An activator of Kv7 channels
Flupirtine is an activator of voltage-gated potassium channel 7 (Kv7/KCNQ).1,2,3 It induces relaxation of preconstricted pulmonary arteries isolated from wild-type and serotonin transporter-overexpressing (SERT+) mice.2 Flupirtine (30 mg/kg per day) decreases mean right ventricular pressure and right ventricular hypertrophy in hypoxia-induced and SERT+ mouse models of pulmonary arterial hypertension. It increases the paw withdrawal threshold in a rat model of streptozotocin-induced diabetic neuropathy when administered at a dose of 10 mg/kg and increases paw withdrawal latency in a rat model of carrageenan-induced paw inflammation when used in combination with morphine.3 Flupirtine also indirectly antagonizes NMDA receptors via its effects on potassium channels.1,4
1.Devulder, J.Flupirtine in pain management: Pharmacological properties and clinical useCNS Drugs25(10)867-881(2010) 2.Morecroft, I., Murray, A., Nilsen, M., et al.Treatment with the Kv7 potassium channel activator flupirtine is beneficial in two independent mouse models of pulmonary hypertensionBr. J. Pharmacol.157(7)1241-1249(2009) 3.Goodchild, C.S., Kolosov, A., Tucker, A.P., et al.Combination therapy with flupirtine and opioid: Studies in rat pain modelsPain Med.9(7)928-938(2008) 4.Kornhuber, J., Bleich, S., Wiltfang, J., et al.Flupirtine shows functional NMDA receptor antagonism by enhancing Mg2+ block via activation of voltage independent potassium channelsJ. Neural Transm. (Vienna)106(9-10)857-867(1999)
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