Please use this identifier to cite or link to this item:
10.1111/j.1742-7843.2011.00742.x
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DC Field | Value | Language |
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dc.contributor.author | Zvejniece, Liga | - |
dc.contributor.author | Svalbe, Baiba | - |
dc.contributor.author | Veinberg, Grigory | - |
dc.contributor.author | Grinberga, Solveiga | - |
dc.contributor.author | Vorona, Maksims | - |
dc.contributor.author | Kalvinsh, Ivars | - |
dc.contributor.author | Dambrova, Maija | - |
dc.date.accessioned | 2021-07-06T08:30:01Z | - |
dc.date.available | 2021-07-06T08:30:01Z | - |
dc.date.issued | 2011-11 | - |
dc.identifier.citation | Zvejniece , 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.issn | 1742-7835 | - |
dc.identifier.uri | https://dspace.rsu.lv/jspui/handle/123456789/5833 | - |
dc.description.abstract | Phenotropil [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.format.extent | 6 | - |
dc.format.extent | 248105 | - |
dc.language.iso | eng | - |
dc.relation.ispartof | Basic and Clinical Pharmacology and Toxicology | - |
dc.rights | info:eu-repo/semantics/openAccess | - |
dc.subject | 3.1 Basic medicine | - |
dc.subject | 1.1. Scientific article indexed in Web of Science and/or Scopus database | - |
dc.subject | Toxicology | - |
dc.subject | Pharmacology | - |
dc.title | Investigation into Stereoselective Pharmacological Activity of Phenotropil | en |
dc.type | /dk/atira/pure/researchoutput/researchoutputtypes/contributiontojournal/article | - |
dc.identifier.doi | 10.1111/j.1742-7843.2011.00742.x | - |
dc.contributor.institution | Rīga Stradiņš University | - |
dc.identifier.url | http://www.scopus.com/inward/record.url?scp=80054061990&partnerID=8YFLogxK | - |
dc.description.status | Peer reviewed | - |
Appears in Collections: | Research outputs from Pure / Zinātniskās darbības rezultāti no ZDIS Pure |
Files in This Item:
File | Size | Format | |
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Investigation_into_Stereoselective_Pharmacological_Activity.pdf | 242.29 kB | Adobe PDF | View/Open |
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