http://www.cnr.it/ontology/cnr/individuo/prodotto/ID282082

Differential modulation of GABA(A) receptor function by aryl pyrazoles (Articolo in rivista)

Type

Articolo in rivista (Classe)
Prodotto della ricerca (Classe)

Label

Differential modulation of GABA(A) receptor function by aryl pyrazoles (Articolo in rivista) (literal)

Anno

2014-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

10.1016/j.ejphar.2014.03.039 (literal)

Alternative label

Mascia, Maria Paola; Ledda, Giovanni; Orru, Alessandro; Marongiu, Alessandro; Loriga, Giovanni; Maciocco, Elisabetta; Biggio, Giovanni; Ruiu, Stefania (2014)
Differential modulation of GABA(A) receptor function by aryl pyrazoles
in European journal of pharmacology
(literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

Mascia, Maria Paola; Ledda, Giovanni; Orru, Alessandro; Marongiu, Alessandro; Loriga, Giovanni; Maciocco, Elisabetta; Biggio, Giovanni; Ruiu, Stefania (literal)

Pagina inizio

1 (literal)

Pagina fine

6 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

733 (literal)

Rivista

European journal of pharmacology (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali

6 (literal)

Note

ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

Consiglio Nazionale delle Ricerche (CNR); Consiglio Nazionale delle Ricerche (CNR); University of Cagliari (literal)

Titolo

Differential modulation of GABA(A) receptor function by aryl pyrazoles (literal)

Abstract

Several aryl pyrazoles characterized by a different molecular structure (flexible vs constrained), but chemically related to rimonabant and AM251, were tested for their ability to modulate the function of recombinant alpha(1)beta(2)gamma(2L) GABA(A) receptors expressed in Xenopus laevis oocytes. The effects of 14Bio-R, NESS 0327, GP1a and GP2a (0.3-30 mu M) were evaluated using a two-electrode voltage-clamp technique. GBio-R and 14Bio-R potentiated GABA-evoked Cl- currents. NESS 0327, GP1a and GP2a did not affect the GABA(A) receptor function, but they acted as antagonists of GBio-R. Moreover, NESS 0327 inhibited the potentiation of the GABA(A) receptor function induced by rimonabant. The benzodiazepine site seems to participate in the action of these compounds. In fact, flumazenil antagonized the potentiation of the GABA(A) receptor induced by 6Bio-R, and NESS 0327 reduced the action of lorazepam and zolpidem. On the contrary, NESS 0327 did not antagonize the action of \"classic\" GABAergic modulators (propanol, anesthetics, barbiturates or steroids). In alpha(1)beta(2) receptors 6Bio-R potentiated the GABAergic function, but flumazenil was still able to antagonize the potentiation induced by 6Bio-R. Aryl pyrazole derivatives activity at the GABA(A) receptor depends on their molecular structure. These compounds bind to both an alpha beta gamma binding site, and to an (alpha/beta site which do not require the gamma subunit and that may provide structural leads for drugs with potential anticonvulsant effects. (C) 2014 Elsevier B.V. All rights reserved. (literal)

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