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

Sep 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.

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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: dx.doi.org/10.1002/cmdc.201100351

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