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184653-84-7

中文名稱 CARABERSAT
英文名稱 Carabersat
CAS 184653-84-7
分子式 C20H20FNO4
分子量 357.38
MOL 文件 184653-84-7.mol
184653-84-7 結構式 184653-84-7 結構式

基本信息

中文別名
卡拉博沙
英文別名
Carabersat
Benzamide, N-[(3R,4S)-6-acetyl-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl]-4-fluoro-

物理化學性質

沸點559.3±50.0 °C(Predicted)
密度1.31±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)13.05±0.60(Predicted)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
Carabersat 是一種有效的抗驚厥劑。
體外研究

[ 3 H]Carabersat ([ 3 H]SB 204269) binds to rat forebrain membranes with moderate affinity (K d 40 nM) and pK i values of 7.3. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a K d of 53 nM. The labelled [ 3 H]Carabersat produces a K d of 32 nM. Carabersat (SB-204269, 1-100 μM) has no effect on Na + current in cultured hippocampal neurones. Carabersat also shows no effect on action potential discharges evoked by elevating external K + . Carabersat (SB-204269) is structurally-related to the benzopyran ATP-sensitive potassium channel (KATP) opener, cromakalim, but has opposite stereochemistry, and the mechanism of action of Carabersat is not thought to involve KATP.

體內研究

Carabersat (5b) significantly elevates anticonvulsant activity in mice.

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