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The antidepressant-like activity of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one involves serotonergic 5-HT_{1A} and 5-HT_{2A/C} receptors activation

The antidepressant-like activity of 6-methoxy-2-[4 ...

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dc.contributor.author Pytka, Karolina [SAP20012919] pl
dc.contributor.author Walczak, Maria [SAP20001007] pl
dc.contributor.author Kij, Agnieszka [SAP14008277] pl
dc.contributor.author Rapacz, Anna [SAP20002291] pl
dc.contributor.author Siwek, Agata [SAP20008614] pl
dc.contributor.author Kazek, Grzegorz [SAP20008717] pl
dc.contributor.author Olczyk, Adrian pl
dc.contributor.author Galuszka, Adam pl
dc.contributor.author Waszkielewicz, Anna [SAP20012444] pl
dc.contributor.author Marona, Henryk [SAP20000903] pl
dc.contributor.author Sapa, Jacek [SAP20001723] pl
dc.contributor.author Filipek, Barbara [SAP20000409] pl
dc.date.accessioned 2017-02-03T06:39:31Z
dc.date.available 2017-02-03T06:39:31Z
dc.date.issued 2015 pl
dc.identifier.issn 0014-2999 pl
dc.identifier.uri http://ruj.uj.edu.pl/xmlui/handle/item/36827
dc.language eng pl
dc.rights Dodaję tylko opis bibliograficzny *
dc.rights.uri *
dc.title The antidepressant-like activity of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one involves serotonergic 5-HT_{1A} and 5-HT_{2A/C} receptors activation pl
dc.type JournalArticle pl
dc.description.physical 537-546 pl
dc.abstract.en Xanthone derivatives have been shown to posses many biological properties. Some of them act within the central nervous system and show neuroprotective or antidepressant like properties. Taking this into account we investigated antidepressant like activity in mice and the possible mechanism of action of 6-methoxy-2-{[}4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-11) - a new xanthone derivative. We demonstrated that HBK-11 produced antidepressant like effects in the forced swim test and tail suspension test, comparable to that of venlafaxine. The combined treatment with sub effective doses of HBK-11 and fluoxetine (but not reboxetine or bupropion) significantly reduced the immobility in the forced swim test. Moreover, the antidepressant like activity of HBK-11 in the aforementioned test was blocked by p-chlorophertylalanine, and significantly reduced by serotonergic 5HT(1A) receptor antagunist - WAY-1006335 and 5HT(2A/C) receptor antagonist - ritanserin. As none of the above treatments influenced the spontaneous locomotor activity, if can be concluded that HBK-11 mediates its activity through a serotonergic system, and its antidepressant like effect involves 5HT(1A) and 5HT(2A/C) receptor activation. Furthermore, at antidepressant like doses HBK-11 did not cause the mice to display locomotor deficits in rotarod or chimney rests. Considering the pharmacokinetic profile, HBK-11 demonstrated rapid absorption after i.p. administration, high clearance value, short terminal half-life, very high volume of distribution and incomplete bioavailabilily. The compound studied had good penetration into the brain tissue of mice. Since studied xanthone derivative seems to present interesting, untypical mechanism of antidepressant-like action i.e. 5HT(2A/C) receptor activation, it may have a potential in the treatment of depressive disorders, and surely requires further studies. pl
dc.description.volume 764 pl
dc.description.points 25 pl
dc.identifier.doi 10.1016/j.ejphar.2015.07.041 pl
dc.identifier.eissn 1879-0712 pl
dc.title.journal European Journal of Pharmacology pl
dc.language.container eng pl
dc.affiliation Wydział Farmaceutyczny : Zakład Farmakodynamiki pl
dc.affiliation Wydział Farmaceutyczny : Zakład Wstępnych Badań Farmakologicznych pl
dc.affiliation Wydział Farmaceutyczny : Zakład Chemii Bioorganicznej pl
dc.affiliation Wydział Farmaceutyczny : Katedra Farmakobiologii pl
dc.affiliation Pion Prorektora ds. badań naukowych i funduszy strukturalnych : Jagiellońskie Centrum Rozwoju Leków pl
dc.affiliation Wydział Farmaceutyczny : Zakład Toksykologii pl
dc.subtype Article pl
dc.rights.original bez licencji pl
.pointsMNiSW [2015 A]: 25

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