem J, et al. Structure-activity relationship of thiopyrimidines as mGluR5 antagonists. Bioorg Med Chem Lett 2006;16:2467-9
   PubMedGoogle Scholar
• Cosford NDP, Smith ND, Huang D. Merck & Co., USA. Heteroaryl substituted pyrrole modulators of metabotropic glutamate receptor-5. WO2003059904 (2003)
   Google Scholar
• Cosford NDP, Huang D, Roppe JR, et al. Merck & Co., USA. Preparation of diaryl substituted pyrrole modulators of metabotropic glutamate receptor -5. WO2004089308 (2004)
   Google Scholar
• Cosford NDP, Chen C, Eastman BW, et al. Merck & Co., USA. Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5. WO2003051833 (2003)
   Google Scholar
• Cosford NDP, Eastman BW, Huang D, et al. Merck & Co., USA. Preparation of diaryl substituted pyrazole modulators of metabotropic glutamate receptor -5. WO2004089303 (2004)
   Google Scholar
• Cosford NDP, Huang D, Smith ND, et al. Merck & Co., USA. A preparation of imidazole derivatives, useful as modulators of metabotropic glutamate receptor -5 (mGluR5). WO2004087653 (2004)
   Google Scholar
• Cosford NDP, Smith ND, Huang D. Merck & Co., USA. Heteroaryl substituted imidazole modulators of metabotropic glutamate receptor-5. WO2003053922 (2003)
   Google Scholar
• Cosford NDP, Tehrani LR, Roppe JR, et al. Merck & Co., USA. Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5. WO2003051315 (2003)
   Google Scholar
• Cosford NDP, Roppe JR, Tehrani LR, et al. Merck & Co., USA. Preparation of diaryl substituted triazole modulators of metabotropic glutamate receptor-5. WO2004089306 (2004)
   Google Scholar
• Cosford ND, Roppe J, Chen C, et al. Merck & Co., USA. Heteroaryl substituted tetrazole modulators of metabotropic glutamate receptor-5. WO2003029210 (2003)
   Google Scholar
• Smith ND, Cosford NDP, Reger TR, et al. Merck & Co., USA. Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5. WO2003077918 (2003)
   Google Scholar
• Roppe J, Smith ND, Huang D, et al. Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. J Med Chem 2004;47:4645-8
   PubMed Web of Science ®Google Scholar
• Poon SF, Eastman BW, Chapman DF, et al. 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. Bioorg Med Chem Lett 2004;14:5477-80
   PubMedGoogle Scholar
• Jaeschke G, Porter R, Buttelmann B, et al. Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists. Bioorg Med Chem Lett 2007;17:1307-11
   PubMedGoogle Scholar
• Wallberg A, Nilsson K, Oesterlund K, et al. Phenyl ureas of creatinine as mGluR5 antagonists. A structure- activity relationship study of fenobam analogues. Bioorg Med Chem Lett 2006;16:1142-5
   PubMedGoogle Scholar
• Ceccarelli SM, Jaeschke G, Buettelmann B, et al. Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mGlu5 receptor antagonists based on the fenobam structure. Bioorg Med Chem Lett 2007;17:1302-6
   PubMedGoogle Scholar
• Bonnefous C, Vernier JM, Hutchinson JH, et al. Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett 2005;15:1197-200
   PubMedGoogle Scholar
• Jaeschke G, Kolczewski S, Porter RHP, et al. F. Hoffmann-La Roche, Switzerland. Preparation of 3-aminopyridine-2-carboxamide derivatives as metabotropic glutamate receptor antagonists for the treatment of CNS disorders. WO2006094639 (2006)
   Google Scholar
• Jaeschke G, Kolczewski S, Porter RHP, et al. F. Hoffmann-La Roche, Switzerland. Preparation of 3-aminopyrazine-2-carboxamide derivatives as metabotropic glutamate receptor antagonists for the treatment of CNS disorders. WO2006094691 (2006)
   Google Scholar
