ADC细胞毒素;ADC Cytotoxin;;InformationTalatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.TargetsIK channel 146 μMIn vitroTalatisamine is a specific blocker for IK channel. External application of talatisamine reversibly inhibited the delayed rectifier K+ current (IK) with an IC50 value of 146.0±5.8 μM in a voltage-dependent manner, but exhibited very slight blocking effect on the voltage-gated Na+ and Ca2+ currents even at the high concentration of 1-3 mM in rat hippocampal neurons. Talatisamine had no allosteric action on IK channel and was a pure blocker binding to the external pore entry of the channel.
参考文献:
1. Wang Y, et al. The newly identified K+ channel blocker talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons. Neurosci Lett. 2012 Jun 19;518(2):122-7.