Cinnarizine 是一种哌嗪衍生物,具有组胺 H1 受体和钙通道阻断活性,具有扩张血管和止吐的特性,可促进脑血流,用于脑中风、创伤后脑症状和脑动脉硬化的研究。
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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.
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)
Cas No.
298-57-7
分子式
C26H28N2
分子量
368.51
别名
Stugeron;Cinarizine;桂利嗪;Dimitronal;Stutgin;Cinnarizine
储存和溶解度
DMSO:68 mg/mL (184.5 mM)
Ethanol:<1 mgml
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years