生物试剂
>
生化试剂
>
信号通路
> 德伦环烷
加入收藏 取消收藏

德伦环烷  

促销价¥{{model.attbuying.price}}

市场价¥0.00

累计销量0 累计评价0 人评论

别称 {{model.alias}}
中文名称 {{model.name}}
英文名称 {{model.enname}}
品牌 {{model.brand}}
CAS {{model.cas}}
分子式
分子量 {{model.molecularweight}}
MDL {{model.mdl}}
货号 {{model.procode}}
数量

+ -

件 库存{{model.attbuying.number}}件
立即购买 加入购物车 下载说明书

看了又看
包装规格：100mg in glass bottle
产品描述：基本信息 产品编号： D10855 产品名称： Deramciclane CAS: 120444-71-5   储存条件 粉末 -20℃ 四年     分子式： C20H31NO 溶于液体 -80℃ 六个月 分子量 301.47 -20℃ 一个月 化学名：  N,N-dimethyl-2-[[(1R,2S,4R)-1,7,7-trimethyl-2-phenyl-2-bicyclo[2.2.1]heptanyl]oxy]ethanamine Solubility (25°C)：   体外:   DMSO 100 mg/mL (331.71 mM; Need ultrasonic) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80 →45% saline Solubility: ≥ 2.5 mg/mL (8.29mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (8.29mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline)  Solubility: ≥ 2.5 mg/mL (8.29mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (8.29mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均 匀。 3.请依序添加每种溶剂：10% DMSO →90% corn oil Solubility: ≥ 2.5 mg/mL (8.29mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (8.29mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.3171mL 16.5854mL 33.1708mL 5mM 0.6634mL 3.3171mL 6.6342mL 10mM 0.3317mL 1.6585mL 3.3171mL   生物活性 产品描述 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。 靶点 5-HT2A Receptor 5-HT2C Receptor 体外研究 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 168nM. Deramciclane also decreases basal phosphoinositide hydrolysis by up to 33% (EC50= 93nM) 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-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist effects. Deramciclane has been shown to have anxiolytic-like activity in several animal tests     推荐实验方法(仅供参考) Animal Administration Mice Male Wistar rats are used. Samples for determination of basal levels of dopamine, DOPAC and HVA are collected for 60 min. and after that the drugs (doses refer to the salts) are given intraperitoneally in a volume of 5mL/kg of body weight. Treatments are Deramciclane fumarate 3 mg/kg (=7.2 µmol/kg), 10 mg/kg (=24 µmol/kg) and 30 mg/kg (=72 µmol/kg); Damphetamine sulfate 2 mg/kg (=5.4 µmol/kg); Ritanserin 1 mg/kg (=2.1 µmol/kg) and Buspirone hydrochloride 5 mg/kg (=12 µmol/kg). All drugs are suspended in 0.5% carboxymethylcellulose (CMC) dissolved in 0.9% saline. Vehicle control group (n=5) are injected intraperitoneally with 5mL/kg of 0.5% CMC solution. There are nine rats in each treatment group.The doses of Deramciclane fumarate are considered to produce plasma levels comparable to therapeutic plasma levels in human beings (3 mg/kg) or about three times higher (10 mg/kg) 1-3 hr after the administration of the drug. Behavioural data from earlier Deramciclane studies in rats indicates that Deramciclane has some antidopaminergic activity at high doses (20- 40 mg/kg). The highest dose of Deramciclane (30 mg/kg) is selected in this dose range. Fairly high doses of the reference drugs are chosen based on the literature and our own experience to detect the ability of selected drugs to modify extracellular dopamine levels in either the striatum or the nucleus accumbens. After administration of each drug, samples are collected for 240 min. and then divided into two aliquots (35 µL/15 µL). The first aliquot of the samples is stored at 4°C and assayed for dopamine within 24 hr. The other aliquot is frozen and stored at -70°C until assayed for DOPAC and HVA.
保存条件：-20℃

猜你喜欢