Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression

Neuropharmacology

Volumn 66, Issue , 2013, Pages 202-214

  Hughes, Z A ^a   Neal, S J ^a   Smith, D L ^a   Sukoff Rizzo, S J ^a   Pulicicchio, C M ^a   Lotarski, S ^a   Lu, S ^a   Dwyer, J M ^a   Brennan, J ^a   Olsen, M ^a   Bender, C N ^a   Kouranova, E ^a   Andree, T H ^a   Harrison, J E ^a   Whiteside, G T ^a   Springer, D ^a   O'Neil, S V ^a   Leonard, S K ^a   Schechter, L E ^a   Dunlop, J ^a   Rosenzweig Lipson, S ^a   Ring, R H ^a   more..

^a PFIZER INC   (United States)

Author keywords

Analgesic; Antidepressant; Anxiolytic; D; Glutamate; Ketamine; Receptor occupancy; STAR

Indexed keywords

[4 DIFLUOROMETHOXY 3 (PYRIDINE 2 YLETHYNYL)PHENYL] 5H PYRROLO[3,4 B]PYRIDINE 6(7H) YL METHANONE; ALPRAZOLAM; ANALGESIC AGENT; ANTIDEPRESSANT AGENT; ANXIOLYTIC AGENT; CELECOXIB; CHLORDIAZEPOXIDE; DULOXETINE; FLUOXETINE; GRN 529; METABOTROPIC RECEPTOR 5; PAROXETINE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANXIETY DISORDER; ARTICLE; COGNITIVE DEFECT; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG RESPONSE; DRUG SAFETY; IN VITRO STUDY; IN VIVO STUDY; MALE; MOTOR COORDINATION; MOUSE; NONHUMAN; NUCLEOTIDE SEQUENCE; PAIN; PRIORITY JOURNAL; RAT; RECEPTOR OCCUPANCY; SEXUAL BEHAVIOR; TREATMENT RESISTANT DEPRESSION;

ALLOSTERIC REGULATION; ANALGESICS; ANIMALS; ANTI-ANXIETY AGENTS; ANTIDEPRESSIVE AGENTS; BEHAVIOR, ANIMAL; BENZAMIDES; CALCIUM; DEPRESSIVE DISORDER, TREATMENT-RESISTANT; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; EXCITATORY AMINO ACID ANTAGONISTS; GLUTAMIC ACID; HEK293 CELLS; HUMANS; MICE; PYRIDINES; RADIOLIGAND ASSAY; RATS; RECEPTORS, METABOTROPIC GLUTAMATE;

EID: 84872163299     PISSN: 00283908     EISSN: 18737064     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2012.04.007     Document Type: Article

References (55)

