Modulation of NMDA receptor function as a treatment for schizophrenia

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 18, 2013, Pages 5034-5044

  Cioffi, Christopher L ^a  

^a ALBANY MOLECULAR RESEARCH INC   (United States)

Author keywords

Agonist Positive allosteric modulator; Glutamate; Glycine d Serine; NMDA receptor; Schizophrenia

Indexed keywords

ADX 71149; AMINOTRANSFERASE INHIBITOR; AMPA RECEPTOR AGONIST; ATYPICAL ANTIPSYCHOTIC AGENT; BITOPERTIN; CYCLOSERINE; DEXTRO AMINO ACID OXIDASE; DIZOCILPINE; GLYCINE; GLYCINE TRANSPORTER 1; KYNURENINE AMINOTRANSFERASE INHIBITOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N [3 (4 FLUOROPHENYL) 3 (4 PHENYLPHENOXY)PROPYL]SARCOSINE; PF 3463275; PLACEBO; POMAGLUMETAD METHIONIL; RO 49178838; SARCOSINE; UNCLASSIFIED DRUG; XANOMELINE;

ARTICLE; BINDING SITE; BLOOD PRESSURE; CALCIUM MOBILIZATION; CATABOLISM; CHANNEL GATING; COGNITION; COGNITIVE DEFECT; DRUG BIOAVAILABILITY; DRUG MEGADOSE; DRUG PENETRATION; DRUG SAFETY; DRUG STRUCTURE; ENZYME SPECIFICITY; EXCITATORY POSTSYNAPTIC POTENTIAL; GASTROINTESTINAL SYMPTOM; HIGH THROUGHPUT SCREENING; HUMAN; IN VITRO STUDY; LIGAND BINDING; MEAN RESIDENCE TIME; MEMORY CONSOLIDATION; MODULATION; NEGATIVE SYNDROME; NERVE CELL PLASTICITY; NEUROTRANSMISSION; NONHUMAN; POSITIVE SYNDROME; PREFRONTAL CORTEX; PROTEIN EXPRESSION; PROTEIN FUNCTION; RECEPTOR DOWN REGULATION; SALIVATION; SCHIZOPHRENIA; SIDE EFFECT; SIGNAL TRANSDUCTION; SWEATING; VOMITING; WORKING MEMORY;

AGONIST; D-SERINE; GLUTAMATE; GLYCINE; NMDA RECEPTOR; POSITIVE ALLOSTERIC MODULATOR; SCHIZOPHRENIA;

DRUG DISCOVERY; HUMANS; MOLECULAR STRUCTURE; RECEPTORS, N-METHYL-D-ASPARTATE; SCHIZOPHRENIA;

EID: 84882716279     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.07.019     Document Type: Review

References (233)

1. K. Mueser, and S. McGurk Lancet 363 2004 2063
2. J.P. McEvoy J. Clin. Psychiatry 68 2007 4
3. M. Green Am. J. Psychiatry 153 1996 321
4. M.F. Green, R.S. Kern, and R.K. Heaton Schizophr. Res. 72 2004 41
5. M. Davidson, S. Galderisi, and M. Weiser Am. J. Psychiatry 166 2009 675
6. W.T. Carpenter, R.R. Conley, R.W. Buchanan, S.J. Enna, and J.T. Coyle Pharmacological Management of Neurological and Psychiatric Disorders 1998 McGraw-Hill New York p 27
7. J.W. Newcomer CNS Drugs 19 Suppl. 1 2005 1
8. S. Miyamoto, G.E. Duncan, C.E. Marx, and J.A. Liberman Mol. Psychiatry 10 2005 79
9. M. Tsuang Biol. Psychiatry 47 2000 210
10. J.J. Mann, and F. Haghighi Biol. Psychiatry 68 2010 403
11. P.F. Sukkivan Nat. Med. 18 2012 210
12. M. Ayalew, H. Le-Niculescu, D.F. Levey, N. Jain, B. Changala, S.D. Patel, E. Winiger, A. Breier, A. Shekhar, R. Amdur, D. Koller, J.I. Nurnberger, A. Corvin, M. Geyer, M.T. Tsuang, D. Salomon, N.J. Schork, A.H. Fanous, M.C. O'Donovan, and A.B. Niculescu Psychiatry 17 2012 887
13. F.M. Benes Biol. Psychiatry 65 2009 1003
14. N.R. Swerdlow Curr. Top. Behav. Neurosci. 4 2011 555
15. D.W. Volk, and D.A. Lewis Curr. Top. Behav. Neurosci. 4 2011 485
16. A. Calsson Neuropsychopharmacology 1 1998 179
17. M. Toda, and A. Abi-Dargham Curr. Psychiatry Rep. 9 2007 329
18. O.D. Howes, and S. Kapur Schizophr. Bull. 35 2009 549
19. D.S. Janowsky, and C. Risch Psychopharmacology 65 1979 73
20. D.C. Javitt Hillside J. Clin. Psychiatry 9 1987 12
21. D.C. Javitt, and S.R. Zukin Am. J. Psychiatry 148 1991 1301
22. J.W. Olney, and N.B. Farber Arch. Gen. Psychiatry 52 1995 998