• Buettelmann B, Ceccarelli SM, Jaeschke G, et al. F. Hoffmann-La Roche, Switzerland. Preparation of thiazole-4-carboxamides as mGluR5a receptor antagonists. WO2006074884 (2006)
   Google Scholar
• Jaeschke G, Kolczewski S, Porter RHP, et al. F. Hoffmann-La Roche, Switzerland. Preparation of naphthyridinamine derivatives as mGlu5 (mGluR5) antagonists for the treatment of CNS disorders. WO2007039512 (2007)
   Google Scholar
• Jaeschke G, Kolczewski S, Porter RHP, et al. F. Hoffmann-La Roche, Switzerland. Preparation of thiazolo[4,5-c]pyridine derivatives for treating or preventing mGluR5 receptor mediated disorders. WO2007054436 (2007)
   Google Scholar
• Kamenecka TM, Bonnefous C, Govek SP, et al. Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists. Bioorg Med Chem Lett 2005;15:4350-3
   PubMedGoogle Scholar
• Kamenecka TM, Vernier J-M, Bonnefous C, et al. Merck & Co., USA. Preparation of bipyridyl amines and ethers as modulators of metabotropic glutamate receptor-5. WO2005021529 (2005)
   Google Scholar
• Wendt JA, Deeter SD, Bove SE, et al. Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett 2007;17:5396-9
   PubMedGoogle Scholar
• Galatsis P, Yamagata K, Wendt JA, et al. Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett 2007;17:6525-8
   PubMedGoogle Scholar
• Glatthar R, Orain D, Spanka C. Novartis, Switzerland. Preparation of nicotinic acid derivatives as modulators of mGluR5 metabotropic glutamate receptors. WO2007071358 (2007)
   Google Scholar
• Keserue G, Weber C, Bielik A, et al. Richter Gedeon, Hungary. Preparation of phenylsulfonylquinolinamines useful in the treatment of mGluR5 metabotropic glutamate receptor-mediated disorders. WO2007072093 (2007)
   Google Scholar
• Gal K, Weber C, Wagner GA, et al. Richter Gedeon, Hungary. Preparation of aryltetrazolylpiperidines as modulators of mGluR5 metabotropic glutamate receptors. WO2007039782 (2007)
   Google Scholar
• Gal K, Weber C, Wagner GA, et al. Richter Gedeon, Hungary. Preparation of 1,2,4-oxadiazole derivatives and their use in the treatment of mGluR5 receptor-mediated disorders. WO2007039781 (2007)
   Google Scholar
• Nogradi K, Keserue G, Bielik A, et al. Richter Gedeon, Hungary. Preparation of thienopyridines as mGlu1 and mGlu5 metabotropic glutamate receptor ligands. WO2007072091 (2007)
   Google Scholar
• Nogradi K, Wagner G, Keserue G, et al. Richter Gedeon, Hungary. Preparation of thienopyridines as modulators of mGluR1 and mGluR5 metabotropic glutamate receptors. WO2007072090 (2007)
   Google Scholar
• Nogradi K, Wagner G, Keserue G, et al. Richter Gedeon, Hungary. Preparation of thienopyridines as mGluR1 and mGluR5 metabotropic glutamate receptor ligands. WO2007072095 (2007)
   Google Scholar
• Nogradi K, Wagner G, Keserue G, et al. Richter Gedeon, Hungary. Preparation of thienopyridones as mGluR1 and mGluR5 metabotropic glutamate receptor antagonists. WO2007072094 (2007)
   Google Scholar
• Galambos J, Vastag M, Bobok AA, et al. Richter Gedeon, Hungary. Preparation of aryl carbamoyl oximes as mGluR5 metabotropic glutamate receptor antagonists. WO2007072089 (2007)
   Google Scholar
• Steckler T, Oliveira AF, Van Dyck C, et al. Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial Water maze task. Behav Brain Res 2005;164:52-60
   PubMedGoogle Scholar
• Severance AJ, Parsey RV, Kumar JS, et al. In vitro and in vivo evaluation of [11C]MPEPy as a potential PET ligand for mGlu5 receptors. Nucl Med Biol 2006;33:1021-7
   PubMedGoogle Scholar
