Retigabine. A Potent and Selective Modulator of KV7 (KCNQ) Channels
The KCNQ family of voltage-gated K+ channels includes 5 known members: KCNQ1 to KCNQ5. Structurally, the KCNQ family belongs to the six transmembrane domain category of K+ channels. KCNQ family members can form either homomultimeric or heteromultimeric channels with different functional consequences. For example KCNQ2 and KCNQ3 heteromultimers give rise to a much larger channel current than when either protein is expressed alone. Indeed, KCNQ2/KCNQ3 heteromultimers are believed to be the molecular correlates of the so-called M current. This current is a K+ neuronal current that is strongly inhibited by the activation of the M1 subtype of the muscarinic acetylcholine receptor. Mutations in either KCNQ2 or KCNQ3 are associated with a form of epilepsy known as benign familial�neonatal convulsions (BNFC).
Retigabine is a potent and selective KV7 (KCNQ, M-) channel modulator (enhancer), which is used in the clinic to treat epilepsy. Retigabine (0.1 to 10 μM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.4. Similar effects were seen with 10 μM retigabine in oocytes expressing the KV7.2/3 heteromeric channel.
Alomone Labs is pleased to offer Retigabine (#R-100).
Ion Channel Modulators; K+ Channel Openers
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