-
1
-
-
77949516412
-
Metabotropic glutamate receptors: Physiology, pharmacology, and disease
-
Niswender, C. M. and Conn, P. J. (2010) Metabotropic glutamate receptors: physiology, pharmacology, and disease Annu. Rev. Pharmacol. Toxicol. 50, 295-322
-
(2010)
Annu. Rev. Pharmacol. Toxicol.
, vol.50
, pp. 295-322
-
-
Niswender, C.M.1
Conn, P.J.2
-
2
-
-
84873904196
-
Pharmacology of metabotropic glutamate receptor allosteric modulators: Structural basis and therapeutic potential for CNS disorders
-
Gregory, K. J., Noetzel, M. J., and Niswender, C. M. (2013) Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders Prog. Mol. Biol. Transl. Sci. 115, 61-121
-
(2013)
Prog. Mol. Biol. Transl. Sci.
, vol.115
, pp. 61-121
-
-
Gregory, K.J.1
Noetzel, M.J.2
Niswender, C.M.3
-
3
-
-
80051728277
-
Progress toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5)
-
Stauffer, S. R. (2011) Progress toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5) ACS Chem. Neurosci. 2, 450-470
-
(2011)
ACS Chem. Neurosci.
, vol.2
, pp. 450-470
-
-
Stauffer, S.R.1
-
4
-
-
80051710347
-
Recent Advances in the Design and Development of Novel Negative Allosteric Modulators of mGlu5
-
Emmitte, K. A. (2011) Recent Advances in the Design and Development of Novel Negative Allosteric Modulators of mGlu5 ACS Chem. Neurosci. 2, 411-432
-
(2011)
ACS Chem. Neurosci.
, vol.2
, pp. 411-432
-
-
Emmitte, K.A.1
-
5
-
-
0032853255
-
2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist
-
DOI 10.1016/S0028-3908(99)00082-9, PII S0028390899000829
-
Gasparini, F., Lingenhohl, K., Stoehr, N., Flor, P. J., Heinrich, M., Vranesic, I., Biollaz, M., Allgeier, H., Heckendorn, R., Urwyler, S., Varney, M. A., Johnson, E. C., Hess, S. D., Rao, S. P., Sacaan, A. I., Santori, E. M., Velicelebi, G., and Kuhn, R. (1999) 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist Neuropharmacology 38, 1493-1503 (Pubitemid 29457731)
-
(1999)
Neuropharmacology
, vol.38
, Issue.10
, pp. 1493-1503
-
-
Gasparini, F.1
Lingenhohl, K.2
Stoehr, N.3
Flor, P.J.4
Heinrich, M.5
Vranesic, I.6
Biollaz, M.7
Allgeier, H.8
Heckendorn, R.9
Urwyler, S.10
Varney, M.A.11
Johnson, E.C.12
Hess, S.D.13
Rao, S.P.14
Sacaan, A.I.15
Santori, E.M.16
Velicelebi, G.17
Kuhn, R.18
-
6
-
-
0033004276
-
SIB-1757 and SIB-1893: Selective, noncompetitive antagonists of metabotropic glutamate receptor type 5
-
Varney, M. A., Cosford, N. D., Jachec, C., Rao, S. P., Sacaan, A., Lin, F. F., Bleicher, L., Santori, E. M., Flor, P. J., Allgeier, H., Gasparini, F., Kuhn, R., Hess, S. D., Velicelebi, G., and Johnson, E. C. (1999) SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5 J. Pharmacol. Exp. Ther. 290, 170-181 (Pubitemid 29302317)
-
(1999)
Journal of Pharmacology and Experimental Therapeutics
, vol.290
, Issue.1
, pp. 170-181
-
-
Varney, M.A.1
Cosford, N.D.P.2
Jachec, C.3
Rao, S.P.4
Sacaan, A.5
Lin, F.-F.6
Bleicher, L.7
Santori, E.M.8
Flor, P.J.9
Allgeier, H.10
Gasparini, F.11
Kuhn, R.12
Hess, S.D.13
Velicelebi, G.14
Johnson, E.C.15
-
7
-
-
84862964996
-
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function
-
Noetzel, M. J., Rook, J. M., Vinson, P. N., Cho, H. P., Days, E., Zhou, Y., Rodriguez, A. L., Lavreysen, H., Stauffer, S. R., Niswender, C. M., Xiang, Z., Daniels, J. S., Jones, C. K., Lindsley, C. W., Weaver, C. D., and Conn, P. J. (2012) Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function Mol. Pharmacol. 81, 120-133
-
(2012)
Mol. Pharmacol.
