Please use this identifier to cite or link to this item:
10.1111/bph.12506
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DC Field | Value | Language |
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dc.contributor.author | Zvejniece, L. | - |
dc.contributor.author | Vavers, E. | - |
dc.contributor.author | Svalbe, B. | - |
dc.contributor.author | Vilskersts, R. | - |
dc.contributor.author | Domracheva, I. | - |
dc.contributor.author | Vorona, M. | - |
dc.contributor.author | Veinberg, G. | - |
dc.contributor.author | Misane, I. | - |
dc.contributor.author | Stonans, I. | - |
dc.contributor.author | Kalvinsh, I. | - |
dc.contributor.author | Dambrova, M. | - |
dc.date.accessioned | 2021-05-14T07:15:01Z | - |
dc.date.available | 2021-05-14T07:15:01Z | - |
dc.date.issued | 2014-02 | - |
dc.identifier.citation | Zvejniece , L , Vavers , E , Svalbe , B , Vilskersts , R , Domracheva , I , Vorona , M , Veinberg , G , Misane , I , Stonans , I , Kalvinsh , I & Dambrova , M 2014 , ' The cognition-enhancing activity of E1R, a novel positive allosteric modulator of sigma-1 receptors ' , British Journal of Pharmacology , vol. 171 , no. 3 , pp. 761-771 . https://doi.org/10.1111/bph.12506 | - |
dc.identifier.issn | 0007-1188 | - |
dc.identifier.uri | https://dspace.rsu.lv/jspui/handle/123456789/4241 | - |
dc.description.abstract | Background and Purpose Here, we describe the in vitro and in vivo effects of (4R,5S)-2-(5-methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide (E1R), a novel positive allosteric modulator of sigma-1 receptors. Experimental Approach E1R was tested for sigma receptor binding activity in a [3H](+)- pentazocine assay, in bradykinin (BK)-induced intracellular Ca2+ concentration ([Ca2+]i) assays and in an electrically stimulated rat vas deferens model. E1R's effects on cognitive function were tested using passive avoidance (PA) and Y-maze tests in mice. A selective sigma-1 receptor antagonist (NE-100), was used to study the involvement of the sigma-1 receptor in the effects of E1R. The open-field test was used to detect the effects of E1R on locomotion. Key Results Pretreatment with E1R enhanced the selective sigma-1 receptor agonist PRE-084's stimulating effect during a model study employing electrically stimulated rat vasa deferentia and an assay measuring the BK-induced [Ca2+]i increase. Pretreatment with E1R facilitated PA retention in a dose-related manner. Furthermore, E1R alleviated the scopolamine-induced cognitive impairment during the PA and Y-maze tests in mice. The in vivo and in vitro effects of E1R were blocked by treatment with the selective sigma-1 receptor antagonist NE-100. E1R did not affect locomotor activity. Conclusion and Implications E1R is a novel 4,5-disubstituted derivative of piracetam that enhances cognition and demonstrates efficacy against scopolamine-induced cholinergic dysfunction in mice. These effects are attributed to its positive modulatory action on the sigma-1 receptor and this activity may be relevant when developing new drugs for treating cognitive symptoms related to neurodegenerative diseases. | en |
dc.format.extent | 11 | - |
dc.format.extent | 1050709 | - |
dc.language.iso | eng | - |
dc.relation.ispartof | British Journal of Pharmacology | - |
dc.rights | info:eu-repo/semantics/openAccess | - |
dc.subject | behaviour | - |
dc.subject | CNS drugs | - |
dc.subject | cognition | - |
dc.subject | E1R | - |
dc.subject | neurodegenerative diseases | - |
dc.subject | racetam | - |
dc.subject | receptor binding | - |
dc.subject | scopolamine | - |
dc.subject | sigma-1 receptor | - |
dc.subject | 3.1 Basic medicine | - |
dc.subject | 1.1. Scientific article indexed in Web of Science and/or Scopus database | - |
dc.subject | Pharmacology | - |
dc.title | The cognition-enhancing activity of E1R, a novel positive allosteric modulator of sigma-1 receptors | en |
dc.type | /dk/atira/pure/researchoutput/researchoutputtypes/contributiontojournal/article | - |
dc.identifier.doi | 10.1111/bph.12506 | - |
dc.contributor.institution | Rīga Stradiņš University | - |
dc.identifier.url | http://www.scopus.com/inward/record.url?scp=84892417640&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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The_cognition_enhancing.pdf | 1.03 MB | Adobe PDF | View/Open |
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