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2-(1-(4-甲基苯基)-3-(1-吡咯烷基)-1-丙烯基)吡啶盐酸盐

用途

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

[ CAS 号 ]:
550-70-9

[ 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

[中文别名 ]:

盐酸曲普立定

[英文别名 ]:

EINECS 208-985-0
MFCD00039044
Triprolidine Hydrochloride
Triprolidine HCl

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.

物理化学性质

[ 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

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)

安全信息

[ 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

详细合成路线

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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%