苯噻啶苹果酸盐

中文名称:

苯噻啶苹果酸盐

中文同义词:

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);苯噻啶苹果酸酯;苯噻啶苹果酸盐;苯噻啶苹果酸盐(偏头痛);双氯芬酸苹果酸盐;苹果酸苯噻;PIZOTIFEN苹果酸

英文名称:

Pizotifen Malate

英文同义词:

sandomygranmalate;sanomtgran;4-(9,10-DIHYDRO-1-THIA-BENZO[F]AZULEN-4-YLIDENE)-1-METHYL-PIPERIDINE, COMPOUND WITH 2-HYDROXY-SUCCINIC ACID;PIZOTYLINE MALATE;PIZOTIFEN MALATE;9,10-Dihydro-4-(1-methylpiperidin-4-ylidene)-4H-benzo[4,5]cyclohepta[1,2-b]thiophene malate (1:1);malic acid, compound with 4-(9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thien-4-ylidene)-1-methylpiperidine (1:1);Einecs 225-970-4

CAS号:

5189-11-7

分子式:

C23H27NO5S

分子量:

429.53

EINECS号:

225-970-4

相关类别:

其他科研原料药;化合物：原料药;小分子抑制剂;医药原料;医药化工类;原料中间体-原料药;医用原料;医药原料药;Active Pharmaceutical Ingredients;Sandomigran, pizotyline;原料药;医药、农药及染料中间体

Mol文件:

5189-11-7.mol

熔点 

185-186° (dec)

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

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.

用途 

本品为抗组胺类药，用于治疗偏头痛

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26-37/39