, vol.81
, pp. 120-133
-
-
Noetzel, M.J.1
Rook, J.M.2
Vinson, P.N.3
Cho, H.P.4
Days, E.5
Zhou, Y.6
Rodriguez, A.L.7
Lavreysen, H.8
Stauffer, S.R.9
Niswender, C.M.10
Xiang, Z.11
Daniels, J.S.12
Jones, C.K.13
Lindsley, C.W.14
Weaver, C.D.15
Conn, P.J.16
-
8
-
-
33846936284
-
Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA
-
DOI 10.1016/j.bmcl.2006.11.081, PII S0960894X06013825
-
Zhao, Z., Wisnoski, D. D., O'Brien, J. A., Lemaire, W., Williams, D. L., Jr., Jacobson, M. A., Wittman, M., Ha, S. N., Schaffhauser, H., Sur, C., Pettibone, D. J., Duggan, M. E., Conn, P. J., Hartman, G. D., and Lindsley, C. W. (2007) Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA Bioorg. Med. Chem. Lett. 17, 1386-1391 (Pubitemid 46240838)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.5
, pp. 1386-1391
-
-
Zhao, Z.1
Wisnoski, D.D.2
O'Brien, J.A.3
Lemaire, W.4
Williams Jr., D.L.5
Jacobson, M.A.6
Wittman, M.7
Ha, S.N.8
Schaffhauser, H.9
Sur, C.10
Pettibone, D.J.11
Duggan, M.E.12
Conn, P.J.13
Hartman, G.D.14
Lindsley, C.W.15
-
9
-
-
79953213637
-
"molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology
-
Wood, M. R., Hopkins, C. R., Brogan, J. T., Conn, P. J., and Lindsley, C. W. (2011) "Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology Biochemistry 50, 2403-2410
-
(2011)
Biochemistry
, vol.50
, pp. 2403-2410
-
-
Wood, M.R.1
Hopkins, C.R.2
Brogan, J.T.3
Conn, P.J.4
Lindsley, C.W.5
-
10
-
-
77958485620
-
Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology
-
Hammond, A. S., Rodriguez, A. L., Townsend, S. D., Niswender, C. M., Gregory, K. J., Lindsley, C. W., and Conn, P. J. (2010) Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology ACS Chem. Neurosci. 1, 702-716
-
(2010)
ACS Chem. Neurosci.
, vol.1
, pp. 702-716
-
-
Hammond, A.S.1
Rodriguez, A.L.2
Townsend, S.D.3
Niswender, C.M.4
Gregory, K.J.5
Lindsley, C.W.6
Conn, P.J.7
-
11
-
-
79953171633
-
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists
-
Lamb, J. P., Engers, D. W., Niswender, C. M., Rodriguez, A. L., Venable, D. F., Conn, P. J., and Lindsley, C. W. (2011) Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists Bioorg. Med. Chem. Lett. 21, 2711-2714
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 2711-2714
-
-
Lamb, J.P.1
Engers, D.W.2
Niswender, C.M.3
Rodriguez, A.L.4
Venable, D.F.5
Conn, P.J.6
Lindsley, C.W.7
-
12
-
-
78649919580
-
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity
-
Rodriguez, A. L., Grier, M. D., Jones, C. K., Herman, E. J., Kane, A. S., Smith, R. L., Williams, R., Zhou, Y., Marlo, J. E., Days, E. L., Blatt, T. N., Jadhav, S., Menon, U. N., Vinson, P. N., Rook, J. M., Stauffer, S. R., Niswender, C. M., Lindsley, C. W., Weaver, C. D., and Conn, P. J. (2010) Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity Mol. Pharmacol. 78, 1105-1123
-
(2010)
Mol. Pharmacol.
, vol.78
, pp. 1105-1123
-
-
Rodriguez, A.L.1
Grier, M.D.2
Jones, C.K.3
Herman, E.J.4
Kane, A.S.5
Smith, R.L.6
Williams, R.7
Zhou, Y.8
Marlo, J.E.9
Days, E.L.10
Blatt, T.N.11
Jadhav, S.12
Menon, U.N.13
Vinson, P.N.14
Rook, J.M.15
Stauffer, S.R.16
Niswender, C.M.17
Lindsley, C.W.18
Weaver, C.D.19
Conn, P.J.20
more..
