5118-29-6

• 常用中文名：美利蒽
• 常用英文名：Melitracen
• CAS号：5118-29-6
• 分子式：C₂₁H₂₅N
• 分子量：291.43000
• 相关类别： 原料药 神经系统用药 抗抑郁、躁狂药
• 发布时间：2018-09-27 13:51:46
• 更新时间：2024-01-12 18:30:18
• 美利曲辛(Melitracene)是一种口服活性三环抗抑郁药,也是一种具有激活特性的双极性胸腺肽。美利曲辛抑制3H-5-HT和14H-5-HT,IC50分别为670nm和5500nm。美利曲辛可用于研究抑郁和焦虑[1][2]。

名称

• 中文名: 美利蒽
• 英文名: 3-(10,10-dimethylanthracen-9-ylidene)-N,N-dimethylpropan-1-amine
• 中文别名: 二甲胺丙烯蒽; 3-[10,10-二甲基-9(10H)-蒽亚基]-N,N-二甲基-1-丙胺
• 英文别名: Melitracen; Melitracene; Adaptol; Thymeol; Trausabun; Meltiracene; 9.9-Dimethyl-10-<3-dimethylamino-propyliden>-9.10-dihydro-anthracen; Dixeran

物化性质

• 密度: 1.046g/cm3
• 沸点: 399.1ºC at 760mmHg
• 分子式: C₂₁H₂₅N
• 分子量: 291.43000
• 闪点: 174.4ºC
• 精确质量: 291.19900
• PSA: 3.24000
• LogP: 4.70930
• 折射率: 1.4900 (estimate)
• 储存条件: 库房通风低温干燥,与食品原料分开存放

生物活性

• 描述: 美利曲辛(Melitracene)是一种口服活性三环抗抑郁药,也是一种具有激活特性的双极性胸腺肽。美利曲辛抑制3H-5-HT和14H-5-HT,IC50分别为670nm和5500nm。美利曲辛可用于研究抑郁和焦虑[1][2]。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 靶点:

  IC50: 670 nM (3H-5-HT), 5500 nM (14H-5-HT)[2]

• 体外研究: 美利曲辛(0-10μM；10分钟)抑制突触体中的3H-5-HT和血小板中的14H-5-HT[2]。细胞活力测定[2]细胞系：雄性白化大鼠的突触体和血小板浓度：0-10μM孵育时间：10分钟结果：突触体中的3H-5-HT和血小板中的14H-5-HT分别受到抑制,IC50分别为670 nM和5500 nM。
• 体内研究: 美利曲辛(10-90 mg/kg；每日口服3个月)影响大鼠的行为、体重和生长[1]。动物模型：雄性和雌性Wistar大鼠[1]剂量：10、30和90mg/kg给药：口服灌胃；每日10-90mg/kg；3个月的结果：随着剂量的增加,大鼠表现出攻击性行为、兴奋性、身体和肝脏重量增加,肝脏轻微萎缩。
• 参考文献:

  [1]. Shimamoto K, et al. Relationship between the restriction of food intake and Melitracen, an antidepressant, in the rat. Acta Sch Med Univ Kioto. 1967 Jul;40(1):25-37.

  [2]. Hyttel J. Effect of a specific 5-HT uptake inhibitor, citalopram (Lu 10-171), on 3H-5-HT uptake in rat brain synaptosomes in vitro. Psychopharmacology (Berl). 1978 Dec 15;60(1):13-8. doi: 10.1007/BF00429172. PMID: 104340.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : CB0770000 CHEMICAL NAME : delta-(sup 9(10),gamma)-Anthracenepropylamine, N,N,10,10-tetramethyl- CAS REGISTRY NUMBER : 5118-29-6 LAST UPDATED : 199612 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C21-H25-N MOLECULAR WEIGHT : 291.47 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 : FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970 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 : FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970 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 : FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970 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 : FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970 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 : FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970

安全

• 海关编码: 2921499090

合成路线

5447-86-9 109-54-6 ~% 5118-29-6

文献：Holm,T. Acta Chemica Scandinavica (1947-1973), 1963 , vol. 17, p. 2437 - 2443

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海关

海关编码	2921499090
中文概述	2921499090 其他芳香单胺及衍生物及它们的盐. 增值税率:17.0% 退税率:9.0% 监管条件:无 最惠国关税:6.5% 普通关税:30.0%
申报要素	品名, 成分含量, 用途
Summary	2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%