• Wyss MT, Ametamey SM, Treyer V, et al. Quantitative evaluation of 11C-ABP688 as PET ligand for the measurement of the metabotropic glutamate receptor subtype 5 using autoradiographic studies and a beta-scintillator. Neuroimage 2007;35:1086-92
   PubMedGoogle Scholar
• Daggett LP, Sacaan AI, Akong M, et al. Molecular and functional characterization of recombinant human metabotropic glutamate receptor subtype 5. Neuropharmacology 1995;34:871-86
   PubMedGoogle Scholar
• Romano C, Sesma MA, McDonald CT, et al. Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain. J Comp Neurol 1995;355:455-69
   PubMed Web of Science ®Google Scholar
• Spooren W, Gasparini F. mGlu5 receptor antagonists: a novel class of anxiolytics? Drug News Perspect 2004;17:251-7
   PubMed Web of Science ®Google Scholar
• Ballard TM, Woolley ML, Prinssen E, et al. The effect of the mGlu5 receptor antagonist MPEP in rodent tests of anxiety and cognition: a comparison. Psychopharmacology 2005;179:218-29
   PubMedGoogle Scholar
• Palucha A, Pilc A. Metabotropic glutamate receptor ligands as possible anxiolytic and antidepressant drugs. Pharmacol Ther 2007;115:116-47
   PubMed Web of Science ®Google Scholar
• Witkin JM, Marek GJ, Johnson BG, et al. Metabotropic glutamate receptors in the control of mood disorders. CNS Neurol Disord Drug Targets 2007;6:87-100
   PubMedGoogle Scholar
• Spooren WP, Vassout A, Neijt HC, et al. Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents. J Pharmacol Exp Ther 2000;295:1267-75
   PubMed Web of Science ®Google Scholar
• Slassi A, Isaac M, Edwards L, et al. Recent advances in non-competitive mGlu5 receptor antagonists and their potential therapeutic applications. Curr Top Med Chem 2005;5:897-911
   PubMed Web of Science ®Google Scholar
• Spooren WP, Gasparini F, Salt TE, et al. Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders. Trends Pharmacol Sci 2001;22:331-7
   PubMedGoogle Scholar
• Wein AJ, Rackley RR. Overactive bladder: a better understanding of pathophysiology, diagnosis and management. J Urol 2006;175:S5-10
   PubMed Web of Science ®Google Scholar
• Klodzinska A, Tatarczynska E, Chojnacka-Wojcik E, et al. Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling. Neuropharmacology 2004;47:342-50
   PubMed Web of Science ®Google Scholar
• Rmialowska M, Wieronska JM, Branski P, et al. MPEP, mGlu5 receptor antagonist, regulates NPYmRNA expression in hippocampal and amygdalar neurons. Pol J Pharmacol 2004;56:709-18
   PubMedGoogle Scholar
• Wieronska JM, Smialowska M, Branski P, et al. In the amygdala anxiolytic action of mGlu5 receptors antagonist MPEP involves neuropeptide Y but not GABAA signaling. Neuropsychopharmacology 2004;29:514-21
   PubMed Web of Science ®Google Scholar
• Stachowicz K, Golembiowska K, Sowa M, et al. Anxiolytic-like action of MTEP expressed in the conflict drinking Vogel test in rats is serotonin dependent. Neuropharmacology 2007
   Google Scholar
• Perez de la Mora M, Lara-Garcia D, Jacobsen KX, et al. Anxiolytic-like effects of the selective metabotropic glutamate receptor 5 antagonist MPEP after its intra-amygdaloid microinjection in three different non-conditioned rat models of anxiety. Eur J Neurosci 2006;23:2749-59
   PubMedGoogle Scholar
• Rodrigues SM, Bauer EP, Farb CR, et al. The group I metabotropic glutamate receptor mGluR5 is required for fear memory formation and long-term potentiation in the lateral amygdala. J Neurosci 2002;22:5219-29
   PubMedGoogle Scholar
