The Sound of Evolution
Retigabine
Mechanism of action:
Retigabine is a voltage-gated potassium channel opener. Retigabine acts directly on KCNQ2 and KCNQ3 potassium channels, which are responsible for generating the M-current, an important current that controls the neuronal resting potential and action potential threshold. Retigabine shifts the activation voltage of these potassium channels toward more hyperpolarized potentials, increasing potassium efflux, causing membrane hyperpolarization, and suppressing repetitive action potential firing.
Reference(s):
1. Porter RJ et al. (2007). Retigabine. Neurotherapeutics.
2. Hermann R et al. (2003). Effects of age and sex on the disposition of retigabine. Clin Pharmacol Ther.
3. Hermann R et al. (2003). Pharmacokinetic interaction between retigabine and lamotrigine in healthy subjects. Eur J Clin Pharmacol.