QF0301B  

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包装规格:1mg 5mg in glass bottle
产品描述:基本信息 产品编号: Q10039  产品名称: QF0301B CAS: 149247-12-1   储存条件 粉末 -20℃ 四年 分子式: C23H28N2O2 溶于液体 -80℃ 二年 分子量: 364.48     化学名:  2-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-3,4-dihydro-2H-naphthalen-1-one Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   生物活性 产品描述 是α1肾上腺素能受体 (α1 adrenergic receptor) 拮抗剂,也可阻断α2肾上腺素受体,5-HT2A和组胺H1受体。 靶点 Adrenergic receptor   体外研究 In isolated rubbed rat aorta rings,QF0301B shows marked α1-adrenoceptor blocking activity,with a pA2 value of 9.00±0.12.QF0301B reverses and competitively antagonizes the inhibitory action produced by clonidine in electrically stimulated rat vas deferens and inhibits the force and rate of contraction in rat isolated atria (pA2=5.91±0.43),competitively antagonizes the contractile effect of 5-HT in rat aorta (pA2=6.75±0.06) and in rat stomach fundus (pA2=7.13±0.48) and the contractions induced by histamine in isolated guinea pig longitudinal ileal muscle (pA2=7.40±0.40). QF0301B shows noncompetitive low action in 5-HT3,muscarinic and nicotinic receptors,or as Ca2+ antagonist. 体内研究 QF0301B (0.1-0.2mg/kg iv) can cause a pronounced and prolonged fall in mean arterial blood pressure accompanied by bradycardia.QF0301B does not significantly modify the cardiovascular effects of either 5-hydroxytryptamine (serotonin,5-HT,75mg/kg iv) or the selective a2-adrenoceptor agonist B-HT 920 (0.2mg/kg iv),but markedly inhibits the hypertensive effect of noradrenaline (5mg/kg iv),a nonselective a-adrenergic receptor agonist.   推荐实验方法(仅供参考) 动物实验:   Rats:Normotensive rats are anaesthetized.When blood pressure and heart rate have stabilized (30 min after cannulation),vehicle (1ml/kg),QF0301B,or prazosin solution (0.1-0.2mg/kg) is injected intravenously via the femoral vein, and the effects on blood pressure and heart rate are observed.
保存条件:-20℃