名称 | Anisotropine Methylbromide |
描述 | Anisotropine Methylbromide is an anticholinergic agent and has been used for relief of gastrointestinal spasm and for the suppression of gastric acid secretion. |
细胞实验 | Human or murine hematopoietic stem and progenitor cells are incubated in the presence of vehicle or the combination of 10 μM Treprostinil and 30 μM forskolin at 37°C for 1 hour and 24 hours. After washing with phosphate-buffered saline at 4°C, cells are stained for externalized phosphatidylserine with the apoptosis kit [2]. |
动物实验 | Male Lewis rats weighing 200-300 g are used in the study. Donor animals receive treprostinil or placebo 24 h before hepatectomy and the corresponding recipient animal receive a similar treatment until the time of sacrifice. The surgeon is blinded to treatment. Recipients are sacrificed at 1, 3, 6, 24 and 48 h post-transplantation to examine the early events after IRI. Treprostinil (100 ng/kg/min) or placebo is administered subcutaneously via an Alzet implantable osmotic pump. This dose is selected to achieve a steady-state plasma concentration in the range of 5-20 ng/mL [3]. . Bone marrow transplanted (BMT) mice are divided into five different groups with each group consisting of 6 to 10 mice. One group of mice is exposed to hypoxia (10% inspired oxygen fraction) in a normobaric chamber whereas the second group (control BMT) of animals are placed in a normoxic chamber with a normal oxygen environment (21% inspired O2 fraction) for 28 days. Sham group mice receive saline treatment whereas two other groups of mice receive Treprostinil infusions of different dose levels (14 ng/kg and 70 ng/kg per minute) and are exposed to hypoxia for 4 weeks. For comparison, human infusion rates in PAH therapy vary from 10 to 60 ng/kg per min[5]. |
体外活性 | Treprostinil对IP、EP2和DP1受体具有高亲和力(Ki分别为32、3.6和4.4 nM),对EP1和EP4受体的亲和力低,而对EP3、FP和TP受体的亲和力更低。IP、DP1和EP2受体的激活均可导致人类肺动脉的血管扩张[1]。Treprostinil抑制了培养的内皮集落形成细胞的活力。由Treprostinil预处理的间充质干细胞的条件培养基能刺激内皮集落形成细胞的增殖[2]。 |
体内活性 | Treprostinil在提高小鼠和人类造血干细胞及前体细胞内cAMP水平方面表现出效能[2]。与安慰剂相比,Treprostinil能够保持窦状内皮细胞衬里并在移植后早期减少血小板沉积。在安慰剂组中,肝组织血流明显受损,而Treprostinil能够维持接近正常水平的血流[3]。Treprostinil处理显著增加了与间充质干细胞结合在Matrigel中植入裸鼠的内皮集落形成细胞的血管形成能力。在间充质干细胞中沉默VEGF-A基因也会阻断Treprostinil的促血管生成效应[4]。与常氧小鼠相比,Treprostinil处理显著减少了细胞的招募。Treprostinil还降低了右心室收缩压,并略微减少了血管重塑,但未能逆转右心室肥大[5]。 |
存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 50 mg/mL (137.99 mM) H2O : 198.7 mM
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关键字 | Anisotropine Methylbromide | gastric acid | mAChR | Muscarinic acetylcholine receptor | Inhibitor | inhibit | anticholinergic | Octatropine | peptic ulcers | Anisotropine | muscarinic |
相关产品 | Rutin | Pilocarpine Hydrochloride | Levamisole hydrochloride | Choline chloride | Pilocarpine nitrate | Tranilast | CLOZAPINE N-OXIDE | Forskolin | Propoxur | Adiphenine hydrochloride | Ribavirin | Nanofin |
相关库 | 抑制剂库 | 抗癌上市药物库 | 经典已知活性库 | 已知活性化合物库 | 抗衰老化合物库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 |