Coburn, Craig A. published the artcileDiscovery of a Pharmacologically Active Antagonist of the Two-Pore-Domain Potassium Channel K2P9.1 (TASK-3), Application In Synthesis of 20029-52-1, the publication is ChemMedChem (2012), 7(1), 123-133, database is CAplus and MEDLINE.
TWIK-related acid-sensitive K+ (K2P9.1, TASK-3) ion channels have the capacity to regulate the activity of neuronal pathways by influencing the resting membrane potential of neurons on which they are expressed. The central nervous system (CNS) expression of these channels suggests potential roles in neurol. disorders, and it is believed that the development of TASK-3 antagonists could lead to the therapeutic treatment of a number of neurol. conditions. While a therapeutic potential for TASK-3 channel modulation exists, there are only a few documented examples of potent and selective small-mol. channel blockers. Herein is described the discovery and lead optimization efforts for a novel series of TASK-3 channel antagonists based on a 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine high-throughput screening lead from which a subseries of potent and selective inhibitors were identified. One compound, I, was profiled in detail with respect to its phys. properties and demonstrated pharmacol. target engagement as indicated by its ability to modulate sleep architecture in rodent EEG telemetry models.
ChemMedChem published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, Application In Synthesis of 20029-52-1.
Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider