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Identification of Benzopyran‐4‐one Derivatives (Isoflavones) as Positive Modulators of GABA A Receptors
Author(s) -
Gavande Navnath,
Karim Nasiara,
Johnston Graham A. R.,
Hanrahan Jane R.,
Chebib Mary
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100120
Subject(s) - isoflavones , gabaa receptor , receptor , xenopus , pharmacology , flumazenil , chemistry , gabaa rho receptor , ion channel , biology , biochemistry , gene
Isoflavones do it too! Enhancement of chloride ion flux at GABA A receptors by positive modulators is an important therapeutic strategy for the treatment of central nervous system (CNS)‐related disorders. Benzopyran‐4‐one derivatives (isoflavones), identified by systematic structure‐driven design, exhibit potent flumazenil‐insensitive positive modulation at human recombinant α 1 β 2 γ 2L receptors expressed in Xenopus oocytes.