-
13
-
-
27844482134
-
A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators
-
DOI 10.1124/mol.105.016139
-
Rodriguez, A. L., Nong, Y., Sekaran, N. K., Alagille, D., Tamagnan, G. D., and Conn, P. J. (2005) A close structural analog of 2-methyl-6- (phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators Mol. Pharmacol. 68, 1793-1802 (Pubitemid 41654362)
-
(2005)
Molecular Pharmacology
, vol.68
, Issue.6
, pp. 1793-1802
-
-
Rodriguez, A.L.1
Nong, Y.2
Sekaran, N.K.3
Alagille, D.4
Tamagnan, G.D.5
Conn, P.J.6
-
14
-
-
67650729937
-
Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines
-
Sharma, S., Kedrowski, J., Rook, J. M., Smith, R. L., Jones, C. K., Rodriguez, A. L., Conn, P. J., and Lindsley, C. W. (2009) Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines J. Med. Chem. 52, 4103-4106
-
(2009)
J. Med. Chem.
, vol.52
, pp. 4103-4106
-
-
Sharma, S.1
Kedrowski, J.2
Rook, J.M.3
Smith, R.L.4
Jones, C.K.5
Rodriguez, A.L.6
Conn, P.J.7
Lindsley, C.W.8
-
15
-
-
78649282776
-
Discovery of N-Aryl Piperazines as Selective mGluR5 Potentiators with Improved in Vivo Utility
-
Zhou, Y., Manka, J. T., Rodriguez, A. L., Weaver, C. D., Days, E. L., Vinson, P. N., Jadhav, S., Hermann, E. J., Jones, C. K., Conn, P. J., Lindsley, C. W., and Stauffer, S. R. (2010) Discovery of N-Aryl Piperazines as Selective mGluR5 Potentiators with Improved In Vivo Utility ACS Med. Chem. Lett. 1, 433-438
-
(2010)
ACS Med. Chem. Lett.
, vol.1
, pp. 433-438
-
-
Zhou, Y.1
Manka, J.T.2
Rodriguez, A.L.3
Weaver, C.D.4
Days, E.L.5
Vinson, P.N.6
Jadhav, S.7
Hermann, E.J.8
Jones, C.K.9
Conn, P.J.10
Lindsley, C.W.11
Stauffer, S.R.12
-
16
-
-
84861570191
-
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM
-
Sheffler, D. J., Wenthur, C. J., Bruner, J. A., Carrington, S. J. S., Vinson, P. N., Gogi, K. K., Blobaum, A. L., Morrison, R. D., Vamos, M., Cosford, N. D. P., Stauffer, S. R., Scott Daniels, J., Niswender, C. M., Jeffrey Conn, P., and Lindsley, C. W. (2012) Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM Bioorg. Med. Chem. Lett. 22, 3921-3925
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 3921-3925
-
-
Sheffler, D.J.1
Wenthur, C.J.2
Bruner, J.A.3
Carrington, S.J.S.4
Vinson, P.N.5
Gogi, K.K.6
Blobaum, A.L.7
Morrison, R.D.8
Vamos, M.9
Cosford, N.D.P.10
Stauffer, S.R.11
Scott Daniels, J.12
Niswender, C.M.13
Jeffrey Conn, P.14
Lindsley, C.W.15
-
17
-
-
84876593223
-
Probing the metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulator (PAM) binding pocket: Discovery of point mutations that engender a "molecular switch" in PAM pharmacology
-
Gregory, K. J., Nguyen, E. D., Reiff, S. D., Squire, E. F., Stauffer, S. R., Lindsley, C. W., Meiler, J., and Conn, P. J. (2013) Probing the metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology Mol. Pharmacol. 83, 991-1006
-
(2013)
Mol. Pharmacol.
, vol.83
, pp. 991-1006
-
-
Gregory, K.J.1
Nguyen, E.D.2
Reiff, S.D.3
Squire, E.F.4
Stauffer, S.R.5
Lindsley, C.W.6
Meiler, J.7
Conn, P.J.8
-
18
-
-
33746484507
-
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
-
DOI 10.1111/j.1471-4159.2006.03886.x
-
Malherbe, P., Kratochwil, N., Muhlemann, A., Zenner, M.-T., Fischer, C., Stahl, M., Gerber, P. R., Jaeschke, G., and Porter, R. H. P. (2006) 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. Neurochem. 98, 601-615 (Pubitemid 44133162)
-
(2006)
Journal of Neurochemistry
, vol.98
, Issue.2
, pp. 601-615
-
-
Malherbe, P.1
Kratochwil, N.2
Muhlemann, A.3
Zenner, M.-T.4
Fischer, C.5
Stahl, M.6
Gerber, P.R.7
Jaeschke, G.8
Porter, R.H.P.9
-
19
-
-
0141569326
-
Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)- pyridine
-
DOI 10.1124/mol.64.4.823
-
Malherbe, P., Kratochwil, N., Zenner, M. T., Piussi, J., Diener, C., Kratzeisen, C., Fischer, C., and Porter, R. H. (2003) Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine Mol. Pharmacol. 64, 823-832 (Pubitemid 37153050)
-
(2003)
Molecular Pharmacology
, vol.64
, Issue.4
, pp. 823-832
-
-
Malherbe, P.1
Kratochwil, N.2
Zenner, M.-T.3
Piussi, J.4
Diener, C.5
Kratzeisen, C.6
Fischer, C.7
Porter, R.H.P.8
-
20
-
-
84867805089
-
Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-selective Negative Allosteric Modulators
-
Molck, C., Harpsoe, K., Gloriam, D. E., Clausen, R. P., Madsen, U., Pedersen, L. O., Jimenez, H. N., Nielsen, S. M., Mathiesen, J. M., and Brauner-Osborne, H. (2012) Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-selective Negative Allosteric Modulators Mol. Pharmacol. 82, 929-937
-
(2012)
Mol. Pharmacol.
, vol.82
, pp. 929-937
-
-
Molck, C.1
Harpsoe, K.2
Gloriam, D.E.3
Clausen, R.P.4
Madsen, U.5
Pedersen, L.O.6
Jimenez, H.N.7
Nielsen, S.M.8
Mathiesen, J.M.9
Brauner-Osborne, H.10
-
21
-
-
29344436808
-
Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′-difluorobenzaldazine on rat mGlu5 receptors
-
Muhlemann, A., Ward, N. A., Kratochwil, N., Diener, C., Fischer, C., Stucki, A., Jaeschke, G., Malherbe, P., and Porter, R. H. (2006) Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′-difluorobenzaldazine on rat mGlu5 receptors Eur. J. Pharmacol. 529, 95-104
-
(2006)
Eur. J. Pharmacol.
, vol.529
, pp. 95-104
-
-
Muhlemann, A.1
Ward, N.A.2
Kratochwil, N.3
Diener, C.4
Fischer, C.5
Stucki, A.6
Jaeschke, G.7
Malherbe, P.8
Porter, R.H.9
-
22
-
-
0034721795
-
The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group i metabotropic glutamate receptors
-
Pagano, A., Ruegg, D., Litschig, S., Stoehr, N., Stierlin, C., Heinrich, M., Floersheim, P., Prezeau, L., Carroll, F., Pin, J. P., Cambria, A., Vranesic, I., Flor, P. J., Gasparini, F., and Kuhn, R. (2000) The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b] chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors J. Biol. Chem. 275, 33750-33758
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 33750-33758
-
-
Pagano, A.1
Ruegg, D.2
Litschig, S.3
Stoehr, N.4
Stierlin, C.5
Heinrich, M.6
Floersheim, P.7
Prezeau, L.8
Carroll, F.9
Pin, J.P.10
Cambria, A.11
Vranesic, I.12
Flor, P.J.13
Gasparini, F.14
Kuhn, R.15
-
23
-
-
84886566347
-
Exploration of Allosteric Agonism Structure-Activity Relationships within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5-((3-Fluorophenyl)ethynyl)-N-(3- methyloxetan-3-yl)picolinamide (ML254)
-
Turlington, M., Noetzel, M. J., Chun, A., Zhou, Y., Gogliotti, R. D., Nguyen, E. D., Gregory, K. J., Vinson, P. N., Rook, J. M., Gogi, K. K., Xiang, Z., Bridges, T. M., Daniels, J. S., Jones, C., Niswender, C. M., Meiler, J., Conn, P. J., Lindsley, C. W., and Stauffer, S. R. (2013) Exploration of Allosteric Agonism Structure-Activity Relationships within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5-((3-Fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl) picolinamide (ML254) J. Med. Chem. 56, 7976-7996
-
(2013)
J. Med. Chem.
, vol.56
, pp. 7976-7996
-
-
Turlington, M.1
Noetzel, M.J.2
Chun, A.3
Zhou, Y.4
Gogliotti, R.D.5
Nguyen, E.D.6
Gregory, K.J.7
Vinson, P.N.8
Rook, J.M.9
Gogi, K.K.10
Xiang, Z.11
Bridges, T.M.12
Daniels, J.S.13
Jones, C.14
Niswender, C.M.15
Meiler, J.16
Conn, P.J.17
Lindsley, C.W.18
Stauffer, S.R.19
-
24
-
-
0037330358
-
3H]-methoxy-PEPy: Potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor
-
DOI 10.1016/S0960-894X(02)00997-6, PII S0960894X02009976
-
Cosford, N. D., Roppe, J., Tehrani, L., Schweiger, E. J., Seiders, T. J., Chaudary, A., Rao, S., and Varney, M. A. (2003) [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor Bioorg. Med. Chem. Lett. 13, 351-354 (Pubitemid 36259690)
-
(2003)
Bioorganic and Medicinal Chemistry Letters
, vol.13
, Issue.3
, pp. 351-354
-
-
Cosford, N.D.P.1
Roppe, J.2
Tehrani, L.3
Schweiger, E.J.4
Seiders, T.J.5
Chaudary, A.6
Rao, S.7
Varney, M.A.8
-
25
-
-
84867831749
-
Investigating Metabotorpic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity and Agonism: Enriching Structure-function Studies and Structure-activity Relationships
-
Gregory, K. J., Noetzel, M. J., Rook, J. M., Vinson, P. N., Stauffer, S. R., Rodriguez, A. L., Emmitte, K. A., Zhou, Y., Chun, A. C., Felts, A. S., Chauder, B. A., Lindsley, C. W., Niswender, C. M., and Conn, P. J. (2012) Investigating Metabotorpic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity and Agonism: Enriching Structure-function Studies and Structure-activity Relationships Mol. Pharmacol. 82, 860-875
-
(2012)
Mol. Pharmacol.
