Please use this identifier to cite or link to this item:
10.1111/j.1742-7843.2011.00742.x
Title: | Investigation into Stereoselective Pharmacological Activity of Phenotropil |
Authors: | Zvejniece, Liga Svalbe, Baiba Veinberg, Grigory Grinberga, Solveiga Vorona, Maksims Kalvinsh, Ivars Dambrova, Maija Rīga Stradiņš University |
Keywords: | 3.1 Basic medicine;1.1. Scientific article indexed in Web of Science and/or Scopus database;Toxicology;Pharmacology |
Issue Date: | Nov-2011 |
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 |
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. |
DOI: | 10.1111/j.1742-7843.2011.00742.x |
ISSN: | 1742-7835 |
Appears in Collections: | Research outputs from Pure / Zinātniskās darbības rezultāti no ZDIS Pure |
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Investigation_into_Stereoselective_Pharmacological_Activity.pdf | 242.29 kB | Adobe PDF | View/Open |
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