187523-35-9
187523-35-9 結(jié)構(gòu)式
基本信息
FLINDOKALNER
BMS-204352 (BMS 204352
(3S)-3-(5-chloro-2-methoxy-phenyl)-3-fluoro-6-(trifluoromethyl)-1H-ind ol-2-one
(3S)-3-(5-Chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-2H-Indol-2-one
2H-Indol-2-one, 3-(5-chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-, (3S)-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
Ki: 3.7 μM (Kv7.1), 230 μM (Kv7.4), 605 μM (Kv7.5)
Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with K
i
s of 230 and 605 μM, respectively.
Flindokalner (1-10 μM) causes inhibition of the Ca
2+
current in a dose-dependent manner, with a Kd of 6 μM and a Hill coefficient of 1.33. Flindokalnerinhibits cardiac L-type Ca
2+
channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes.
Flindokalner (BMS-204352) (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect.
In shock-based conditioned model of anxiety in male Wistar rats, Flindokalner (3-60 mg/kg; i.p.) engenderes an anxiolytic profile.
| Animal Model: | Female NMRI or male C57 mice (20-25 g) (Anxiolytic Models) |
| Dosage: | i.p. |
| Administration: | 3, 10, 30 mg/kg |
| Result: | Significantly and dose dependently increased time spent in the open areas, reduced latency to enter an open area, and increased the number of entries in to the open areas in Zero Maze. |