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5-HT1A modulator 1  ≥98%

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包装规格：10mg in glass bottle
产品描述：基本信息 产品编号： H10376 产品名称： 5-HT1A modulator 1 CAS: 142477-34-7   储存条件 粉末 -20℃ 四年     分子式： C21H25N3O2S 溶于液体 -80℃ 6个月 分子量 358.18 -20℃ 1个月 化学名：  6-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-3-methyl-1,3-benzothiazol-2-one Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜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。   生物活性 产品描述 一种5HT1A，肾上腺素能 α1 和多巴胺 D2 受体具有非常高的亲和力，IC50 分别为 2±0.3nM，10±3nM 和 40±9nM。 靶点 sPLA2 2nM (IC50) 5-HT2A Receptor 500nM (IC50) 5-HT2C Receptor 4000nM (IC50) α1 receptor 10nM (IC50) D2 receptor 40nM (IC50)       体外研究 5-HT1A modulator 1 (Compound 24) also displays affinities for the 5HT1B, 5-HT2A and 5-HT2C receptor with IC50s of 300±55nM, 500±75nM, and 4000±440nM, respectively. 体内研究 5-HT1A modulator 1 (Compound 24) shows clear antagonist action at 5HT2A receptor subtype in mice. The antagonism is nearly complete at the dose of 1 mg/kg ip for 5-HT1A modulator 1 (94% of antagonism, p<0.01). 5-HT1A modulator 1 completely blocks the stereotypies and the climbing at the dose of 1 mg/kg ip (100% of antagonism). 5-HT1A modulator 1 is also tested in rats, using the same paradigm. After oral administration, 5-HT1A modulator 1 significantly (p<0.05) reduces the hyperactivity by 50% at the doses of 2 and 4 mg/kg po, respectively 63% and 58% of antagonism for 5-HT1A modulator 1; the antagonism is complete (103% and 108%) at the respective doses of 8 and 16 mg/kg po for 5-HT1A modulator 1 (p<0.01). 特征     推荐实验方法(仅供参考) Kinase Assay Binding is determined using membranes prepared from bovine hippocampus. The receptor is labeled with 0.5nM [3H]-8- hydroxydipropylaminotetralin (8-OH-DPAT) by incubation at 25°C for 30 min with 11 concentrations of the test compounds (1-105nM). Nonspecific binding is determined using 10-5 Mbuspirone. Competition experiments are analyzed using the iterative nonlinear least-squares curve-fitting program Inplot 4, graphpad; IC50 values are calculated using the ChengPrusoff equation   Animal Administration Rats Wistar rats (n=6) are used. 5-HT1A modulator 1 is tested at pharmacological doses (1 and 2 mg/kg ip, respectively) and at high doses (32 and 64 mg/kg ip) in rats. The intensity of forepaw treading is expressed as percentage of the maximal possible score. The 5HT1A agonist 8-OH-DPAT induces forepaw treading and is used as a reference compound. Mice  Swiss mice are injected with the test compound (e.g., 5-HT1A modulator 1, 0.25 and 1 mg/kg ip) before an injection of 5HTP (400 mg/kg ip). The number of head twiches occurring in a 10 min period starting 10 min after the injection of 5HTP is counted. Cyproheptadine is used as reference compound.
保存条件：-20℃

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