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)

Alternative label

• Mascia MP, Ledda G, Orrù A, Marongiu A, Loriga G, Maciocco E, Biggio G, Ruiu S (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 MP, Ledda G, Orrù A, Marongiu A, Loriga G, Maciocco E, Biggio G, Ruiu S (literal)

Pagina inizio

• 1 (literal)

Pagina fine

• 6 (literal)

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• 733 (literal)

Rivista

• European journal of pharmacology (Rivista)

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

• Istituto di Neuroscienze, Istituto di Farmacologia Translazionale, Università degli Studi di 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 ?1?2?2L GABAA receptors expressed in Xenopus laevis oocytes. The effects of 6Bio-R, 14Bio-R, NESS 0327, GP1a and GP2a (0.3-30 ?M) were evaluated using a two-electrode voltage-clamp technique. 6Bio-R and 14Bio-R potentiated GABA-evoked Cl(-) currents. NESS 0327, GP1a and GP2a did not affect the GABAA receptor function, but they acted as antagonists of 6Bio-R. Moreover, NESS 0327 inhibited the potentiation of the GABAA 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 GABAA 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 ?1?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 GABAA receptor depends on their molecular structure. These compounds bind to both an ??? binding site, and to an ?/? site which do not require the ? subunit and that may provide structural leads for drugs with potential anticonvulsant effects. (literal)

Prodotto di

• Istituto di neuroscienze (IN) (Istituto)
• Neurobiologia delle dipendenze (ME.P02.009.001) (Modulo)
• Drug design, drug delivery e valutazione preclinica di nuove entità chimiche (ME.P06.032.001) (Modulo)

Autore CNR

• GIOVANNI BIGGIO (Unità di personale esterno)
• GIOVANNI LORIGA (Unità di personale interno)
• ELISABETTA MACIOCCO (Unità di personale interno)
• MARIA PAOLA MASCIA (Persona)
• STEFANIA RUIU (Unità di personale interno)

Incoming links:

Autore CNR di

• MARIA PAOLA MASCIA (Persona)
• STEFANIA RUIU (Unità di personale interno)
• ELISABETTA MACIOCCO (Unità di personale interno)
• GIOVANNI BIGGIO (Unità di personale esterno)
• GIOVANNI LORIGA (Unità di personale interno)

Prodotto

• Istituto di neuroscienze (IN) (Istituto)
• Drug design, drug delivery e valutazione preclinica di nuove entità chimiche (ME.P06.032.001) (Modulo)
• Neurobiologia delle dipendenze (ME.P02.009.001) (Modulo)

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

• European journal of pharmacology (Rivista)