7456-24-8

• 常用中文名：二甲替嗪
• 常用英文名：Dimetotiazine
• CAS号：7456-24-8
• 分子式：C₁₉H₂₅N₃O₂S₂
• 分子量：391.55100
• 相关类别： 原料药 抗变态反应药 抗组胺药
• 发布时间：2018-07-12 10:21:52
• 更新时间：2024-01-13 22:07:43
• 二甲噻嗪(Dimethothiazine,Dimetotiazine；Fonazine)是一种口服活性三环抗组胺、抗5-羟色胺药物,对去脑强直有很高的活性,具有轻微的镇静作用和催眠作用。二甲噻嗪可以减少或消除去脑猫的静态和动态纺丝运动对肌梭的影响。二甲噻嗪可用于研究偏头痛和痉挛[1][2][3]。

名称

• 中文名: 二甲替嗪
• 英文名: 10-[2-(dimethylamino)propyl]-N,N-dimethylphenothiazine-2-sulfonamide
• 英文别名: dimethothiazine; FONAZINE; Dimetiotazine; Dimethodin; 10-(2-dimethylamino-propyl)-10H-phenothiazine-2-sulfonic acid dimethylamide; Dimetotiazinum [INN-Latin]; N,N-Dimethyl-10-(2-dimethylaminopropyl)-phenothiazin-2-sulfonamide; Dimetotiazine; Dimetotiazine [INN:BAN]; Bayer 1483; Dimetotiazina [INN-Spanish]; Dimetiotazin; Dimethothiazin

物化性质

• 密度: 1.235g/cm3
• 沸点: 533.7ºC at 760 mmHg
• 分子式: C₁₉H₂₅N₃O₂S₂
• 分子量: 391.55100
• 闪点: 276.6ºC
• 精确质量: 391.13900
• PSA: 77.54000
• LogP: 4.63550
• 折射率: 1.612

生物活性

• 描述: 二甲噻嗪(Dimethothiazine,Dimetotiazine；Fonazine)是一种口服活性三环抗组胺、抗5-羟色胺药物,对去脑强直有很高的活性,具有轻微的镇静作用和催眠作用。二甲噻嗪可以减少或消除去脑猫的静态和动态纺丝运动对肌梭的影响。二甲噻嗪可用于研究偏头痛和痉挛[1][2][3]。
• 相关类别:
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
• 靶点:

  Histamine, 5-HT[1]

• 体内研究: 二甲噻嗪(0.5-16 mg/kg；静脉注射；单剂量)可降低猫的去脑强直[2]。动物模型：猫(去脑模型；颈动脉被夹闭,大脑中段大约在丘之间)[2]剂量：0.5、1、2、4、8和16 mg/kg,静脉注射。；单剂量结果：一级和二级终末的放电频率降低了1-4mg/kg。在准备完整的腹根时,降低了肌梭拉伸的敏感性。降低了动态熔断器纤维的活性。
• 参考文献:

  [1]. Nattero G, et al. Use of dimethothiazine in the prevention of hemicrania. Minerva Med. 1977 Mar 17;68(13):839-45.

  [2]. Maxwell DR, Rhodes KF. The effects of dimethothiazine on muscle spindle activity in the decerebrate cat. Br J Pharmacol. 1970 Jul;39(3):520-32.

  [3]. Griffiths MI, et al. The use of dimethothiazine in the treatment of childhood cerebral palsy. Dev Med Child Neurol. 1973 Feb;15(1):25-32.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : SP5250000 CHEMICAL NAME : Phenothiazine-2-sulfonamide, 10-(2-(dimethylamino)propyl)-N,N-dimethyl- CAS REGISTRY NUMBER : 7456-24-8 LAST UPDATED : 199612 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C19-H25-N3-O2-S2 MOLECULAR WEIGHT : 391.59 WISWESSER LINE NOTATION : T C666 BN ISJ B1Y1&N1&1 ESWN1&1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 740 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 190 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 475 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 100 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 600 mg/kg SEX/DURATION : female 9-14 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 4,381,1970