名称 | Buclizine dihydrochloride |
描述 | Buclizine dihydrochloride (Buclina) is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine dihydrochloride binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine dihydrochloride exerts its anti-emetic effect by binding to and blocking the muscarinic and histamine receptors in the vomiting center of the central nervous system (CNS). This may prevent activation of the chemoreceptor trigger zone (CTZ) and may reduce nausea and vomiting. |
激酶实验 | Topoisomerase I Catalytic Actioity Assay [1]: Topoisomerase I Catalytic Actioity Assay: The enzymatic activity is analyzed by the DNA unwinding assay. DNA topoisomerase I, from TopoGEN (1 unit, which is defined as the amount of enzyme that converts 0.5 μg of superhelical DNA to the relaxed state in 30 minutes at 37 °C), is incubated with 0.5 μg of 6x174 RF DNA, in the presence or absence of Beta-Lapachone, in 20 μL of relaxation buffer (50 mM Tris (pH 7.5). 50 mM KCI, 10 mM MgCl2, 0.5 mM dithiothreitol, 0.5 mM EDTA, 30 μg/mL bovine serum albumin) for 30 minutes at 37 °C. Reactions are stopped by adding 1% SDS and proteinase K (50 μg/mL). After an additional 1-hour incubation at 37 °C, the products are separated by electrophoresis in 1% agarose gel in TAE buffer (0.04 M tris acetate, 0.001 M EDTA). The gel is stained with ethidium bromide after electrophoresis. The photographic negative is scanned with an NIH image analysis system. |
体外活性 | Buclizine hydrochloride, a piperazine derivative, is a sedating antihistamine with antimuscarinic and moderate sedative action. Buclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which buclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects. [1] |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 11 mg/mL (21.74 mM), Sonication is recommended.
|
关键字 | teratogen | Inhibitor | MCF-7 | anti-tumor activity | antiallergic | antihistamine | inhibit | Buclizine Dihydrochloride | UCB 4445 | Histamine Receptor | UCB4445 | Buclizine dihydrochloride | Buclizine |
相关产品 | Famotidine | Meclizine dihydrochloride | Lidocaine | Sodium butanoate | Alginic acid | Alverine citrate | Levamisole hydrochloride | Dapoxetine hydrochloride | Choline chloride | Propoxur | Adiphenine hydrochloride | Ribavirin |
相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | FDA 上市药物库 | GPCR靶点分子库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 疼痛相关化合物库 | 药物功能重定位化合物库 | 抗癌药物库 |