• Han JS, Neugebauer V. mGluR1 and mGluR5 antagonists in the amygdala inhibit different components of audible and ultrasonic vocalizations in a model of arthritic pain. Pain 2005;113:211-22
   PubMedGoogle Scholar
• Patel JB, Martin C, Malick JB. Differential antagonism of the anticonflict effects of typical and atypical anxiolytics. Eur J Pharmacol 1982;86:295-8
   PubMedGoogle Scholar
• Kugaya A, Sanacora G. Beyond monoamines: glutamatergic function in mood disorders. CNS Spectr 2005;10:808-19
   PubMed Web of Science ®Google Scholar
• Pittenger C, Sanacora G, Krystal JH. The NMDA receptor as a therapeutic target in major depressive disorder. CNS Neurol Disord Drug Targets 2007;6:101-15
   PubMedGoogle Scholar
• Liebrenz M, Borgeat A, Leisinger R, et al. Intravenous ketamine therapy in a patient with a treatment-resistant major depression. Swiss Med Wkly 2007;137:234-6
   PubMed Web of Science ®Google Scholar
• Liebrenz M, Stohler R, Borgeat A. Repeated intravenous ketamine therapy in a patient with treatment-resistant major depression. World J Biol Psychiatry 2007;1-4
   Google Scholar
• Ostroff R, Gonzales M, Sanacora G. Antidepressant effect of ketamine during ECT. Am J Psychiatry 2005;162:1385-6
   PubMed Web of Science ®Google Scholar
• Collett VJ, Collingridge GL. Interactions between NMDA receptors and mGlu5 receptors expressed in HEK293 cells. Br J Pharmacol 2004;142:991-1001
   PubMedGoogle Scholar
• Pilc A, Klodzinska A, Branski P, et al. Multiple MPEP administrations evoke anxiolytic- and antidepressant-like effects in rats. Neuropharmacology 2002;43:181-7
   PubMed Web of Science ®Google Scholar
• Li X, Need AB, Baez M, et al. Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice. J Pharmacol Exp Ther 2006;319:254-9
   PubMed Web of Science ®Google Scholar
• Wieronska JM, Szewczyk B, Branski P, et al. Antidepressant-like effect of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist in the olfactory bulbectomized rats. Amino Acids 2002;23:213-6
   PubMed Web of Science ®Google Scholar
• Walker K, Bowes M, Panesar M, et al. Metabotropic glutamate receptor subtype 5 (mGlu5) and nociceptive function. I. Selective blockade of mGlu5 receptors in models of acute, persistent and chronic pain. Neuropharmacology 2001;40:1-9
   PubMedGoogle Scholar
• Walker K, Reeve A, Bowes M, et al. mGlu5 receptors and nociceptive function II. mGlu5 receptors functionally expressed on peripheral sensory neurones mediate inflammatory hyperalgesia. Neuropharmacology 2001;40:10-9
   PubMed Web of Science ®Google Scholar
• Zhu CZ, Wilson SG, Mikusa JP, et al. Assessing the role of metabotropic glutamate receptor 5 in multiple nociceptive modalities. Eur J Pharmacol 2004;506:107-18
   PubMed Web of Science ®Google Scholar
• Zhu CZ, Hsieh G, Ei-Kouhen O, et al. Role of central and peripheral mGluR5 receptors in post-operative pain in rats. Pain 2005;114:195-202
   PubMed Web of Science ®Google Scholar
• Goadsby PJ. Recent advances in understanding migraine mechanisms, molecules and therapeutics. Trends Mol Med 2007;13:39-44
   PubMed Web of Science ®Google Scholar
• Goadsby PJ. Migraine pathophysiology. Headache 2005;45(Suppl 1):S14-24
   PubMed Web of Science ®Google Scholar
• Goadsby PJ, Lipton RB, Ferrari MD. Migraine – current understanding and treatment. N Engl J Med 2002;346:257-70
   PubMed Web of Science ®Google Scholar
• Tan HJ, Suganthi C, Dhachayani S, et al. The coexistence of anxiety and depressive personality traits in migraine. Singapore Med J 2007;48:307-10
