Related Experiment Video
Updated: Sep 30, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
N-Arylated pyrrolidin-2-ones and morpholin-3-ones as potassium channel openers
Pi-Hui Liang1, Ling-Wei Hsin, Chen-Yu Cheng
1Institute of Pharmaceutical Sciences, College of Medicine, National Taiwan University, Taipei, Taiwan.
Abstract:
Based on the most stable conformation of ZD6169, a series of N-arylated derivatives of oxazolidindione (2), morpholin-3-one (3-5), piperidin-2-one (6), and pyrrolidin-2-one (7-13) was synthesized and evaluated for potassium channel opening activity. In the in-vitro assays, N-(4-benzoylphenyl)-piperidin-2-on (6) and N-(4-benzoylphenyl)-3,3-dimethyl-pyrrolidin-2-one (9) demonstrated potent and selective relaxant activity at the bladder detrusor muscle [IC50, bladder)=7.4 and 6.7 microM, respectively; IC50 ratio (portal vein/bladder)=41 and 51, respectively].
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Non-gated Ion Channels
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
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Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.

