Počet záznamů: 1  

Neurosteroids as positive and negative allosteric modulators of ligand-gated ion channels: P2X receptor perspective

  1. 1.
    SYSNO ASEP0572394
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevNeurosteroids as positive and negative allosteric modulators of ligand-gated ion channels: P2X receptor perspective
    Tvůrce(i) Sivčev, Sonja (FGU-C) RID, ORCID
    Kudová, Eva (UOCHB-X) RID, ORCID
    Zemková, Hana (FGU-C) RID, ORCID
    Celkový počet autorů3
    Číslo článku109542
    Zdroj.dok.Neuropharmacology. - : Elsevier - ISSN 0028-3908
    Roč. 234, Aug 15 (2023)
    Poč.str.14 s.
    Jazyk dok.eng - angličtina
    Země vyd.GB - Velká Británie
    Klíč. slovaP2X receptors ; ion channels ; neurosteroids ; allosteric modulators ; extracellular ATP
    Obor OECDPhysiology (including cytology)
    CEPLQ1604 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy
    Způsob publikováníOmezený přístup
    Institucionální podporaFGU-C - RVO:67985823 ; UOCHB-X - RVO:61388963
    UT WOS000984666300001
    EID SCOPUS85152443752
    DOI10.1016/j.neuropharm.2023.109542
    AnotaceNeurosteroids are steroids synthesized de novo in the brain from cholesterol in an independent manner from peripheral steroid sources. The term “neuroactive steroid“ includes all steroids independent of their origin, and newly synthesized analogs of neurosteroids that modify neuronal activities. In vivo application of neuroactive steroids induces potent anxiolytic, antidepressant, anticonvulsant, sedative, analgesic and amnesic effects, mainly through interaction with the γ-aminobutyric acid type-A receptor (GABAAR). However, neuroactive steroids also act as positive or negative allosteric regulators on several ligand-gated channels including N-methyl-d-aspartate receptors (NMDARs), nicotinic acetylcholine receptors (nAChRs) and ATP-gated purinergic P2X receptors. Seven different P2X subunits (P2X1-7) can assemble to form homotrimeric or heterotrimeric ion channels permeable for monovalent cations and calcium. Among them, P2X2, P2X4, and P2X7 are the most abundant within the brain and can be regulated by neurosteroids. Transmembrane domains are necessary for neurosteroid binding, however, no generic motif of amino acids can accurately predict the neurosteroid binding site for any of the ligand-gated ion channels including P2X. Here, we will review what is currently known about the modulation of rat and human P2X by neuroactive steroids and the possible structural determinants underlying neurosteroid-induced potentiation and inhibition of the P2X2 and P2X4 receptors.
    PracovištěFyziologický ústav
    KontaktLucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400
    Rok sběru2024
    Elektronická adresahttps://doi.org/10.1016/j.neuropharm.2023.109542
Počet záznamů: 1  

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