Investigation into Stereoselective Pharmacological Activity of Phenotropil

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dc.contributor.authorZvejniece, Liga
dc.contributor.authorSvalbe, Baiba
dc.contributor.authorVeinberg, Grigory
dc.contributor.authorGrinberga, Solveiga
dc.contributor.authorVorona, Maksims
dc.contributor.authorKalvinsh, Ivars
dc.contributor.authorDambrova, Maija
dc.contributor.institutionRīga Stradiņš University
dc.date.accessioned2021-07-06T08:30:01Z
dc.date.available2021-07-06T08:30:01Z
dc.date.issued2011-11
dc.description.abstractPhenotropil [N-carbamoylmethyl-4-aryl-2-pyrrolidone (2-(2-oxo-4-phenyl-pyrrolidin-1-yl) acetamide; carphedon)] is clinically used in its racemic form as a nootropic drug that improves physical condition and cognition. The aim of this study was to compare the stereoselective pharmacological activity of R- and S-enantiomers of phenotropil in different behavioural tests. Racemic phenotropil and its enantiomers were tested for locomotor, antidepressant and memory-improving activity and influence on the central nervous system (CNS) using general pharmacological tests in mice. After a single administration, the amount of compound in brain tissue extracts was determined using an ultra performance liquid chromatography-tandem mass spectrometry (UPLC/MS/MS) method in a positive ion electrospray mode. In the open-field test, a significant increase in locomotor activity was observed after a single administration of R-phenotropil at doses of 10 and 50mg/kg and S-phenotropil at a dose of 50mg/kg. In the forced swim test, R-phenotropil induced an antidepressant effect at doses of 100 and 50mg/kg, and S-phenotropil was active at a dose of 100mg/kg. R-phenotropil significantly enhanced memory function in a passive avoidance response test at a dose of 1 mg/kg; the S-enantiomer did not show any activity in this test. However, the concentrations of R- and S-phenotropils in brain tissue were similar. In conclusion, the antidepressant and increased locomotor activity relies on both R- and S-phenotropils, but the memory-improving activity is only characteristic of R-phenotropil. These results may be important for the clinical use of optically pure isomers of phenotropil.en
dc.description.statusPeer reviewed
dc.format.extent6
dc.format.extent248105
dc.identifier.citationZvejniece, L, Svalbe, B, Veinberg, G, Grinberga, S, Vorona, M, Kalvinsh, I & Dambrova, M 2011, 'Investigation into Stereoselective Pharmacological Activity of Phenotropil', Basic and Clinical Pharmacology and Toxicology, vol. 109, no. 5, pp. 407-412. https://doi.org/10.1111/j.1742-7843.2011.00742.x
dc.identifier.doi10.1111/j.1742-7843.2011.00742.x
dc.identifier.issn1742-7835
dc.identifier.urihttps://dspace.rsu.lv/jspui/handle/123456789/5833
dc.identifier.urlhttp://www.scopus.com/inward/record.url?scp=80054061990&partnerID=8YFLogxK
dc.language.isoeng
dc.relation.ispartofBasic and Clinical Pharmacology and Toxicology
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subject3.1 Basic medicine
dc.subject1.1. Scientific article indexed in Web of Science and/or Scopus database
dc.subjectToxicology
dc.subjectPharmacology
dc.titleInvestigation into Stereoselective Pharmacological Activity of Phenotropilen
dc.type/dk/atira/pure/researchoutput/researchoutputtypes/contributiontojournal/article

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