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Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N-Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F18%3A00498559" target="_blank" >RIV/61388963:_____/18:00498559 - isvavai.cz</a>

  • Alternative codes found

    RIV/67985823:_____/18:00498559 RIV/00216208:11320/18:10439840

  • Result on the web

    <a href="https://www.frontiersin.org/articles/10.3389/fphar.2018.01299/full" target="_blank" >https://www.frontiersin.org/articles/10.3389/fphar.2018.01299/full</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.3389/fphar.2018.01299" target="_blank" >10.3389/fphar.2018.01299</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N-Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif

  • Original language description

    Herein, we report the synthesis, structure-activity relationship study, and biological evaluation of neurosteroid inhibitors of N-methyl-D-aspartate receptors (NMDARs) receptors that employ an amide structural motif, relative to pregnanolone glutamate (PAG) a compound with neuroprotective properties. All compounds were found to be more potent NMDAR inhibitors (IC50 values varying from 1.4 to 21.7 mu M) than PAG (IC50 = 51.7 mu M). Selected compound 6 was evaluated for its NMDAR subtype selectivity and its ability to inhibit AMPAR/GABAR responses. Compound 6 inhibits the NMDARs (8.3 receptors (8.3 +/- 2.1 mu M) more strongly than it does at the GABAR and AMPARs (17.0 receptors (17.0 +/- 0.2 mu M and 276.4 +/- 178.7 mu M, respectively). In addition, compound 6 (10 mu M) decreases the frequency of action potentials recorded in cultured hippocampal neurons. Next, compounds 3, 5-7, 9, and 10 were not associated with mitotoxicity, hepatotoxicity nor ROS induction. Lastly, we were able to show that all compounds have improved rat and human plasma stability over PAG.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10608 - Biochemistry and molecular biology

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Others

  • Publication year

    2018

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Frontiers in Pharmacology

  • ISSN

    1663-9812

  • e-ISSN

  • Volume of the periodical

    9

  • Issue of the periodical within the volume

    Nov 12

  • Country of publishing house

    CH - SWITZERLAND

  • Number of pages

    16

  • Pages from-to

  • UT code for WoS article

    000449859800001

  • EID of the result in the Scopus database

    2-s2.0-85056740159