度硫平

度硫平用途

Dothiepin是一种具有镇静/抗焦虑活性的抗抑郁药。多蒂平是一种抑制剂,它更喜欢去甲肾上腺素的摄取,而不是血清素的摄取。多蒂平通过抑制神经元摄取促进去甲肾上腺素能神经传递。多蒂平也是组胺H1受体的拮抗剂,没有心脏毒性。Dothiepin在心因性面部疼痛、特发性纤维肌痛综合征或类风湿性关节炎中表现出显著的镇痛活性[1]。

度硫平名称

[ CAS 号 ]:
113-53-1

[ 中文名 ]:
度琉平

[ 英文名 ]:
(E)-Dosulepin

[中文别名 ]:

度硫平

[英文别名 ]:

Methiaden
Dothiepin
Dolsulepine
Dosulepin
Prothiadene
Dosulepine
досулепин
iz914
Dothep
trans-dothiepin

度硫平生物活性

[ 描述 ]:

[ 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 H1-receptor, Noradrenaline uptake (α1-and α2-adrenoceptors and serotonin 5HT1 and 5HT2-receptors)[1]

[参考文献]

[1]. Lancaster SG, et al. Dothiepin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs. 1989 Jul;38(1):123-47.

度硫平物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
430.9±44.0 °C at 760 mmHg

[ 熔点 ]:
55-57ºC

[ 分子式 ]:
C₁₉H₂₁NS

[ 分子量 ]:
295.44

[ 闪点 ]:
214.4±28.4 °C

[ 精确质量 ]:
295.139465

[ PSA ]:
28.54000

[ LogP ]:
4.34

[ 外观性状 ]:
淡黄色低熔点固体

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.661

度硫平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UI1555000

CHEMICAL NAME :: Propylamine, N,N-dimethyl-3-(dibenzo(b,e)thiepin-delta-sup(11(6H), gamma))-

CAS REGISTRY NUMBER :: 113-53-1

LAST UPDATED :: 199712

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C19-H21-N-S

MOLECULAR WEIGHT :: 295.47

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

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Cardiac - arrhythmias (including changes in conduction)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 4500 ug/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 3214 ug/kg/12D-I

TOXIC EFFECTS :: Behavioral - changes in psychophysiological tests

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 2143 ug/kg/8D-I

TOXIC EFFECTS :: Behavioral - sleep Behavioral - hallucinations, distorted perceptions Behavioral - changes in psychophysiological tests

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 150 mg/kg

SEX/DURATION :: male 6 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

REFERENCE :: ACNSAX Activitas Nervosa Superior. (Avicenum, Malostranske nam. 28, Prague 1, Czechoslovakia) V.1- 1959- Volume(issue)/page/year: 15,114,1973

度硫平

度硫平用途

度硫平名称

度硫平生物活性

度硫平物理化学性质

度硫平毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

度硫平安全信息

度硫平合成路线

详细合成路线

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