Overview
- Kikuchi, K. et al. (2005) Br. J. Pharmacol. 144, 840.
Alomone Labs Miconazole nitrate Blocks KV11.1 channels expressed in Xenopus oocytes.A. Time course of KV11.1 current inhibition by 10 and 50 µM Miconazole nitrate (#M-206). Currents were elicited by two 200 ms steps: to +40 mV and then to -40 mV (HP -100mV, every 10s, demonstrated above current traces in B). B. Superimposed example traces of current responses before and during perfusion of 10 and 50 µM Miconazole nitrate, as indicated.
- Grizel, A.V. et al. (2014) Acta. Naturae. 6, 10.
- Kikuchi, K. et al. (2005) Br. J. Pharmacol. 144, 840.
KV channels are voltage-gated potassium ion channels. These channels play a significant role in various cellular processes including the release of neurotransmitters, maintenance of cardiac activity, regulation of apoptosis and cell growth1.
Miconazole is a synthetic antifungal derivative of imidazole. It is a blocker of KV11.1 (hERG), KV1.3 and KV1.5 channels and has an effective concentration of 1-100 μM and an IC50 2.1 μM for the hERG channel in HEK 293 cells. Miconazole inhibits hERG peak tail current in a concentration dependent manner (0.4-40 μM) without being frequency dependent and without affecting other channel kinetics. Blocking hERG channel by Miconazole requires channel activation.
Miconazole is used primarily for the topical treatment of candida skin infections but can also be administered vaginally or orally. It selectively affects the integrity of fungal cell membranes because of their high content of ergosterol thus differentiating them from mammalian cell membrane. Miconazole increases the risk of cardiac arrhythmia via the inhibition of various cytochrome P-450 enzymes in the liver and GI tract causing a rise in plasma of QT interval prolonging drugs and also via direct inhibition of the hERG channel2.
Miconazole nitrate (#M-206) is a highly pure, synthetic, and biologically active compound.
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