550-70-9

• 常用中文名：2-(1-(4-甲基苯基)-3-(1-吡咯烷基)-1-丙烯基)吡啶盐酸盐
• 常用英文名：Triprolidine hydrochloride
• CAS号：550-70-9
• 分子式：C₁₉H₂₃ClN₂
• 分子量：314.85200
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 组胺受体
• 发布时间：2018-12-25 18:20:36
• 更新时间：2024-01-09 20:14:35
• Triprolidine 是一种有口服活性的,第一代组胺 H1 受体 (histamine H1-receptor) 拮抗剂,可用于过敏性鼻炎的研究。在大鼠中,Triprolidine 能阻滞脊髓运动和感觉。

名称

• 中文名: 2-(1-(4-甲基苯基)-3-(1-吡咯烷基)-1-丙烯基)吡啶盐酸盐
• 英文名: triprolidine hydrochloride (anh.)
• 中文别名: 盐酸曲普立定
• 英文别名: EINECS 208-985-0; MFCD00039044; Triprolidine Hydrochloride; Triprolidine HCl

物化性质

• 密度: 1.061g/cm3
• 沸点: 435.4ºC at 760mmHg
• 熔点: 59-61ºC
• 分子式: C₁₉H₂₃ClN₂
• 分子量: 314.85200
• 闪点: 217.1ºC
• 精确质量: 314.15500
• PSA: 16.13000
• LogP: 4.65740
• 储存条件: 2-8°C

生物活性

• 描述: Triprolidine 是一种有口服活性的,第一代组胺 H1 受体 (histamine H1-receptor) 拮抗剂,可用于过敏性鼻炎的研究。在大鼠中,Triprolidine 能阻滞脊髓运动和感觉。
• 相关类别:
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
• 靶点:

  H1 Receptor

• 体内研究: 曲普利啶(292.81-1467.20μg/kg；鞘内注射)对大鼠脊髓运动和感觉阻滞产生剂量依赖性效应[3]。动物模型：雄性Sprague-Dawley大鼠(300-350 g)[3]剂量：292.81μg/kg,488.02μg/kg,733.60μg/kg,1098.83μg/kg,1467.20μg/kg给药：鞘内注射结果：诱发剂量依赖性脊髓阻滞。
• 参考文献:

  [1]. K J Simons, et al. An investigation of the H1-receptor antagonist triprolidine: pharmacokinetics and antihistaminic effects. J Allergy Clin Immunol. 1986 Feb;77(2):326-30.

  [2]. D L Deal, et al. Disposition and metabolism of triprolidine in mice. Drug Metab Dispos. Nov-Dec 1992;20(6):920-7.

  [3]. Jann-Inn Tzeng, et al. Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats. J Pharm Pharmacol. 2018 Dec;70(12):1654-1661.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UT7657000 CHEMICAL NAME : Pyridine, 2-(3-(1-pyrrolidinyl)-1-p-tolylpropenyl)-, monohydrochloride, (E)- CAS REGISTRY NUMBER : 550-70-9 LAST UPDATED : 199803 DATA ITEMS CITED : 8 MOLECULAR FORMULA : C19-H22-N2.Cl-H MOLECULAR WEIGHT : 314.89 WISWESSER LINE NOTATION : T6NJ BYR D1&2- AT5NTJ &GH HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 840 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 22,375,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 495 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,525,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 247 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,525,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 21 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 8,171,1953 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >5 mg/kg TOXIC EFFECTS : Behavioral - tremor Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea REFERENCE : BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 8,171,1953 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 81570 No. of Facilities: 842 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 990 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 81570 No. of Facilities: 178 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 2378 (estimated) No. of Female Employees: 1467 (estimated)

安全

• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 22-36/37/38
• 安全声明 (欧洲): 26-36
• 危险品运输编码: UN 3249
• WGK德国: 3
• RTECS号: UT7658000
• 包装等级: III
• 危险类别: 6.1(b)
• 海关编码: 2933990090

合成路线

486-12-4 ~51% 550-70-9

文献：HIKAL LIMITED Patent: WO2009/84035 A1, 2009 ; Location in patent: Page/Page column 11-12 ;

13573-69-8 ~% 550-70-9

文献：WO2007/141803 A2, ; Page/Page column 6-7 ;

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海关

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%