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5189-11-7

中文名称 苯噻啶苹果酸盐
英文名称 Pizotifen Malate
CAS 5189-11-7
分子式 C23H27NO5S
分子量 429.53
MOL 文件 5189-11-7.mol
更新日期 2023/03/20 15:41:17
5189-11-7 结构式 5189-11-7 结构式

基本信息

中文别名
苹果酸苯噻
苯噻啶苹果酸盐
苯噻啶苹果酸酯
双氯芬酸苹果酸盐
PIZOTIFEN苹果酸
苯噻啶苹果酸盐(偏头痛)
9,10-二氢-4-(1-甲基哌啶-4-亚基)-4H-苯并[4,5]环庚烷并[1,2-b]噻吩苹果酸盐 (1:1)
英文别名
mosegor
sanomtgran
bc105malate
litecmalate
malate(1:1)
Pizotifen Mala
Einecs 225-970-4
PIZOTIFEN MALATE
sandomygranmalate
PIZOTYLINE MALATE
所属类别
生物化工:5-HT Receptor 拮抗剂

物理化学性质

熔点185-186° (dec)
储存条件Keep in dark place,Inert atmosphere,2-8°C
溶解度酸水溶液(微溶,加热)、DMSO(微溶)、甲醇(微溶)
形态固体
颜色白色至灰白色
稳定性吸湿性

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335
危险品标志Xi
危险类别码36/37/38
安全说明26-37/39

应用领域

用途1
本品为抗组胺类药,用于治疗偏头痛

常见问题列表

生物活性
Pizotifen Malate (BC-105)用于治疗经常性偏头痛。
靶点

5-HT 2A Receptor

5-HT 1C Receptor

体外研究

Pizotifen malate (BC-105 malate) is a potent 5-HT 2 receptor antagonist, with a high affinity for 5-HT 1C binding site. Pizotifen is an antidepresent 5-HT 2A receptor antagonist and has the capacity to inhibit serotonin-enhanced ADP-induced platelet aggregation.

体内研究

The weights of the fetuses are significantly reduced by all administered doses of Pipethiadene and Pizotifen malate (BC-105 malate) ; the weights of the placentas are significantly reduced after 0.6 and 1.2 mg/kg Pipethiadene and only after the middle dose of Pizotifen malate. The means of the implantations, live, dead fetuses, resorptions and the occurrence of external, skeletal and visceral anomalies do not differ from the control group. The number of chromosome aberrations in the bone marrow cells of treated mice does not differ significantly from the negative control group. The micronucleus test reveals no elevation in the frequency of micronuclei as compared to the control group. After the two higher doses of both Pipethiadene and Pizotifen maleate, the mitotic indices are lower than in the control group.

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