23. J.T. Coyle Harv. Rev. Psychiatry 3 1996 241
24. J.W. Olney, J.W. Newcomer, and N.B. Farber J. Psychiatry Res. 33 1999 523
25. J.H. Krystal, D.C. D'Souza, D. Mathalon, E. Perry, A. Belger, and R. Hoffman Psychopharmacology 169 2003 215
26. J.T. Coyle Cell. Mol. Neurobiol. 26 2006 363
27. G.J. Marek, B. Behl, A.Y. Bespalov, G. Gross, Y. Lee, and H. Schoemaker Mol. Pharmacol. 77 2009 317
28. J. Lisman, J. Coyle, R. Green, D. Javitt, F. Benes, S. Heckers, and A. Grace Trends Neurosci. 31 2008 234
29. D.C. Javitt Isr. J. Psychiatry Relat. Sci. 47 2010 4
30. F. Lopez-Munoz, and C. Alamo Clin. Neuropharmacol. 34 2011 234
31. H. Homayoun, and B. Moghaddam J. Neurosci. 27 2007 11496
32. D.A. Lewis, A.A. Curley, J.R. Glausier, and D.W. Volk Cell 35 2012 57
33. D. Li, and L. He Genet. Med. 9 2007 4
34. S. Bagade, and M.B. McQueen Nat. Genet. 40 2008 827
35. S. Endele, G. Rosenberger, K. Geider, B. Popp, C. Tamer, I. Stefanova, M. Milh, F. Kortum, A. Fritsch, F.K. Pientka, Y. Hellenbroich, V.M. Kalscheuer, J. Kohlhase, U. Moog, G. Rappold, A. Rauch, H. Ropers, S. von Spiczak, H. Ionnies, N. Villeneuve, L. Villard, B. Zabel, M. Zenker, B. Laube, A. Reis, D. Wieczorek, L. Van Maldergem, and K. Kutsche Nat. Genet. 42 2010 1021
36. T.V. Bliss, and G.L. Collingridge Nature 361 1993 31
37. T.V. Bliss, and G.L. Collingridge Trends Neurosci. 18 1993 54
38. S.F. Traynelis, L.P. Wollmuth, C.J. McBain, F.S. Menniti, K.M. Vance, K.K. Ogden, K.B. Hansen, H. Yuan, S.J. Myers, and R. Dingledine Pharmacol. Rev. 2010 405
39. D. Wojciech, and C.G. Parsons Pharmacol. Rev. 50 1998 597
40. K.K. Ogden, and S.F. Traynelis Cell 32 2011 726
41. D.T. Monaghan, M.W. Irvine, B.M. Costa, G. Fang, and D.E. Jane Neurochem. Int. 61 2012 581
42. R.F. Field, A.G. Walker, and P.J. Conn Cell 17 2011 689
43. T. Yoshida, M. Iyo, and K. Hashimoto Curr. Psychiatry Rev. 8 2012 140
44. A. Bartolomeis, C. Sarappa, S. Magara, and F. Lasevoli Eur. J. Pharmacol. 682 2012 1
45. F.S. Menniti, C.W. Lindsley, P.J. Conn, J. Pandit, P. Zagouraz, and R.A. Volkmann Curr. Top. Med. Chem. 13 2013 26
46. D.C. Javitt, S.R. Zukin, U. Heresco-Levy, and D. Umbricht Schizophr. Bull. 38 2012 958
47. M.J. Noetzel, C.K. Jones, and P.J. Conn Discov. Med. 78 2012 335
48. U. Heresco-Levy, D.C. Javitt, M. Ermilov, C. Mordel, G. Silipo, and M. Lichtenstein Arch. Gen. Psychiatry 56 1999 29
49. B. Borowsky, E. Mezey, and B.J. Hoffman Neuron 10 1993 851
50. J. Gomeza, K. Ohno, and H. Betz Curr. Opin. Drug Discovery Dev. 5 2003 675
51. V. Eulenburg, W. Armsen, H. Betz, and J. Gomeza Trends Biochem. 30 2005 325
52. F. Zafra, C. Gomeza, L. Olivares, C. Aragon, and C. Gimenez Eur. J. Neurosci. 7 1995 1342
53. B. Cubelos, C. Gimenez, and F. Zafra Cereb. Cortex 15 2005 448
54. S. Supplisson, and C. Bergman J. Neurosci. 17 1997 4580
55. H. Lane, Y. Liu, C. Lin, Y. Huang, C. Liao, Y.C. Chang, and G.E. Tsai Int. J. Neuropsychopharmacol. 13 2010 451
56. G. Tsai, H. Lane, P. Yang, M. Chong, and N. Lange Biol. Psychiatry 55 2004 452
57. B.N. Atkinson, M. De Vivo, S.M. Lechner, L. Kowalski, Y. Zheng, and M.A. Klitenkick Soc. Neurosci. Abs. 26 2000 1653
58. B.N. Atkinson, S.C. Bell, M. De Vivo, S.M. Lechner, L. Kowalski, V.I. Ognyanov, C.S. Tham, C. Tsai, J. Jia, D. Ashton, and M.A. Klitenick Mol. Pharmacol. 60 2001 1414
59. Man, T.; Milot, G.; Porter, W. J.; Reel, J. K.; Rudyk, H. C. E.; Valli, M. J.; Walter, M. W.; Patent Appl. WO 2005/100301.
