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Titolo:
Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655
Autore:
Szabados, T; Gigler, G; Gacsalyi, I; Gyertyan, I; Levay, G;
Indirizzi:
EGIS Pharmaceut Ltd, Dept CNS Pharmacol, H-1475 Budapest 10, Hungary EGIS Pharmaceut Ltd Budapest Hungary 10 col, H-1475 Budapest 10, Hungary
Titolo Testata:
BRAIN RESEARCH BULLETIN
fascicolo: 3, volume: 55, anno: 2001,
pagine: 387 - 391
SICI:
0361-9230(200106)55:3<387:COAAAN>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
NON-NMDA ANTAGONISTS; GLOBAL-ISCHEMIA; GYKI-52466; GLUTAMATE; NBQX; MICE; RAT;
Keywords:
GYKI 52466; global cerebral ischaemia; MgCl2; audiogenic seizure; maximal electroshock; DBA/2j mice;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Gacsalyi, I EGIS Pharmaceut Ltd, Dept CNS Pharmacol, POB 100, H-1475 Budapest 10, Hungary EGIS Pharmaceut Ltd POB 100 Budapest Hungary 10 t 10, Hungary
Citazione:
T. Szabados et al., "Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655", BRAIN RES B, 55(3), 2001, pp. 387-391

Abstract

GYKI 52466 [1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine], a non-competitive AMPA [alpha -amino-3-hydroxy-5-methyl-4-isoxazolepropionate] and kainate receptor antagonist and its two analogues, GYKI 53405 [1-(4-aminophenyl)-3-acetyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine] and GYKI 53655 [1-(4-aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine] were investigatedin two seizure models and in MgCl2 induced global cerebral ischaemia, as an acute neuroprotective model. The ED50 values of GYKI 52466 for suppression of the tonic and clonic phases of sound-induced seizures were 3.6 and 4.3mg/kg, respectively. The corresponding data for GYKI 53405 were 1.1 and 3.1 mg/kg, while ED50 values of GYKI 53655 were 1.3 and 2.0 mg/kg, respectively. The inhibition of seizure evoked by maximal electroshock was also foundto be remarkable: the ED50 values of GYKI 52466 and its two analogues were6.9, 2.6, and 2.2 mg/kg, respectively. All compounds prolonged the survival times in MgCl2 induced global cerebral ischaemia test in a close-dependent fashion, with PD50 (dose of 50% prolongation) values of 24.1, 8.3, and 8.2 mg/kg intraperitoneal respectively. In audiogenic seizure model the duration of anticonvulsant action of 10 mg/kg GYKI 52466 and 5 mg/kg GYKI 53405,GYKI 53655 were examined, too. The effect of GYKI 52466 decreased to 50% after 2 h, while the analogues showed more than 80% seizure suppression 3 h after treatment. After 6 h the effect of GYKI 53655 decreased to zero, while the effect of GYKI 52466, remained on the 50% level. (C) 2001 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 18:59:24