1. S.M. Ametamey, V. Treyer, J. Streffer, M.T. Wyss, M. Schmidt, M. Blagoev, S. Hintermann, Y. Auberson, F. Gasparini, U.C. Fischer, and A. Buck Human PET studies of metabotropic glutamate receptor subtype 5 with 11C-ABP688 Journal of Nuclear Medicine 48 2007 247 252
2. M. Banasr, G.M.I. Chowdhury, R. Terwilliger, S.S. Newton, R.S. Duman, K.L. Behar, and G. Sanacora Glial pathology in an animal model of depression: reversal of stress-induced cellular, metabolic and behavioral deficits by the glutamate-modulating drug riluzole Molecular Psychiatry 15 2010 501 511
3. R.M. Berman, A. Cappiello, A. Anand, D.A. Oren, G.R. Heninger, D.S. Charney, and J.H. Krystal Antidepressant effects of ketamine in depressed patients Biological Psychiatry 47 2000 351 354
4. E. Berry-Kravis, D. Hessl, S. Coffey, C. Hervey, A. Schneider, J. Yuhas, J. Hutchison, M. Snape, M. Tranfaglia, D.V. Nguyen, and R. Hagerman A pilot open label, single dose trial of fenobam in adults with fragile X syndrome Journal of Medical Genetics 46 2009 266 271
5. J. Brodkin, C. Busse, S.J. Sukoff, and M.A. Varney Anxiolytic-like activity of the mGluR5 antagonist MPEP: a comparison with diazepam and buspirone Pharmacology Biochemistry and Behavior 73 2002 359 366
6. C.S. Busse, J. Brodkin, D. Tattersall, J.J. Anderson, N. Warren, L. Tehrani, L.J. Bristow, M.A. Varney, and N.D.P. Cosford The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[lsqb](2-methyl-1,3- thiazol-4-yl)ethynyl[rsqb]pyridine (MTEP) in rodent models of anxiety Neuropsychopharmacology 29 2004 1971 1979
7. S. Chaki, R. Yoshikawa, S. Hirota, T. Shimazaki, M. Maeda, N. Kawashima, T. Yoshimizu, A. Yasuhara, K. Sakagami, S. Okuyama, S. Nakanishi, and A. Nakazato MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity Neuropharmacology 46 2004 457 467
8. Y. Cheng, and W.H. Prusoff Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction Biochemical Pharmacology 22 1973 3099 3108
9. P.J. Conn, and J.-P. Pin Pharmacology and functions of metabotropic glutamate receptors Annual Review of Pharmacology and Toxicology 37 1997 205 237
10. W. Danysz, J.T. Wroblewski, and E. Costa Learning impairment in rats by N-methyl-D-Aspartate receptor antagonists Neuropharmacology 27 1988 653 656
11. E. De Leonibus, F. Manago, F. Giordani, F. Petrosino, S. Lopez, A. Oliverio, M. Amalric, and A. Mele Metabotropic glutamate receptors 5 blockade reverses spatial memory deficits in a mouse model of Parkinson's disease Neuropsychopharmacology 34 2008 729 738
12. E. Engin, D. Treit, and C.T. Dickson Anxiolytic- and antidepressant-like properties of ketamine in behavioral and neurophysiological animal models Neuroscience 161 2009 359 369
13. M. Fava, A.J. Rush, J.E. Alpert, G.K. Balasubramani, S.R. Wisniewski, C.N. Carmin, M.M. Biggs, S. Zisook, A. Leuchter, R. Howland, D. Warden, and M.H. Trivedi Difference in treatment outcome in outpatients with anxious versus nonanxious depression: a STAR*D report American Journal of Psychiatry 165 2008 342 351
14. L.S.B. Garcia, C.M. Comim, S.S. Valvassori, G.Z. Réus, L.M. Barbosa, A.C. Andreazza, L. Stertz, G.R. Fries, E.C. Gavioli, F. Kapczinski, and J. Quevedo Acute administration of ketamine induces antidepressant-like effects in the forced swimming test and increases BDNF levels in the rat hippocampus Progress in Neuro-Psychopharmacology and Biological Psychiatry 32 2008 140 144
15. A.L. Garcia-Garcia, N. Elizalde, D. Matrov, J. Harro, S.M. Wojcik, E. Venzala, M.J. Ramírez, J. Del Rio, and R.M. Tordera Increased vulnerability to depressive-like behavior of mice with decreased expression of VGLUT1 Biological Psychiatry 66 2009 275 282
16. A. Gravius, A. Dekundy, J. Nagel, L. More, M. Pietraszek, and W. Danysz Investigation on tolerance development to subchronic blockade of mGluR5 in models of learning, anxiety, and levodopa-induced dyskinesia in rats Journal of Neural Transmission 115 2008 1609 1619
17. R.E. Harbut, and G.E. Correll Successful treatment of a nine-year case of complex regional pain syndrome type-I (reflex sympathetic dystrophy) with intravenous ketamine-infusion therapy in a warfarin-Anticoagulated adult female patient Pain Medicine 3 2002 147 155
18. K. Hashimoto, A. Sawa, and M. Iyo Increased levels of glutamate in brains from patients with mood disorders Biological Psychiatry 62 2007 1310 1316
19. C.A. Heidbreder, M. Bianchi, L.P. Lacroix, S. Faedo, E. Perdona, R. Remelli, P. Cavanni, and F. Crespi Evidence that the metabotropic glutamate receptor 5 antagonist MPEP may act as an inhibitor of the norepinephrine transporter in vitro and in vivo Synapse 50 2003 269 276
20. Z.A. Hughes, F. Liu, B.J. Platt, J.M. Dwyer, C.M. Pulicicchio, G. Zhang, L.E. Schechter, S. Rosenzweig-Lipson, and M. Day WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent Neuropharmacology 54 2008 1136 1142
21. J.H. Krystal, L.P. Karper, J.P. Seibyl, G.K. Freeman, R. Delaney, J.D. Bremner, G.R. Heninger, M.B. Bowers Jr.; and D.S. Charney Subanesthetic effects of the noncompetitive NMDA antagonist, ketamine, in humans: psychotomimetic, perceptual, cognitive, and neuroendocrine responses Archives of General Psychiatry 51 1994 199 214
22. N. Kumar, A. Laferriere, J.S.C. Yu, T. Poon, and T.J. Coderre Metabotropic glutamate receptors (mGluRs) regulate noxious stimulus-induced glutamate release in the spinal cord dorsal horn of rats with neuropathic and inflammatory pain Journal of Neurochemistry 114 2010 281 290
23. C.J. LaBuda, and P.J. Little Pharmacological evaluation of the selective spinal nerve ligation model of neuropathic pain in the rat Journal of Neuroscience Methods 144 2005 175 181
24. A.F. Leuchter, M.M. Husain, I.A. Cook, M.H. Trivedi, S.R. Wisniewski, W.S. Gilmer, J.F. Luther, M. Fava, and A.J. Rush Painful physical symptoms and treatment outcome in major depressive disorder: a STAR*D (sequenced treatment alternatives to relieve depression) report Psychological Medicine 40 2010 239 251
25. X. Li, J.P. Tizzano, K. Griffey, M. Clay, T. Lindstrom, and P. Skolnick Antidepressant-like actions of an AMPA receptor potentiator (LY392098) Neuropharmacology 40 2001 1028 1033
26. X. Li, J.M. Witkin, A.B. Need, and P. Skolnick Enhancement of antidepressant potency by a potentiator of AMPA receptors Cellular and Molecular Neurobiology 23 2003 419 430
27. S. Maeng, C.A. Zarate Jr.; J. Du, R.J. Schloesser, J. McCammon, G. Chen, and H.K. Manji Cellular mechanisms underlying the antidepressant effects of ketamine: role of [alpha]-Amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptors Biological Psychiatry 63 2008 349 352
28. J.C.A. Marin, and P.J. Goadsby Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine? Expert Opinion on Investigational Drugs 19 2010 555 561
29. Y.S. Mineur, M.R. Picciotto, and G. Sanacora Antidepressant-like effects of ceftriaxone in male C57BL/6J mice Biological Psychiatry 61 2007 250 252
30. H. Mitani, Y. Shirayama, T. Yamada, K. Maeda, J.C.R. Ashby, and R. Kawahara Correlation between plasma levels of glutamate, alanine and serine with severity of depression Progress in Neuro-Psychopharmacology and Biological Psychiatry 30 2006 1155 1158
31. M.C. Montana, L.F. Cavallone, K.K. Stubbert, A.D. Stefanescu, E.D. Kharasch, and R.W. Gereau The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine Journal of Pharmacology & Experimental Therapeutics 330 2009 834 843
32. A.M.D. Mowla, M.M.D. Mosavinasab, and A. Pani Does fluoxetine have any effect on the cognition of patients with mild cognitive impairment?: a double-blind, placebo-controlled, clinical trial Journal of Clinical Psychopharmacology 27 2007 67 70
33. D.M. O'Leary, V. Movsesyan, S. Vicini, and A.I. Faden Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antagonism British Journal of Pharmacology 131 2000 1429 1437
34. A. Palucha, and A. Pilc Metabotropic glutamate receptor ligands as possible anxiolytic and antidepressant drugs Pharmacology & Therapeutics 115 2007 116 147
35. A. Palucha, P. Branski, B. Szewczyk, J.M. Wieronska, K. Klak, and A. Pilc Potential antidepressant-like effect of MTEP, a potent and highly selective mGluR5 antagonist Pharmacology Biochemistry and Behavior 81 2005 901 906
36. M. Papp, and E. Moryl Antidepressant activity of non-competitive and competitive NMDA receptor antagonists in a chronic mild stress model of depression European Journal of Pharmacology 263 1994 1 7
37. J.C. Pecknold, D.J. McClure, L. Appeltauer, L. Wrzesinski, and T. Allan Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study Journal of Clinical Psychopharmacology 2 1982 129 133
38. C. Pittenger, V. Coric, M. Banasr, M. Bloch, J.H. Krystal, G. Sanacora, C. Pittenger, V. Coric, M. Banasr, M. Bloch, J.H. Krystal, and G. Sanacora Riluzole in the treatment of mood and anxiety disorders CNS Drugs 22 2008 761 786