60. K. Hashimoto, Y. Fujita, T. Ishima, S. Chaki, and M. Iyo Eur. Neuropsychopharmacol. 18 2008 414
61. G.G. Kinney, C. Sur, M. Burno, P.J. Mallorga, J.B. Williams, D.J. Figueroa, M. Wittmann, W. Lemaire, and P.J. Conn J. Neurosci. 23 2003 7586
62. K.R. Aubrey, and R.J. Vandenberg Br. J. Pharmacol. 134 2001 1429
63. K.W. Perry, J.F. Falcone, M.J. Fell, J.W. Ryder, H. Yu, P.L. Love, J. Katner, K.D. Gordon, M.R. Wade, T. Man, G.G. Nomikos, L.A. Phebus, A.J. Cauvin, K.W. Johnson, C.K. Jones, B.J. Hoffmann, G.E. Sandusky, M.W. Walter, W.J. Porter, L. Yang, K.M. Merchant, H.E. Shannon, and K.A. Svensson Neuropharmacology 55 2008 743
64. C.L. Cioffi, S. Liu, and M.A. Wolf Annu. Rep. Med. Chem. 45 2010 19 Chapter 2
65. L.G. Harsing, G. Zsilla, P. Matyus, K.M. Nagy, B. Marko, Z. Gyarmati, and J. Timar Act Physiol. Hung. 99 2012 1
66. Albert, J. S.; Wood, M. W. Targets and Emerging Therapies for Schizophrenia, Albert, J. S.; Michael, W. Wood (Eds.), John Wiley & Sons, 2012, p 233.
67. D.C. Javitt Novel Antischizophrenia Treatments M.A. Geyer, G. Gross, Handbook of Experimental Pharmacology 213 2012 Springer Berlin, Heidelberg 367
68. P. Chue Curr. Pharm. Des. 19 2013 1311
69. Lindsley, C. W.; Conn, J. P.; Williams, R.; Jones, C. K.; Sheffer, D. J. Patent Appl. WO2011007899-A1.
70. C.L. Cioffi, M.A. Wolf, P.R. Guzzo, K. Sadalapure, V. Parthasarathy, D. Dethe, J. Maeng, E. Carulli, D.T.J. Loong, X. Fang, M. Hu, P. Gupta, M. Chung, M. Bai, N. Moore, M. Luche, Y. Khmelnitsky, P.L. Love, M.A. Watson, A.J. Mhyre, and S. Liu Bioorg. Med. Chem. Lett. 23 2013 1257
71. Lange, U.; Heutling, A.; Amberg, W.; Ochse, M.; Behl, B.; Hornberger, W.; Mezler, M. Patent Appl. WO2010092181-A1.
72. Yasuhara, A.; Sakagami, K.; Ohta, H.; Hayashi, M.; Shirasaki, Y.; Yamamoto, S.; Shimazakai, Y.; Araki, Y.; Abe, K.; Sun, X. WO2011007899-A1.
73. Giovannini, R.; Bertani, B.; Ferrara, M.; Lingard, I.; Mazzaferro, R.; Rosenbrock, H. WO2013017657-A1.
74. Kolczewski, S.; Pinnard, E.; Stalder, H. WO2010086251-A1.
75. Kolczewski, S.; Pinnard, E. US20110053904-A1.
76. Yamaoto, S.; Ohta, H.; Abe, K.; Araki, Y.; Moriya, M.; Sun, X.; Yasuhara, A. WO2012081665.
77. R. Depoortere, G. Dargazzanli, G. Estesnne-Bouhtou, A. Coste, C. Lanneau, C. Desvignes, M. Poncelet, M. Heaulme, V. Santucci, M. Decobert, A. Cudennec, C. Voltz, D. Boulay, J.P. Terranove, J. Stemmelin, P. Roger, B. Marabout, M. Sevrin, X. Vige, B. Biton, R. Steinberg, D. Francon, R. Alonso, P. Avenet, F. Oury-Donat, G. Perrault, G. Griebel, P. George, P. Soubrie, and B. Scatton Neuropsychopharmacology 30 2005 1963
78. D. Boulay, P. Pichat, G. Dargazanli, G. Estenne-Bouhtou, J.P. Terranove, N. Rogacki, J. Stemmelin, A. Coste, C. Lanneau, C. Desvignes, C. Cohen, R. Alonso, X. Vige, B. Biton, R. Steinberg, M. Sevrin, F. Oury-Donat, P. George, O. Bergis, G. Griebel, P. Avenet, and B. Scatton Pharmacol. Biochem. Behav. 91 2008 47
79. D. Alberti, J.L. Moreau, and J. Lengyel Neuropharmacology 62 2012 1152
80. H. Nishikawa, T. Inoue, T. Izumi, S. Nakagawa, and T. Koyama Behav. Pharmacol. 21 2010 576
81. B.M. Roberts, C.L. Shaffer, P.A. Seymour, C.J. Schmidt, G.V. Williams, and S.A. Castner NeuroReport 21 2010 390
82. D.C. D'Souza, N. Singh, J. Elander, M. Carbuto, B. Pittman, J. Udo de Haes, M. Sjogren, P. Peeters, M. Ranganathan, and J. Schipper Neuropsychopharmacology 37 2012 1036
83. D. Umbricht, M. Martin-Kacklam, and E. Pizzagalli Schizophr. Bull. 37 2011 324
84. http://clinicaltrials.gov/show/NCT01192906.
85. M. Mezler, W. Hornberger, R. Mueller, M. Scmidt, W. Amberg, W. Braje, M. Ochse, H. Schoemaker, and B. Behl Mol. Phramacol. 74 2008 1705
86. Alberti, D.; Moreau, J.; Pinard, E.; Borroni, E.; Hainzl, D.; Lengyel, J.; Hauser, N.; Mory, R.; Knoflach, F.; Wettstein, J. G. Glycine transporter type 1 (GlyT1) inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia, Poster presented at the ACNP 49th annual meeting, Miami Beach, FA, December 5-9, 2010.
