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Titolo:
Do antiepileptics phenytoin, carbamazepine, and loreclezole show GABA(A) receptor subtype selectivity in rat brain sections?
Autore:
Holopainen, IE; Kivela, R; Korpi, ER;
Indirizzi:
Univ Turku, Dept Pharmacol & Clin Pharmacol, FIN-20520 Turku, Finland UnivTurku Turku Finland FIN-20520 n Pharmacol, FIN-20520 Turku, Finland Turku Univ Hosp, Dept Pediat Neurol, FIN-20520 Turku, Finland Turku Univ Hosp Turku Finland FIN-20520 Neurol, FIN-20520 Turku, Finland
Titolo Testata:
NEUROCHEMICAL RESEARCH
fascicolo: 1, volume: 26, anno: 2001,
pagine: 89 - 94
SICI:
0364-3190(200101)26:1<89:DAPCAL>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
SUBUNIT MESSENGER-RNAS; A RECEPTOR; BINDING; ACID; PHARMACOLOGY; DRUGS; BUTYLBICYCLOPHOSPHOROTHIONATE; ANTAGONISTS; MODULATION; SITE;
Keywords:
GABA(A) receptor; carbamazepine; phenytoin; loreclezole; [S-35]TBPS binding; autoradiography;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Holopainen, IE Univ Turku, Dept Pharmacol & Clin Pharmacol, Kiinamyllynkatu 10, FIN-20520Turku, Finland Univ Turku Kiinamyllynkatu 10 Turku Finland FIN-20520 land
Citazione:
I.E. Holopainen et al., "Do antiepileptics phenytoin, carbamazepine, and loreclezole show GABA(A) receptor subtype selectivity in rat brain sections?", NEUROCHEM R, 26(1), 2001, pp. 89-94

Abstract

[S-35]t-Butylbicyclophosphorothionate ([S-35]TBPS), a convulsant site ligand of GABA(A) receptors, was used in autoradiography with rat brain sections to test suggested receptor subtype-selective actions of antiepileptics phenytoin, carbamazepine and loreclezole on native GABA(A) receptors. At maximal 100 muM concentration, both phenytoin and carbamazepine decreased [S-35]TBPS binding only by 10%, indicating that their low potency and efficacy prevents their use as al subunit-identifying compounds. Ten muM loreclezole did not affect the binding, but a further increase in loreclezole concentration strongly decreased it. The action of loreclezole, assumed to reflect beta2/3 subunit-containing receptors:, varied from brain region to region, but the effects were unrelated to the regional expression profiles of beta subunit variants. We conclude that in autoradiographic [S-35]TBPS binding assay neither carbamazepine, phenytoin nor loreclezole are useful tools in characterizing brain regional heterogeneity of GABA(A) receptors in rats and that only loreclezole exhibits high, pharmacologically relevant efficacy.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 10:22:09