Overview
- Peretz, A. et al. (2005) Mol. Pharmacol. 67, 1053.
Alomone Labs Meclofenamic acid enhances KCNQ2/KCNQ3 heteromeric channels expressed in Xenopus oocytes.A. Time course of KCNQ2/KCNQ3 current enhancement by 250 µM Meclofenamic acid (#M-210). Currents were elicited by application of voltage step from a holding potential of -100 mV to -60 mV (700 msec). B. Superimposed example traces of current responses before and during perfusion of 250 µM Meclofenamic acid, as indicated.
Meclofenamic acid (meclofenamate) acts as a KCNQ2/Q3 channel opener by causing a hyperpolarizing shift of the voltage activation curve and by slowing down the deactivation kinetics leading to membrane hyperpolarization1. Its EC50 value is reported to be 25 μM1. KCNQ2 (Kv7.2) and KCNQ3 (Kv7.3) are voltage-gated K+ channel subunits that underlie the neuronal M current (IM), a noninactivating, slowly deactivating subthreshold K+ current that opposes depolarizing current and act to stabilize membrane potential and control neuronal excitability3.
It belongs to the non-steroidal anti-inflammatory (NSAIDs) class of drugs. Meclofenamate also plays a role as a nonselective inhibitor of COX-1 and COX-2 (cyclooxygenases) that produces prostaglandins, chemicals that are responsible for pain, fever, and inflammation1.
Meclofenamate has the ability to reduce evoked and spontaneous neuronal action potentials and enhance M-current in rat cortical neurons1. It has been suggested that meclofenamate could be a useful drug for investigating functional properties and roles of gap junction coupling and electrical synapses2.