39. R.H.P. Porter, G. Jaeschke, W. Spooren, T.M. Ballard, B. Buttelmann, S. Kolczewski, J.-U. Peters, E. Prinssen, J. Wichmann, E. Vieira, A. Muhlemann, S. Gatti, V. Mutel, and P. Malherbe Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity Journal of Pharmacology and Experimental Therapeutics 315 2005 711 721
40. B.M. Roberts, D.E. Holden, C.L. Shaffer, P.A. Seymour, F.S. Menniti, C.J. Schmidt, G.V. Williams, and S.A. Castner Prevention of ketamine-induced working memory impairments by AMPA potentiators in a nonhuman primate model of cognitive dysfunction Behavioural Brain Research 212 2010 41 48
41. R.C.P. Rosen, R.M.M.D. Lane, and M.M.D. Menza Effects of SSRIs on sexual function: a critical review Journal of Clinical Psychopharmacology 19 1999 67 85
42. A.J. Rush, M. Fava, S.R. Wisniewski, P.W. Lavori, M.H. Trivedi, H.A. Sackeim, M.E. Thase, A.A. Nierenberg, F.M. Quitkin, T.M. Kashner, D.J. Kupfer, J.F. Rosenbaum, J. Alpert, J.W. Stewart, P.J. McGrath, M.M. Biggs, K. Shores-Wilson, B.D. Lebowitz, L. Ritz, G. Niederehe, and S. D. I. G Sequenced treatment alternatives to relieve depression (STAR*D): rationale and design Controlled Clinical Trials 25 2004 119 142
43. G. Sanacora, R. Gueorguieva, C.N. Epperson, Y.-T. Wu, M. Appel, D.L. Rothman, J.H. Krystal, and G.F. Mason Subtype-specific alterations of {gamma}-Aminobutyric acid and glutamate in patients with major depression Archives of General Psychiatry 61 2004 705 713
44. C.N. Sang NMDA-receptor antagonists in neuropathic pain: experimental methods to clinical trials Journal of Pain and Symptom Management 19 2000 21 25
45. D.D. Schoepp, R.A. Wright, L.R. Levine, B. Gaydos, and W.Z. Potter LY354740, an mGlu2/3 receptor agonist as a novel approach to treat anxiety/stress Stress 6 2003 189 197
46. H.C. Schulberg, W. Katon, G.E. Simon, and A.J. Rush Treating major depression in primary care practice: an update of the agency for health care policy and research practice guidelines Archives of General Psychiatry 55 1998 1121 1127
47. A. Simonyi, T.R. Schachtman, and G.R.J. Christoffersen Metabotropic glutamate receptor subtype 5 antagonism in learning and memory European Journal of Pharmacology 639 2010 17 25
48. W.P.J.M. Spooren, A. Vassout, H.C. Neijt, R. Kuhn, F. Gasparini, S. Roux, R.D. Porsolt, and C. Gentsch Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents Journal of Pharmacology and Experimental Therapeutics 295 2000 1267 1275
49. S.J. Sukoff Rizzo, L.E. Schechter, and S. Rosenzweig-Lipson A novel approach for predicting antidepressant-induced sexual dysfunction in rats Psychopharmacology 195 2008 459 467
50. S.J. Sukoff Rizzo, S.K. Leonard, A. Gilbert, P. Dollings, D.L. Smith, M.-Y. Zhang, L. Di, B.J. Platt, S. Neal, J.M. Dwyer, C.N. Bender, J. Zhang, T. Lock, D. Kowal, A. Kramer, A. Randall, C. Huselton, K. Vishwanathan, S.Y. Tse, J. Butera, R.H. Ring, S. Rosenzweig-Lipson, Z.A. Hughes, and J. Dunlop The metabotropic glutamate receptor 7 allosteric modulator AMN082: a monoaminergic agent in disguise? Journal of Pharmacology and Experimental Therapeutics 338 2011 345 352
51. N.R. Sullivan, L. Leventhal, J. Harrison, V.A. Smith, T.A. Cummons, T.B. Spangler, S.-C. Sun, P. Lu, A.J. Uveges, B.W. Strassle, M.J. Piesla, R. Ramdass, A. Barry, J. Schantz, W. Adams, G.T. Whiteside, A. Adedoyin, and P.G. Jones Pharmacological characterization of the muscarinic agonist (3R,4R)-3-(3- hexylsulfanyl-pyrazin-2-yloxy)-1-Aza-bicyclo[2.2.1]heptane (WAY-132983) in in vitro and in vivo models of chronic pain Journal of Pharmacology and Experimental Therapeutics 322 2007 1294 1304
52. E. Tatarczynska, A. Klodzinska, E. Chojnacka-Wojcik, A. Palucha, F. Gasparini, R. Kuhn, and A. Pilc Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist British Journal of Pharmacology 132 2001 1423 1430
53. R. Trullas, and P. Skolnick Functional antagonists at the NMDA receptor complex exhibit antidepressant actions European Journal of Pharmacology 185 1990 1 10
54. C.A. Zarate Jr.; J.B. Singh, P.J. Carlson, N.E. Brutsche, R. Ameli, D.A. Luckenbaugh, D.S. Charney, and H.K. Manji A randomized trial of an N-methyl-D-Aspartate antagonist in treatment-resistant major depression Archives of General Psychiatry 63 2006 856 864
55. M. Zink, B. Vollmayr, P.J. Gebicke-Haerter, and F.A. Henn Reduced expression of glutamate transporters vGluT1, EAAT2 and EAAT4 in learned helpless rats, an animal model of depression Neuropharmacology 58 2010 465 473