   PubMedGoogle Scholar
• Markou A. The role of metabotropic glutamate receptors in drug reward, motivation and dependence. Drug News Perspect 2007;20:103-8
   PubMedGoogle Scholar
• Chiamulera C, Epping-Jordan MP, Zocchi A, et al. Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice. Nat Neurosci 2001;4:873-4
   PubMed Web of Science ®Google Scholar
• McGeehan AJ, Janak PH, Olive MF. Effect of the mGluR5 antagonist 6-methyl-2-(phenylethynyl)pyridine (MPEP) on the acute locomotor stimulant properties of cocaine, D-amphetamine, and the dopamine reuptake inhibitor GBR12909 in mice. Psychopharmacology (Berl) 2004;174:266-73
   PubMedGoogle Scholar
• Dravolina OA, Danysz W, Bespalov AY. Effects of group I metabotropic glutamate receptor antagonists on the behavioral sensitization to motor effects of cocaine in rats. Psychopharmacology (Berl) 2006;187:397-404
   PubMedGoogle Scholar
• Kotlinska J, Bochenski M. Comparison of the effects of mGluR1 and mGluR5 antagonists on the expression of behavioral sensitization to the locomotor effect of morphine and the morphine withdrawal jumping in mice. Eur J Pharmacol 2007;558:113-8
   PubMedGoogle Scholar
• McGeehan AJ, Olive MF. The mGluR5 antagonist MPEP reduces the conditioned rewarding effects of cocaine but not other drugs of abuse. Synapse 2003;47:240-2
   PubMed Web of Science ®Google Scholar
• Herzig V, Schmidt WJ. Effects of MPEP on locomotion, sensitization and conditioned reward induced by cocaine or morphine. Neuropharmacology 2004;47:973-84
   PubMedGoogle Scholar
• Popik P, Wróbel M. Morphine conditioned reward is inhibited by MPEP, the mGluR5 antagonist. Neuropharmacology 2002;43:1210-7
   PubMedGoogle Scholar
• Aoki T, Narita M, Shibasaki M, et al. Metabotropic glutamate receptor 5 localized in the limbic forebrain is critical for the development of morphine-induced rewarding effect in mice. Eur J Neurosci 2004;20:1633-8
   PubMedGoogle Scholar
• Tessari M, Pilla M, Andreoli M, et al. Antagonism at metabotropic glutamate 5 receptors inhibits nicotine- and cocaine-taking behaviours and prevents nicotine-triggered relapse to nicotine-seeking. Eur J Pharmacol 2004;499:121-33
   PubMed Web of Science ®Google Scholar
• Lee B, Platt DM, Rowlett JK, et al. Attenuation of behavioral effects of cocaine by the Metabotropic Glutamate Receptor 5 Antagonist 2-Methyl-6-(phenylethynyl)-pyridine in squirrel monkeys: comparison with dizocilpine. J Pharmacol Exp Ther 2005;312:1232-40
   PubMed Web of Science ®Google Scholar
• Paterson NE, Markou A. The metabotropic glutamate receptor 5 antagonist MPEP decreased break points for nicotine, cocaine and food in rats. Psychopharmacology (Berl) 2005;179:255-61
   PubMed Web of Science ®Google Scholar
• Palucha A, Branski P, Pilc A. Selective mGlu5 receptor antagonist MTEP attenuates naloxone-induced morphine with-drawal symptoms. Pol J Pharmacol 2004;56:863-6
   PubMedGoogle Scholar
• Rasmussen K, Martin H, Berger JE, et al. The mGlu5 receptor antagonists MPEP and MTEP attenuate behavioral signs of morphine withdrawal and morphine-withdrawal-induced activation of locus coeruleus neurons in rats. Neuropharmacology 2005;48:173-80
   PubMedGoogle Scholar
• Paterson NE, Semenova S, Gasparini F, et al. The mGluR5 antagonist MPEP decreased nicotine self-administration in rats and mice. Psychopharmacology (Berl) 2003;167:257-64
   PubMed Web of Science ®Google Scholar
