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苯噻啶苹果酸盐

苯噻啶苹果酸盐用途

Pizotifen malate 是 5-HT2 受体的有效拮抗剂,并对5-HT1C 有高亲和力。

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苯噻啶苹果酸盐名称

[ CAS 号 ]:
5189-11-7

[ 中文名 ]:
苯噻啶苹果酸盐

[ 英文名 ]:
Pizotifen malate

[中文别名 ]:

双氯芬酸苹果酸盐

[英文别名 ]:

Sanomtgran
Sandomigran malate
Litec malate
Pizotyline malate
Pizotifen hydrogen malate
Pizotifen malate
Mosegor
Sandomygran malate
Sandomigran
Sandomigran,pizotyline

苯噻啶苹果酸盐生物活性

[ 描述 ]:

Pizotifen malate 是 5-HT2 受体的有效拮抗剂,并对5-HT1C 有高亲和力。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

研究领域 >> 神经疾病

天然产物 >> 生物碱

[ 靶点 ]

5-HT2A Receptor

5-HT1C Receptor

[体外研究]

Pizotifen是一种有效的5-HT2受体拮抗剂,对5-HT1C结合位点具有高亲和力[1]。 Pizotifen是一种抗过敏的5-HT2A受体拮抗剂,具有抑制5-羟色胺增强的ADP诱导的血小板聚集的能力[2]。

[体内研究]

所有给药剂量的Pipethiadene和Pizotifen malate都显着降低了胎儿的体重;在0.6和1.2 mg/kg Pipethiadene之后,并且仅在中等剂量的Pizotifen苹果酸盐后,胎盘的重量显着减少。植入,活体,死胎,再吸收以及外部,骨骼和内脏异常的发生方式与对照组没有差异。处理小鼠的骨髓细胞中的染色体畸变数与阴性对照组没有显着差异。与对照组相比,微核试验显示微核的频率没有升高。在两种较高剂量的Pipethiadene和Pizotifen马来酸盐后,有丝分裂指数低于对照组[3]。

[动物实验]

从妊娠第4天至第16天，以0.24,0.6和1.2mg / kg的剂量将小鼠[3]苹果酸马替替尼口服给予三组瑞士小鼠。对照组用蒸馏水处理。在妊娠第19天，处死小鼠并测定细胞遗传学检查和子宫内容物（活胎，异常和死胎的数量以及植入，再吸收的数量）。检查活体胎儿的外部，内脏和骨骼畸形[3]。

[参考文献]

[1]. Mylecharane EJ, et al. 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52.

[2]. Lin OA, et al. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026.

[3]. Ujházy E, et al. Teratological and cytogenetical evaluation of two antihistamines (pipethiadene and pizotifen maleate) in mice. Agents Actions. 1988 Apr;23(3-4):376-8.

[相关活性小分子]

苯噻啶苹果酸盐物理化学性质

[ 沸点 ]:
436.7ºC at 760 mmHg

[ 熔点 ]:
185-186° (dec)

[ 分子式 ]:
C₂₃H₂₇NO₅S

[ 分子量 ]:
429.53

[ 闪点 ]:
217.9ºC

[ PSA ]:
106.08000

[ LogP ]:
4.02390

[ 外观性状 ]:
固体

[ 储存条件 ]:
2–8 °C

苯噻啶苹果酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM7165500

CAS REGISTRY NUMBER :: 5189-11-7

LAST UPDATED :: 198910

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H21-N-S.C4-H6-O5

MOLECULAR WEIGHT :: 429.57

WISWESSER LINE NOTATION :: T C576 BY FS&T&J BU- DT6N DYTJ A1 &QV1U1VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 600 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - visual field changes Cardiac - pulse rate increase, without fall in BP Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 63,59,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 19,19,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 43 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 19,19,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 19 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 19,19,1969

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苯噻啶苹果酸盐安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-37/39

[ 海关编码 ]:
2934999090

苯噻啶苹果酸盐海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%