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194 related items for PubMed ID: 23856046

  • 1. Discovery, synthesis, and structure-activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators.
    Kubas H, Meyer U, Krueger B, Hechenberger M, Vanejevs M, Zemribo R, Kauss V, Ambartsumova R, Pyatkin I, Polosukhin AI, Abel U.
    Bioorg Med Chem Lett; 2013 Aug 15; 23(16):4493-500. PubMed ID: 23856046
    [Abstract] [Full Text] [Related]

  • 2. Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
    Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL.
    J Med Chem; 2014 Feb 13; 57(3):861-77. PubMed ID: 24392688
    [Abstract] [Full Text] [Related]

  • 3. Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.
    Noeske T, Trifanova D, Kauss V, Renner S, Parsons CG, Schneider G, Weil T.
    Bioorg Med Chem; 2009 Aug 01; 17(15):5708-15. PubMed ID: 19574055
    [Abstract] [Full Text] [Related]

  • 4. Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
    Kubas H, Meyer U, Hechenberger M, Klein KU, Plitt P, Zemribo R, Spexgoor HW, van Assema SG, Abel U.
    Bioorg Med Chem Lett; 2013 Dec 01; 23(23):6370-6. PubMed ID: 24125886
    [Abstract] [Full Text] [Related]

  • 5. A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core.
    Duvey G, Perry B, Le Poul E, Poli S, Bonnet B, Lambeng N, Charvin D, Donovan-Rodrigues T, Haddouk H, Gagliardi S, Rocher JP.
    Bioorg Med Chem Lett; 2013 Aug 15; 23(16):4523-7. PubMed ID: 23850200
    [Abstract] [Full Text] [Related]

  • 6. Computational analysis of negative and positive allosteric modulator binding and function in metabotropic glutamate receptor 5 (in)activation.
    Dalton JA, Gómez-Santacana X, Llebaria A, Giraldo J.
    J Chem Inf Model; 2014 May 27; 54(5):1476-87. PubMed ID: 24793143
    [Abstract] [Full Text] [Related]

  • 7. Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.
    Wágner G, Wéber C, Nyéki O, Nógrádi K, Bielik A, Molnár L, Bobok A, Horváth A, Kiss B, Kolok S, Nagy J, Kurkó D, Gál K, Greiner I, Szombathelyi Z, Keseru GM, Domány G.
    Bioorg Med Chem Lett; 2010 Jun 15; 20(12):3737-41. PubMed ID: 20483612
    [Abstract] [Full Text] [Related]

  • 8. Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).
    Williams DL, Lindsley CW.
    Curr Top Med Chem; 2005 Jun 15; 5(9):825-46. PubMed ID: 16178729
    [Abstract] [Full Text] [Related]

  • 9. Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.
    Ritzén A, Sindet R, Hentzer M, Svendsen N, Brodbeck RM, Bundgaard C.
    Bioorg Med Chem Lett; 2009 Jun 15; 19(12):3275-8. PubMed ID: 19443216
    [Abstract] [Full Text] [Related]

  • 10. Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: hit-to-lead optimization.
    Nógrádi K, Wágner G, Domány G, Bobok A, Magdó I, Kiss B, Kolok S, Fónagy K, Gyertyán I, Háda V, Kóti J, Gál K, Farkas S, Keserű GM, Greiner I, Szombathelyi Z.
    Bioorg Med Chem Lett; 2014 Aug 15; 24(16):3845-9. PubMed ID: 25017030
    [Abstract] [Full Text] [Related]

  • 11. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
    Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N, David B, Funk C, Guba W, Harrison A, Hartung T, Honer M, Huwyler J, Kuratli M, Niederhauser U, Pähler A, Peters JU, Petersen A, Prinssen E, Ricci A, Rueher D, Rueher M, Schneider M, Spurr P, Stoll T, Tännler D, Wichmann J, Porter RH, Wettstein JG, Lindemann L.
    J Med Chem; 2015 Feb 12; 58(3):1358-71. PubMed ID: 25565255
    [Abstract] [Full Text] [Related]

  • 12. Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
    Chae E, Shin YJ, Ryu EJ, Ji MK, Ryune Cho N, Lee KH, Jeong HJ, Kim SJ, Choi Y, Seok Oh K, Park CE, Soo Yoon Y.
    Bioorg Med Chem Lett; 2013 Apr 01; 23(7):2134-9. PubMed ID: 23434029
    [Abstract] [Full Text] [Related]

  • 13. Virtual screening for selective allosteric mGluR1 antagonists and structure-activity relationship investigations for coumarine derivatives.
    Noeske T, Jirgensons A, Starchenkovs I, Renner S, Jaunzeme I, Trifanova D, Hechenberger M, Bauer T, Kauss V, Parsons CG, Schneider G, Weil T.
    ChemMedChem; 2007 Dec 01; 2(12):1763-73. PubMed ID: 17868161
    [Abstract] [Full Text] [Related]

  • 14. Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
    Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR.
    J Med Chem; 2004 Nov 18; 47(24):5825-8. PubMed ID: 15537338
    [Abstract] [Full Text] [Related]

  • 15. Synthesis, structure-activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators.
    Hirose W, Kato Y, Yamamoto T, Kassai M, Takata M, Hayashi S, Arai Y, Imai S, Yoshida K.
    Bioorg Med Chem Lett; 2016 Aug 15; 26(16):3866-9. PubMed ID: 27432763
    [Abstract] [Full Text] [Related]

  • 16. Recent progress in the discovery and development of negative allosteric modulators of mGluR5.
    Lindsley CW, Emmitte KA.
    Curr Opin Drug Discov Devel; 2009 Jul 15; 12(4):446-57. PubMed ID: 19562641
    [Abstract] [Full Text] [Related]

  • 17. Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs.
    Wenthur CJ, Morrison RD, Daniels JS, Conn PJ, Lindsley CW.
    Bioorg Med Chem Lett; 2014 Jun 15; 24(12):2693-8. PubMed ID: 24794112
    [Abstract] [Full Text] [Related]

  • 18. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.
    O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, Conn PJ, Williams DL.
    Mol Pharmacol; 2003 Sep 15; 64(3):731-40. PubMed ID: 12920211
    [Abstract] [Full Text] [Related]

  • 19. Positive and negative modulation of group I metabotropic glutamate receptors.
    Vanejevs M, Jatzke C, Renner S, Müller S, Hechenberger M, Bauer T, Klochkova A, Pyatkin I, Kazyulkin D, Aksenova E, Shulepin S, Timonina O, Haasis A, Gutcaits A, Parsons CG, Kauss V, Weil T.
    J Med Chem; 2008 Feb 14; 51(3):634-47. PubMed ID: 18173231
    [Abstract] [Full Text] [Related]

  • 20. Structure-based discovery and development of metabotropic glutamate receptor 5 negative allosteric modulators.
    Bennett KA, Christopher JA, Tehan BG.
    Adv Pharmacol; 2020 Feb 14; 88():35-58. PubMed ID: 32416871
    [Abstract] [Full Text] [Related]

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