Access of inhibitory neurosteroids to the NMDA receptor

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F12%3A33143002" target="_blank" >RIV/61989592:15310/12:33143002 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/67985823:_____/12:00379112 RIV/61388963:_____/12:00379112

Výsledek na webu

<a href="http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2011.01816.x/abstract;jsessionid=AC688D0796D6A68D8D0E67DA50B1D2A7.d04t03" target="_blank" >http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2011.01816.x/abstract;jsessionid=AC688D0796D6A68D8D0E67DA50B1D2A7.d04t03</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1111/j.1476-5381.2011.01816.x" target="_blank" >10.1111/j.1476-5381.2011.01816.x</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Access of inhibitory neurosteroids to the NMDA receptor

Popis výsledku v původním jazyce

BACKGROUND AND PURPOSE NMDA receptors are glutamatergic ionotropic receptors involved in excitatory neurotransmission, synaptic plasticity and excitotoxic cell death. Many allosteric modulators can influence the activity of these receptors positively ornegatively, with behavioural consequences. 20-Oxo-5 beta-pregnan-3a-yl sulphate (pregnanolone sulphate; PA-6) is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective. We tested the hypothesis that the interaction of PA-6 with the plasma membrane is critical for its inhibitory effect at NMDA receptors. EXPERIMENTAL APPROACH Electrophysiological recordings and live microscopy were performed on heterologous HEK293 cells expressing GluN1/GluN2B receptors and cultured rat hippocampal neurons. KEY RESULTS Our experiments showed that the kinetics of the steroid inhibition were slow and not typical of drug-receptor interaction in an aqueous solution. In addition, the recovery from steroid inhibition was accelerated by

Název v anglickém jazyce

Access of inhibitory neurosteroids to the NMDA receptor

Popis výsledku anglicky

BACKGROUND AND PURPOSE NMDA receptors are glutamatergic ionotropic receptors involved in excitatory neurotransmission, synaptic plasticity and excitotoxic cell death. Many allosteric modulators can influence the activity of these receptors positively ornegatively, with behavioural consequences. 20-Oxo-5 beta-pregnan-3a-yl sulphate (pregnanolone sulphate; PA-6) is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective. We tested the hypothesis that the interaction of PA-6 with the plasma membrane is critical for its inhibitory effect at NMDA receptors. EXPERIMENTAL APPROACH Electrophysiological recordings and live microscopy were performed on heterologous HEK293 cells expressing GluN1/GluN2B receptors and cultured rat hippocampal neurons. KEY RESULTS Our experiments showed that the kinetics of the steroid inhibition were slow and not typical of drug-receptor interaction in an aqueous solution. In addition, the recovery from steroid inhibition was accelerated by

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

ED - Fyziologie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2012

Kód důvěrnosti údajů

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

Název periodika

British Journal of Pharmacology

ISSN

0007-1188

e-ISSN

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Svazek periodika

166

Číslo periodika v rámci svazku

3

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

15

Strana od-do

1069-1083

Kód UT WoS článku

000303923000021

EID výsledku v databázi Scopus

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