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Merck
CN

Modulation of K

British journal of pharmacology (2017-05-14)
Harinath Sale, Samrat Roy, Jayakumar Warrier, Srinivasan Thangathirupathy, Yoganand Vadari, Shruthi K Gopal, Prasad Krishnamurthy, Manjunath Ramarao
摘要

Activators of K Conventional electrophysiological methods were used to assess the effects of ITP-2 on hERG1a and hERG1a/1b channels expressed heterologously in HEK-293 cells. ITP-2 selectively increased test pulse currents (EC ITP-2 may serve as another novel lead molecule for designing robust activators of hERG channels. hERG1a/1b gating kinetics were differentially modulated by ITP-2 leading to altered sensitivity. ITP-2 is capable of activating an LQT2 mutant and may be potentially useful in the development of LQT2 therapeutics.