Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Lurasidone hydrochloride 是多巴胺 D2和5-HT7的拮抗剂，IC50值分别为 1.68 和 0.495 nM，用于治疗精神分裂症和双相情感障碍。它也是5-HT1A 受体的部分激动剂，IC50值为 6.75 nM。
| 产品描述 | Lurasidone hydrochloride is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder. |
| 靶点活性 | noradrenaline α2C:10.8 nM, 5-HT1A:6.75 nM, 5-HT2A:2.03 nM, 5-HT7:0.495 nM, D2 receptor:1.68 nM |
| 体外活性 | Lurasidone antagonizes dopamine-stimulated [35S]GTPγS binding at human dopamine D2L receptor in a concentration-dependent manner with a KB value of 2.8 nM. Lurasidone antagonizes 5-HT-stimulated cAMP accumulation in the CHO/h5-HT7 cells with a KB value of 2.6 nM. Lurasidone partially stimulates [35S]GTPγS binding to the membrane preparation for human 5-HT1A receptors with a maximum effect of 33%. Lurasidone dose-dependently increases the ratio of DOPAC/dopamine in rat frontal cortex and striatum. [1] |
| 体内活性 | The inhibitory actions of Lurasidone on MAP-induced hyperactivity persists for more than 8 hours, and the ED50 values of the action at 1 hour, 2 hours, 4 hours, and 8 hours after the treatment are 2.3 mg/kg, 0.87 mg/kg, 1.6 mg/kg, and 5.0 mg/kg, respectively. Lurasidone (1 mg/kg–10 mg/kg) dose-dependently inhibits conditioned avoidance response in rats with ED50 of 6.3 mg/kg. Lurasidone dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia in rats with ED50 of 5.6 mg/kg and 3.0 mg/kg, respectively. Lurasidone (0.3 mg/kg–30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the Vogel's conflict test with MED of 10 mg/kg. Lurasidone (3 mg/kg, 2 weeks) significantly suppresses hyperactivity behavior in olfactory bulbectomy model rats. Lurasidone (700 mg/kg–1000 mg/kg) slightly prolongs the duration of loss of righting reflexes elicited by hexobarbital (anesthesia) in mice in a dose-dependent manner. [1] Lurasidone (30 mg/kg, p.o.) significantly and dose-dependently reverses the MK-801-induced impairment of the passive-avoidance response of rats. [2] Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced learning impairment in the Morris water maze test in rats. Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced reference memory impairment and moderately but not significantly attenuates MK-801-induced working memory impairment in the radial-arm maze test. [3] Lurasidone (10 mg/kg) treatment increases total BDNF mRNA levels in rat prefrontal cortex and, to less extent, in hippocampus. Lurasidone (10 mg/kg) significantly increases the levels of mature BDNF protein in rat prefrontal cortex, without affect the protein levels of the neurotrophin (both precursor and mature forms) in hippocampal extracts. [4] |
| 别名 | SM-13496 (Hydrochloride), SM-13496, Lurasidone HCl, 盐酸鲁拉西酮 |
| 分子量 | 529.14 |
| 分子式 | C28H36N4O2S·HCl |
| CAS No. | 367514-88-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 5.29 mg/mL (10 mM), Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
参考文献文献引用
剂量换算对于不同动物的给药剂量换算，您也可以参考 更多...
体内实验配液计算器请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法： 比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)， 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。
体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300， 混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。
计算器bottom
您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。
Lurasidone hydrochloride 367514-88-3 GPCR/G Protein Neuroscience 5-HT Receptor Dopamine Receptor Norepinephrine SM13496 SM-13496 (Hydrochloride) Inhibitor 5-hydroxytryptamine Receptor SM-13496 Lurasidone Lurasidone HCl inhibit 盐酸鲁拉西酮 SM 13496 Serotonin Receptor inhibitor
沪公网安备 31010602006700号
