524-83-4

• 常用中文名：乙苯托品
• 常用英文名：Ethybenztropine
• CAS号：524-83-4
• 分子式：C₂₂H₂₇NO
• 分子量：321.45600
• 相关类别： 原料药 神经系统用药 拟胆碱药
• 发布时间：2018-03-21 08:00:00
• 更新时间：2024-01-02 17:58:19
• 乙苯并托品(Ponalid)是一种毒蕈碱受体阻滞剂。乙苯托品是一种抗胆碱能和抗组胺能药物[1]。

名称

• 中文名: 乙苯托品
• 英文名: Etybenzatropine
• 英文别名: Ponalide; UK-738; ethybenztropine; VK-738; Ethylbenatropine

物化性质

• 密度: 1.1g/cm3
• 沸点: 422.8ºC at 760mmHg
• 分子式: C₂₂H₂₇NO
• 分子量: 321.45600
• 闪点: 124ºC
• 精确质量: 321.20900
• PSA: 12.47000
• LogP: 4.74580
• 折射率: 1.597

生物活性

• 描述: 乙苯并托品(Ponalid)是一种毒蕈碱受体阻滞剂。乙苯托品是一种抗胆碱能和抗组胺能药物[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 >> 神经疾病
• 靶点:

  Muscarinic Receptor[1]

• 体外研究: 乙苯托品(10μM)抑制新纹状体切片中3H-DA的摄取。
• 体内研究: 乙苯并托品(25μg,中脑NRM微量注射)阻断家兔中缝正中核(NRM)微量注射卡巴胆碱的高热反应[1]。乙苯托品(30-60μg/kg,由第四脑室给药)可有效预防犬心律失常[2]。乙苯托品(50 mg/kg,i.p.)可减少大鼠体内儿茶酚胺的积累[3]。动物模型：心律失常犬[2]剂量：30-60μg/kg给药：第四脑室给药结果：产生轻微低血压(从未超过25mm Hg的下降)和轻微窦性心动过速。心律失常转为窦性心律。
• 参考文献:

  [1]. A K Saxena, et al. Presence of cholinoceptors in mesencephalic raphe nuclei concerned in thermoregulation in rabbits. Clin Exp Pharmacol Physiol. 1984 Mar-Apr;11(2):105-10.

  [2]. M Rozear, et al. Effects of intracerebroventricular l-hyoscyamine, ethybenztropine and procaine on cardiac arrhythmias induced in dogs by pentylenetetrazol, picrotoxin or deslanoside. Int J Neuropharmacol. 1968 Jan;7(1):1-6.

  [3]. LARS-OVE FARNEBO, et al. Effect of some antiparkinsonian drugs on catecholamine neurons. Journal of Pharmacy and Pharmacology, 1970, 22(10): 733-737.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : RD0525000 CHEMICAL NAME : Nortropane, 3-(diphenylmethoxy)-8-ethyl- CAS REGISTRY NUMBER : 524-83-4 LAST UPDATED : 199712 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C22-H27-N-O MOLECULAR WEIGHT : 321.50 WISWESSER LINE NOTATION : T56 A ANTJ A2 GOYR&R HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 560 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,228,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 18500 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FMXXAJ French Medicament Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Discontinued. Volume(issue)/page/year: #2235M TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 66 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,228,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 12 mg/kg TOXIC EFFECTS : Autonomic Nervous System - parasympatholytic REFERENCE : EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967- Volume(issue)/page/year: 9,304,1970 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 215 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,228,1972 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 6 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,228,1972

安全

• 海关编码: 2933990090

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%