Blocking the channel: A pharmacologically active antagonist of the two-pore-domain potassium ion channel K2P9.1 (TASK-3)

September 27, 2011
Blocking the channel: A pharmacologically active antagonist of the two-pore-domain potassium ion channel K2P9.1 (TASK-3)

Treatment of neurological conditions such as sleep–wake control, cognition, and depression could be possible by modulation of the TWIK-related acid-sensitive K+ ion channel (TASK-3, or K2P9.1).

A collaborative effort involving scientists at Merck Research Laboratories (USA) and WuXi AppTec (Shanghai, China) led by Craig A. Coburn has identified a new class of potent small-molecule TASK-3 channel blockers through hypothesis-driven screening and a medicinal chemistry lead optimization program, and their results are reported in ChemMedChem.

The team profiled one compound in detail and demonstrated central nervous system (CNS) target engagement in rodent electroencephalogram (EEG) telemetry models where compound-induced modulation of quantitative EEG power and architecture appeared absent in knock-out animals that lack this channel subunit. This promising lead compound could prove valuable for further exploration in the challenging field of modulators.

Explore further: Smoking linked to sleep disturbances

More information: Craig A. Coburn, Discovery of a Pharmacologically Active Antagonist of the Two-Pore-Domain Potassium Channel K2P9.1 (TASK-3), ChemMedChem 2012, 7, No. 1, Permalink to the article:

Related Stories

Smoking linked to sleep disturbances

February 4, 2008

New research shows that cigarette smokers are four times as likely as nonsmokers to report feeling unrested after a night’s sleep. The study, appearing in the February issue of CHEST, the peer-reviewed journal of the American ...

Drug prevents seizure progression in model of epilepsy

May 4, 2009

Carnegie Mellon University researchers have identified a new anticonvulsant compound that has the potential to stop the development of epilepsy. The findings are published in the March issue of the journal Epilepsia.

Scorpion has welcome sting for heart bypass patients

October 22, 2010

A toxin found in the venom of the Central American bark scorpion (Centruroides margaritatus) could hold the key to reducing heart bypass failures, according to research from the University of Leeds.

Recommended for you

Scientists create revolutionary material to clean oil spills

November 30, 2015

Deakin University scientists have manufactured a revolutionary material that can clean up oil spills, which could save the earth from potential future disasters such as any repeat of the 2010 Gulf Coast BP disaster that wreaked ...

A new form of real gold, almost as light as air

November 25, 2015

Researchers at ETH Zurich have created a new type of foam made of real gold. It is the lightest form ever produced of the precious metal: a thousand times lighter than its conventional form and yet it is nearly impossible ...


Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.