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Updated: Jun 24, 2026
11:33
Isolation and Kv Channel Recordings in Murine Atrial and Ventricular Cardiomyocytes
Published on: March 12, 2013
Neural KCNQ (Kv7) channels
David A Brown1, Gayle M Passmore
1Department of Pharmacology, University College London, London, UK. d.a.brown@ucl.ac.uk
British Journal of Pharmacology
|March 21, 2009
Summary
Kv7 potassium channels (Kv7.2-Kv7.5) regulate neuronal excitability. Drugs targeting these channels, like flupirtine and retigabine, reduce excitability and show therapeutic potential for pain and seizures.
Area of Science:
- Neuroscience
- Molecular Biology
- Pharmacology
Background:
- KCNQ genes encode Kv7 potassium channel subunits, with Kv7.2-Kv7.5 expressed in the nervous system.
- Kv7.2 and Kv7.3 subunits form the M-channel, crucial for regulating neuronal excitability.
- M-channels are inhibited by muscarinic receptors via phospholipase C, impacting neuronal firing patterns.
Purpose of the Study:
- To elucidate the role of Kv7/M-channels in neuronal excitability.
- To investigate the physiological consequences of M-channel modulation in various neuronal systems.
- To explore the therapeutic potential of Kv7 channel modulators in pain and neurological disorders.
Main Methods:
- Analysis of KCNQ gene function and Kv7 subunit expression.
- Electrophysiological studies on neuronal excitability.
- Pharmacological manipulation using M-channel blockers (linopirdine, XE991) and activators (flupirtine, retigabine).
- Investigation of KCNQ2 gene disruption effects.
Main Results:
- M-channel closure by muscarinic receptors increases neuronal excitability in sympathetic, sensory, and hippocampal neurons.
- M-channel blockade facilitates repetitive firing, enhances after-depolarizations, and induces spontaneous firing.
- Kv7 channel activators like flupirtine and retigabine reduce neuronal excitability by shifting voltage gating.
- Flupirtine acts as a central analgesic, while retigabine shows promise as an anticonvulsant and analgesic.
Conclusions:
- Kv7/M-channels are critical regulators of neuronal excitability, with implications for cholinergic signaling and neuronal function.
- Modulation of Kv7 channels offers a promising therapeutic strategy for conditions involving neuronal hyperexcitability, such as pain and epilepsy.
- Kv7 channel activators demonstrate significant potential for treating chronic pain and seizure disorders.
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07:31Profiling Voltage-gated Potassium Channel mRNA Expression in Nigral Neurons using Single-cell RT-PCR Techniques
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