184653-84-7

中文名称 CARABERSAT

英文名称 Carabersat

CAS 184653-84-7

分子式 C20H20FNO4

分子量 357.38

MOL 文件 184653-84-7.mol

184653-84-7 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

卡拉博沙

英文别名

Carabersat
Benzamide, N-[(3R,4S)-6-acetyl-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl]-4-fluoro-

物理化学性质

沸点559.3±50.0 °C(Predicted)

密度1.31±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度溶于二甲基亚砜

酸度系数(pKa)13.05±0.60(Predicted)

形态Solid

颜色White to off-white

常见问题列表

生物活性

Carabersat 是一种有效的抗惊厥剂。

体外研究

[ 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.

体内研究

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