87. K. Kopec, D.G. Flood, M. Gasior, B.W. McKenna, E. Zuvich, J. Schreiber, J.M. Salvino, J.T. Durkin, M.A. Ator, and M.J. Marino Biochem. Pharmacol. 80 2010 1407
88. J. Passchier, G. Gentile, R. Porter, H. Herdon, C. Salinas, S. Jakobsen, H. Audrain, M. Laruelle, and R.N. Gunn Synapse 64 2010 542
89. R.N. Gunn, V. Murthy, A.M. Catafau, G. Searle, S. Bullich, M. Slifstein, D. Oullet, S. Zamuner, R. Herance, C. Salinas, R. Pardo-Lozano, E.A. Rabiner, M. Farre, and M. Laruelle Synapse 65 2011 1319
90. T.G. Hamill, W. Eng, A.S.R. Jennings, R.T. Lewis, S. Thomas, S. Wood, L.J. Street, D.D. Wisnoski, S.W. Wolkenberg, C.W. Lindsley, S.M. Sanabria-Bohorquez, S. Patel, C. Ryan, J. Cook, C. Sur, H.D. Burns, and R. Hargreaves Synapse 65 2011 261
91. D.F. Wong, S. Ostrowitzki, Y. Zhou, V. Raymont, C. Hofmann, E. Borroni, A. Kumar, N. Parkar, J.R. Brasic, J. Hilton, R.F. Dannals, and M. Martin-Facklam NeuroImage 75 2013 282
92. A. Panatier, D.T. Theodosis, J.P. Mothet, B. Touquet, L. Pollegioni, D.A. Poulain, and S.H. Oliet Cell 125 2006 775
93. T. Matsui, M. Sekiguchi, A. Hashimoto, U. Tomita, T. Nishikawa, and K.J. Wada J. Neurochem. 65 1995 454
94. U. Heresco-Levy, D.C. Javitt, R. Ebstein, A. Vass, P. Lichtenberg, G. Bar, S. Catinari, and M. Ermilov Biol. Psychiatry 57 2005 577
95. C. Madeira, M.E. Freitas, C. Vargas-Lopes, H. Wolosker, and R. Panizzutti Schizophr. Res. 101 2008 76
96. K. Hashimoto, Y. Fujita, M. Horio, S. Kunitachi, M. Iyo, D. Ferraris, and T. Tsukamoto Biol. Psychiatry 65 2009 1103
97. S.M. Smith, J.M. Uslaner, and P.H. Hutson Open Med. Chem. J. 4 2010 3
98. D.V. Ferraris, and T. Tsukamoto Curr. Pharm. Des. 17 2011 103
99. V. Labrie, A.H.C. Wong, and J.C. Roder Neuropharmacology 62 2012 1484
100. S. Sacchi, E. Rosini, L. Pollegioni, and G. Molla Curr. Pharm. Des. 19 2013 2499
101. H.J. Tuominen, J. Tiihonen, and K. Wahlbeck Eur. Neuropsychophramacol. 16 2005 59
102. D.C. Goff Schizophr. Bull. 5 2012 936
103. D.C. Goff, C. Cather, J.D. Gottlieb, A.E. Evins, J. Walsh, L. Raeke, M.W. Otto, D. Schoenfeld, and M.F. Green Schizophr. Res. 106 2008 320
104. A. Sheinin, S. Shait, and M. Benveniste Neuropharmacology 41 2001 151
105. B.G. Hillman, S.C. Gupta, D.J. Stairs, A. Buonanno, and S.M. Dravid Neurobiol. Learn Mem. 2011 404
106. M. Beneyto, and J.H. Meador-Woodrfuff Neuropsychopharmacology 33 2008 2175
107. S.M. Dravid, P.B. Burger, A. Prakash, M.T. Geballe, R. Yadav, P. Le, K. Vellano, J.P. Snyder, and S.F. Tranelis J. Neurosci. 30 2010 2741
108. J.R. Moskal, A.G. Kuo, C. Weiss, P.L. Wood, A.O. Hanson, S. Kelso, R.B. Harris, and J.F. Disterhoft Neuropharmacology 49 2005 1077
109. X. Zhang, J.A. Sullivan, J.R. Moskal, and P.K. Stanton Neuropharmacology 55 2008 1238
110. J. Burgdorf, X. Zhang, C. Weiss, E. Matthews, J.F. Disterhoft, P.K. Stanton, and J.R. Moskal Neurobiol. Aging 32 2011 698
111. http://www.naurex.com/index.html.
