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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.
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 | 库存 | 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 |
密度 | 1.01 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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