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Anticonvulsant Action of GluN2A-Preferring Antagonist PEAQX in Developing Rats
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SYSNO ASEP 0542146 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Anticonvulsant Action of GluN2A-Preferring Antagonist PEAQX in Developing Rats Tvůrce(i) Mareš, Pavel (FGU-C) RID, ORCID
Tsenov, Grygoriy (FGU-C) RID, ORCID
Kubová, Hana (FGU-C) RID, ORCIDČíslo článku 415 Zdroj.dok. Pharmaceutics. - : MDPI
Roč. 13, č. 3 (2021)Poč.str. 15 s. Jazyk dok. eng - angličtina Země vyd. CH - Švýcarsko Klíč. slova NMDA receptors ; GluN2A subunit ; anticonvulsant action ; pentylenetetrazol-induced seizures ; cortical epileptic afterdischarges ; immature rats Vědní obor RIV FR - Farmakologie a lékárnická chemie Obor OECD Pharmacology and pharmacy CEP GA19-11931S GA ČR - Grantová agentura ČR GA18-09296S GA ČR - Grantová agentura ČR EF16_025/0007444 GA MZd - Ministerstvo zdravotnictví Způsob publikování Open access Institucionální podpora FGU-C - RVO:67985823 UT WOS 000634070000001 EID SCOPUS 85103080287 DOI 10.3390/pharmaceutics13030415 Anotace The GluN2A subunit of N-methyl-D-aspartate (NMDA) receptors becomes dominant during postnatal development, overgrowing the originally dominant GluN2B subunit. The aim of our study was to show changes of anticonvulsant action of the GluN2A subunit-preferring antagonist during postnatal development of rats. Possible anticonvulsant action of GluN2A-preferring antagonist of NMDA receptors P = [[[(1S)-1-(4-bromophenyl)ethyl]amino](1,2,3,4-tetrahydro-2,3-dioxo-5-quinoxalinyl)methyl]phosphonic acid tetrasodium salt (PEAQX) (5, 10, 20 mg/kg s.c.) was tested in 12-, 18-, and 25-day-old rats in three models of convulsive seizures. Pentylenetetrazol-induced generalized seizures with a loss of righting reflexes generated in the brainstem were suppressed in all three age groups in a dose-dependent manner. Minimal clonic seizures with preserved righting ability exhibited only moderately prolonged latency after the highest dose of PEAQX. Anticonvulsant action of all three doses of PEAQX against cortical epileptic afterdischarges (generated in the forebrain) was found in the 25-day-old animals. The highest dose (20 mg/kg) was efficient also in the two younger groups, which might be due to lower specificity of PEAQX and its partial affinity to the GluN2B subunit. Our results are in agreement with the postero-anterior maturation gradient of subunit composition of NMDA receptors (i.e., an increase of GluN2A representation). In spite of the lower selectivity of PEAQX, our data demonstrate, for the first time, developmental differences in comparison with an antagonist of NMDA receptors with a dominant GluN2B subunit. Pracoviště Fyziologický ústav Kontakt Lucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400 Rok sběru 2022 Elektronická adresa https://www.mdpi.com/1999-4923/13/3/415
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