, vol.82
, pp. 860-875
-
-
Gregory, K.J.1
Noetzel, M.J.2
Rook, J.M.3
Vinson, P.N.4
Stauffer, S.R.5
Rodriguez, A.L.6
Emmitte, K.A.7
Zhou, Y.8
Chun, A.C.9
Felts, A.S.10
Chauder, B.A.11
Lindsley, C.W.12
Niswender, C.M.13
Conn, P.J.14
-
26
-
-
84857732011
-
Discovery of 2-(2-Benzoxazoyl amino)-4-Aryl-5-Cyanopyrimidine as Negative Allosteric Modulators (NAMs) of Metabotropic Glutamate Receptor 5 (mGlu5): From an Artificial Neural Network Virtual Screen to an in Vivo Tool Compound
-
Mueller, R., Dawson, E. S., Meiler, J., Rodriguez, A. L., Chauder, B. A., Bates, B. S., Felts, A. S., Lamb, J. P., Menon, U. N., Jadhav, S. B., Kane, A. S., Jones, C. K., Gregory, K. J., Niswender, C. M., Conn, P. J., Olsen, C. M., Winder, D. G., Emmitte, K. A., and Lindsley, C. W. (2012) Discovery of 2-(2-Benzoxazoyl amino)-4-Aryl-5-Cyanopyrimidine as Negative Allosteric Modulators (NAMs) of Metabotropic Glutamate Receptor 5 (mGlu5): From an Artificial Neural Network Virtual Screen to an In Vivo Tool Compound ChemMedChem 7, 406-414
-
(2012)
ChemMedChem
, vol.7
, pp. 406-414
-
-
Mueller, R.1
Dawson, E.S.2
Meiler, J.3
Rodriguez, A.L.4
Chauder, B.A.5
Bates, B.S.6
Felts, A.S.7
Lamb, J.P.8
Menon, U.N.9
Jadhav, S.B.10
Kane, A.S.11
Jones, C.K.12
Gregory, K.J.13
Niswender, C.M.14
Conn, P.J.15
Olsen, C.M.16
Winder, D.G.17
Emmitte, K.A.18
Lindsley, C.W.19
-
27
-
-
66749109859
-
Structure-activity relationships comparing N-(6-methylpyridin-yl)- substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists
-
Kulkarni, S. S., Zou, M. F., Cao, J., Deschamps, J. R., Rodriguez, A. L., Conn, P. J., and Newman, A. H. (2009) Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6- (substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl) thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists J. Med. Chem. 52, 3563-3575
-
(2009)
