کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358206 | 981324 | 2016 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion](/preview/png/1358206.png)
A phytochemical investigation of the lipophilic extract of Hypericum lissophloeus (smoothbark St. John’s wort, Hypericaceae) was conducted, resulting in the isolation and identification of a new chromanone derivative: 5,7-dihydroxy-2,3-dimethyl-6-(3-methyl-but-2-enyl)-chroman-4-one (1). This compound was demonstrated to act as a potent stimulator of currents elicited by GABA in recombinant α1β2γ2 GABAA receptors, with a half-maximal potentiation observed at a concentration of about 4 μM and a maximal potentiation of >4000%. Significant potentiation was already evident at a concentration as low as 0.1 μM. Extent of potentiation strongly depends on the type of α subunit, the type of β subunit and the presence of the γ subunit.
Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 4, 15 February 2016, Pages 681–685