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吡拉明马来酸盐 促销  ≥98%

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熔点：100 - 104°C
包装规格：5g in glass bottle
溶解性：溶于DMSO（≥100mg/mL）
产品描述：基本信息 产品编号： M11214 产品名称： Mepyramine maleate CAS: 59-33-6   储存条件 粉末 室温 四年 分子式： C17H23N3O.C4H4O4 溶于液体 -80℃(避光) 6个月 分子量： 401.46 -20℃(避光) 1个月 化学名：  N,N-dimethyl-N'-{[4-(methyloxy)phenyl]methyl}-N'-pyridin-2-ylethane-1,2-diamine (2Z)-but-2-enedioate Solubility (25°C)：   体外:   DMSO 80mg/mL warmed with 50ºC water bath (199.27mM) Ethanol 80mg/mL warmed with 50ºC water bath (199.27mM) Water 80mg/mL (199.27mM) 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.4909mL 12.4545mL 24.9091mL 5mM 0.4982mL 2.4909mL 4.9818mL 10mM 0.2491mL 1.2455mL 2.4909mL 50mM 0.0498mL 0.2491mL 0.4982mL   生物活性 产品描述 第一代抗组胺剂，为 histamine H1 受体拮抗剂，对 H1，H2 和 H3 受体的 Kd 值分别为 0.8nM，5200nM 和 >3000nM，对 H1 受体的 pKd 值为 9.4。 靶点 Kd:0.8nM (Histamine H1 receptor),5200nM (Histamine H2 receptor),>3000nM (Histamine H3 receptor) pKd:9.4 (Histamine H1 receptor)   体外研究 Mepyramine maleate is an antagonist of histamine H1 receptor,with Kds of 0.8nM,5200nM and>3000nM for H1,H2,and H3 receptor,respectively,and a pKd of 9.4 for H1 receptor.Mepyramine binds to the H1 receptor with different Kds in Guinea pig brain (0.8nM),rat brain (9.1nM) and DDT1-MF-2 and BC3H1 cell (276nM).Mepyramine decreases the InsP levels in CHO-gpH1 cells,with log EC50 of -7.94±0.11,and reduces the the maximal response to ATP in CHO-gpH1 cells. 体内研究 Mepyramine obviously decreases the second phase of nociceptive response via i.p at 10 and 20mg/kg,but shows no significant effect at 5mg/kg in rats.   推荐实验方法(仅供参考) 细胞实验:   Briefly,cells are seeded in 24-well cluster dishes and cultured for 24h (70-80% confluence) in DMEM.Cells are then washed,and the medium is replaced for DMEM without calf serum plus the addition of myo-[3H]inositol (2μCi/mL) and cultured for 24h.Thereafter,the medium is aspirated and replaced with DMEM without calf serum containing 10mM LiCl and incubated for 20 min.Cells are then stimulated for 20 min with histamine in concentrations ranging from 1nM to 100μM in a final volume of 300μL in the presence or absence of [3H]inositol the concentrations indicated in each particular experiment.The incubation is stopped by the addition of 900μL of cold chloroform,methanol,0.12M HCl (1:2:1 v/v, freshly prepared),and phases are split by the addition of 300μL of water and 300μL of chloroform.The mixture is then centrifuged at 1500×g for 10 min,and the total water-soluble inositol phosphate fraction is purified by anion exchange chromatography.Radioactivity of the eluted fractions is measured using a liquid scintillation counter.Results are expressed as the ratio obtained when total [3H]inositol phosphate radioactivity is normalized to total [3H]inositol radioactivity recovered from the initial water wash of the columns.   动物实验:   Rats Healthy adult male albino Wistar rats weighing 200-220g are maintained in polypropylene cages with 6 rats in each cage with food and water available ad libitum.Mepyramine is dissolved in normal saine.Mepyramine at doses of 5,10,and 20mg/kg and intraperitoneally injected 30 min before induction of nociception. Physostigmine at doses of 0.05,0.1,and 0.2mg/kg,and atropine at a dose of 2mg/kg,are subcutaneously administered 20 and 40 min before induction of formalininduced pain,respectively.Atropine (2mg/kg,s.c.) is injected 20 min before subcutaneous injection of physostigmine (0.1mg/kg).In combined treatment, intraperitoneal injections of mepyramine (10mg/kg) and famotidine (20mg/kg) are performed 10 min before physostigmine (0.1mg/kg,s.c.) and 10 min after atropine (0.2mg/kg,s.c.) administrations.Drug solutions are intraperitoneally injected in a volum of 1mL/kg,using a 25-gauge injection needle.Subcutaneous injections of drug solutions are perfoemed in a constant volume 0.2mL per rat at the neck region using a 27-gauge injection needle.
保存条件：室温

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