Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,480 | 5日内发货 | ||
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists. |
体外活性 | Deramciclane is a new anti-anxiety drug that can bind to 5-HT2A/2C receptor with high affinity. The interaction between deracixan and serotonin 5-HT2C receptor was further characterized using receptor phosphoinositide hydrolysis assay and receptor autoradiography. Deramciclane antagonizes 5-HT2C receptor-mediated 5-HT stimulated phosphoinositide hydrolysis with IC50 value of 168 nM. In the physiological system of the choroid plexus nervous system, diracic clane can also reduce the hydrolysis of basic inositol phosphate by as much as 33% (EC50 = 93 nM), which indicates that deracic clane has inverse agonism at this receptor Agent properties. |
体内活性 | Compared with basal levels, at any time point, doramamine 3 and 10 mg/kg did not significantly change dopamine levels, while at 40-100 minutes and 160-240 minutes, delamethasone 30 mg/kg was significant Increased dopamine levels (P <0.05). Deramciclane is a putative anti-serotoninergic compound that reduces 5-HT-induced phosphoinositide hydrolysis and multiple effects caused by serotoninergic agonists. The receptor binding curve of Deramciclane is comparable to that of ritanserin. Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors without direct stimulatory agonist effects. In some animal experiments, deraciciran has been shown to have anxiolytic effects. |
别名 | EGIS-3886 |
分子量 | 301.47 |
分子式 | C20H31NO |
CAS No. | 120444-71-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Deramciclane 120444-71-5 GPCR/G Protein Neuroscience 5-HT Receptor EGIS3886 EGIS-3886 EGIS 3886 Inhibitor inhibitor inhibit