• Bespalov AY, Dravolina OA, Sukhanov I, et al. Metabotropic glutamate receptor (mGluR5) antagonist MPEP attenuated cue- and schedule-induced reinstatement of nicotine self-administration behavior in rats. Neuropharmacology 2005;49(Suppl 1):167-78
   PubMed Web of Science ®Google Scholar
• Bäckström P, Bachteler D, Koch S, et al. mGluR5 antagonist MPEP reduces ethanol-seeking and relapse behavior. Neuropsychopharmacology 2004;29:921-8
   PubMed Web of Science ®Google Scholar
• Cowen MS, Krstew E, Lawrence AJ. Assessing appetitive and consummatory phases of ethanol self-administration in C57BL/6J mice under operant conditions: regulation by mGlu5 receptor antagonism. Psychopharmacology (Berl) 2007;190:21-9
   PubMedGoogle Scholar
• Hodge CW, Miles MF, Sharko AC, et al. The mGluR5 antagonist MPEP selectively inhibits the onset and maintenance of ethanol self-administration in C57BL/6J mice. Psychopharmacology (Berl) 2006;183:429-38
   PubMed Web of Science ®Google Scholar
• Cowen MS, Djouma E, Lawrence AJ. The metabotropic glutamate 5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine reduces ethanol self-administration in multiple strains of alcohol-preferring rats and regulates olfactory glutamatergic systems. J Pharmacol Exp Ther 2005;315:590-600
   PubMed Web of Science ®Google Scholar
• McMillen BA, Crawford MS, Kulers CM, et al. Effects of a metabotropic, mglu5, glutamate receptor antagonist on ethanol consumption by genetic drinking rats. Alcohol Alcohol 2005;40:494-7
   PubMedGoogle Scholar
• Schroeder JP, Overstreet DH, Hodge CW. The mGluR5 antagonist MPEP decreases operant ethanol self-administration during maintenance and after repeated alcohol deprivations in alcohol-preferring (P) rats. Psychopharmacology (Berl) 2005;179:262-70
   PubMed Web of Science ®Google Scholar
• Slattery JA, Page AJ, Dorian CL, et al. Potentiation of mouse vagal afferent mechanosensitivity by ionotropic and metabotropic glutamate receptors. J Physiol 2006;577:295-306
   PubMedGoogle Scholar
• Young RL, Page AJ, O'Donnell TA, et al. Peripheral versus central modulation of gastric vagal pathways by metabotropic glutamate receptor 5. Am J Physiol Gastrointest Liver Physiol 2007;292:G501-11
   Google Scholar
• Jensen J, Lehmann A, Uvebrant A, et al. Transient lower esophageal sphincter relaxations in dogs are inhibited by a metabotropic glutamate receptor 5 antagonist. Eur J Pharmacol 2005;519:154-7
   PubMed Web of Science ®Google Scholar
• Frisby CL, Mattsson JP, Jensen JM, et al. Inhibition of transient lower esophageal sphincter relaxation and gastroesophageal reflux by metabotropic glutamate receptor ligands. Gastroenterology 2005;129:995-1004
   PubMed Web of Science ®Google Scholar
• Datamonitor. Pipeline insight: upper GI disorders; 2007
   Google Scholar
• Spooren WP, Gasparini F, Bergmann R, et al. Effects of the prototypical mGlu(5) receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine on rotarod, locomotor activity and rotational responses in unilateral 6-OHDA-lesioned rats. Eur J Pharmacol 2000;406:403-10
   PubMedGoogle Scholar
• Ossowska K, Konieczny J, Wolfarth S, et al. Blockade of the metabotropic glutamate receptor subtype 5 (mGluR5) produces antiparkinsonian-like effects in rats. Neuropharmacology 2001;41:413-20
   PubMed Web of Science ®Google Scholar
• Breysse N, Baunez C, Spooren W, et al. Chronic but not acute treatment with a metabotropic glutamate 5 receptor antagonist reverses the akinetic deficits in a rat model of parkinsonism. J Neurosci 2002;22:5669-78
