A positive-gating modulator of IKCa1/KCa3.1 channels
Kinase experiment: | To fully evaluate the selectivity of the naphthooxazole SKA-121, seven-point concentration-response curves on KCa2.1, KCa2.2, KCa2.3 and KCa3.1 are determined with 250 nM free Ca2+ in the internal solution[1]. |
Animal experiment: | Mice[1] Twelve-week-old male C57Bl/6J mice are used. For i.v. application, SKA-121 is dissolved at 5 mg/mL in a mixture of 10% CremophorEL and 90% phosphate-buffered saline and then injected at 10? mg/kg into the tail vein (n=8 mice per compound). Another group of mice (n=8) receive SKA-121 orally. At various time points after the injection, blood is collected into EDTA blood sample collection tubes either from the saphenous vein or by cardiac puncture under deep isoflurane anesthesia. After the cardiac puncture, mice are sacrificed by cutting the heart, and then the brain is removed. Individual mice are typically used for three times points (two blood collections from the saphenous vein plus the terminal blood collection). |
参考文献: [1]. Coleman N, et al. New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol Pharmacol. 2014 Sep;86(3):342-57. | |
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