Selective inhibition of extra-synaptic α5-GABA A receptors by S44819, a new therapeutic agent

Autor: Lori-An Etherington, Adrienn Pálvölgyi, Katalin Pallagi, Ferenc A. Antoni, Adam R. Brown, József Barkóczy, Delia Belelli, Olivia Monteiro, Szabolcs Kertesz, Ben G. Gunn, Michael Spedding, Balázs Mihalik, Istvan Gacsalyi, István Ling, Matthew R. Livesey, Péter Varga, Jeremy J. Lambert

Publikováno v: Etherington, L-A, Mihalik, B, Pálvölgyi, A, Ling, I, Pallagi, K, Kertész, S, Varga, P, Gunn, B, Brown, A, Livesey, M, Monteiro, O, Belelli, D, Barkóczy, J, Spedding, M, Gacsályi, I, Antoni, F & Lambert, J 2017, ' Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. ', Neuropharmacology, pp. 30379-9 . https://doi.org/10.1016/j.neuropharm.2017.08.012

In the mammalian central nervous system (CNS) GABAA receptors (GABAARs) mediate neuronal inhibition and are important therapeutic targets. GABAARs are composed of 5 subunits, drawn from 19 proteins, underpinning expression of 20–30 GABAAR subtypes.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c42c09c14917f391a41a6b52b26e2be7
https://doi.org/10.1016/j.neuropharm.2017.08.012

Loop-F of the α-subunit determines the pharmacologic profile of novel competitive inhibitors of GABA A receptors

Autor: Tamás A. Martinek, Istvan Gacsalyi, Katalin Megyeri, Ferenc Bogár, Adrienn Pálvölgyi, István Ling, Ferenc A. Antoni, Balázs Mihalik, Ferenc Bartha, József Barkóczy

Publikováno v: European Journal of Pharmacology. 798:129-136

The neurotransmitter γ-amino butyric acid (GABA) has a fundamental role in CNS function and ionotropic (GABAA) receptors that mediate many of the actions of GABA are important therapeutic targets. This study reports the mechanism of action of novel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::92fa262ada488896cbdee7d76040328d
https://doi.org/10.1016/j.ejphar.2017.01.033

Behavioural pharmacology of the α5-GABA

Autor: István, Gacsályi, Krisztina, Móricz, Gábor, Gigler, János, Wellmann, Katalin, Nagy, István, Ling, József, Barkóczy, József, Haller, Jeremy J, Lambert, Gábor, Szénási, Michael, Spedding, Ferenc A, Antoni

Publikováno v: Neuropharmacology. 125

Previous work has shown that S44819 is a novel GABAA receptor (GABA

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::09ebde6f1ae563b73702ec08b70bc26c
https://pubmed.ncbi.nlm.nih.gov/28694097

(Phenylpiperazinyl-butyl)oxindoles as Selective 5-HT7 Receptor Antagonists

Autor: Katalin Pallagi, György Lévay, Balázs Volk, József Barkóczy, Gyula Simig, Szabolcs Udvari, Kompagne Hajnalka, Andras Egyed, Michael Spedding, Laszlo G. Harsing, Istvan Gacsalyi, Tibor Mezei, Endre Hegedüs

Publikováno v: Journal of Medicinal Chemistry. 51:2522-2532

A series of potent 5-hydroxytryptamine 7 (5-HT 7) ligands has been synthesized that contain a 1,3-dihydro-2 H-indol-2-one (oxindole) skeleton. The binding of these compounds to the 5-HT 7 and 5-HT 1A receptors was measured. Despite the structural sim

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0d468c377c2e67ea1cfb5761c902161
https://doi.org/10.1021/jm070279v

Neuroprotective and anticonvulsant effects of EGIS-8332, a non-competitive AMPA receptor antagonist, in a range of animal models

Autor: Gabor Gigler, Miklos Vegh, Szabolcs Kertesz, József Barkóczy, Annamária Simó, Angéla Benedek, Márta Ágoston, Geza Szabo, Marko Bernadett Martonne, Gábor Szénási, Istvan Gacsalyi, Gábor Kapus, Éva Matucz, Laszlo G. Harsing, György Lévay, Krisztina Moricz, Mihály Albert

Publikováno v: British Journal of Pharmacology. 152:151-160

Background and purpose: Blockade of AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors is a good treatment option for a variety of central nervous system disorders. The present study evaluated the neuroprotective and anticonvulsan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::dd3966238aab0b5fb764132994000a9e
https://doi.org/10.1038/sj.bjp.0707362