112. S. Erhardt, L. Schwieler, L. Nilsson, K. Linderholm, and G. Enberg Physiol. Behav. 92 2007 203
113. S. Erhardt, S. Olsson, and G. Enberg CNS Drugs 23 2009 91
114. S. Erhardt, K. Blennow, C. Nordin, E. Skogh, L.H. Lindstrom, and G. Enberg Neurosci. Lett. 313 2001 96
115. R. Schwarcz, A. Rassoulpour, H.Q. Wu, D. Medoff, C.A. Tamminga, and R.C. Roberts Biol. Psychiatry 50 2001 521
116. M.C. Potter, G.I. Elmer, R. Bergeron, E.X. Albuquerque, P. Guidetti, H. Wu, and R. Scwarcz Neuropsychophramacology 35 2010 1734
117. R. Pellicciari, R.C. Rizzo, G. Costantino, M. Marinozzi, L. Amori, P. Guidetti, H. Wu, R. Schwarcz, and S. Erhardt ChemMedChem 1 2006 528
118. L. Amori, H. Wu, M. Marinozzi, R. Pellicciari, P. Guidetti, and R. Schwarcz Neuroscience 156 2009 196
119. L. Amori, P. Guidetti, R. Pellicciari, R. Kajii, and R. Schwarcz J. Neurochem. 109 2009 316
120. F. Rossi, C. Valentian, S. Garavaglia, K. Sathyasaikumar, R. Schwarcz, K. Okuwaki, S. Ono, Y. Kajii, and M. Rizzi J. Med. Chem. 52 2010 5684
121. J.L. Henderson, A. Sawant-Basak, J.B. Tuttle, A.B. Dounay, L.A. McAllister, J. Pandit, S. Rong, X. Hou, B.M. Bechle, J. Kim, V. Parikh, S. Ghosh, E. Evrard, L.E. Zawadzke, M.A. Salafia, B. Rago, R.S. Obach, A. Clark, K.R. Fonseca, C. Chang, and P.R. Verhoest Med. Chem. Commun. 4 2013 125
122. A.B. Dounay, M. Anderson, B.M. Bechle, E. Evrard, X. Gan, J. Kim, L.A. McAllister, J. Pandit, S. Rong, M.A. Salafia, and J.B. Tuttle Bioorg. Med. Chem. Lett. 23 2013 1961
123. A.B. Dounay, M. Anderson, B.M. Bechle, B.M. Campbell, M.M. Claffey, A. Evdokimov, E. Evrard, K.R. Fonseca, X. Gan, S. Ghosh, M.M. Hayward, W. Horner, J. Kim, L.A. McAllister, J. Pandit, V. Paradis, V.D. Parikh, A.R. Reese, S. Rong, M.A. Salafia, K. Schuyten, C.A. Strick, J.B. Tuttle, J. Valentine, H. Wang, L.E. Zawadzke, and P.R. Verhoest ACS Med. Chem. Lett. 3 2012 187
124. (b) http://www.schizophreniaforum.org/new/detail.asp?id=1654.
125. C.L. Palmer, L. Cotton, and J.M. Henley Pharmacol. Rev. 57 2005 253
126. B. Sommer, K. Keinanen, and T.A. Verdoorn Science 249 1990 1580
127. M. Mansour, N. Nagarajan, and R.B. Nehring Neuron 32 2001 841
128. E. Gouaux J. Physiol. 554 2004 249
129. I.H. Greger, and J.A. Estaban Curr. Opin. Neurobiol. 17 2007 289
130. R. Malinow, and R.C. Malenka Annu. Rev. Neurosci. 25 2002 103
131. S.F. Traynelis, L.P. Wollmuth, C.J. McBain, F.S. Menniti, K.M. Vance, K.K. Ogden, K.B. Hansen, H. Yuan, S.J. Myers, and R. Dingeldine Pharmacol. Rev. 62 2010 405
132. G. Lynch, and C. Gall Trends Neurosci. 29 2006 554
133. P. Chang, D. Verbich, and R.A. McKinney Eur. J. Neurosci. 35 2012 1908
134. B. Pirotte, P. Francotte, E. Goffin, and P. de Tullio Expert Opin. Ther. Pat. 23 2013 615
135. A. Christopoulos Nat. Rev. Drug. Disc. 1 2001 198
136. F.S. Menniti, C.W. Lindsley, P.J. Conn, J. Pandit, P. Zagouras, and R.A. Volkmann Curr. Top. Med. Chem. 13 2013 26
137. U. Staubli, G. Rogers, and G. Lynch Proc. Natl. Acad. Sci. U.S.A. 1994 91
138. M.T. Rogen, U.V. Staubli, and J.E. LeDoux J. Neurosci. 17 1997 5928
139. I. Zivkovic, D.M. Thompson, M. Bertolino, D. Uzunov, M. DiBella, and E. Costa J. Pharmacol. Ther. 272 1995 300
140. C. Lebrun, E. Piliere, and P. Lestage Eur. J. Pharmacol. 401 2000 205
141. M.L. Wooley, K.A. Waters, J.E. Gartlon, L.P. Lacroix, C. Jennings, and F. Shaugnessey Psychopharmacology 202 2009 343
142. D.C. Goff, J.S. Lamberti, A.C. Leon, M.F. Green, A.L. Miller, and J. Patel Neuropsychopharmacology 33 2007 1461
143. J.P. Conn, and J.P. Pin Annu. Rev. Pharmacol. Toxicol. 37 1997 205
144. J.N. Kew, and J.A. Kemp Psychopharmacology 179 2005 4
145. H. Awad, G.W. Hubert, Y. Smith, A.I. Levey, and J.P. Conn J. Neurosci. 20 2000 7871
146. W.D. Shipe, S.E. Wolkenberg, D.L. Williams, and C.W. Lindsley Curr. Opin. Drug. Discovery Dev. 8 2005 449
147. J.P. Conn, A. Christopoulos, and C.W. Lindsley Nat. Rev. Drug Disc. 8 2009 41
148. T.M. Piers, D.H. Kim, B.C. Kim, P. Regan, D.J. Whitcomb, and K. Cho Front. Pharmacol. 3 2012 1
149. J.P. Tizzano, K.I. Griffey, and D.D. Schoepp Neuropharmacology 34 1995 1063
150. L. Camon, P. Vives, N.L. De Vera, and E. Martinez Cell Mol. Life Sci. 51 1998 339
151. C. Thomsen, and N.O. Dalby Neuropharmacology 34 1998 1063
152. J.A. O'Brien, W. Lemaire, T.B. Chen, R.S. Chang, D.J. Jacobson, P.J. Conn, and D.L. Williams Mol. Pharmacol. 64 2003 731
153. J.A. O'Brien, W. Lemaire, M. Wittmann, D.J. Jacobson, S.N. Ha, D.D. Wisnoski, C.W. Lindsley, H.J. Schaffhauser, B. Rowe, C. Sur, M.E. Duggan, D.J. Pettibone, P.J. Conn, and D.L. Williams J. Pharmacol. Exp. Ther. 309 2004 568
154. D.L. Williams, and C.W. Lindsley Curr. Top. Med. Chem. 5 2005 825
155. Le Poul, E.; Bessis, A. S.; Lutgens, R.; Bonnet, B.; Rocher, J. P.; Epping-Jordan, M. P.; Mutel, V. 5th International Metabotropic Glutamate Receptors Meeting, 2005, Taormina, Italy.
