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GSK189254A

GSK189254A

产品编号 TQ0066   CAS 720690-73-3
别名: GSK189254

GSK189254A 是一种有效的特异性组胺 H3 受体拮抗剂,对人类和大鼠H3的pKi 值分别为9.59到9.90和8.51到9.17之间。

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GSK189254A, CAS 720690-73-3
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产品目录号及名称: GSK189254A (TQ0066)
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纯度: 98.71%
纯度: 98.04%
纯度: 98.04%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GSK189254A is a potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3).
靶点活性 mouse H3 receptor:8.51-9.17 (pKi), human H3 receptor:9.59-9.90 (pKi)
体外活性 GSK189254 has a high affinity for both recombinant H3 receptors expressed in HEK-293-MSR-II cells and native H3 receptors expressed in the cerebral cortex of several species. GSK189254 generally exhibits a higher affinity for human and pig H3 receptors compared with mouse, rat, and dog H3 receptors. GSK189254 may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer’s disease and other cognitive disorders [1].
体内活性 In Ox+/+ and Ox?/? mice, acute administration of GSK189254 increases W and decreases slow wave and paradoxical sleep to a similar degree to modafinil, while it reduces narcoleptic episodes in Ox?/? mice [2]. GSK189254 (0.3-3 mg/kg p.o.) increases the release of acetylcholine, noradrenaline, and dopamine in the anterior cingulate cortex and acetylcholine in the dorsal hippocampus. GSK189254 significantly improves the performance of rats in diverse cognition paradigms, including passive avoidance, water maze, object recognition, and attentional set shift [1].
动物实验 Pharmacokinetic studies with GSK189254 are conducted in conscious male Sprague-Dawley rats. Animals receive an intravenous infusion of GSK189254 (n=3) administered at a nominal dose level of 1 mg of free base/kg for 1 h via the femoral vein cannula (10 mL/h/kg). GSK189254 is dissolved in 0.9% (w/v) saline at a target concentration of 0.1 mg free base/mL and filtered with a 0.22-mm Millex-GV filter before administration. After an ish out of at least 2 days, the same rats received a single oral administration of GSK189254 by gastric gavage to achieve a target dose of 2 mg of free base/kg. GSK189254 is formulated in 1% (w/v) aqueous methylcellulose at a target concentration of 0.4 mg free base/mL [1]. The vehicle consists of 0.05 mL NaCl at 0.9% containing methylcellulose at 1%. GSK189254 is a dissolved in-vehicle solution. The effects of acute and repeat administration of GSK189254 on the sleep-wake cycle in wild-type (Ox+/+) and orexin knockout (Ox?/?) mice is investigated. GSK189254 (3 and 10 mg/kg, p.o.) is administered on the sleep-wake cycle in Ox+/+ and Ox?/? mice, dosed at 10 h. The oral administration dose of GSK189254 is 10 mg/kg [2].
别名 GSK189254
分子量 351.4421
分子式 C21H25N3O2
CAS No. 720690-73-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 24 mg/mL (68.29 mM), Need ultrasonic

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Medhurst AD, et al. GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. 2. Guo RX, et al. Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.Br J Pharmacol. 2009 May;157(1):104-17.
Noberastine Enerisant HCl Linetastine Impromidine hydrochloride Talastine Donetidine Oxatomide Dalcotidine

相关化合物库

该产品包含在如下化合物库中:
抗帕金森病化合物库 经典已知活性库 GPCR靶点分子库 抑制剂库 临床期小分子药物库 ReFRAME 相关化合物库 组胺&褪黑色素化合物库 神经信号分子库 神经退行性疾病化合物库 神经递质受体化合物库

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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。

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Keywords

GSK189254A 720690-73-3 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor GSK-189254 GSK 189254 GSK-189254A GSK189254 inhibit Inhibitor inhibitor

 

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