87-00-3

• 常用中文名：后马托品
• 常用英文名：Homatropine
• CAS号：87-00-3
• 分子式：C₁₆H₂₁NO₃
• 分子量：275.34300
• 相关类别： 原料药 神经系统用药 拟胆碱药
• 发布时间：2018-03-23 08:00:00
• 更新时间：2024-01-02 19:55:33
• 霍马托品是一种口服活性毒蕈碱乙酰胆碱受体拮抗剂,可用作抗胆碱药[1]。

名称

• 中文名: 后马托品
• 英文名: [(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 2-hydroxy-2-phenylacetate
• 中文别名: 扁桃酰托品碱; 8-甲基-8-氮杂双环[3.2.1]辛烷-3-醇羟基(苯基)乙酸酯
• 英文别名: Omatropina [DCIT]; Homatropin; Homotropine; DL-mandelic acid-tropane-3endo-yl ester; Homoatropine; homatropine; Mandelyltropeine; Homatropine [BAN]; Methylhomatropinum; DL-Mandelsaeure-tropan-3endo-ylester; EINECS 201-716-8; homatropine hydrobromide; 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester; Mandelytropeine; MFCD00067305

物化性质

• 密度: 1.21 g/cm3
• 沸点: 403.3ºC
• 熔点: 100ºC
• 分子式: C₁₆H₂₁NO₃
• 分子量: 275.34300
• 闪点: 197.7ºC
• 精确质量: 275.15200
• PSA: 49.77000
• LogP: 1.82630

生物活性

• 描述: 霍马托品是一种口服活性毒蕈碱乙酰胆碱受体拮抗剂,可用作抗胆碱药[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 >> 神经疾病
• 体外研究: 霍马托品(20μM)单独在豚鼠心房中产生的剂量比为259,与溴化六甲铵(HY-B0569)联合在豚鼠心房时产生的剂量率仅为95.0[1]。Homatropine与胃中的毒蕈碱受体(pA2=7.13)和心房中的毒鼠碱受体(p A2=7.21)具有亲和力,反应速率(p A2=7.07)[2]。
• 体内研究: 甲基溴化霍马托品(9 mm x 5 mm锥形栓剂)可迅速阻断迷走神经刺激对大鼠脉搏率和静脉注射乙酰胆碱对血压的影响[3]。动物模型：雄性白化大鼠[3]剂量：9 mm x 5 mm锥形栓剂给药：通过栓剂结果：阻断对迷走神经刺激和乙酰胆碱的心血管反应；插入栓剂后10-20分钟,在2-16Hz、5V范围内的迷走神经刺激对脉搏率的影响实际上被消除,并在45-60分钟保持不变。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : YM5600000 CHEMICAL NAME : 1-alpha-H,5-alpha-H-Tropan-3-alpha-ol, mandelate (ester) CAS REGISTRY NUMBER : 87-00-3 BEILSTEIN REFERENCE NO. : 0087959 LAST UPDATED : 199712 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C16-H21-N-O3 MOLECULAR WEIGHT : 275.38 WISWESSER LINE NOTATION : T56 A ANTJ A1 GOVYQR HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 180 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,156,1959 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1307 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2035763 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 370 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2035763 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1800 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2035763 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84350 No. of Facilities: 170 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 2582 (estimated)

安全

• 海关编码: 2933990090

合成路线

611-71-2 120-29-6 ~% 87-00-3

文献：Journal fuer Praktische Chemie (Leipzig), , vol. <2> 117, p. 147

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%