10563-70-9

• 常用中文名：Melitracen hydrochloride
• 常用英文名：Melitracen hydrochloride
• CAS号：10563-70-9
• 分子式：C₂₁H₂₆ClN
• 分子量：327.891
• 相关类别： 原料药 神经系统用药 抗抑郁、躁狂药
• 发布时间：2018-03-24 08:00:00
• 更新时间：2024-01-02 10:01:41
• Melitracen hydrochloride 是一种具有口服活性的双相抗抑郁药和抗焦虑药。Melitracen hydrochloride 可以通过突触前膜抑制 Norepinephrine 和 5-HT (5-羟色胺) 的吸收,从而诱导突触空间中单胺递质的增加。

名称

• 中文名: 盐酸美利蒽
• 英文名: 3-(10,10-dimethylanthracen-9-ylidene)-N,N-dimethylpropan-1-amine,hydrochloride
• 中文别名: 盐酸美利曲辛; 3-[10,10-二甲基-9(10H)-蒽亚基]-N,N-二甲基丙胺盐酸盐
• 英文别名: 3-(10,10-Dimethyl-9(10H)-anthracenylidene)-N,N-dimethyl-1-propanamine Hydrochloride; 9,10-Dihydro-10,10-dimethyl-9-(3-dimethylaminopropylidene)anthracene Hydrochloride; U 24973A; EINECS 234-150-5; Thymeol hydrochloride; N,N-Dimethyl-3-(10,10-dimethyl-9(10H)-anthrylidene)propylamine Hydrochloride; 3-(10,10-Dimethyl-9(10H)-anthracenylidene)-N,N-dimethyl-1-propanamine hydrochloride (1:1); 9-[3-(Dimethylamino)propylidene]-10,10-dimethyl-9,10-dihydroanthracene Hydrochloride; Dixeran; Melitracene hydrochloride; U-24,973A; MELITRACEN HYDROCHLORIDE; Melitracen HCl; 3-(10,10-Dimethylanthracen-9(10H)-ylidene)-N,N-dimethylpropan-1-amine hydrochloride (1:1); N 7001; Trausabun; N,N,10,10-Tetramethyl-D9(10H),g-anthracenepropylamine Hydrochloride; 1-Propanamine, 3-(10,10-dimethyl-9(10H)-anthracenylidene)-N,N-dimethyl-, hydrochloride (1:1)

物化性质

• 密度: 1.046 g/cm3
• 沸点: 399.1ºC at 760 mmHg
• 熔点: 245-248ºC
• 分子式: C₂₁H₂₆ClN
• 分子量: 327.891
• 闪点: 174.4ºC
• 精确质量: 327.175385
• PSA: 3.24000
• LogP: 5.51130
• 外观性状: 结晶固体
• 蒸汽压: 1.4E-06mmHg at 25°C
• 折射率: 1.607
• 储存条件: Refrigerator

生物活性

• 描述: Melitracen hydrochloride 是一种具有口服活性的双相抗抑郁药和抗焦虑药。Melitracen hydrochloride 可以通过突触前膜抑制 Norepinephrine 和 5-HT (5-羟色胺) 的吸收,从而诱导突触空间中单胺递质的增加。
• 相关类别:
  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
• 靶点:

  5-HT receptor[1]

• 体内研究: 单次口服丙咪嗪或美利曲嗪可使小鼠出现明显且持久的瞳孔扩大。美利曲辛的散瞳作用更显著,持续时间更长。美利他嗪对行为兴奋更有效。单次口服美利曲辛可降低脑干、大脑皮层、脾脏和肾上腺中的儿茶酚胺水平[2]。每日给药13周和15周后,大鼠脑干、大脑皮层和脾脏儿茶酚胺水平均未见明显变化。然而,肾上腺中的肾上腺素水平略有下降[2]。
• 参考文献:

  [1]. Xiaoqian Zhou , et al. The Efficacy of Flupentixol-Melitracen in the Adjuvant Therapy of Ulcerative Colitis in the Chinese Population: A Meta-Analysis. Gastroenterol Res Pract. 2019 Feb 28;2019:3480732.

  [2]. K Shimamoto, et al. Myriatic Effect of 9-(gamma-dimethylamino-propylidene)-10, 10-diemthyl-9, 10-dihydroanthracene Hydrochloride (Melitracen) in Mice and Rats. Acta Sch Med Univ Kioto. 1967 Jul;40(1):38-47.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : CB0875000 CHEMICAL NAME : delta(sup 9(10H)),gamma-Anthracenepropylamine, N,N,10,10-tetramethyl-, hydrochloride CAS REGISTRY NUMBER : 10563-70-9 LAST UPDATED : 199604 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C21-H25-N.Cl-H MOLECULAR WEIGHT : 327.93 WISWESSER LINE NOTATION : L C666 BY IHJ BU3N1&1 I1 I1 &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 : 170 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: -,80,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 96 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: -,80,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 760 mg/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: 3,390,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 315 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: -,80,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 131 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: -,80,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 275 mg/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: 3,390,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 52 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 24,121,1966