   PubMed Web of Science ®Google Scholar
• Oueslati A, Breysse N, Amalric M, et al. Dysfunction of the cortico-basal ganglia-cortical loop in a rat model of early parkinsonism is reversed by metabotropic glutamate receptor 5 antagonism. Eur J Neurosci 2005;22:2765-74
   PubMedGoogle Scholar
• Samadi P, Gregoire L, Morissette M, et al. mGluR5 metabotropic glutamate receptors and dyskinesias in MPTP monkeys. Neurobiol Aging 2007. Epub 2007 Mar 10
   PubMedGoogle Scholar
• Mela F, Marti M, Dekundy A, et al. Antagonism of metabotropic glutamate receptor type 5 attenuates l-DOPA-induced dyskinesia and its molecular and neurochemical correlates in a rat model of Parkinson's disease. J Neurochem 2007;101:483-97
   PubMed Web of Science ®Google Scholar
• Thanvi B, Lo N, Robinson T. Levodopa-induced dyskinesia in Parkinson's disease: clinical features, pathogenesis, prevention and treatment. Postgrad Med J 2007;83:384-8
   PubMed Web of Science ®Google Scholar
• Thanvi BR, Lo TC. Long term motor complications of levodopa: clinical features, mechanisms, and management strategies. Postgrad Med J 2004;80:452-8
   PubMed Web of Science ®Google Scholar
• Vernon AC, Palmer S, Datla KP, et al. Neuroprotective effects of metabotropic glutamate receptor ligands in a 6-hydroxydopamine rodent model of Parkinson's disease. Eur J Neurosci 2005;22:1799-806
   PubMed Web of Science ®Google Scholar
• Vernon AC, Zbarsky V, Datla KP, et al. Subtype selective antagonism of substantia nigra pars compacta Group I metabotropic glutamate receptors protects the nigrostriatal system against 6-hydroxydopamine toxicity in vivo. J Neurochem 2007;103(3):1075-91
   PubMed Web of Science ®Google Scholar
• Armentero MT, Fancellu R, Nappi G, et al. Prolonged blockade of NMDA or mGluR5 glutamate receptors reduces nigrostriatal degeneration while inducing selective metabolic changes in the basal ganglia circuitry in a rodent model of Parkinson's disease. Neurobiol Dis 2006;22:1-9
   PubMed Web of Science ®Google Scholar
• Moldrich RX, Chapman AG, De Sarro G, et al. Glutamate metabotropic receptors as targets for drug therapy in epilepsy. Eur J Pharmacol 2003;476:3-16
   PubMedGoogle Scholar
• Merlin LR, Taylor GW, Wong RK. Role of metabotropic glutamate receptor subtypes in the patterning of epileptiform activities in vitro. J Neurophysiol 1995;74:896-900
   PubMedGoogle Scholar
• Merlin LR, Wong RK. Role of group I metabotropic glutamate receptors in the patterning of epileptiform activities in vitro. J Neurophysiol 1997;78:539-44
   PubMed Web of Science ®Google Scholar
• Wong RK, Bianchi R, Chuang SC, et al. Group I mGluR-induced epileptogenesis: distinct and overlapping roles of mGluR1 and mGluR5 and implications for antiepileptic drug design. Epilepsy Curr 2005;5:63-8
   PubMedGoogle Scholar
• Wong RK, Bianchi R, Taylor GW, et al. Role of metabotropic glutamate receptors in epilepsy. Adv Neurol 1999;79:685-98
   PubMedGoogle Scholar
• Fix AS, Schoepp DD, Olney JW, et al. Neonatal exposure to D,L-2-amino-3-phosphonopropionate (D,L-AP3) produces lesions in the eye and optic nerve of adult rats. Brain Res Dev Brain Res 1993;75:223-33
   PubMedGoogle Scholar
• McDonald JW, Fix AS, Tizzano JP, et al. Seizures and brain injury in neonatal rats induced by 1S,3R-ACPD, a metabotropic glutamate receptor agonist. J Neurosci 1993;13:4445-55
   PubMedGoogle Scholar
• Chapman AG, Nanan K, Williams M, et al. Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893). Neuropharmacology 2000;39:1567-74
