XE-991

A detailed overview of XE-991, a potassium channel blocker

XE-991 is a chemical compound known for its role as a selective blocker of the M-type potassium channels. These channels are crucial in regulating the excitability of neurons and other excitable cells. XE-991 is often used in research to study the physiological and pathological roles of these channels.

Chemical Properties

XE-991 is a derivative of the compound linopirdine. It is chemically classified as a 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone. The molecular formula of XE-991 is C23H17N3O, and it has a molecular weight of 351.4 g/mol.

Mechanism of Action

XE-991 acts by selectively inhibiting the M-type potassium channels, which are composed of KCNQ2 and KCNQ3 subunits. These channels are responsible for the M-current, a non-inactivating potassium current that stabilizes the resting membrane potential and controls neuronal excitability. By blocking these channels, XE-991 increases neuronal excitability, which can be useful in studying the role of M-currents in various physiological and pathological processes.

Pharmacological Effects

The blockade of M-type potassium channels by XE-991 has several effects:

• Increased Neuronal Excitability: By inhibiting the M-current, XE-991 can lead to increased firing of neurons, which is useful in studying conditions like epilepsy and other hyperexcitability disorders.
• Cognitive Enhancement: Some studies suggest that XE-991 may enhance cognitive function by modulating neuronal excitability and synaptic plasticity.
• Potential Therapeutic Uses: While primarily a research tool, the modulation of M-currents by XE-991 has potential implications in treating neurological disorders such as epilepsy, Alzheimer's disease, and schizophrenia.

Research Applications

XE-991 is widely used in neuroscience research to:

• Study the role of M-type potassium channels in neuronal excitability and synaptic transmission.
• Investigate the pathophysiology of neurological disorders associated with altered M-current activity.
• Explore potential therapeutic targets for drugs aimed at modulating neuronal excitability.

Safety and Toxicity

As with many research chemicals, the safety and toxicity profile of XE-991 is not fully characterized. It is primarily used in vitro and in animal models, and researchers should handle it with appropriate safety precautions.

Also see

• M-type potassium channel
• KCNQ2
• KCNQ3
• Neuronal excitability
• Potassium channel blockers