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ReN-1869 hydrochloride  ≥98%

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包装规格：25mg 50mg 100mg in glass bottle
产品描述：基本信息 产品编号： R10493 产品名称： ReN-1869 hydrochloride CAS: 170149-76-5   储存条件 粉末 -20℃ 四年 分子式： C24H28ClNO2 溶于液体 -80℃ 二年 分子量： 397.94     化学名：  (R)-1-(3-(10,11-Dihydro-5-H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-3-piperidinecarboxylic acid hydrochloride 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 一种新型的选择性组胺 H1 受体拮抗剂，高亲和力作用于组胺 H1 受体 (豚鼠脑) 和非选择性 σ 位点 (豚鼠脑)，Ki 值分别为 0.19±0.04μM 和 0.45μM。 靶点 Ki:0.19±0.04μM (histamine H1 receptor)   体外研究 ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H1 receptor antagonism.Binding studies with radioactively labelled ReN 1869 reveals high affinity only for the histamine H1 receptor in addition to some affinity for a sigma site.ReN 1869 is profiled for activity at 10μM at various receptors,transporters,enzymes and ion channels.ReN 1869 only demonstrates affinity to the histamine H1 receptor (guinea pig brain,[3H]pyrilamine) with a Ki of 0.19±0.04μM and the non-selective σ site [guinea pig brain,[3H]1,3-di-tolylguanidine (DTG)] with a Ki of 0.45μM.ReN 1869 dose-dependently reduces the responses with IC50 of 1.70±0.002μM. 体内研究 The in vivo binding of [3H]Mepyramine to mouse spinal cord and cerebellar histamine H1 receptors is dose-dependently inhibited by ReN 1869.ReN 1869 (in doses as low as 10μg/kg i.p.) significantly inhibits the histamine-evoked paw edema.The ED50 is approximately 300μg/kg.Interestingly, even a high dose of Mepyramine (10mg/kg) is unable to inhibit significantly this type of edema (0.29±0.06 versus 0.34±0.05 in controls,n=7).ReN 1869 (1mg/kg s.c.) is administered 30 min before paw injection with carrageenan and has no effect on the development of the paw edema.Dexamethasone (1mg/kg s.c.) is given 1h before carrageenan and expectedly diminished the edema. This effect is not affected by the simultaneous administration of 1mg/kg ReN 1869.   推荐实验方法(仅供参考) 激酶实验： ReN 1869 is labelled with 3H in the tricyclic ring system resulting in a specific activity of 40 Ci/mmol.Thawed membranes (1mg protein/tube),test compounds and [3H]ReN 1869 are added to test tubes in a final volume of 0.5mL.Unless otherwise indicated, the concentration of the radioligand is 5nM and non-specific binding is defined as the binding in the presence of 10μM ReN 1869.Samples are incubated for 120 min at 37℃ in a shaking water bath.Free and bound radioactivity is separated by filtration over Whatman GF/F filters that are washed with 25mL of ice-cold buffer (20mM Tris-HCl,pH 7.4).Radioligand bound to filters accounted for 5-700 dpm that is subtracted before calculating specific binding.The in vivo binding of [3H]Mepyramine to mouse spinal cord and cerebellar histamine H1 receptors is dose-dependently inhibited by ReN 1869.ReN 1869 (in doses as low as 10μg/kg i.p.) significantly inhibits the histamine-evoked paw edema.The ED50 is approximately 300μg/kg.Interestingly,even a high dose of Mepyramine (10mg/kg) is unable to inhibit significantly this type of edema (0.29±0.06 versus 0.34±0.05 in controls,n=7).ReN 1869 (1mg/kg s.c.) is administered 30 min before paw injection with carrageenan and has no effect on the development of the paw edema.Dexamethasone (1mg/kg s.c.) is given 1h before carrageenan and expectedly diminished the edema.This effect is not affected by the simultaneous administration of 1mg/kg ReN 1869.
保存条件：-20℃

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