中文名 | 德伦环烷 |
英文名 | DERAMCICLANE |
别名 | 德伦环烷 化合物 T10996 |
英文别名 | EGIS-3886 DERAMCICLANE DERAMCLCLANE N,N-Dimethyl-2-[[(1R,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]hept-2-yl]oxy]ethanamine N,N-Dimethyl-2-(((1R,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]heptan-2-yl)oxy)ethanamine N,N-dimethyl-2-(((1S,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]heptan-2-yl)oxy)ethanamine N,N-dimethyl-2-[[(1R,3S,4R)-4,7,7-trimethyl-3-phenyl-3-bicyclo[2.2.1]heptanyl]oxy]ethanamine Ethanamine, N,N-dimethyl-2-[[(1R,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]hept-2-yl]oxy]- |
CAS | 120444-71-5 |
化学式 | C20H31NO |
分子量 | 301.47 |
密度 | 1.01±0.1 g/cm3(Predicted) |
沸点 | 375.2±25.0 °C(Predicted) |
酸度系数 | pKa 9.61±0.03(H2O t=25±0.1 I=0.1(NaCl)) (Uncertain) |
存储条件 | Room Temprature |
体外研究 | Deramciclane is a novel anxiolytic agent that binds with high affinity to 5-HT 2A / 2C receptors. The interactions of Deramciclane with the serotonin 5-HT 2C receptor are characterized further using receptor phosphoinositide hydrolysis assays and receptor autoradiography. Deramciclane antagonizes 5-HT 2C receptor mediated 5-HT-stimulated phosphoinositide hydrolysis with an IC 50 value of 168 nM. Deramciclane also decreases basal phosphoinositide hydrolysis by up to 33% (EC 50 = 93 nM) in a physiological system in the choroid plexus, suggesting that Deramciclane possesses inverse agonist properties at this receptor. |
体内研究 | Deramciclane 3 and 10 mg/kg does not change the dopamine levels significantly at any time point versus the basal level whereas 30 mg/kg of Deramciclane significantly increases the levels at 40-100 min and at 160-240 min (P<0.05). Deramciclane is a putative antiserotonergic compound that reduces 5-HT-induced phosphoinositol hydrolysis and a variety of actions caused by serotonergic agonists. The receptor binding profile of Deramciclane is rather similar to that of ritanserin. Deramciclane has a high affinity for 5-HT 2A and 5-HT 2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT 2C receptors without direct stimulatory agonist effects. Deramciclane has been shown to have anxiolytic-like activity in several animal tests. |
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