Minakami R, Katsuki F, Yamamoto T, Nakamura K, Sugiyama H (March 1994). "Molecular cloning and the functional expression of two isoforms of human metabotropic glutamate receptor subtype 5". Biochemical and Biophysical Research Communications. 199 (3): 1136–43. doi:10.1006/bbrc.1994.1349. PMID7908515.
Chen Y, Goudet C, Pin JP, Conn PJ (March 2008). "N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors". Molecular Pharmacology. 73 (3): 909–18. doi:10.1124/mol.107.040097. PMID18056795. S2CID82273.
Bespalov AY, Dravolina OA, Sukhanov I, Zakharova E, Blokhina E, Zvartau E, et al. (2005). "Metabotropic glutamate receptor (mGluR5) antagonist MPEP attenuated cue- and schedule-induced reinstatement of nicotine self-administration behavior in rats". Neuropharmacology. 49 (Suppl 1): 167–78. doi:10.1016/j.neuropharm.2005.06.007. PMID16023685. S2CID37283433.
Slassi A, Isaac M, Edwards L, Minidis A, Wensbo D, Mattsson J, et al. (2005). "Recent advances in non-competitive mGlu5 receptor antagonists and their potential therapeutic applications". Current Topics in Medicinal Chemistry. 5 (9): 897–911. doi:10.2174/1568026054750236. PMID16178734.
Hu Y, Dong L, Sun B, Guillon MA, Burbach LR, Nunn PA, et al. (January 2009). "The role of metabotropic glutamate receptor mGlu5 in control of micturition and bladder nociception". Neuroscience Letters. 450 (1): 12–7. doi:10.1016/j.neulet.2008.11.026. PMID19027050. S2CID26773751.
Jesse CR, Wilhelm EA, Bortolatto CF, Savegnago L, Nogueira CW (May 2009). "Selective blockade of mGlu5 metabotropic glutamate receptors is hepatoprotective against fulminant hepatic failure induced by lipopolysaccharide and D-galactosamine in mice". Journal of Applied Toxicology. 29 (4): 323–9. doi:10.1002/jat.1413. PMID19153979. S2CID22498124.
Simonyi A, Schachtman TR, Christoffersen GR (Jul 2005). "The role of metabotropic glutamate receptor 5 in learning and memory processes". Drug News & Perspectives. 18 (6): 353–61. doi:10.1358/dnp.2005.18.6.927927. PMID16247513.
Palucha A, Pilc A (July 2007). "Metabotropic glutamate receptor ligands as possible anxiolytic and antidepressant drugs". Pharmacology & Therapeutics. 115 (1): 116–47. doi:10.1016/j.pharmthera.2007.04.007. PMID17582504.
Christoffersen GR, Simonyi A, Schachtman TR, Clausen B, Clement D, Bjerre VK, et al. (August 2008). "MGlu5 antagonism impairs exploration and memory of spatial and non-spatial stimuli in rats". Behavioural Brain Research. 191 (2): 235–45. doi:10.1016/j.bbr.2008.03.032. PMID18471908. S2CID205877961.
Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, et al. (December 2008). "ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities". The Journal of Pharmacology and Experimental Therapeutics. 327 (3): 827–39. doi:10.1124/jpet.108.136580. PMID18753411. S2CID19362501.
Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, et al. (March 2007). "Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA". Bioorganic & Medicinal Chemistry Letters. 17 (5): 1386–91. doi:10.1016/j.bmcl.2006.11.081. PMID17210250.
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, et al. (May 2004). "A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain". The Journal of Pharmacology and Experimental Therapeutics. 309 (2): 568–77. doi:10.1124/jpet.103.061747. PMID14747613. S2CID10103555.
Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, et al. (May 2007). "Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses". Molecular Pharmacology. 71 (5): 1389–98. doi:10.1124/mol.106.032425. PMID17303702. S2CID7004830.
de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, et al. (June 2006). "Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes". Journal of Medicinal Chemistry. 49 (11): 3332–44. doi:10.1021/jm051252j. PMID16722652.
