首页 GPCR/G Protein Histamine Receptor Stugeron
Stugeron
编号 T0903     别名: Cinnarizine, Dimitronal, Stutgin, Cinarizine
CAS 298-57-7     分子式 C26H28N2     分子量 368.51
靶点: Calcium Channel; H1 receptor;
Cinnarizine is a piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.
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规格 库存 单价 数量
25 mg 上海现货 154.00
50 mg 上海现货 277.00
100 mg 上海现货 498.00
200 mg 上海现货 896.00
1 mL * 10 mM (in DMSO) 上海现货 385.00
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生物活性

产品描述

Cinnarizine is a piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.

靶点活性

Calcium Channel,

H1 receptor,

体外活性

Cinnarizine inhibits melanogenesis in B16 cells by a dose-dependent manner at the non-cytotoxic concentrations and is a histamine receptor antagonists[3].

体内活性

Cinnarizine has anticonvulsive properties in rats and mice. It could provide a direct neuroprotective effect against the damaging influx of calcium and also prevent neuronal damage as a result of MES- and PTZ-induced seizures[2]. Cinnarizine induces behavioural changes such as alopecia, bucolingual dyskinesia and reduction of motor activity in female parkin knock out (PK-KO) mice but not in wild-type (WT) controls.PK-KO mice have high striatal dopamine levels and increased dopamine metabolism in spite of low reduced tyrosine hydroxylase protein. Cinnarizine, which blocks dopamine receptors and increases dopamine release, further increased dopamine metabolism[3]. Its half-life is 4 hours.

细胞实验

MTT assay is performed to examine the viability of cells. Afterwards, the cells are incubated with the samples for 48 h, the culture medium is removed and replaced with 1 mg/mL MTT solution dissolved in phosphate-buffered saline (PBS) and incubated for an additional 2 h. The MTT solution is then removed and DMSO was added, following which the absorbance of the dissolved formazan crystals is determined at 570 nm by a spectrophotometer.(Only for Reference)

细胞系: mouse B16 melanoma cells(4A5)

动物实验

动物模型:albino mice

化学信息

分子量

368.51

分子式

C26H28N2

CAS

298-57-7

溶解度

DMSO: 68 mg/mL (184.5 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.714 ml 13.568 ml 27.136 ml
5 mM 0.543 ml 2.714 ml 5.427 ml
10 mM 0.271 ml 1.357 ml 2.714 ml
50 mM 0.054 ml 0.271 ml 0.543 ml
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