Comparative study of taurine and tauropyrone : GABA receptor binding, mitochondrial processes and behaviour

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dc.contributor.authorDzirkale, Zane
dc.contributor.authorPupure, Jolanta
dc.contributor.authorRumaks, Juris
dc.contributor.authorSvirskis, Simons
dc.contributor.authorVanina, Marija
dc.contributor.authorMezhapuke, Rudolfs
dc.contributor.authorSile, Velga
dc.contributor.authorFernandes, Maria Augusta
dc.contributor.authorDuburs, Gunars
dc.contributor.authorKlusa, Vija
dc.date.accessioned2022-02-03T11:05:01Z
dc.date.available2022-02-03T11:05:01Z
dc.date.issued2011-02
dc.description.abstractObjectives Taurine, a sulfur-containing amino acid, has high hydrophilicity and is poorly absorbed. Tauropyrone, a taurine-containing 1,4-dihydropyridine derivative, is suggested to have greater activity than taurine owing to improved physicochemical properties that facilitate delivery of the compound to target cells. The aim of this study was to determine whether the 1,4-dihydropyridine moiety in tauropyrone improves the pharmacological efficacy of taurine in vitro and in vivo. Methods The effects of taurine and tauropyrone, as well as of the 1,4-dihydropyridine moiety were compared in in-vitro experiments to determine the binding to GABA receptors and influence on mitochondrial processes (isolated rat liver mitochondria), and in in-vivo tests to assess the influence on behavioural effects caused by the GABA-A receptor ligands, bicuculline, diazepam and ethanol. Key findings Unlike taurine, tauropyrone did not display binding activity for the GABA-A receptor, and only taurine (but not tauropyrone) at low doses (0.1, 1.0 and 10 mg/kg) antagonised the bicuculline-induced convulsion effect. Taurine and tauropyrone had no effect on diazepam myorelaxing action, and they both exerted a comparable 'anti-ethanol' effect (shortening of the ethanol-sleeping time). Taurine and tauropyrone did not influence processes of mitochondrial bioenergetics. Conclusions The action of tauropyrone at the level of the GABA-A receptor differs qualitatively from that of taurine, probably because of its 1,4-dihydropyridine moiety, which may hinder access to the GABA-A receptor GABA site. Tauropyrone does not show improved pharmacological efficacy in in-vitro and in-vivo studies in comparison with taurine.en
dc.description.statusPeer reviewed
dc.format.extent8
dc.format.extent627240
dc.identifier.citationDzirkale, Z, Pupure, J, Rumaks, J, Svirskis, S, Vanina, M, Mezhapuke, R, Sile, V, Fernandes, M A, Duburs, G & Klusa, V 2011, 'Comparative study of taurine and tauropyrone : GABA receptor binding, mitochondrial processes and behaviour', Journal of Pharmacy and Pharmacology, vol. 63, no. 2, pp. 230-237. https://doi.org/10.1111/j.2042-7158.2010.01204.x
dc.identifier.doi10.1111/j.2042-7158.2010.01204.x
dc.identifier.issn0022-3573
dc.identifier.urihttps://dspace.rsu.lv/jspui/handle/123456789/7444
dc.identifier.urlhttp://www.scopus.com/inward/record.url?scp=78751563028&partnerID=8YFLogxK
dc.language.isoeng
dc.relation.ispartofJournal of Pharmacy and Pharmacology
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subject1,4-dihydropyridine
dc.subjectGABA receptor ligands
dc.subjectmitochondrial processes
dc.subjecttaurine
dc.subjecttauropyrone
dc.subject3.1 Basic medicine
dc.subject1.1. Scientific article indexed in Web of Science and/or Scopus database
dc.subjectPharmacology
dc.subjectPharmaceutical Science
dc.titleComparative study of taurine and tauropyrone : GABA receptor binding, mitochondrial processes and behaviouren
dc.type/dk/atira/pure/researchoutput/researchoutputtypes/contributiontojournal/article

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