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, et al. (April 2005). "A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models". The Journal of Pharmacology and Experimental Therapeutics. 313 (1): 199–206. doi:10.1124/jpet.104.079244. PMID15608073. S2CID14946765.
Raboisson P, Breitholtz-Emanuelsson A, Dahllöf H, Edwards L, Heaton WL, Isaac M, et al. (November 2012). "Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development". Bioorganic & Medicinal Chemistry Letters. 22 (22): 6974–6979. doi:10.1016/j.bmcl.2012.08.100. PMID23046966.
Minakami R, Katsuki F, Yamamoto T, Nakamura K, Sugiyama H (March 1994). "Molecular cloning and the functional expression of two isoforms of human metabotropic glutamate receptor subtype 5". Biochemical and Biophysical Research Communications. 199 (3): 1136–43. doi:10.1006/bbrc.1994.1349. PMID7908515.
Chen Y, Goudet C, Pin JP, Conn PJ (March 2008). "N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors". Molecular Pharmacology. 73 (3): 909–18. doi:10.1124/mol.107.040097. PMID18056795. S2CID82273.
Bespalov AY, Dravolina OA, Sukhanov I, Zakharova E, Blokhina E, Zvartau E, et al. (2005). "Metabotropic glutamate receptor (mGluR5) antagonist MPEP attenuated cue- and schedule-induced reinstatement of nicotine self-administration behavior in rats". Neuropharmacology. 49 (Suppl 1): 167–78. doi:10.1016/j.neuropharm.2005.06.007. PMID16023685. S2CID37283433.
Slassi A, Isaac M, Edwards L, Minidis A, Wensbo D, Mattsson J, et al. (2005). "Recent advances in non-competitive mGlu5 receptor antagonists and their potential therapeutic applications". Current Topics in Medicinal Chemistry. 5 (9): 897–911. doi:10.2174/1568026054750236. PMID16178734.
Gasparini F, Bilbe G, Gomez-Mancilla B, Spooren W (September 2008). "mGluR5 antagonists: discovery, characterization and drug development". Current Opinion in Drug Discovery & Development. 11 (5): 655–65. PMID18729017.
Hu Y, Dong L, Sun B, Guillon MA, Burbach LR, Nunn PA, et al. (January 2009). "The role of metabotropic glutamate receptor mGlu5 in control of micturition and bladder nociception". Neuroscience Letters. 450 (1): 12–7. doi:10.1016/j.neulet.2008.11.026. PMID19027050. S2CID26773751.
Jesse CR, Wilhelm EA, Bortolatto CF, Savegnago L, Nogueira CW (May 2009). "Selective blockade of mGlu5 metabotropic glutamate receptors is hepatoprotective against fulminant hepatic failure induced by lipopolysaccharide and D-galactosamine in mice". Journal of Applied Toxicology. 29 (4): 323–9. doi:10.1002/jat.1413. PMID19153979. S2CID22498124.
Simonyi A, Schachtman TR, Christoffersen GR (Jul 2005). "The role of metabotropic glutamate receptor 5 in learning and memory processes". Drug News & Perspectives. 18 (6): 353–61. doi:10.1358/dnp.2005.18.6.927927. PMID16247513.
Palucha A, Pilc A (July 2007). "Metabotropic glutamate receptor ligands as possible anxiolytic and antidepressant drugs". Pharmacology & Therapeutics. 115 (1): 116–47. doi:10.1016/j.pharmthera.2007.04.007. PMID17582504.
Christoffersen GR, Simonyi A, Schachtman TR, Clausen B, Clement D, Bjerre VK, et al. (August 2008). "MGlu5 antagonism impairs exploration and memory of spatial and non-spatial stimuli in rats". Behavioural Brain Research. 191 (2): 235–45. doi:10.1016/j.bbr.2008.03.032. PMID18471908. S2CID205877961.
Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, et al. (December 2008). "ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities". The Journal of Pharmacology and Experimental Therapeutics. 327 (3): 827–39. doi:10.1124/jpet.108.136580. PMID18753411. S2CID19362501.
Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, et al. (March 2007). "Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA". Bioorganic & Medicinal Chemistry Letters. 17 (5): 1386–91. doi:10.1016/j.bmcl.2006.11.081. PMID17210250.
