Investigations on the pharmacology of the cardioprotective guanidine ME10092

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dc.contributor.authorDambrova, Maija
dc.contributor.authorLiepinsh, Edgars
dc.contributor.authorKirjanova, Olga
dc.contributor.authorPetrovska, Ramona
dc.contributor.authorPugovich, Osvalds
dc.contributor.authorBaumane, Larisa
dc.contributor.authorUhlen, Staffan
dc.contributor.authorKalvinsh, Ivars
dc.contributor.authorOliver, Douglas
dc.contributor.authorWikberg, Jarl E.S.
dc.date.accessioned2021-07-06T12:10:01Z
dc.date.available2021-07-06T12:10:01Z
dc.date.issued2004-08
dc.description.abstractThe guanidine compound ME10092 (1-(3,4-dimethoxy-2-chlorobenzylideneamino)- guanidine), which possesses a strong cardioprotective effect to ischemia-reperfusion, was assessed for different pharmacological actions that may underlie its cardioprotective effect. In the living rat ME10092 decreased the blood pressure and heart rate in a dose-dependent manner. We found ME10092 to bind to α1- and α2-adrenoreceptors with moderate affinity (Ki values 1-4 μM), and to block adrenaline-elicited contractile responses in isolated guinea pig aortas. Our results indicate that ME10092 possesses a certain anti-oxidant profile. Thus, in a competitive manner and with low affinity it inhibited the bovine milk xanthine oxidase enzyme, as well as NAD(P)H oxidase driven oxyradical formation in membrane fractions isolated from the rat brain. By using electron paramagnetic resonance we here show that, after its systemic administration, ME10092 modulates the nitric oxide (NO) content in several tissues of the rat in a time-dependent manner. However, in vitro ME10092 inhibited the activities of nitric oxide synthases nNOS and eNOS, but not that of iNOS. Our data give evidence that the cardioprotective effect of ME10092 could be mediated through pharmacological mechanisms that include some modulation of NO production, as well as possible inhibition of radical formation during ischemia-reperfusion.en
dc.description.statusPeer reviewed
dc.format.extent9
dc.format.extent312610
dc.identifier.citationDambrova, M, Liepinsh, E, Kirjanova, O, Petrovska, R, Pugovich, O, Baumane, L, Uhlen, S, Kalvinsh, I, Oliver, D & Wikberg, J E S 2004, 'Investigations on the pharmacology of the cardioprotective guanidine ME10092', Journal of Cardiovascular Pharmacology, vol. 44, no. 2, pp. 178-186. https://doi.org/10.1097/00005344-200408000-00006
dc.identifier.doi10.1097/00005344-200408000-00006
dc.identifier.issn0160-2446
dc.identifier.urihttps://dspace.rsu.lv/jspui/handle/123456789/5835
dc.identifier.urlhttp://www.scopus.com/inward/record.url?scp=3242798168&partnerID=8YFLogxK
dc.language.isoeng
dc.relation.ispartofJournal of Cardiovascular Pharmacology
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectAdrenoreceptor
dc.subjectGuanidine
dc.subjectNAD(P)H oxidase
dc.subjectNitric oxide synthase
dc.subjectXanthine oxidase
dc.subject3.1 Basic medicine
dc.subject1.1. Scientific article indexed in Web of Science and/or Scopus database
dc.subjectPharmacology
dc.subjectCardiology and Cardiovascular Medicine
dc.titleInvestigations on the pharmacology of the cardioprotective guanidine ME10092en
dc.type/dk/atira/pure/researchoutput/researchoutputtypes/contributiontojournal/article

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