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Deramciclane

(Synonyms: EGIS-3886)

目录号: PL01262 纯度: ≥98%

Deramciclane 对 5-HT2A 和 5-HT2C 受体具有高亲和力。Deramciclane 作为两种受体亚型的拮抗剂，对 5-HT2C 受体具有反向激动剂特性，无直接刺激激动剂。

CAS No. :120444-71-5

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PL01262-50mg	50mg	询价	询价
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PL01262-10mM*1mLinDMSO	10mM*1mLinDMSO	¥6188.00	请登录

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中文名称	Deramciclane
中文别名	N,N-二甲基-2-(((1S,2S,4R)-1,7,7-三甲基-2-苯基双环[2.2.1]-2-庚基)氧基)乙胺;德伦环烷
英文名称	Deramciclane
英文别名	N,N-Dimethyl-2-(((1R,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]heptan-2-yl)oxy)ethanamine;Ethanamine, N,N-dimethyl-2-(((1R,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo(2.2.1)hept-2-yl)oxy)-;N,N-dimethyl-2-((1S,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]heptan-2-yloxy)ethanamine;N,N-dimethyl-2-[[(1R,3S,4R)-4,7,7-trimethyl-3-phenyl-3-bicyclo[2.2.1]heptanyl]oxy]ethanamine;(1R,2S,4R)-(-)-2-[(2'-{N,N-dimethylamino}-ethoxy-)]-2-[phenyl]-1,7,7,-tri-[methyl]-bicyclo[2.2.1]heptane;(1R,2S,4R)-(-)-2-phenyl 2-(dimethylaminoethoxy)-1,7,7-trimethyl-bicyclo[2.2.1]heptane;[14C]-Deramciclane;Deramciclane;deramciclane,(1R,2S,4R)-isomer;DERAMCLCLANE;Ethanamine,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-((1,7,7-trimethyl-2-phenylbicyclo(2.2.1)hept-2-yl)oxy)-,(1R-exo);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]hept-2-yl]oxy]ethanamine
Cas No.	120444-71-5
分子式	C₂₀H₃₁NO
分子量	301.47
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
详情描述	Deramciclane 对 5-HT2A 和 5-HT2C 受体具有高亲和力。Deramciclane 作为两种受体亚型的拮抗剂，对 5-HT2C 受体具有反向激动剂特性，无直接刺激激动剂。

产品详情	Deramciclane 对 5-HT_2A 和 5-HT_2C 受体具有高亲和力。Deramciclane 作为两种受体亚型的拮抗剂，对 5-HT_2C 受体具有反向激动剂特性，无直接刺激激动剂。
生物活性	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.
性状	Oil
IC50 & Target[1][2]	5-HT2A Receptor 5-HT2C Receptor
体外研究(In Vitro)	Deramciclane is a novel anxiolytic agent that binds with high affinity to 5-HT2A/2C receptors. The interactions of Deramciclane with the serotonin 5-HT2C receptor are characterized further using receptor phosphoinositide hydrolysis assays and receptor autoradiography. Deramciclane antagonizes 5-HT2C receptor mediated 5-HT-stimulated phosphoinositide hydrolysis with an IC50 value of 168 nM. Deramciclane also decreases basal phosphoinositide hydrolysis by up to 33% (EC50= 93 nM) in a physiological system in the choroid plexus, suggesting that Deramciclane possesses inverse agonist properties at this receptor. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not i
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (331.71 mM; Need ultrasonic)配制储备液

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Deramciclane

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