Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies (Articolo in rivista)

Type
Label
  • Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies (Articolo in rivista) (literal)
Anno
  • 2008-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/jm8006728 (literal)
Alternative label
  • Nunzio Denora1; Valentino Laquintana1; Maria Giuseppina Pisu3; Riccardo Dore2; Luca Murru2; Andrea Latrofa1; Giuseppe Trapani1; Enrico Sanna2 (2008)
    Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies
    in Journal of medicinal chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Nunzio Denora1; Valentino Laquintana1; Maria Giuseppina Pisu3; Riccardo Dore2; Luca Murru2; Andrea Latrofa1; Giuseppe Trapani1; Enrico Sanna2 (literal)
Pagina inizio
  • 6876 (literal)
Pagina fine
  • 6888 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 51 (literal)
Rivista
Note
  • PubMe (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • 1Dipartimento Farmaco-Chimico, Facolta`di Farmacia, UniVersita` degli Studi di Bari, Bari, Italy 2Dipartimento di Biologia Sperimentale, Sezione di Neuroscienze, UniVersita` di Cagliari, Cittadella UniVersitaria Monserrato, Monserrato (Cagliari), Italy 3National Research Council (C.N.R.), Institute of Neuroscience, Cagliari, Italy (literal)
Titolo
  • Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies (literal)
Abstract
  • A series of imidazopyridine acetamides were synthesized to evaluate the effects of structural changes at both central (CBRs) and peripheral benzodiazepine receptors (PBRs). These changes include the introduction of polar substituents or ionizable functional groups at the 2- and 8-position of the imidazopyridine skeleton. The results suggest that substituents endowed with hydrogen bonding acceptor and/or donor properties in the para position of the phenyl ring lead to high affinity for PBR. In electrophysiological studies, it was found that compounds 9, 12, 13, and 28 markedly enhanced GABA-evoked Cl (-) currents in Xenopus oocytes expressing alpha 1beta 2gamma 2 GABA A receptors. The capability of flumazenil to reduce the stimulatory effect exerted by compound 9 supports the conclusion that the modulatory effects of the examined compounds occur involving the CBR. The ability of compound 16 to increase GABA A receptor-mediated miniature inhibitory postsynaptic currents in CA1 pyramidal neurons is indicative of its ability to stimulate the local synthesis and secretion of neurosteroids. (literal)
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