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Optimization of Novel α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators and the Discovery of a Preclinical Development Candidate Molecule (RGH-560).
Ledneczki I, Némethy Z, Molnár KD, Tapolcsányi P, Ilkei V, Vágó I, Kolok S, Thán M, Laszy J, Balázs O, Krámos B, Szigetvári Á, Bata I, Makó A, Visegrády A, Fodor L, Vastag M, Lévay G, Lendvai B, Greiner I, Éles J. Ledneczki I, et al. Among authors: laszy j. J Med Chem. 2023 Dec 14;66(23):16276-16302. doi: 10.1021/acs.jmedchem.3c01635. Epub 2023 Nov 21. J Med Chem. 2023. PMID: 37989278
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: laszy j. 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 novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
Ledneczki I, Tapolcsányi P, Gábor E, Visegrády A, Vass M, Éles J, Holm P, Horváth A, Pocsai A, Mahó S, Greiner I, Krámos B, Béni Z, Kóti J, Káncz AE, Thán M, Kolok S, Laszy J, Balázs O, Bugovits G, Nagy J, Vastag M, Szájli Á, Bozó É, Lévay G, Lendvai B, Némethy Z. Ledneczki I, et al. Among authors: laszy j. Eur J Med Chem. 2021 Mar 15;214:113189. doi: 10.1016/j.ejmech.2021.113189. Epub 2021 Jan 14. Eur J Med Chem. 2021. PMID: 33540354
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: laszy j. 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
Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile.
Agai-Csongor E, Nógrádi K, Galambos J, Vágó I, Bielik A, Magdó I, Ignácz-Szendrei G, Keseru GM, Greiner I, Laszlovszky I, Schmidt E, Kiss B, Sághy K, Laszy J, Gyertyán I, Zájer-Balázs M, Gémesi L, Domány G. Agai-Csongor E, et al. Among authors: laszy j. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5340-4. doi: 10.1016/j.bmcl.2007.08.015. Epub 2007 Aug 15. Bioorg Med Chem Lett. 2007. PMID: 17720494
Cariprazine (RGH-188), a potent D3/D2 dopamine receptor partial agonist, binds to dopamine D3 receptors in vivo and shows antipsychotic-like and procognitive effects in rodents.
Gyertyán I, Kiss B, Sághy K, Laszy J, Szabó G, Szabados T, Gémesi LI, Pásztor G, Zájer-Balázs M, Kapás M, Csongor EÁ, Domány G, Tihanyi K, Szombathelyi Z. Gyertyán I, et al. Among authors: laszy j. Neurochem Int. 2011 Nov;59(6):925-35. doi: 10.1016/j.neuint.2011.07.002. Epub 2011 Jul 13. Neurochem Int. 2011. PMID: 21767587
19 results