   PubMed Web of Science ®Google Scholar
• Lojkova D, Mares P. Anticonvulsant action of an antagonist of metabotropic glutamate receptors mGluR5 MPEP in immature rats. Neuropharmacology 2005;49(Suppl 1):219-29
   PubMedGoogle Scholar
• Mares P, Mikulecka A. MPEP, an antagonist of metabotropic glutamate receptors, exhibits anticonvulsant action in immature rats without a serious impairment of motor performance. Epilepsy Res 2004;60:17-26
   PubMedGoogle Scholar
• Loscher W, Dekundy A, Nagel J, et al. mGlu1 and mGlu5 receptor antagonists lack anticonvulsant efficacy in rodent models of difficult-to-treat partial epilepsy. Neuropharmacology 2006;50:1006-15
   PubMed Web of Science ®Google Scholar
• Yan QJ, Rammal M, Tranfaglia M, et al. Suppression of two major Fragile X Syndrome mouse model phenotypes by the mGluR5 antagonist MPEP. Neuropharmacology 2005;49:1053-66
   PubMed Web of Science ®Google Scholar
• Aronica E, Leenstra S, van Veelen CW, et al. Glioneuronal tumors and medically intractable epilepsy: a clinical study with long-term follow-up of seizure outcome after surgery. Epilepsy Res 2001;43:179-91
   PubMed Web of Science ®Google Scholar
• Aronica E, Yankaya B, Jansen GH, et al. Ionotropic and metabotropic glutamate receptor protein expression in glioneuronal tumours from patients with intractable epilepsy. Neuropathol Appl Neurobiol 2001;27:223-37
   PubMed Web of Science ®Google Scholar
• Corti C, Clarkson RW, Crepaldi L, et al. Gene structure of the human metabotropic glutamate receptor 5 and functional analysis of its multiple promoters in neuroblastoma and astroglioma cells. J Biol Chem 2003;278:33105-19
   PubMedGoogle Scholar
• Park S-Y, Lee S-A, Han I-H, et al. Clinical significance of metabotropic glutamate receptor 5 expression in oral squamous cell carcinoma. Oncology Reports 2007;17:81-7
   PubMedGoogle Scholar
• Leonardi A, Testa R, Poggesi E, Recordati SA. Selective mGlu5 antagonists for treatment of neuromuscular dysfunction of the lower urinary tract. WO067002A3 (2004)
   Google Scholar
• Jensen PS, Youngstrom EA, Steiner H, et al. Consensus report on impulsive aggression as a symptom across diagnostic categories in child psychiatry: implications for medication studies. J Am Acad Child Adolesc Psychiatry 2007;46:309-22
   PubMed Web of Science ®Google Scholar
• McDougle CJ, Stigler KA, Posey DJ. Treatment of aggression in children and adolescents with autism and conduct disorder. J Clin Psychiatry 2003;64(Suppl 4):16-25
   PubMedGoogle Scholar
• Navarro JF, Postigo D, Martin M, et al. Antiaggressive effects of MPEP, a selective antagonist of mGlu5 receptors, in agonistic interactions between male mice. Eur J Pharmacol 2006;551:67-70
   PubMedGoogle Scholar
• Reiss AL, Hall SS. Fragile X syndrome: assessment and treatment implications. Child Adolesc Psychiatr Clin N Am 2007;16:663-75
   PubMedGoogle Scholar
• Garber K, Smith KT, Reines D, et al. Transcription, translation and fragile X syndrome. Curr Opin Genet Dev 2006;16:270-5
   PubMedGoogle Scholar
• Bear MF. Therapeutic implications of the mGluR theory of fragile X mental retardation. Genes Brain Behav 2005;4:393-8
   PubMedGoogle Scholar
• Catania MV, D'Antoni S, Bonaccorso CM, et al. Group I metabotropic glutamate receptors: a role in neurodevelopmental disorders? Mol Neurobiol 2007;35:298-307
   PubMed Web of Science ®Google Scholar
• Dolen G, Bear MF. Courting a cure for fragile X. Neuron 2005;45:642-4
   PubMedGoogle Scholar