80-50-2

• 常用中文名：溴甲辛托品
• 常用英文名：Endovalpin
• CAS号：80-50-2
• 分子式：C₂₇H₄₃NO₉
• 分子量：525.63200
• 相关类别： 生物化工 抑制剂 丝裂原活化蛋白激酶(MAPK) ERK 抑制剂
• 发布时间：2018-07-10 13:05:41
• 更新时间：2024-01-23 13:22:21
• 甲溴化异丙肾上腺素是一种口服活性抗胆碱能毒蕈碱拮抗剂。甲溴化异丙肾上腺素可抑制胃酸分泌,并用作消化性溃疡的辅助药物[1]。

名称

• 中文名: 溴甲辛托品
• 英文名: anisotropine methylbromide
• 中文别名: O-乙酰基-L-肉碱盐酸盐; 甲溴辛托品
• 英文别名: octatropine methylbromide; Methoxy(benzene-2,4,6-d3); Anisole-2,4,6-d3; 1,3,5-trideuterio-2-methoxy-benzene; CHOLINE IODIDE 1-HYDROXY-α-PHENYLCYCLOPENTANEACETATE; 2,4,6-Trideutero-anisol; anisotropine methobromide; 2,4,6-Trideuterio-anisol; anisotropine methyl bromide; 2,4,6-trideuterioanisole

物化性质

• 熔点: 329ºC
• 分子式: C₂₇H₄₃NO₉
• 分子量: 525.63200
• 精确质量: 525.29400
• PSA: 174.31000
• 储存条件: 2-8°C

生物活性

• 描述: 甲溴化异丙肾上腺素是一种口服活性抗胆碱能毒蕈碱拮抗剂。甲溴化异丙肾上腺素可抑制胃酸分泌,并用作消化性溃疡的辅助药物[1]。
• 相关类别:
  信号通路 >> 神经信号通路 >> mAChR
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR
  研究领域 >> 代谢疾病
• 体内研究: 甲溴化异丙肾上腺素(静脉注射,0.5μM和0.1ml,一次)可阻断清醒或麻醉狗的乙酰胆碱诱导的发声、肠痉挛和肠收缩[1]。动物模型：体重2.5-5.0kg的狗[1]剂量：0.5μM,0.1ml给药：静脉注射；一次结果：抑制乙酰胆碱诱导的发声,最大抑制率为85.1%,抑制乙酰胆碱酯酶诱导的肠痉挛,最大抑制为79%。
• 参考文献:

  [1]. K Nakayama, et al. Effects of anisotropine methylbromide (Valpin) and its mixture with sulpyrine on vocalization response and spasm of intestine induced by acetylcholine in dogs. Jpn J Pharmacol. 1972 Apr;22(2):215-20.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : YM3710000 CHEMICAL NAME : 1-alpha-H,5-alpha-H-Tropanium, 3-alpha-hydroxy-8-methyl-, bromide, 2-propylvalerate CAS REGISTRY NUMBER : 80-50-2 LAST UPDATED : 199504 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C17-H32-N-O2.Br MOLECULAR WEIGHT : 362.41 WISWESSER LINE NOTATION : T56 A AKTJ A1 A1 GOVY3&3 &E 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 : 705 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: 6,24,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 850 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: 6,24,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 129 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: 6,24,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 133 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: 6,24,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 6300 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,70,1968 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M2759 No. of Facilities: 10 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 197 (estimated) No. of Female Employees: 59 (estimated)

安全

• 符号: GHS07, GHS09
• 信号词: Warning
• 危害声明: H302-H312-H332-H400
• 警示性声明: P273-P280
• 个人防护装备: dust mask type N95 (US);Eyeshields;Gloves
• 危害码 (欧洲): Xn: Harmful;N: Dangerous for the environment;
• 风险声明 (欧洲): R20/21/22
• 安全声明 (欧洲): 36-61-60
• 危险品运输编码: UN 3077 9/PG 3
• WGK德国: 3
• RTECS号: YM3710000