156. R.M. Cleva, and M.F. Olive Molecules 16 2011 2097
157. S.R. Stauffer ACS Chem. Neurosci. 2 2011 450
158. C.W. Lindsley, and S.R. Stauffer Pharm. Pat. Analyst 2 2013 93
159. J.A. O'Brien, W. Lemaire, T. Chen, R.S. Chang, D.J. Jacobson, S.N. Ha, C.W. Lindsley, H.J. Schaffhauser, C. Sur, D.J. Pettibone, P.J. Conn, and D.L. Williams Mol. Pharmacol. 64 2003 731
160. Z. Zhao, D.D. Wisnoski, J.A. O'Brien, W. Lemaire, D.L. Williams, D.J. Jacobson, M. Wittmann, S.N. Ha, H.J. Schaffhauser, C. Sur, D.J. Pettibone, M.E. Duggan, P.J. Conn, G.D. Hartman, and C.W. Lindsley Bioorg. Med. Chem. Lett. 17 2007 1386
161. Y. Zhang, A.L. Rodriguez, and J.P. Conn J. Pharmacol. Exp. Ther. 315 2005 1212
162. M.J. Noetzel, K.J. Gregory, P.N. Vinson, J.T. Manka, S.R. Stauffer, C.W. Lindsley, C.M. Niswender, Z. Xiang, and P.J. Conn Mol. Pharmacol. 83 2013 835
163. C.W. Lindsley, D.D. Wisnoski, W.H. Leister, J.A. O'Brien, W. Lemaire, D.L. Williams, M. Burno, C. Sur, G.G. Kinney, D.J. Pettibone, M.E. Duggan, P.J. Conn, and J.R. Huff J. Med. Chem. 47 2004 5825
164. G.G. Kinney, J.A. O'Brien, W. Lemaire, M. Burno, D.J. Bickel, M.K. Clements, T.B. Chen, D.D. Wisnoski, C. Lindsley, P.R. Tiller, S. Smith, M.A. Jacobson, C. Sur, M.E. Duggan, D.J. Pettibone, P.J. Conn, and D.L. Williams J. Pharmacol. Exp. Ther. 313 2005 199
165. J.M. Darrah, M.R. Stefani, and B. Moghaddam Behav. Pharmacol. 19 2008 225
166. M.R. Stefani, and B. Moghaddam Eur. J. Pharmacol. 639 2010 26
167. S.W. Fowler, A.K. Ramsey, J.M. Walker, P. Serfozo, M.F. Olive, T.R. Schachtman, and A. Simonyi Neurobiol. Learn. Mem. 95 2011 73
168. J.D. Vardigan, S.L. Huszar, C.H. McNaughton, P.H. Hutson, and J.M. Uslaner Pharmacol. Biochem. Behav. 95 2010 223
169. C.M. Reichel, M. Schwendt, J.F. McGintty, M.F. Olive, and R.E. See Neuropsychopharmacology 36 2011 782
170. C.R. Hopkins, C.W. Lindsley, and C.M. Niswender Future Med. Chem. 1 2009 501
171. M.R. Wood, C.R. Hopkins, J.T. Brogan, P.J. Conn, and C.W. Lindsley Biochemistry 50 2011 2403
172. J.P. Lamb, D.W. Engers, C.M. Niswender, A.L. Rodriguez, D.F. Venable, P.J. Conn, and C.W. Lindsley Bioorg. Med. Chem. Lett. 21 2011 2711
173. K.J. Gregory, E.D. Nguyen, S.D. Reiff, E.F. Squire, S.R. Stauffer, C.W. Lindsley, J. Meiler, and P.J. Conn Mol. Pharmacol. 83 2013 991
174. S. Parmentier-Batteur, P.H. Hutson, K. Menzel, J.M. Uslaner, B.A. Mattson, J.A. O'Brien, B.C. Magliaro, T. Forest, C.A. Stump, R.M. Tynebor, N. Lambeng, H. Faure, E. Le Poul, S. Poli, T.W. Rosahl, J. Rocher, R. Hargreaves, and T.M. Williams Neuropharmacology 25 2013 25
175. D.D. Schoepp, and G.J. Marek CNS Neurol. Disord. Drug Targets 1 2002 215
176. J.A. Monn, M.J. Valli, S.M. Massey, R.A. Wright, C.R. Salhoff, J.P. Tizzano, M.J. Kallman, D.R. Helton, and D.D. Schoepp J. Med. Chem. 40 1997 528
177. J.A. Monn, M.J. Valli, S.M. Massey, M.M. Hassen, T.J. Kress, J.P. Wepsiec, A.R. Harkess, J.L. Grutsch, R.A. Wright, B.G. Johnson, S.L. Andis, A. Kingston, R. Tomlinson, R. Lewis, K.R. Griffey, J.P. Tizzano, and D.D. Schoepp J. Med. Chem. 42 1999 1027
178. S.T. Patil, L. Zhang, F. Martenyi, S.L. Lowe, K.A. Jackson, B.V. Andreev, A.S. Avedisova, L.M. Bardenstein, A.M. Gurovich, M.A. Morozova, S.N. Mosolov, N.G. Neznanov, A.M. Reznik, A.B. Smulevich, V.A. Tochilov, B.G. Johnson, J.A. Monn, and D.D. Schoepp Nat. Med. 13 2007 1102
179. http://clinicaltrials.gov/ct2/show/NCT01487083.
180. M.E. Fraley Exp. Opin. Ther. Pat. 19 2009 1259
181. A.A. Trabanco, J. Cid, H. Lavreysen, G.J. Macdonald, and G. Tresadern Curr. Med. Chem. 18 2011 47
182. Matsuda, Y.; Hattori, N.; Sakagami, K.; Amada, H.; Urabe, H.; Tamita, T.; Shimono, R.; Yasuhara, A.; Masuda, S.; Konishi, K.; Nakamura, T.; Yamamoto, S. WO2013062074-A1.
183. M.P. Johnson, D. Barda, T.C. Britton, R. Emkey, J.P. Hornback, and D.D. Schoepp Psychopharmacology 179 2005 271
184. R. Galici, N.G. Echemendia, A.L. Rodriguez, and J.P. Conn J. Pharmacol. Exp. Ther. 315 2005 1181
185. R. Galici, C.K. Jones, H. Kamondanai, N. Yi, N.G. Echemendia, L.C. Williams, T. de Paulis, and J.P. Conn J. Pharmacol. Exp. Ther. 318 2006 173
186. S.P. Govek, C. Bonnefous, J.H. Hutchinson, T. Kamenecka, J. McQuiston, R. Pracitto, L.X. Zhao, M.F. Gardner, J.K. James, L.P. Daggett, B.A. Rowe, H. Scaffhauser, L.J. Bristow, U.C. Campbell, D.E. Rodrigues, and J.M. Vernier Bioorg. Med. Chem. Lett. 15 2005 4068
187. http://www.addextherapeutics.com.
188. T.I. Bonner Trends Neurosci. 12 1989 148
189. S.T. Rouse, M.J. Marino, and L.T. Potter Life Sci. 64 1999 501
190. L.A. Volpicelli, and A.I. Levey Br. J. Pharmacol. 145 2004 59
191. T.J. Raedler, F.P. Bymaster, R. Tandon, D. Copolov, and B. Dean Mol. Psychiatry 12 2007 232
192. E. Scarr, and B. Dean J. Neurochem. 107 2008 1188
193. D.J. Foster, C.K. Jones, and P.J. Conn Discov. Med. 14 2012 413
194. F.P. Bymaster, D.L. McKinze, C.C. Felder, and J. Wess Neurochemistry 28 2003 437
195. J. Wess Annu. Rev. Pharmacol. Ther. 117 2008 232
196. D. Dean, J.M. Crook, K. Opeskin, C. Hill, N. Keks, and D.L. Copolov Mol. Psychiatry 1 1996 54
197. J.M. Crook, E. Tomaskovic-Crook, D.L. Copolov, and B. Dean Biol. Psychiatry 48 2000 381
198. J.M. Crook, E. Tomaskovic-Crook, D.L. Copolov, and B. Dean Am. J. Psychiatry 158 2001 918
199. B. Dean, M. McLeod, D. Keriakous, J. McKenzie, and E. Scarr Mol. Psychiatry 7 2002 1083
200. D. Liao, C.J. Hong, and H.M. Chen Neuropsychobiology 48 2003 72
201. F.P. Bymaster, C.A. Whitesitt, H.E. Shannon, N. DeLapp, J.S. Ward, D.O. Calligaro, L.A. Shipley, J.L. Buelke-Sam, N.C. Bodick, L. Farde, M.J. Sheardown, P.H. Oelson, K.T. Hansen, P.D. Suzdak, M.D.B. Swedberg, P. Sauergerg, and C.H. Mitch Drug Dev. Res. 40 1997 158
202. A. Shekhar, W.Z. Potter, J. Lightfoot, J. Lienemann, S. Dube, C. Mallinckrodt, F.P. Bymaster, D.L. Mckinzie, and C.C. Lalder Am. J. Psychiatry 165 2008 1033
203. W.Y. Chan, D.L. McKinzie, S. Bose, S.N. Mitchell, J.M. Witkin, R.C. Thompson, A. Christopoulos, S. Lazareno, N.J.M. Birdsall, F.P. Bymaster, and C.C. Felder Proc. Nat. Acad. Sci. U.S.A. 105 2008 10978
204. T.M. Bridges, E.P. LeBois, C.R. Hopkins, M.R. Wood, C.K. Jones, P.J. Conn, and C.W. Lindsley Drug News Perspect. 23 2010 229
205. S.D. Kuduk, and D.C. Beshore Exp. Opin. Ther. Pat. 22 2012 1385
206. G.J. Digby, M.J. Noetzel, M. Bubser, T.J. Utley, A.G. Walker, N.E. Byun, E.P. Lebois, Z. Xiang, D.J. Sheffler, H.P. Cho, A.A. Davis, N.E. Nemirovsky, S.E. Mennenga, B.W. Camp, H.A. Bimonte-Nelson, J. Bode, K. Italiano, C.W. Lindsley, C.K. Jones, and P.J. Conn J. Neurosci. 32 2012 8532
207. P.R. Reid, T.M. Bridges, D.J. Sheffler, H.P. Cho, L.M. Lewis, E. Days, J.S. Daniels, C.K. Jones, C.M. Niswender, C.D. Waever, P.J. Conn, C.W. Lindsley, and M.R. Wood Bioorg. Med. Chem. Lett. 21 2011 2697
208. Conn, J. P.; Wood, M. R.; Hopkins, C. R.; Melancon, B. J.; Poslusney, M.; Engers, D. W.; Shortell, B. D. Patent Appl. WO2013063549-A1.
