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MaxiPost

Names

[ CAS No. ]:
187523-35-9

[ Name ]:
MaxiPost

[Synonym ]:
[14C]-Flindokalner
MaxiPost
(3S)-3-(5-Chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one
(3S)-(+)-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indol-2-one
(S)-(+)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-trifluoromethyl-1,3-dihydroindol-2-one
Flindokalner
Flindokalner [USAN:INN]
Maxipost (TN)

Biological Activity

[Description]:

Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

Ki: 3.7 μM (Kv7.1), 230 μM (Kv7.4), 605 μM (Kv7.5)[1]


[In Vitro]

Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with Kis of 230 and 605 μM, respectively[1]. Flindokalner (1-10 μM) causes inhibition of the Ca2+ current in a dose-dependent manner, with a Kd of 6 μM and a Hill coefficient of 1.33. Flindokalnerinhibits cardiac L-type Ca2+ channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes[2].

[In Vivo]

Flindokalner (BMS-204352) (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect[1]. In shock-based conditioned model of anxiety in male Wistar rats, Flindokalner (3-60 mg/kg; i.p.) engenderes an anxiolytic profile[1]. Animal Model: Female NMRI or male C57 mice (20-25 g) (Anxiolytic Models)[1] 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.

[References]

[1]. Korsgaard MP, et al. Anxiolytic effects of Maxipost (BMS-204352) and retigabine via activation of neuronal Kv7channels. J Pharmacol Exp Ther. 2005 Jul;314(1):282-92.

[2]. Son YK, et al. The inhibitory effect of Ca2+-activated K+ channel activator, BMS on L-type Ca2+ channels in rat ventricular myocytes. Life Sci. 2011 Aug 29;89(9-10):331-6.

Chemical & Physical Properties

[ Density]:
1.5g/cm3

[ Boiling Point ]:
436.9ºC at 760mmHg

[ Molecular Formula ]:
C16H10ClF4NO2

[ Molecular Weight ]:
359.70300

[ Flash Point ]:
218ºC

[ Exact Mass ]:
359.03400

[ PSA ]:
38.33000

[ LogP ]:
4.67060

[ Vapour Pressure ]:
7.82E-08mmHg at 25°C

[ Index of Refraction ]:
1.574

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P280-P304 + P340 + P312-P305 + P351 + P338-P337 + P313

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
NM3249000

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds