4317-14-0

• 常用中文名：Amitriptylinoxide
• 常用英文名：Amitriptylinoxide
• CAS号：4317-14-0
• 分子式：C₂₀H₂₃NO
• 分子量：293.40
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 5-HT受体
• 发布时间：2017-02-08 18:33:05
• 更新时间：2024-01-02 20:30:08
• 阿米替林氧化物(Equilibrin)是阿米替林的类似物和代谢产物,具有类似的抗抑郁功效[1]。

名称

• 英文名: amitriptyline N-oxide
• 英文别名: amitriptyline-N-oxide; amitriptylinoxide; 5-(3-Dimethylaminopropyliden)dibenzo<a.d>cycloheptan-N-oxid; Amitriptylinoxide (inn); Amitriptylin-N-oxid

物化性质

• 分子式: C₂₀H₂₃NO
• 分子量: 293.40
• 精确质量: 293.17800
• PSA: 29.43000
• LogP: 4.20210

生物活性

• 描述: 阿米替林氧化物(Equilibrin)是阿米替林的类似物和代谢产物,具有类似的抗抑郁功效[1]。
• 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
• 参考文献:

  [1]. J Tegeler, et al. Double-blind study of the therapeutic efficacy and tolerability of amitriptylinoxide in comparison with amitriptyline. Pharmacopsychiatry. 1990 Jan;23(1):45-9.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : HO9550000 CHEMICAL NAME : 5H-Dibenzo(a,d)cycloheptene-delta(sup 5),gamma-propylamine, 10,11-dihydro-N,N-dimethyl-N- oxide CAS REGISTRY NUMBER : 4317-14-0 LAST UPDATED : 199612 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C20-H23-N-O MOLECULAR WEIGHT : 293.44 WISWESSER LINE NOTATION : L C676 BY&T&J BU3KO&1&1 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 : 1800 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 110 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 25 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 330 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 320 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 87 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 330 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 330 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 330 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3600 mg/kg/4W-I TOXIC EFFECTS : Liver - fatty liver degeneration Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 36500 mg/kg/1Y-C TOXIC EFFECTS : Liver - fatty liver degeneration Endocrine - changes in thyroid weight REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 24640 mg/kg/1Y-I TOXIC EFFECTS : Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2500 mg/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 28,1898,1978

合成路线

50-48-6 ~% 4317-14-0

文献：Gowda, Narendra B.; Rao, Gopal Krishna; Ramakrishna, Ramesha A. Tetrahedron Letters, 2010 , vol. 51, # 43 p. 5690 - 5693

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