激活Ca 2+激活的K +通道;Activates Ca 2+ -activated K + channels;NS309是钙离子激活的钾离子通道(KCa2和KCa3.1)的阳性调节剂,能增强钙离子的敏感性,对BK通道无活性。;NS309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels); increases Ca2+ sensitivity. Displays no activity at BK channels.A Ca2+-activated IK/SK potassium channel activator
1. Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current I(AHP) and modulates the firing properties of hippocampal pyramidal neurons. 2. C Hougaard, et al. Selective positive modulation of the SK3 and SK2 subtypes of small conductance Ca2+-activated K+ channels. Br J Pharmacol. 2007 Jul; 151(5): 655–665. 3. Nichole Coleman, et al. New Positive Ca2+-Activated K+ Channel Gating Modulators with Selectivity for KCa3.1. Mol Pharmacol. 2014 Sep; 86(3): 342–357. 4. Dorte Strøbaek, et al. Activation of human IK and SK Ca2+-activated K+ channels by NS309 (6,7-dichloro-1H-indole-2,3-dione 3-oxime). Biochim Biophys Acta. 2004 Oct 11;1665(1-2):1-5. 5. Shankar P Parajuli, et al. NS309 decreases rat detrusor smooth muscle membrane potential and phasic contractions by activating SK3 channels. Br J Pharmacol. 2013 Apr; 168(7): 1611–1625. 6. Jie Zhu, et al. Activation of SK/KCa Channel Attenuates Spinal Cord Ischemia-Reperfusion Injury via Anti-oxidative Activity and Inhibition of Mitochondrial Dysfunction in Rabbits. Front Pharmacol. 2019; 10: 325.