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Items: 1 to 20 of 114

1.

Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics.

Cho HP, Garcia-Barrantes PM, Brogan JT, Hopkins CR, Niswender CM, Rodriguez AL, Venable DF, Morrison RD, Bubser M, Daniels JS, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Biol. 2014 Oct 17;9(10):2334-46. doi: 10.1021/cb500560h. Epub 2014 Aug 28.

2.

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.

Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW.

J Med Chem. 2015 Oct 22;58(20):7959-71. doi: 10.1021/acs.jmedchem.5b00727. Epub 2015 Oct 8.

3.

Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology.

Gregory KJ, Nguyen ED, Reiff SD, Squire EF, Stauffer SR, Lindsley CW, Meiler J, Conn PJ.

Mol Pharmacol. 2013 May;83(5):991-1006. doi: 10.1124/mol.112.083949. Epub 2013 Feb 26.

4.

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.

Niswender CM, Jones CK, Lin X, Bubser M, Thompson Gray A, Blobaum AL, Engers DW, Rodriguez AL, Loch MT, Daniels JS, Lindsley CW, Hopkins CR, Javitch JA, Conn PJ.

ACS Chem Neurosci. 2016 Sep 21;7(9):1201-11. doi: 10.1021/acschemneuro.6b00036. Epub 2016 Aug 5.

5.

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 AL, Grier MD, Jones CK, Herman EJ, Kane AS, Smith RL, Williams R, Zhou Y, Marlo JE, Days EL, Blatt TN, Jadhav S, Menon UN, Vinson PN, Rook JM, Stauffer SR, Niswender CM, Lindsley CW, Weaver CD, Conn PJ.

Mol Pharmacol. 2010 Dec;78(6):1105-23. doi: 10.1124/mol.110.067207. Epub 2010 Oct 5.

6.

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.

Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5107-10. doi: 10.1016/j.bmcl.2015.10.013. Epub 2015 Oct 9.

7.

Targeting metabotropic glutamate receptors for novel treatments of schizophrenia.

Maksymetz J, Moran SP, Conn PJ.

Mol Brain. 2017 Apr 26;10(1):15. doi: 10.1186/s13041-017-0293-z. Review.

8.

Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.

Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ.

Mol Pharmacol. 2012 Nov;82(5):860-75. doi: 10.1124/mol.112.080531. Epub 2012 Aug 3.

9.

Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.

Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):751-756. doi: 10.1016/j.bmcl.2015.12.104. Epub 2016 Jan 2.

10.

Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators.

Lundström L, Bissantz C, Beck J, Wettstein JG, Woltering TJ, Wichmann J, Gatti S.

Br J Pharmacol. 2011 Sep;164(2b):521-37. doi: 10.1111/j.1476-5381.2011.01409.x.

11.

Deleterious GRM1 mutations in schizophrenia.

Ayoub MA, Angelicheva D, Vile D, Chandler D, Morar B, Cavanaugh JA, Visscher PM, Jablensky A, Pfleger KD, Kalaydjieva L.

PLoS One. 2012;7(3):e32849. doi: 10.1371/journal.pone.0032849. Epub 2012 Mar 20.

12.

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.

Noetzel MJ, Rook JM, Vinson PN, Cho HP, Days E, Zhou Y, Rodriguez AL, Lavreysen H, Stauffer SR, Niswender CM, Xiang Z, Daniels JS, Jones CK, Lindsley CW, Weaver CD, Conn PJ.

Mol Pharmacol. 2012 Feb;81(2):120-33. doi: 10.1124/mol.111.075184. Epub 2011 Oct 21.

13.

N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.

Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1894-900. doi: 10.1016/j.bmcl.2016.03.026. Epub 2016 Mar 9.

14.

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

Rook JM, Noetzel MJ, Pouliot WA, Bridges TM, Vinson PN, Cho HP, Zhou Y, Gogliotti RD, Manka JT, Gregory KJ, Stauffer SR, Dudek FE, Xiang Z, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Biol Psychiatry. 2013 Mar 15;73(6):501-9. doi: 10.1016/j.biopsych.2012.09.012. Epub 2012 Nov 7.

15.

Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.

Bridges TM, Rook JM, Noetzel MJ, Morrison RD, Zhou Y, Gogliotti RD, Vinson PN, Xiang Z, Jones CK, Niswender CM, Lindsley CW, Stauffer SR, Conn PJ, Daniels JS.

Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2.

16.

Group I and group II metabotropic glutamate receptor allosteric modulators as novel potential antipsychotics.

Walker AG, Conn PJ.

Curr Opin Pharmacol. 2015 Feb;20:40-5. doi: 10.1016/j.coph.2014.11.003. Epub 2014 Nov 27. Review.

17.

Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.

Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND.

J Med Chem. 2014 May 22;57(10):4154-72. doi: 10.1021/jm5000563. Epub 2014 May 9.

18.

Pharmacological enhancement of mGlu1 metabotropic glutamate receptors causes a prolonged symptomatic benefit in a mouse model of spinocerebellar ataxia type 1.

Notartomaso S, Zappulla C, Biagioni F, Cannella M, Bucci D, Mascio G, Scarselli P, Fazio F, Weisz F, Lionetto L, Simmaco M, Gradini R, Battaglia G, Signore M, Puliti A, Nicoletti F.

Mol Brain. 2013 Nov 19;6:48. doi: 10.1186/1756-6606-6-48.

19.

Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site.

Knoflach F, Mutel V, Jolidon S, Kew JN, Malherbe P, Vieira E, Wichmann J, Kemp JA.

Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7. Epub 2001 Oct 23. Erratum in: Proc Natl Acad Sci U S A 2001 Dec 18;98(26):15393.

20.

Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype.

Sams AG, Mikkelsen GK, Brodbeck RM, Pu X, Ritzén A.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3407-10. doi: 10.1016/j.bmcl.2011.03.103. Epub 2011 Apr 5.

PMID:
21531137

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