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Page 1
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization.
Nógrádi K, Wágner G, Domány G, Bobok A, Magdó I, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Gyertyán I, Kóti J, Gál K, Farkas S, Keserű GM, Greiner I, Szombathelyi Z. Nógrádi K, et al. Among authors: szombathelyi z. Bioorg Med Chem Lett. 2015 Apr 15;25(8):1724-1729. doi: 10.1016/j.bmcl.2015.02.073. Epub 2015 Mar 7. Bioorg Med Chem Lett. 2015. PMID: 25791451
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. Wágner G, et al. Among authors: szombathelyi z. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3737-41. doi: 10.1016/j.bmcl.2010.04.075. Epub 2010 Apr 22. Bioorg Med Chem Lett. 2010. PMID: 20483612
Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.
Galambos J, Wágner G, Nógrádi K, Bielik A, Molnár L, Bobok A, Horváth A, Kiss B, Kolok S, Nagy J, Kurkó D, Bakk ML, Vastag M, Sághy K, Gyertyán I, Gál K, Greiner I, Szombathelyi Z, Keseru GM, Domány G. Galambos J, et al. Among authors: szombathelyi z. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4371-5. doi: 10.1016/j.bmcl.2010.06.075. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20615697
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.
Agai-Csongor E, Domány G, Nógrádi K, Galambos J, Vágó I, Keserű GM, Greiner I, Laszlovszky I, Gere A, Schmidt E, Kiss B, Vastag M, Tihanyi K, Sághy K, Laszy J, Gyertyán I, Zájer-Balázs M, Gémesi L, Kapás M, Szombathelyi Z. Agai-Csongor E, et al. Among authors: szombathelyi z. Bioorg Med Chem Lett. 2012 May 15;22(10):3437-40. doi: 10.1016/j.bmcl.2012.03.104. Epub 2012 Apr 4. Bioorg Med Chem Lett. 2012. PMID: 22537450
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.
Galambos J, Domány G, Nógrádi K, Wágner G, Keserű GM, Bobok A, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Kóti J, Szakács Z, Béni Z, Gál K, Szombathelyi Z, Greiner I. Galambos J, et al. Among authors: szombathelyi z. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1249-52. doi: 10.1016/j.bmcl.2016.01.024. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26774652
Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.
Galambos J, Bielik A, Krasavin M, Orgován Z, Domány G, Nógrádi K, Wágner G, Balogh GT, Béni Z, Kóti J, Szakács Z, Bobok A, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Laszy J, Halász AS, Balázs O, Gál K, Greiner I, Szombathelyi Z, Keserű GM. Galambos J, et al. Among authors: szombathelyi z. J Med Chem. 2017 Mar 23;60(6):2470-2484. doi: 10.1021/acs.jmedchem.6b01858. Epub 2017 Mar 1. J Med Chem. 2017. PMID: 28212015
Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators.
Galambos J, Bielik A, Wágner G, Domány G, Kóti J, Béni Z, Szigetvári Á, Sánta Z, Orgován Z, Bobok A, Kiss B, Mikó-Bakk ML, Vastag M, Sághy K, Krasavin M, Gál K, Greiner I, Szombathelyi Z, Keserű GM. Galambos J, et al. Among authors: szombathelyi z. Eur J Med Chem. 2017 Jun 16;133:240-254. doi: 10.1016/j.ejmech.2017.03.071. Epub 2017 Mar 29. Eur J Med Chem. 2017. PMID: 28390229
Effects of RGH-237 [N-{4-[4-(3-aminocarbonyl-phenyl)-piperazin-1-yl]-butyl}-4-bromo-benzamide], an orally active, selective dopamine D(3) receptor partial agonist in animal models of cocaine abuse.
Gyertyán I, Kiss B, Gál K, Laszlovszky I, Horváth A, Gémesi LI, Sághy K, Pásztor G, Zájer M, Kapás M, Csongor EA, Domány G, Tihanyi K, Szombathelyi Z. Gyertyán I, et al. Among authors: szombathelyi z. J Pharmacol Exp Ther. 2007 Mar;320(3):1268-78. doi: 10.1124/jpet.106.107920. Epub 2006 Dec 14. J Pharmacol Exp Ther. 2007. PMID: 17170312
Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: II. behavioural characterisation of RG-15.
Gyertyán I, Sághy K, Laszy J, Elekes O, Kedves R, Gémesi LI, Pásztor G, Zájer-Balázs M, Kapás M, Agai Csongor E, Domány G, Kiss B, Szombathelyi Z. Gyertyán I, et al. Among authors: szombathelyi z. Naunyn Schmiedebergs Arch Pharmacol. 2008 Nov;378(5):529-39. doi: 10.1007/s00210-008-0311-x. Epub 2008 Jun 12. Naunyn Schmiedebergs Arch Pharmacol. 2008. PMID: 18548231
32 results