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Items: 32

1.

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.

Eur J Med Chem. 2017 Jun 16;133:240-254. doi: 10.1016/j.ejmech.2017.03.071. Epub 2017 Mar 29.

PMID:
28390229
2.

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.

J Med Chem. 2017 Mar 23;60(6):2470-2484. doi: 10.1021/acs.jmedchem.6b01858. Epub 2017 Mar 1.

PMID:
28212015
3.

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.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1249-52. doi: 10.1016/j.bmcl.2016.01.024. Epub 2016 Jan 11.

PMID:
26774652
4.

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.

Bioorg Med Chem Lett. 2015 Apr 15;25(8):1724-1729. doi: 10.1016/j.bmcl.2015.02.073. Epub 2015 Mar 7.

PMID:
25791451
5.

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. doi: 10.1016/j.bmcl.2014.06.057. Epub 2014 Jun 27.

PMID:
25017030
6.

Cariprazine (RGH-188), a D₃-preferring dopamine D₃/D₂ receptor partial agonist antipsychotic candidate demonstrates anti-abuse potential in rats.

Román V, Gyertyán I, Sághy K, Kiss B, Szombathelyi Z.

Psychopharmacology (Berl). 2013 Mar;226(2):285-93. doi: 10.1007/s00213-012-2906-7. Epub 2012 Nov 9.

PMID:
23138433
7.

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.

Bioorg Med Chem Lett. 2012 May 15;22(10):3437-40. doi: 10.1016/j.bmcl.2012.03.104. Epub 2012 Apr 4.

PMID:
22537450
8.

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.

Neurochem Int. 2011 Nov;59(6):925-35. doi: 10.1016/j.neuint.2011.07.002. Epub 2011 Jul 13.

PMID:
21767587
9.

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.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4371-5. doi: 10.1016/j.bmcl.2010.06.075. Epub 2010 Jun 17.

PMID:
20615697
10.

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. doi: 10.1016/j.bmcl.2010.04.075. Epub 2010 Apr 22. Erratum in: Bioorg Med Chem Lett. 2011 Jun 15;21(12):3837-8.

PMID:
20483612
11.

Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile.

Kiss B, Horváth A, Némethy Z, Schmidt E, Laszlovszky I, Bugovics G, Fazekas K, Hornok K, Orosz S, Gyertyán I, Agai-Csongor E, Domány G, Tihanyi K, Adham N, Szombathelyi Z.

J Pharmacol Exp Ther. 2010 Apr;333(1):328-40. doi: 10.1124/jpet.109.160432. Epub 2010 Jan 21.

PMID:
20093397
12.

Gene expression profiling identifies key estradiol targets in the frontal cortex of the rat.

Sárvári M, Hrabovszky E, Kalló I, Galamb O, Solymosi N, Likó I, Molnár B, Tihanyi K, Szombathelyi Z, Liposits Z.

Endocrinology. 2010 Mar;151(3):1161-76. doi: 10.1210/en.2009-0911. Epub 2010 Jan 12.

PMID:
20068009
13.

Neuroprotective effects of vinpocetine and its major metabolite cis-apovincaminic acid on NMDA-induced neurotoxicity in a rat entorhinal cortex lesion model.

Nyakas C, Felszeghy K, Szabó R, Keijser JN, Luiten PG, Szombathelyi Z, Tihanyi K.

CNS Neurosci Ther. 2009 Summer;15(2):89-99. doi: 10.1111/j.1755-5949.2009.00078.x.

PMID:
19492990
14.

Comparative pharmacology of adrenergic alpha(2C) receptors coupled to Ca(2+) signaling through different Galpha proteins.

Kurko D, Bekes Z, Gere A, Baki A, Boros A, Kolok S, Bugovics G, Nagy J, Szombathelyi Z, Ignácz-Szendrei G.

Neurochem Int. 2009 Dec;55(7):467-75. doi: 10.1016/j.neuint.2009.04.015. Epub 2009 May 6.

PMID:
19426776
15.

Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: I. neurochemical characterisation of RG-15.

Kiss B, Laszlovszky I, Horváth A, Némethy Z, Schmidt E, Bugovics G, Fazekas K, Gyertyán I, Agai-Csongor E, Domány G, Szombathelyi Z.

Naunyn Schmiedebergs Arch Pharmacol. 2008 Nov;378(5):515-28. doi: 10.1007/s00210-008-0308-5. Epub 2008 Jun 13.

PMID:
18551280
16.

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.

Naunyn Schmiedebergs Arch Pharmacol. 2008 Nov;378(5):529-39. doi: 10.1007/s00210-008-0311-x. Epub 2008 Jun 12.

PMID:
18548231
17.

Synthesis and evaluation of 2'-hydroxyethyl trans-apovincaminate derivatives as antioxidant and cognitive enhancer agents.

Nemes A, Czibula L, Szántay C Jr, Gere A, Kiss B, Laszy J, Gyertyán I, Szombathelyi Z, Szántay C.

J Med Chem. 2008 Feb 14;51(3):479-86. doi: 10.1021/jm070618k. Epub 2008 Jan 10.

PMID:
18183943
18.

Concerted action of antiepileptic and antidepressant agents to depress spinal neurotransmission: Possible use in the therapy of spasticity and chronic pain.

Thán M, Kocsis P, Tihanyi K, Fodor L, Farkas B, Kovács G, Kis-Varga A, Szombathelyi Z, Tarnawa I.

Neurochem Int. 2007 Mar;50(4):642-52. Epub 2007 Jan 13.

PMID:
17280740
19.

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.

J Pharmacol Exp Ther. 2007 Mar;320(3):1268-78. Epub 2006 Dec 14.

PMID:
17170312
20.
21.

Flow cytometry-based method to analyze the change in Tau phosphorylation in a hGSK-3beta and hTau over-expressing EcR-293 cell line.

Kurko D, Boros A, Dezso P, Urbányi Z, Sárvári M, Nagy J, Szombathelyi Z, Szendrei GI.

Neurochem Int. 2006 Apr;48(5):374-82. Epub 2006 Jan 18.

PMID:
16420965
22.

Inducible expression and pharmacological characterization of recombinant rat NR1a/NR2A NMDA receptors.

Kurkó D, Dezso P, Boros A, Kolok S, Fodor L, Nagy J, Szombathelyi Z.

Neurochem Int. 2005 Apr;46(5):369-79.

PMID:
15737435
23.

NR2B receptors are involved in the mediation of spinal segmental reflex potentials but not in the cumulative motoneuronal depolarization in vitro.

Kocsis P, Kovács G, Farkas S, Horváth C, Szombathelyi Z, Tarnawa I.

Brain Res Bull. 2004 Aug 30;64(2):133-8.

PMID:
15342100
24.

NR2B containing NMDA receptor dependent windup of single spinal neurons.

Kovács G, Kocsis P, Tarnawa I, Horváth C, Szombathelyi Z, Farkas S.

Neuropharmacology. 2004 Jan;46(1):23-30.

PMID:
14654094
25.

NR2B subunit selective NMDA antagonists inhibit neurotoxic effect of alcohol-withdrawal in primary cultures of rat cortical neurones.

Nagy J, Horváth C, Farkas S, Kolok S, Szombathelyi Z.

Neurochem Int. 2004 Jan;44(1):17-23.

PMID:
12963084
26.

Participation of AMPA- and NMDA-type excitatory amino acid receptors in the spinal reflex transmission, in rat.

Kocsis P, Tarnawa I, Szombathelyi Z, Farkas S.

Brain Res Bull. 2003 Apr 15;60(1-2):81-91.

PMID:
12725896
27.

Identification of metabolic pathways involved in the biotransformation of tolperisone by human microsomal enzymes.

Dalmadi B, Leibinger J, Szeberényi S, Borbás T, Farkas S, Szombathelyi Z, Tihanyi K.

Drug Metab Dispos. 2003 May;31(5):631-6.

PMID:
12695352
28.
29.

[Mydeton: a centrally acting muscle relaxant drug from Gedeon Richter LTD].

Kocsis P, Tarnawa I, Kovács G, Szombathelyi Z, Farkas S.

Acta Pharm Hung. 2002;72(1):49-61. Hungarian.

PMID:
12426787
30.

Vasodilator and angioprotective activity of 1-ethyl-1-hydroxyalkyl-octahydroindolo[2,3a]quinolizine derivates.

Szombathelyi Z, Kárpáti E, Kalaus G, Szabó L, Szántay C.

Arzneimittelforschung. 1991 Jun;41(6):621-5.

PMID:
1930350
31.

[Experiences with isolated organ studies on pathological human arteries].

Szombathelyi Z, Kárpáti E, Till A.

Acta Pharm Hung. 1991 Jan;61(1):48-60. Hungarian.

PMID:
1872191
32.

Comparative in vitro study of RGH-2981, a new peripheral blood flow enhancer on animal and pathological human arteries.

Szombathelyi Z, Kárpáti E, Till A.

Pol J Pharmacol Pharm. 1989 Nov-Dec;41(6):591-5.

PMID:
2485906

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