120444-71-5
120444-71-5 结构式
基本信息
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]-
物理化学性质
常见问题列表
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5-HT 2A Receptor
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5-HT 2C Receptor
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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.
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.