184653-84-7
184653-84-7 結(jié)構(gòu)式
基本信息
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(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
[ 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.
Carabersat (5b) significantly elevates anticonvulsant activity in mice.