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, et al. (May 2004). "A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain". The Journal of Pharmacology and Experimental Therapeutics. 309 (2): 568–77. doi:10.1124/jpet.103.061747. PMID14747613. S2CID10103555.
Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, et al. (May 2007). "Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses". Molecular Pharmacology. 71 (5): 1389–98. doi:10.1124/mol.106.032425. PMID17303702. S2CID7004830.
de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, et al. (June 2006). "Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes". Journal of Medicinal Chemistry. 49 (11): 3332–44. doi:10.1021/jm051252j. PMID16722652.
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, et al. (April 2005). "A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models". The Journal of Pharmacology and Experimental Therapeutics. 313 (1): 199–206. doi:10.1124/jpet.104.079244. PMID15608073. S2CID14946765.
Raboisson P, Breitholtz-Emanuelsson A, Dahllöf H, Edwards L, Heaton WL, Isaac M, et al. (November 2012). "Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development". Bioorganic & Medicinal Chemistry Letters. 22 (22): 6974–6979. doi:10.1016/j.bmcl.2012.08.100. PMID23046966.
Chen Y, Goudet C, Pin JP, Conn PJ (March 2008). "N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors". Molecular Pharmacology. 73 (3): 909–18. doi:10.1124/mol.107.040097. PMID18056795. S2CID82273.
Bespalov AY, Dravolina OA, Sukhanov I, Zakharova E, Blokhina E, Zvartau E, et al. (2005). "Metabotropic glutamate receptor (mGluR5) antagonist MPEP attenuated cue- and schedule-induced reinstatement of nicotine self-administration behavior in rats". Neuropharmacology. 49 (Suppl 1): 167–78. doi:10.1016/j.neuropharm.2005.06.007. PMID16023685. S2CID37283433.
Hu Y, Dong L, Sun B, Guillon MA, Burbach LR, Nunn PA, et al. (January 2009). "The role of metabotropic glutamate receptor mGlu5 in control of micturition and bladder nociception". Neuroscience Letters. 450 (1): 12–7. doi:10.1016/j.neulet.2008.11.026. PMID19027050. S2CID26773751.
Jesse CR, Wilhelm EA, Bortolatto CF, Savegnago L, Nogueira CW (May 2009). "Selective blockade of mGlu5 metabotropic glutamate receptors is hepatoprotective against fulminant hepatic failure induced by lipopolysaccharide and D-galactosamine in mice". Journal of Applied Toxicology. 29 (4): 323–9. doi:10.1002/jat.1413. PMID19153979. S2CID22498124.
Christoffersen GR, Simonyi A, Schachtman TR, Clausen B, Clement D, Bjerre VK, et al. (August 2008). "MGlu5 antagonism impairs exploration and memory of spatial and non-spatial stimuli in rats". Behavioural Brain Research. 191 (2): 235–45. doi:10.1016/j.bbr.2008.03.032. PMID18471908. S2CID205877961.
Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, et al. (December 2008). "ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities". The Journal of Pharmacology and Experimental Therapeutics. 327 (3): 827–39. doi:10.1124/jpet.108.136580. PMID18753411. S2CID19362501.
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, et al. (May 2004). "A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain". The Journal of Pharmacology and Experimental Therapeutics. 309 (2): 568–77. doi:10.1124/jpet.103.061747. PMID14747613. S2CID10103555.
Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, et al. (May 2007). "Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses". Molecular Pharmacology. 71 (5): 1389–98. doi:10.1124/mol.106.032425. PMID17303702. S2CID7004830.
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, et al. (April 2005). "A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models". The Journal of Pharmacology and Experimental Therapeutics. 313 (1): 199–206. doi:10.1124/jpet.104.079244. PMID15608073. S2CID14946765.
Chiamulera C, Epping-Jordan MP, Zocchi A, Marcon C, Cottiny C, Tacconi S, et al. (September 2001). "Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice". Nature Neuroscience. 4 (9): 873–4. doi:10.1038/nn0901-873. PMID11528416. S2CID1314227.
