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

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F23%3A00572394" target="_blank" >RIV/61388963:_____/23:00572394 - isvavai.cz</a>

  • Alternative codes found

    RIV/67985823:_____/23:00572394 RIV/00216208:11310/23:10480008

  • Result on the web

    <a href="https://doi.org/10.1016/j.neuropharm.2023.109542" target="_blank" >https://doi.org/10.1016/j.neuropharm.2023.109542</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.neuropharm.2023.109542" target="_blank" >10.1016/j.neuropharm.2023.109542</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

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

  • Original language description

    Neurosteroids 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.

  • 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

    30105 - Physiology (including cytology)

Result continuities

  • Project

    <a href="/en/project/LQ1604" target="_blank" >LQ1604: BIOCEV: from Fundamental to Applied Research</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2023

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Neuropharmacology

  • ISSN

    0028-3908

  • e-ISSN

    1873-7064

  • Volume of the periodical

    234

  • Issue of the periodical within the volume

    Aug 15

  • Country of publishing house

    GB - UNITED KINGDOM

  • Number of pages

    14

  • Pages from-to

    109542

  • UT code for WoS article

    000984666300001

  • EID of the result in the Scopus database

    2-s2.0-85152443752