Flindokalner_product_DataBase

Bioactivity

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].

Target

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

Invitro

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:

Name

Flindokalner

CAS

187523-35-9

Formula

C16H10ClF4NO2

Molar Mass

359.70

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Flindokalner

CAS: 187523-35-9 F: C16H10ClF4NO2 W: 359.70