Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu 5 PAM

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 12, 2012, Pages 3921-3925

  Sheffler, Douglas J ^a,b   Wenthur, Cody J ^a   Bruner, Joshua A ^a   Carrington, Sheridan J S ^a   Vinson, Paige N ^a   Gogi, Kiran K ^a   Blobaum, Anna L ^a,b   Morrison, Ryan D ^a,b   Vamos, Mitchell ^d   Cosford, Nicholas D P ^d   Stauffer, Shaun R ^a,c   Scott Daniels, J ^a,b   Niswender, Colleen M ^a   Jeffrey Conn, P ^a,b   Lindsley, Craig W ^a,b  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^c VANDERBILT UNIVERSITY   (United States)

^d BURNHAM INSTITUTE   (United States)

Author keywords

Metabotropic glutamate receptor 3; mGlu3; Molecular switch; NAM

Indexed keywords

LIGAND; METABOTROPIC RECEPTOR 3; ML 289; UNCLASSIFIED DRUG; VU 0092273; VU 0463597;

ALLOSTERISM; ARTICLE; CONCENTRATION RESPONSE; DRUG ACTIVITY; DRUG BINDING; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; IC 50; MOLECULAR INTERACTION; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ALLOSTERIC REGULATION; CELL LINE; CENTRAL NERVOUS SYSTEM; DRUG DISCOVERY; GLUTAMIC ACID; HUMANS; MICROSOMES, LIVER; MOLECULAR PROBES; PERMEABILITY; PIPERIDINES; RECEPTORS, METABOTROPIC GLUTAMATE; SENSITIVITY AND SPECIFICITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84861570191     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.04.112     Document Type: Article

References (31)

1. D.D. Schoepp, D.E. Jane, and J.A. Monn Neuropharmacology 38 1999 1431
2. P.J. Conn, and J.-P. Pin Annu. Rev. Pharmacol. Toxicol. 37 1997 205
3. B.J. Melancon, C.R. Hopkins, M.R. Wood, K.A. Emmitte, C.M. Niswender, A. Christopoulos, P.J. Conn, and C.W. Lindsley J. Med. Chem. 55 2012 1445
4. P.J. Conn, A. Christopolous, and C.W. Lindsley Nat. Rev. Drug Disc. 8 2009 41
5. P.J. Conn, C.W. Lindsley, and C. Jones Trends Pharmacol. Sci. 30 2009 25
6. A.J. Robichaud, D.W. Engers, C.W. Lindsley, and C.R. Hopkins ACS Chem. Neurosci. 2 2011 433
7. D.J. Sheffler, A.B. Pinkerton, R. Dahl, A. Markou, and N.D.P. Cosford ACS Chem. Neurosci. 2 2011 382
8. D.R. Owen ACS Chem. Neurosci. 2 2011 394
9. K.A. Emmitte ACS Chem. Neurosci. 2 2011 443
10. S.R. Stauffer ACS Chem. Neurosci. 2 2011 450
11. G. Suzuki, N. Tsukamoto, H. Fushiki, A. Kawagishi, M. Nakamura, H. Kurihara, M. Mitsuya, M. Ohkubo, and H. Ohta J. Pharmacol. Exp. Ther. 323 2007 147
12. P.J. Harrision, L. Lyon, L.J. Sartorius, P.W.J. Burnet, and T.A. Lane J. Psychopharmacol. 22 2008 308
13. J.N.C. Kew, and J.A. Kemp Psychopharmacology 179 2005 4
14. T.J. Woltering, J. Wichmann, E. Goetschi, F. Knoflach, T.M. Ballard, J. Huwyler, and S. Gatti Bioorg. Med. Chem. Lett. 20 2010 6969
15. C. Corti, G. Battaglia, G. Molinaro, B. Riozzi, A. Pittaluga, M. Corsi, M. Mugnaini, F. Nicoletti, and V. Bruno J. Neurosci. 27 2007 8297
16. B. Moghaddam, and B.W. Adams Science 281 1998 1349
17. F. Matrrisciano, I. Panaccione, M. Zusso, P. Giusti, R. Tatarelli, L. Iacovelli, A.A. Mathe, S.H. Gruber, F. Nicoletti, and P. Girardi Mol. Psychiarty 12 2007 704
18. A. Markou Biol. Psychiatry 61 2007 17
19. B. Campo, M. Kalinichev, N. Lambeng, M. El Yacoubi, I. Royer-Urios, M. Schneider, C. Legarnd, D. Parron, F. Girard, A. Bessif, S. Poli, J.-M. Vaugeois, E. Le Poul, and S. Celanire J. Neurogenet. 24 2011 152
20. F. Caraci, G. Molinaro, G. Battaglia, M.L. Giuffrida, B. Riozzi, A. Traficante, V. Bruno, M. Cannella, S. Mero, X. Wang, B.A. Heinz, E.S. Nisenbaum, T.C. Britton, F. Drago, M.A. Sortino, A. Copani, and F. Nicoletti Mol. Pharm. 79 2011 618
21. C.M. Niswender, K.A. Johnson, Q. Luo, J.E. Ayala, C. Kim, P.J. Conn, and C.D. Weaver Mol. Pharm. 73 2008 1213
22. S. Sharma, A. Rodriguez, P.J. Conn, and C.W. Lindsley Bioorg. Med. Chem. Lett. 18 2008 4098
23. S. Sharma, J. Kedrowski, J.M. Rook, J.M. Smith, C.K. Jones, A.L. Rodriguez, P.J. Conn, and C.W. Lindsley J. Med. Chem. 52 2010 4103
24. M.R. Wood, C.R. Hopkins, J.T. Brogan, P.J. Conn, and C.W. Lindsley Biochemistry 50 2011 2403
25. R. Williams, J.T. Manka, A.L. Rodriguez, P.N. Vinson, C.M. Niswender, C.D. Weaver, C.K. Jones, P.J. Conn, C.W. Lindsley, and S.R. Stauffer Bioorg. Med. Chem. Lett. 21 2011 1350
26. A.L. Rodriguez, M.D. Grier, C.K. Jones, E.J. Herman, A.S. Kane, R.L. Smith, R. Williams, Y. Zhou, J.E. Marlo, E.L. Days, T.N. Blatt, S. Jadhav, U. Menon, P.N. Vinson, J.M. Rook, S.R. Stauffer, C.M. Niswender, C.W. Lindsley, C.D. Weaver, and P. Conn J. Mol. Pharm. 78 2010 1105
27. A. Ritzen, R. Sindet, M. Hentzer, N. Svendsen, R.M. Brodbeck, and C. Bungaard Bioorg. Med. Chem. Lett. 19 2009 3275
28. W.H. Leister, K.A. Strauss, D.D. Wisnoski, Z. Zhao, and C.W. Lindsley J. Comb. Chem. 5 2003 322
29. For full information on the targets in the Lead Profiling Screen at Ricerca, please see: www.ricerca.com.
30. For information on the MLPCN please see: http://mli.nih.gov/mli/mlpcn/.
31. To request your free sample of ML289, please email: craig. lindsley@vanderbilt.edu.