1332454-07-5

PK-THPP is a potent TWIK-related acid-sensitive K(+) ion channel (TASK-3 ion channel) blocker (IC50s are 35 nM and 300 nM for TASK-3 and TASK-1, respectively)[1]. PK-THPP increases breathing rate and induces respiratory alkalosis in rats[2].

PK-THPP is a potent antagonist of tandem pore potassium channel subunit TASK-3 (KCNK9, K2P9.1) with an IC50 value of 35 nM for TASK-3 compared to 303 nM for TASK-1 and with >140 fold selectivity over a wider range of potassium channels. PK-THPP was found to act as a respiratory stimulant, stimulating breathing in isoflurane-anesthetized rats.

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[1] Coburn CA,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. DOI:10.1002/cmdc.201100351
[2] Cotten JF. 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. DOI:10.1213/ANE.0b013e318284469d