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dc.contributor.authorJanockova, Janaen_GB
dc.contributor.authorDolezal, Rafaelen_GB
dc.contributor.authorNepovimova, Eugenieen_GB
dc.contributor.authorKobrlova, Terezaen_GB
dc.contributor.authorBenkova, Marketaen_GB
dc.contributor.authorKuca, Kamilen_GB
dc.contributor.authorKonecny, Janen_GB
dc.contributor.authorMezeiova, Evaen_GB
dc.contributor.authorMelikova, Michaelaen_GB
dc.contributor.authorHepnarova, Vendulaen_GB
dc.contributor.authorRing, Avien_GB
dc.contributor.authorSoukup, Ondrejen_GB
dc.contributor.authorKorabecny, Janen_GB
dc.date.accessioned2019-01-02T12:53:10Z
dc.date.accessioned2019-01-09T08:17:35Z
dc.date.available2019-01-02T12:53:10Z
dc.date.available2019-01-09T08:17:35Z
dc.date.issued2018
dc.identifier.citationJanockova, Dolezal, Nepovimova, Kobrlova, Benkova, Kuca, Konecny, Mezeiova, Melikova, Hepnarova, Ring A, Soukup, Korabecny. Investigation of new orexin 2 receptor modulators using in silico and in vitro methods. Molecules. 2018;23(11)en_GB
dc.identifier.urihttp://hdl.handle.net/123456789/76246
dc.identifier.urihttp://hdl.handle.net/20.500.12242/2505
dc.descriptionJanockova, Jana; Dolezal, Rafael; Nepovimova, Eugenie; Kobrlova, Tereza; Benkova, Marketa; Kuca, Kamil; Konecny, Jan; Mezeiova, Eva; Melikova, Michaela; Hepnarova, Vendula; Ring, Avi; Soukup, Ondrej; Korabecny, Jan. Investigation of new orexin 2 receptor modulators using in silico and in vitro methods. Molecules 2018 ;Volum 23.(11)en_GB
dc.description.abstractThe neuropeptides, orexin A and orexin B (also known as hypocretins), are produced in hypothalamic neurons and belong to ligands for orphan G protein-coupled receptors. Generally, the primary role of orexins is to act as excitatory neurotransmitters and regulate the sleep process. Lack of orexins may lead to sleep disorder narcolepsy in mice, dogs, and humans. Narcolepsy is a neurological disorder of alertness characterized by a decrease of ability to manage sleep-wake cycles, excessive daytime sleepiness, and other symptoms, such as cataplexy, vivid hallucinations, and paralysis. Thus, the discovery of orexin receptors, modulators, and their causal implication in narcolepsy is the most important advance in sleep-research. The presented work is focused on the evaluation of compounds L1–L11 selected by structure-based virtual screening for their ability to modulate orexin receptor type 2 (OX2R) in comparison with standard agonist orexin-A together with their blood-brain barrier permeability and cytotoxicity. We can conclude that the studied compounds possess an affinity towards the OX2R. However, the compounds do not have intrinsic activity and act as the antagonists of this receptor. It was shown that L4 was the most potent antagonistic ligand to orexin A and displayed an IC50 of 2.2 µM, offering some promise mainly for the treatment of insomnia.en_GB
dc.language.isoenen_GB
dc.subjectTermSet Emneord::Narkolepsi
dc.subjectTermSet Emneord::Søvn
dc.subjectTermSet Emneord::Oreksin
dc.titleInvestigation of new orexin 2 receptor modulators using in silico and in vitro methodsen_GB
dc.typeArticleen_GB
dc.date.updated2019-01-02T12:53:10Z
dc.identifier.cristinID1647801
dc.identifier.cristinID1647801
dc.identifier.doi10.3390/molecules23112926
dc.source.issn1420-3049
dc.type.documentJournal article
dc.relation.journalMolecules


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