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NRA-0160  

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包装规格：25mg 50mg 100mg in glass bottle
产品描述：基本信息 产品编号： N10678 产品名称： NRA-0160 CAS: 204718-47-8   储存条件 粉末 -20℃ 四年   分子式： C24H23F2N3Os 溶于液体 -80℃ 二年 分子量： 439.52     化学名：  4-(4-fluorophenyl)-5-[2-[4-[(3-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-1,3-thiazole-2-carboxamide 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 一种血管紧张素II受体 (AT1R) 拮抗剂，常用于高血压的相关研究。 靶点 Dopamine Receptor 5-HT Receptor Adrenergic Receptor 体内研究 NRA0160 (0.1,1,or 3mg/kg,i.p.) has no effect on PCP-induced hyperlocomotion,stereotypy or ataxia in SD rats.NRA0160,at any dose,does not reduce cumulated counts of locomotion and cumulated scores of stereotypy emerging, and has no effect on extracellular glutamate levels and locomotor activity emerged after saline injection.NRA0160 dose-dependently and significantly reverses the effects of MAP on both A9 and Al0 dopamine neurons.NRA0160 is slightly more potent in reversiig the effects of MAP on A10 (ED50=1.0mg/kg) than on A9 dopamine neurons (ED50=1.3mg/kg).NRA0160 reverses the effect of AP0 on both A9 and A10 dopamine neurons.ED50 values for the effects of NRA0160 on APO-induced inhibition of A9 and A10 dopamine neurons are 1.3mg/kg and 0.5mg/kg,respectively.   推荐实验方法(仅供参考) 动物实验:   Methamphetamine (MAP,1mg/kg,iv) or apomorphine (APO,40μg/kg iv.) and incremental doses of NRA0160 or G745870 (the starting dose is 0.1mg/kg with sequential doses of 0.2,0.7 and 2mg/kg) are administered every 2-3 min (drug-induced changes usually reached their plateaus in 2-3 min) via an i.v.catheter implanted in the femoral vein of rats. Drug-induced changes (after reaching plateau) in neuronal activities which are plotted as percent changes from the preinjection baseline rate,are recorded over a 5 min period and defined as 100%.The % inhibition is calculated and ED50 values are determined.The ED50 values are analyzed by fitting it to the four parametric logistic functions, using non-linear least square regression (-) Apomorphine hydrochloride,methamphetamine HCl and L 745870 3HCl are dissolved in 0.9% saline with the addition of 0.1% ascorbic acid for apomorphine.NRA0160 is dissolved in a minimal amount of 0.5N HCl and distilled water for injection,then titrated is with 0.5N NaOH to a final pH of 5.
保存条件：-20℃

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