Powder: -20°C for 3 years | In solvent: -80°C for 1 year
5-HT1A modulator 1 对 5-HT1A、α1-肾上腺素能受体和 D2 受体具有非常高的亲和力(IC50s = 2 nM、10 nM 和 40 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 4,660 | 现货 | ||
5 mg | ¥ 9,670 | 现货 | ||
10 mg | ¥ 12,800 | 现货 | ||
25 mg | ¥ 19,300 | 现货 | ||
50 mg | ¥ 25,900 | 现货 | ||
100 mg | ¥ 35,200 | 现货 |
产品描述 | 5-HT1A modulator 1 displays very high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM). |
靶点活性 | 5-HT2C receptor:4000 nM, D2 receptor:40 nM, α1-adrenoceptor:10 nM, 5-HT1B receptor:300 nM, 5-HT2A receptor:500 nM, SPLA2:2 nM |
体外活性 | 5-HT1A modulator 1 对5-HT1B、5-HT2A和5-HT2C具有亲和力(IC50分别为300nM,500nM和4000nM)[1]。 |
体内活性 | 5-HT1A modulator 1 (1 mg/kg; i.p)在小鼠中表现出对5-HT2A亚型94%的拮抗作用。5-HT1A modulator 1 (1 mg/kg;腹腔内)完全阻断定型行为和攀爬行为。在大鼠中,5-HT1A modulator 1 (口服,2 mg/kg和4mg/kg)分别显示63%和58%的拮抗作用,而在每千克8mg和16mg剂量时,拮抗作用完全(分别为103%和108%)。5-HT1A modulator 1 显著减少50%[1]的过动行为。 |
激酶实验 | Binding was determined using membranes prepared from bovine hippocampus. Receptors were labeled with 0.5 nM [3H]-8-OH-DPAT by incubating with 11 concentrations of test compounds (1-10^5 nM) for 30 min at 25°C. Nonspecific binding was determined using 10 μM buspirone. Competition experiments were analyzed using the iterative nonlinear least squares curve fitting program Inplot 4, GraphPad. IC50 values were calculated using the Cheng-Prusoff equation. |
动物实验 | Inject Swiss mice with test compounds (e.g. 5-HT1A modulators 1, 0.25 and 1 mg/kg i.p) prior to injection of 5-HTP (400 mg/kg i.p). Count the number of head twitches that occurred during the 10 minutes starting 10 minutes after the injection of 5HTP. Cyproheptadine was used as reference compound. Wistar rats (n=6) were used. 5-HT1A Modulator 1 was tested at pharmacological doses (1 and 2 mg/kg i.p) and high doses (32 and 64 mg/kg i.p). The intensity of forepaw pedaling was expressed as a percentage of the maximum possible score. The 5-HT1A agonist 8-OH-DPAT induced forepaw trampling and was used as a reference compound. |
别名 | 5-HT1Amodulator1 |
分子量 | 383.51 |
分子式 | C21H25N3O2S |
CAS No. | 142477-34-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5 mg/mL (13.04 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6075 mL | 13.0375 mL | 26.0749 mL | 65.1873 mL |
5 mM | 0.5215 mL | 2.6075 mL | 5.215 mL | 13.0375 mL | |
10 mM | 0.2607 mL | 1.3037 mL | 2.6075 mL | 6.5187 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
5-HT1A modulator 1 142477-34-7 GPCR/G Protein Metabolism Neuroscience 5-HT Receptor Dopamine Receptor Phospholipase Adrenergic Receptor 5-HT1Amodulator1 Inhibitor inhibitor inhibit