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120444-71-5

中文名稱 德倫環(huán)烷
英文名稱 DERAMCICLANE
CAS 120444-71-5
分子式 C20H31NO
分子量 301.47
MOL 文件 120444-71-5.mol
120444-71-5 結(jié)構(gòu)式 120444-71-5 結(jié)構(gòu)式

基本信息

中文別名
德倫環(huán)烷
英文別名
EGIS-3886
DERAMCLCLANE
DERAMCICLANE
DERAMCICLANE ISO 9001:2015 REACH
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-(((1S,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]heptan-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-[[(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]-
所屬類別
有機(jī)原料:環(huán)烴

物理化學(xué)性質(zhì)

沸點(diǎn)375.2±25.0 °C(Predicted)
密度1.01±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)pKa 9.61±0.03(H2O t=25±0.1 I=0.1(NaCl)) (Uncertain)
形態(tài)Oil
顏色Light yellow to yellow

常見問題列表

生物活性
Deramciclane 對 5-HT2A 和 5-HT2C 受體具有高親和力。Deramciclane 作為兩種受體亞型的拮抗劑,對 5-HT2C 受體具有反向激動劑特性,無直接刺激激動劑。
靶點(diǎn)

5-HT 2A Receptor

5-HT 2C Receptor

體外研究

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.

體內(nèi)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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