Počet záznamů: 1  

Modulation of GABA and glycine receptors in rat pyramidal hippocampal neurones by 3 alpha 5 beta-pregnanolone derivatives

  1. 1.
    SYSNO ASEP0492171
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevModulation of GABA and glycine receptors in rat pyramidal hippocampal neurones by 3 alpha 5 beta-pregnanolone derivatives
    Tvůrce(i) Bukanova, J. V. (RU)
    Solntseva, E. I. (RU)
    Kolbaev, S. N. (RU)
    Kudová, Eva (UOCHB-X) RID, ORCID
    Zdroj.dok.Neurochemistry International. - : Elsevier - ISSN 0197-0186
    Roč. 118, Sep (2018), s. 145-151
    Poč.str.7 s.
    Jazyk dok.eng - angličtina
    Země vyd.GB - Velká Británie
    Klíč. slovaneurosteroid ; GABA receptor ; glycine receptor ; pregnanolone ; structure-activity relationship
    Vědní obor RIVCE - Biochemie
    Obor OECDBiochemistry and molecular biology
    CEPTE01020028 GA TA ČR - Technologická agentura ČR
    Institucionální podporaUOCHB-X - RVO:61388963
    UT WOS000439674200016
    EID SCOPUS85048388816
    DOI10.1016/j.neuint.2018.06.002
    AnotaceThe ability of pregnanolone glutamate (PA-Glu), pregnanolone hemisuccinate (PA-hSuc) and pregnanolone hemipimelate (PA-hPim), neuroactive steroids with a negative modulatory effect on excitatory N-methyl-D-aspartate receptors, to influence the functional activity of inhibitory gamma-aminobutyric acid and glycine receptors was estimated. The GABA- and glycine-induced chloride currents (I-GABA and I-Gly) were measured in isolated pyramidal neurons of the rat hippocampus using the patch-clamp technique. Compound PA-Glu was found to potentiate I-GABA and to inhibit loy, while PA-hSuc and PA-hPim inhibited both I-GABA and I-Gly. Moreover, PA-Glu, PA-hSuc, and PA-hPim had a greater effect on desensitization than on the peak amplitude of I-Gly. At a high concentration of glycine (500 mu M), the effect of neurosteroids on the peak amplitude of I-Gly disappeared, and the acceleration of desensitization remained. The conversion of PA-Glu into androstane glutamate (AND-Glu), an analogue that lacks the C-17 acetyl moiety, completely eliminated the effects on these receptors. Our results indicate that the C-17 acetyl moiety is crucial for the action on I-GABA and I-Gly. Our results indicate that the pregnanolone derivatives, in contrast to the androstane analogues, modulate I-GABA and I-Gly at low micromolar concentrations and this family of neurosteroids can be useful for future structure-activity relationship studies of the steroid modulation of other receptor types.
    PracovištěÚstav organické chemie a biochemie
    Kontaktasep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434
    Rok sběru2019
Počet záznamů: 1  

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