J. Med. Chem.
, vol.52
, pp. 3563-3575
-
-
Kulkarni, S.S.1
Zou, M.F.2
Cao, J.3
Deschamps, J.R.4
Rodriguez, A.L.5
Conn, P.J.6
Newman, A.H.7
-
28
-
-
9644281056
-
Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity
-
DOI 10.1016/j.bmc.2004.09.042, PII S0968089604007564
-
Alagille, D., Baldwin, R. M., Roth, B. L., Wroblewski, J. T., Grajkowska, E., and Tamagnan, G. D. (2005) Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity Bioorg. Med. Chem. 13, 197-209 (Pubitemid 39575705)
-
(2005)
Bioorganic and Medicinal Chemistry
, vol.13
, Issue.1
, pp. 197-209
-
-
Alagille, D.1
Baldwin, R.M.2
Roth, B.L.3
Wroblewski, J.T.4
Grajkowska, E.5
Tamagnan, G.D.6
-
29
-
-
79955468360
-
Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl) benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5
-
Zou, M. F., Cao, J., Rodriguez, A. L., Conn, P. J., and Newman, A. H. (2011) Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl) benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 Bioorg. Med. Chem. Lett. 21, 2650-2654
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 2650-2654
-
-
Zou, M.F.1
Cao, J.2
Rodriguez, A.L.3
Conn, P.J.4
Newman, A.H.5
-
30
-
-
84885187910
-
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety
-
Felts, A. S., Rodriguez, A. L., Morrison, R. D., Venable, D. F., Manka, J. T., Bates, B. S., Blobaum, A. L., Byers, F. W., Daniels, J. S., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W., and Emmitte, K. A. (2013) Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety Bioorg. Med. Chem. Lett. 23, 5779-5785
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 5779-5785
-
-
Felts, A.S.1
Rodriguez, A.L.2
Morrison, R.D.3
Venable, D.F.4
Manka, J.T.5
Bates, B.S.6
Blobaum, A.L.7
Byers, F.W.8
Daniels, J.S.9
Niswender, C.M.10
Jones, C.K.11
Conn, P.J.12
Lindsley, C.W.13
Emmitte, K.A.14
-
31
-
-
84886019044
-
N-Aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in pre-clinical models of NMDA hypofunction and cognitive enhancement
-
Gregory, K. J., Herman, E. J., Ramsey, A. J., Hammond, A. S., Byun, N. E., Stauffer, S. R., Manka, J. T., Jadhav, S., Bridges, T. M., Weaver, C. D., Niswender, C. M., Steckler, T., Drinkenburg, W. H., Ahnaou, A., Lavreysen, H., Macdonald, G. J., Bartolome, J. M., Mackie, C., Hrupka, B. J., Caron, M. G., Daigle, T. L., Lindsley, C. W., Conn, P. J., and Jones, C. K. (2013) N-Aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in pre-clinical models of NMDA hypofunction and cognitive enhancement J. Pharmacol. Exp. Ther. 347, 438-457
-
(2013)
J. Pharmacol. Exp. Ther.
, vol.347
, pp. 438-457
-
-
Gregory, K.J.1
Herman, E.J.2
Ramsey, A.J.3
Hammond, A.S.4
Byun, N.E.5
Stauffer, S.R.6
Manka, J.T.7
Jadhav, S.8
Bridges, T.M.9
Weaver, C.D.10
Niswender, C.M.11
Steckler, T.12
Drinkenburg, W.H.13
Ahnaou, A.14
Lavreysen, H.15
MacDonald, G.J.16
Bartolome, J.M.17
MacKie, C.18
Hrupka, B.J.19
Caron, M.G.20
Daigle, T.L.21
Lindsley, C.W.22
Conn, P.J.23
Jones, C.K.24
more..
-
32
-
-
79955941160
-
Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator
-
Spear, N., Gadient, R. A., Wilkins, D. E., Do, M., Smith, J. S., Zeller, K. L., Schroeder, P., Zhang, M., Arora, J., and Chhajlani, V. (2011) Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator Eur. J. Pharmacol. 659, 146-154
-
(2011)
Eur. J. Pharmacol.
, vol.659
, pp. 146-154
-
-
Spear, N.1
Gadient, R.A.2
Wilkins, D.E.3
Do, M.4
Smith, J.S.5
Zeller, K.L.6
Schroeder, P.7
Zhang, M.8
Arora, J.9
Chhajlani, V.10
-
33
-
-
78449302090
-
4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators
-
Xiong, H., Brugel, T. A., Balestra, M., Brown, D. G., Brush, K. A., Hightower, C., Hinkley, L., Hoesch, V., Kang, J., Koether, G. M., McCauley, J. P., Jr., McLaren, F. M., Panko, L. M., Simpson, T. R., Smith, R. W., Woods, J. M., Brockel, B., Chhajlani, V., Gadient, R. A., Spear, N., Sygowski, L. A., Zhang, M., Arora, J., Breysse, N., Wilson, J. M., Isaac, M., Slassi, A., and King, M. M. (2010) 4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators Bioorg. Med. Chem. Lett. 20, 7381-7384
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 7381-7384
-
-
Xiong, H.1
Brugel, T.A.2
Balestra, M.3
Brown, D.G.4
Brush, K.A.5
Hightower, C.6
Hinkley, L.7
Hoesch, V.8
Kang, J.9
Koether, G.M.10
Mccauley Jr., J.P.11
McLaren, F.M.12
Panko, L.M.13
Simpson, T.R.14
Smith, R.W.15
Woods, J.M.16
Brockel, B.17
Chhajlani, V.18
Gadient, R.A.19
Spear, N.20
Sygowski, L.A.21
Zhang, M.22
Arora, J.23
Breysse, N.24
Wilson, J.M.25
Isaac, M.26
Slassi, A.27
King, M.M.28
more..
