Retigabine

CAS No.	150812-12-7	Cat. No.	BCP04194
Name	Retigabine
Synonyms	Retigabin;D-23129;D 23129;D23129; GKE 841; GKE-841; GKE841; GW 582892X; WAY 143841; WAY-143841; WAY143841; Ezogabine;
Formula	C16H18FN3O2	M. Wt	303.33

Description	The compound was shown to activate a K+ current in neuronal cells. The pharmacology of the induced current displays concordance with the published pharmacology of the M-channel, which recently was correlated to the KCNQ2/3 K+ channel heteromultimere. Retigabine is a novel anticonvulsant with an unknown mechanism of action. Application of 10 μM retigabine to oocytes expressing the KCNQ2/3 heteromeric channel shifted both the activation threshold and voltage for half-activation by approximately 20 mV in the hyperpolarizing direction, leading to an increase in current amplitude at test potentials between ?80 mV and +20 mV. Retigabine also had a marked effect on KCNQ current kinetics, increasing the rate of channel activation but slowing deactivation at a given test potential. Retigabine shifted the voltage dependence of channel activation with an EC50value of 1.6 ± 0.3 μM (slope factor was 1.2 ± 0.1,n = 4 to 5 cells per concentration). Retigabine (0.1 to 10 μM) also slowed the rate of cha
Pathways	Ion Channel/Membrane Transporter
Targets	Potassium Channel

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