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多虑平

多虑平用途

多塞平作为三环类抗抑郁药,可抑制5-羟色胺和去甲肾上腺素的再摄取。多塞平对特应性皮炎、慢性荨麻疹有治疗作用,可改善认知过程,保护中枢神经系统。多塞平也被认为是对抗氧化应激的保护因子[1][2][3]。

多虑平名称

[ CAS 号 ]:
1668-19-5

[ 中文名 ]:
多虑平

[ 英文名 ]:
Doxepin

[中文别名 ]:

多塞平

[英文别名 ]:

Quitaxon
Aponal
P-3693A
Doxepine
Curatin
Docepin

多虑平生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> PI3K/Akt/mTOR 信号通路 >> mTOR

信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K

信号通路 >> PI3K/Akt/mTOR 信号通路 >> AKT

研究领域 >> 神经疾病

[体外研究]

多塞平的保护作用与通过PI3K/AKT/mTOR信号通路增强PSD-95和突触蛋白1表达有关[4]。Western Blot分析[4]细胞系：SH-SY5Y人神经母细胞瘤细胞系浓度：10ng/mL孵育时间：2h结果：提高了SH-SY5 Y细胞中PSD-95、突触蛋白1和p-AKT的蛋白表达水平,降低了SH-SY5Y细胞中p-mTOR的蛋白表达。

[体内研究]

多塞平(每天一次腹腔注射1mg/kg和5mg/kg多塞平,持续21天)可保护大鼠免受aβ1-42诱导的记忆损伤[4]。动物模型：SD雄性大鼠[4]剂量：1,5mg/kg给药：多塞平(腹腔注射1mg/kg和5mg/kg多塞平,每日一次,共21天)结果：1 mg/kg多塞平治疗后,改善海马和颞叶中PSD-95和突触蛋白1的蛋白表达水平,降低海马和颞叶中p-AKT的蛋白表达。

[参考文献]

[1]. AnnemiekVermeeren, et al. Effects of the use of hypnotics on cognition. Progress in brain research vol. 190 (2011): 89-103.

[2]. G Hajak, et al. Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study. The Journal of clinical psychiatry vol. 62,6 (2001): 453-63.

[3]. Mahsa Gharzi, et al. Effects of different doses of doxepin on passive avoidance learning in rats. Advanced biomedical research vol. 2 66. 30 Jul. 2013.

[4]. Jimei Bu, et al. Mechanism underlying the effects of doxepin on β-amyloid -induced memory impairment in rats. Iran J Basic Med Sci. 2017 Sep;20(9):1044-1049.

多虑平物理化学性质

[ 密度 ]:
1.122 g/cm3

[ 沸点 ]:
413.3ºC at 760 mmHg

[ 熔点 ]:
187-189ºC

[ 分子式 ]:
C₁₉H₂₁NO

[ 分子量 ]:
279.37600

[ 闪点 ]:
121.3ºC

[ 精确质量 ]:
279.16200

[ PSA ]:
12.47000

[ LogP ]:
3.96240

[ 外观性状 ]:
白色结晶固体

[ 蒸汽压 ]:
4.87E-07mmHg at 25°C

[ 折射率 ]:
1.5000 (estimate)

[ 储存条件 ]:
Store at RT

多虑平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HQ4300000

CHEMICAL NAME :: Dibenz(b,e)oxepin-delta(sup 11(6H)),gamma-propylamine, N,N-dimethyl-

CAS REGISTRY NUMBER :: 1668-19-5

LAST UPDATED :: 199107

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C19-H21-N-O

MOLECULAR WEIGHT :: 279.41

WISWESSER LINE NOTATION :: T C676 BY IO JHJ BU3N1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - bronchiectasis

REFERENCE :: CTOXAO Clinical Toxicology. (New York, NY) V.1-18, 1968-81. For publisher information, see JTCTDW. Volume(issue)/page/year: 10,327,1977

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 147 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic 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: 15,863,1965

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 182 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic 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: 15,863,1965

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 16 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic 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: 15,863,1965

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 135 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic 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: 15,863,1965

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 79 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic 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: 15,863,1965

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 26 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic 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: 15,863,1965

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 11 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic 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: 15,863,1965

多虑平安全信息

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
25

[ 安全声明 (欧洲) ]:
36/37/39-45

[ 海关编码 ]:
2932999099

多虑平合成路线

详细合成路线

多虑平上下游产品

多虑平上游产品

多虑平下游产品

多虑平制备

三苯膦和1，3-二溴丙烷反应制得3-溴丙基溴化三苯膦，继续与无水二甲胺反应，得到3-二甲氨基丙基溴化苯三膦氢酸盐，再与6，11-二氢二苯并[b，e]噁庚-11-酮反应，得到多虑平。中间体6，11-二氢二苯并[b，e]噁庚-11-酮的合成方法可参见Belg.pat，641498

多虑平海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧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

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

多虑平