5189-11-7

• 常用中文名：苯噻啶苹果酸盐
• 常用英文名：Pizotifen malate
• CAS号：5189-11-7
• 分子式：C₂₃H₂₇NO₅S
• 分子量：429.53
• 相关类别： 生物化工 抑制剂 神经信号通路(Neuronal Signaling) 5-HT Receptor 拮抗剂
• 发布时间：2018-07-08 18:51:37
• 更新时间：2024-01-02 11:24:53
• Pizotifen malate 是 5-HT2 受体的有效拮抗剂,并对5-HT1C 有高亲和力。

名称

• 中文名: 苯噻啶苹果酸盐
• 英文名: pizotifen malate
• 中文别名: 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); 双氯芬酸苹果酸盐
• 英文别名: 4-(9,10-Dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)-1-methylpiperidine (2Z)-2-butenedioate (1:1); 4-(9,10-Dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)-1-methylpiperidinium hydrogen (2Z)-but-2-enedioate (1:1:1); Sanomtgran; Sandomigran malate; 4-(4,5-dihydrobenzo[1,2]cyclohepta[3,4-b]thiophen-10-ylidene)-1-methylpiperidine,2-hydroxybutanedioic acid; Litec malate; Piperidine, 4-(9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thien-4-ylidene)-1-methyl-, (2Z)-2-butenedioate (1:1); Pizotyline malate; Pizotifen hydrogen malate; Pizotifen malate; Mosegor; Sandomygran malate; Sandomigran; piperidinium, 4-(9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thien-4-ylidene)-1-methyl- (2Z)-2-butenedioate, hydrogen salt (1:1:1); Sandomigran,pizotyline

物化性质

• 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

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.

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

安全

• 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

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%