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腺苷A3受体拮抗剂(重组人受体的Ki=4.03nM);对腺苷A3受体的选择性是A1和A2A受体的2,500倍以上;100nM时可降低猪冠状动脉平滑肌细胞中腺苷诱导的ERK1/2磷酸化;100nM时可增加大鼠海马切片缺血模型中氧-葡萄糖剥夺引起的场EPSP幅度降低;2µg时可降低大鼠脑池内硝普钠引起的心率增加。An adenosine A3 receptor antagonist (Ki = 4.03 nM for the recombinant human receptor); >2,500-fold selective for adenosine A3 over A1 and A2A receptors; decreases adenosine-induced phosphorylation of ERK1/2 in isolated porcine coronary artery smooth muscle cells at 100 nM; increases oxygen-glucose deprivation-induced reductions in the amplitude of field EPSPs in a rat hippocampal slice model of ischemia at 100 nM; reduces sodium nitroprusside-induced heart rate increases in rats at 2 µg intracisternally.
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