Pharmacological characterization of some selected 4,5-dihydro-4-oxo-1,2,4-triazolo〔1,5-a〕quinoxaline-2-carboxylates and 3-hydroxyquinazoline-2,4-diones as (S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-propionic acid receptor antagonists

DOI Web Site Web Site 被引用文献1件 参考文献41件
  • Catarzi Daniela
    Dipartimento di Scienze Farmaceutiche, Universita' degli Studi di Firenze, Polo Scientifico
  • Lenzi Ombretta
    Dipartimento di Scienze Farmaceutiche, Universita' degli Studi di Firenze, Polo Scientifico
  • Colotta Vittoria
    Dipartimento di Scienze Farmaceutiche, Universita' degli Studi di Firenze, Polo Scientifico
  • Varano Flavia
    Dipartimento di Scienze Farmaceutiche, Universita' degli Studi di Firenze, Polo Scientifico
  • Poli Daniela
    Dipartimento di Scienze Farmaceutiche, Universita' degli Studi di Firenze, Polo Scientifico
  • Filacchioni Guido
    Dipartimento di Scienze Farmaceutiche, Universita' degli Studi di Firenze, Polo Scientifico
  • Lingenhöhl Kurt
    Novartis Institutes for Biomedical Research, Neuroscience, Novartis Pharma A.G.
  • Ofner Silvio
    Novartis Institutes for Biomedical Research, Neuroscience, Novartis Pharma A.G.

書誌事項

タイトル別名
  • Pharmacological Characterization of Some Selected 4,5-Dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates and 3-Hydroxyquinazoline-2,4-diones as (S)-2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-propionic Acid Receptor Antagonists

この論文をさがす

抄録

In the present study, some selected, previously reported 4,5-dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates (TQXs) and 3-hydroxy-quinazoline-2,4-diones (QZs), were evaluated for their affinity at the (S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-propionic acid (AMPA) receptor in the [3H]-6-cyano-7-nitroquinoxaline-2,3-dione ([3H]-CNQX) binding assay. Electrophysiological experiments were performed in oocytes expressing rat homomeric GluR3 subunits in order to assess the pharmacological profile of the tested compounds. The binding data, together with those regarding the functional activity, confirmed that most of the TQXs and QZs reported herein are potent AMPA receptor antagonists. When tested for their ability to prevent sound-induced seizures in DBA/2 mice, some of these derivatives showed anticonvulsant properties.

収録刊行物

被引用文献 (1)*注記

もっと見る

参考文献 (41)*注記

もっと見る

キーワード

詳細情報 詳細情報について

問題の指摘

ページトップへ