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Lusaperidone  ≥95%

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产品描述：基本信息 产品编号： L10414 产品名称： Lusaperidone CAS: 214548-46-6   储存条件 粉末 -20℃ 四年     分子式： C22H21N3O2 溶于液体 -80℃ 6个月 分子量： 359.42 -20℃ 1个月 化学名：  2-Methyl-3-[2-(1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine-2-yl)ethyl]-4H-pyrido[1,2-a]pyrimidine-4-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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.7823mL 13.9113mL 27.8226mL 5mM 0.5565mL 2.7823mL 5.5645mL   生物活性 产品描述 一种α2肾上腺素受体 (adrenergic receptor) 拮抗剂，对α2A和α2C的 Ki 值分别为0.13和0.15nM。 靶点 Ki:0.13nM (α2A adrenergic receptor),0.15nM (α2C adrenergic receptor)   体外研究 Lusaperidone has subnanomolar affinity for α2A and α2C adrenergic receptor (Ki=0.13 and 0.15nM,respectively) and shows nanomolar affinity for the hα2B adrenergic receptor and h5-HT7 receptors (Ki=1 and 5nM,respectively).Lusaperidone interacts weakly (Ki values ranging between 81 and 920nM) with dopamine-hD2L,-hD3 and -hD4,h5-HT1D-, h5-HT1F-,h5-HT2A-,h5-HT2C-,and h5-HT5A receptors.Lusaperidone,tested up to 10μM,interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study.Lusaperidone has been shown to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human α2A and α2C adrenoceptors expressed in cell lines (Kb is 2.8 and 4.4nM,respectively) and is a full antagonist on both receptor subtypes. 体内研究 Lusaperidone occupies the α2A and α2C adrenergic receptor with an ED50 of 0.014mg/kg sc (0.009-0.019) and 0.026mg/kg sc (0.022-0.030),respectively.The uptake of R107474 after in vivo intravenous administration is very rapid;in most tissues (including the brain) it reaches maximum concentration at 5 min after tracer injection.   推荐实验方法(仅供参考) 动物实验:   Rats:Radio labeled Lusaperidone (24–28 GBq/μmol) is injected into the tail vein of diethyl ether anesthetized male Wistar rats (200–250g).The rats received 30–40 MBq (injected at the start of the experiment) in 300μL saline including 10% (v/v) ethanol.The rats are sacrificed by cervical dislocation at 5,10,20,and 30 min post injection under diethyl ether anesthesia.A blood sample is taken by cardiac puncture and selected tissues are rapidly dissected and weighed.The radioactivity is measured.
保存条件：-20℃

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