-
34
-
-
34247477329
-
Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses
-
DOI 10.1124/mol.106.032425
-
Chen, Y., Nong, Y., Goudet, C., Hemstapat, K., de Paulis, T., Pin, J. P., and Conn, P. J. (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 Mol. Pharmacol. 71, 1389-1398 (Pubitemid 46661543)
-
(2007)
Molecular Pharmacology
, vol.71
, Issue.5
, pp. 1389-1398
-
-
Chen, Y.1
Nong, Y.2
Goudet, C.3
Hemstapat, K.4
De Paulis, T.5
Pin, J.-P.6
Conn, P.J.7
-
35
-
-
33744801125
-
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
-
DOI 10.1021/jm051252j
-
de Paulis, T., Hemstapat, K., Chen, Y., Zhang, Y., Saleh, S., Alagille, D., Baldwin, R. M., Tamagnan, G. D., and Conn, P. J. (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 J. Med. Chem. 49, 3332-3344 (Pubitemid 43830531)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.11
, pp. 3332-3344
-
-
De Paulis, T.1
Hemstapat, K.2
Chen, Y.3
Zhang, Y.4
Saleh, S.5
Alagille, D.6
Baldwin, R.M.7
Tamagnan, G.D.8
Conn, P.J.9
-
36
-
-
20144381462
-
A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models
-
DOI 10.1124/jpet.104.079244
-
Kinney, G. G., O'Brien, J. A., Lemaire, W., Burno, M., Bickel, D. J., Clements, M. K., Chen, T. B., Wisnoski, D. D., Lindsley, C. W., Tiller, P. R., Smith, S., Jacobson, M. A., Sur, C., Duggan, M. E., Pettibone, D. J., Conn, P. J., and Williams, D. L., Jr. (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 J. Pharmacol. Exp. Ther. 313, 199-206 (Pubitemid 40411343)
-
(2005)
Journal of Pharmacology and Experimental Therapeutics
, vol.313
, Issue.1
, pp. 199-206
-
-
Kinney, G.G.1
O'Brien, J.A.2
Lemaire, W.3
Burno, M.4
Bickel, D.J.5
Clements, M.K.6
Chen, T.-B.7
Wisnoski, D.D.8
Lindsley, C.W.9
Tiller, P.R.10
Smith, S.11
Jacobson, M.A.12
Sur, C.13
Duggan, M.E.14
Pettibone, D.J.15
Conn, P.J.16
Williams Jr., D.L.17
-
37
-
-
84857713749
-
Structure-activity relationships for negative allosteric mGluR5 modulators
-
Kaae, B. H., Harpsoe, K., Kvist, T., Mathiesen, J. M., Molck, C., Gloriam, D., Jimenez, H. N., Uberti, M. A., Nielsen, S. M., Nielsen, B., Brauner-Osborne, H., Sauerberg, P., Clausen, R. P., and Madsen, U. (2012) Structure-activity relationships for negative allosteric mGluR5 modulators ChemMedChem 7, 440-451
-
(2012)
ChemMedChem
, vol.7
, pp. 440-451
-
-
Kaae, B.H.1
Harpsoe, K.2
Kvist, T.3
Mathiesen, J.M.4
Molck, C.5
Gloriam, D.6
Jimenez, H.N.7
Uberti, M.A.8
Nielsen, S.M.9
Nielsen, B.10
Brauner-Osborne, H.11
Sauerberg, P.12
Clausen, R.P.13
Madsen, U.14
-
38
-
-
80052082999
-
Structural insights into agonist-induced activation of G-protein-coupled receptors
-
Deupi, X. and Standfuss, J. (2011) Structural insights into agonist-induced activation of G-protein-coupled receptors Curr. Opin. Struct. Biol. 21, 541-551
-
(2011)
Curr. Opin. Struct. Biol.
