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Deramciclane

Deramciclane

产品编号 T10996   CAS 120444-71-5
别名: EGIS-3886

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.

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Deramciclane Chemical Structure
Deramciclane, CAS 120444-71-5
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
其他形式的 Deramciclane:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Deramciclane (T10996)
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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TargetMol Library Books参考文献

1. P?lvim?ki EP, et al. Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation. Psychopharmacology (Berl). 1998 Mar;136(2):99-104. 2. K??ri?inen TM, et al. Comparison of the effects of deramciclane, ritanserin and buspirone on extracellular dopamine and its metabolites in striatum and nucleus accumbens of freely moving rats. Basic Clin Pharmacol Toxicol. 2008 Jan;102(1):50-8.
2'-O-Methylisoliquiritigenin LY 344864 racemate PRX-08066 Metergoline SB-616234-A CP-809101 hydrochloride Daurinoline ST1936 oxalate

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Keywords

Deramciclane 120444-71-5 GPCR/G Protein Neuroscience 5-HT Receptor EGIS3886 EGIS-3886 EGIS 3886 Inhibitor inhibitor inhibit

 

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