209. P.R. Reid, T.M. Bridges, D.J. Sheffler, H.P. Cho, L.M. Lewis, E. Days, J.S. Daniels, C.K. Jones, C.M. Niswender, C.D. Weaver, J.P. Conn, C.W. Lindsley, and M.R. Wood Bioorg. Med. Chem. Lett. 21 2011 2697
210. S. Vincini, J.F. Wang, J.H. Li, W.J. Zhu, Y.H. Wang, and J. Luo Neurophysiology 79 1998 555
211. E.M. Quinlan, D. Lebel, I. Brosh, and E. Barkai Neuron 41 2004 185
212. C. Akazawa, R. Shigemoto, Y. Bessho, S. Nakanishi, and N. Mizunao J. Comp. Neurol. 347 1994 150
213. S. Jones, and A.J. Gibb J. Physiol. London 569 2005 209
214. H. Monyer, N. Burnashev, D.J. Laurie, B. Sakmann, and P.H. Seeburg Neuron 12 1994 529
215. K. Williams Mol. Pharmacol. 44 1993 851
216. K.W. Muir Curr. Opin. Pharmacol. 6 2006 53
217. F. Perin-Dureau, J. Rachline, J. Neyton, and P. Paoletti J. Neurosci. 22 2002 5955
218. E. Karakas, N. Simorowski, and H. Furukawa EMBO J. 28 2009 3910
219. L. Mony, L. Krzackzkowski, M. Leonetti, A. Le Goff, K. Alarcon, J. Neyton, H. Bertrand, F. Acher, and P. Paoletti Mol. Pharmacol. 75 2009 60
220. E. Karakas, N. Simorowski, and H. Furukawa Nature 475 2011 249
221. B.L. Chenard, J. Bordner, T.W. Butler, L.K. Chambers, M.A. Collins, D.L. De Costa, M.F. Ducat, M.L. Dumaont, C.B. Fox, and E.E. Mena J. Med. Chem. 38 1995 3138
222. F. Menniti, B.L. Chenard, M.A. Collins, M.F. Ducat, I. Shalaby, and F. White Eur. J. Pharmacol. 331 1997 117
223. R.E. Merchant, M.R. Bullock, C.A. Carmack, A.K. Shah, K.D. Wilner, G. Ko, and S.A. Williams Ann. N.Y. Acad. Sci. 890 1999 42
224. M.R. Bullock, R.E. Merchant, C.A. Carmack, E. Doppenberg, A.K. Shah, K.D. Wilner, G. Ko, and S.A. Williams Ann. N.Y. Acad. Sci. 890 1999 51
225. S.H. Preskorn, B. Baker, S. Kolluri, F.S. Menniti, M. Krams, and J.W. Landen J. Clin. Psychopharmacol. 28 2008 631
226. K. Williams, A.M. Zappia, D.B. Pritchett, Y.M. Shen, and P.B. Molinoff Mol. Pharmacol. 45 1994 803
227. P. Paoletti, J. Neyton, and P. Ascher Neuron 15 1995 1109
228. M. Horak, K. Vleck, M. Petrovic, H. Chodounska, and L. Vyklicky J. Neurosci. 24 2004 10318
229. P. Mullasseril, K.B. Hansen, K.M. Vance, K.K. Ogden, H.J. Yaun, N.L. Kurtkaya, R. Santangelo, A.G. Orr, P. Le, K.M. Vellano, D.C. Liotta, and S.F. Traynelis Nat. Commun. 1 2010 90
230. E. Bettini, A. Sava, C. Griffante, C. Carignani, A. Buson, A.M. Capelli, M. Negri, F. Andreetta, S.A. Senar-Sancho, L. Guiral, and F. Cardullo J. Pharmacol. Exp. Ther. 335 2010 636
231. T.M. Acker, H. Yuan, K.B. Hansen, K.M. Vance, K.K. Ogden, H.S. Jensen, P.B. Burger, P. Mullasseril, J.P. Snyder, D.C. Liotta, and S.F. Traynelis Mol. Pharmacol. 80 2011 782
232. C.A. Mosely, T.M. Acker, K.B. Hansen, P. Mullasseril, K.T. Andersen, P. Le, K.M. Vellano, H. Brauner-Osborne, D.C. Liotta, and S.F. Traynelis J. Med. Chem. 53 2010 5476
233. B.M. Costa, M.W. Irvine, G. Fang, R.J. Eaves, M.B. Mayo-Martin, B. Laube, D.E. Jane, and D.T. Maonaghan Neuropharmacology 62 2012 1730