PK-THPP

Based on 20 reference(s) in Google Scholar 80 100 20

Axon 2403

CAS [1332454-07-5]

MF C29H32N4O2
MW 468.59

Purity: 99%
Soluble in DMSO

PK-THPP

Description

Potent TASK-3 (KCNK9) antagonist (IC50 value 303 nM and 35nM for TASK-1 and TASK-3, respectively) with >140 fold selectivity over a wider range of potassium channels. PK-THPP produced a significant increase in active wake with a concurrent decrease in both REM and delta sleep immediately following administration to wild-type (WT) mice, and stimulated breathing by increasing tidal volume and breathing rate in isoflurane-anesthetized rats. PK-THPP induced a respiratory alkalosis and increased oxygenation.

D.P. Flaherty et al. Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3968-73.

C.A. Coburn et al. Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3). ChemMedChem. 2012 Jan 2;7(1):123-33.

J.F. Cotten. TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats. Anesth Analg. 2013 Apr;116(4):810-6.

Potent TASK-3 antagonist with selectivity over a wide range of potassium channels

Chemical name

1-(1-(6-(Biphenylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)piperidin-4-yl)butan-1-one

Parent CAS No.

[1332454-07-5]

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PK-THPP

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