, vol.21
, pp. 541-551
-
-
Deupi, X.1
Standfuss, J.2
-
39
-
-
0036839162
-
MAMMOTH (Matching molecular models obtained from theory): An automated method for model comparison
-
DOI 10.1110/ps.0215902
-
Ortiz, A. R., Strauss, C. E., and Olmea, O. (2002) MAMMOTH (matching molecular models obtained from theory): an automated method for model comparison Protein Sci. 11, 2606-2621 (Pubitemid 35191136)
-
(2002)
Protein Science
, vol.11
, Issue.11
, pp. 2606-2621
-
-
Ortiz, A.R.1
Strauss, C.E.M.2
Olmea, O.3
-
40
-
-
84879770850
-
Assessment and challenges of ligand docking into comparative models of G-protein coupled receptors
-
Nguyen, E. D., Norn, C., Frimurer, T. M., and Meiler, J. (2013) Assessment and challenges of ligand docking into comparative models of G-protein coupled receptors PLoS One 8, e67302
-
(2013)
PLoS One
, vol.8
, pp. 67302
-
-
Nguyen, E.D.1
Norn, C.2
Frimurer, T.M.3
Meiler, J.4
-
41
-
-
79955955515
-
The Implication of the First Agonist Bound Activated GPCR X-ray Structure on GPCR in Silico Modeling
-
Tautermann, C. S. and Pautsch, A. (2011) The Implication of the First Agonist Bound Activated GPCR X-ray Structure on GPCR in Silico Modeling ACS Med. Chem. Lett. 2, 414-418
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 414-418
-
-
Tautermann, C.S.1
Pautsch, A.2
-
42
-
-
77955415857
-
3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats
-
Felts, A. S., Lindsley, S. R., Lamb, J. P., Rodriguez, A. L., Menon, U. N., Jadhav, S., Jones, C. K., Conn, P. J., Lindsley, C. W., and Emmitte, K. A. (2010) 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats Bioorg. Med. Chem. Lett. 20, 4390-4394
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 4390-4394
-
-
Felts, A.S.1
Lindsley, S.R.2
Lamb, J.P.3
Rodriguez, A.L.4
Menon, U.N.5
Jadhav, S.6
Jones, C.K.7
Conn, P.J.8
Lindsley, C.W.9
Emmitte, K.A.10
-
43
-
-
77952756998
-
LowModeMD - Implicit low-mode velocity filtering applied to conformational search of macrocycles and protein loops
-
Labute, P. (2010) LowModeMD - implicit low-mode velocity filtering applied to conformational search of macrocycles and protein loops J. Chem. Inf. Model. 50, 792-800
-
(2010)
J. Chem. Inf. Model.
, vol.50
, pp. 792-800
-
-
Labute, P.1
-
44
-
-
58149094776
-
RosettaLigand docking with full ligand and receptor flexibility
-
Davis, I. W. and Baker, D. (2009) RosettaLigand docking with full ligand and receptor flexibility J. Mol. Biol. 385, 381-392
-
(2009)
J. Mol. Biol.
, vol.385
, pp. 381-392
-
-
Davis, I.W.1
Baker, D.2
-
45
-
-
84855945133
-
Rosetta Ligand docking with flexible XML protocols
-
Lemmon, G. and Meiler, J. (2012) Rosetta Ligand docking with flexible XML protocols Methods Mol. Biol. 819, 143-155
-
(2012)
Methods Mol. Biol.
, vol.819
, pp. 143-155
-
-
Lemmon, G.1
Meiler, J.2
-
46
-
-
33750056673
-
ROSETTALIGAND: Protein-small molecule docking with full side-chain flexibility
-
DOI 10.1002/prot.21086
-
Meiler, J. and Baker, D. (2006) ROSETTALIGAND: protein-small molecule docking with full side-chain flexibility Proteins 65, 538-548 (Pubitemid 44583205)
-
(2006)
Proteins: Structure, Function and Genetics
, vol.65
, Issue.3
, pp. 538-548
-
-
Meiler, J.1
Baker, D.2
-
47
-
-
4444283656
-
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity
-
DOI 10.1021/jm049828c
-
Roppe, J., Smith, N. D., Huang, D., Tehrani, L., Wang, B., Anderson, J., Brodkin, J., Chung, J., Jiang, X., King, C., Munoz, B., Varney, M. A., Prasit, P., and Cosford, N. D. (2004) Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity J. Med. Chem. 47, 4645-4648 (Pubitemid 39195554)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.19
, pp. 4645-4648
-
-
Roppe, J.1
Smith, N.D.2
Huang, D.3
Tehrani, L.4
Wang, B.5
Anderson, J.6
Brodkin, J.7
Chung, J.8
Jiang, X.9
King, C.10
Munoz, B.11
Varney, M.A.12
Prasit, P.13
Cosford, N.D.P.14
-
48
-
-
16244403316
-
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP
-
DOI 10.1016/j.bmcl.2004.12.047
-
Alagille, D., Baldwin, R. M., Roth, B. L., Wroblewski, J. T., Grajkowska, E., and Tamagnan, G. D. (2005) Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP Bioorg. Med. Chem. Lett. 15, 945-949 (Pubitemid 40458628)
-
(2005)
Bioorganic and Medicinal Chemistry Letters
, vol.15
, Issue.4
, pp. 945-949
-
-
Alagille, D.1
Baldwin, R.M.2
Roth, B.L.3
Wroblewski, J.T.4
Grajkowska, E.5
Tamagnan, G.D.6
|