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113-53-1

113-53-1结构式

常用中文名：度硫平
常用英文名：(E)-Dosulepin
CAS号：113-53-1
分子式：C₁₉H₂₁NS
分子量：295.44
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：2018-05-26 08:00:00
更新时间：2024-01-02 20:22:32
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]。

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中文名	度琉平
英文名	dothiepin
中文别名	度硫平
英文别名	1-Propanamine, 3-dibenzo[b,e]thiepin-11(6H)-ylidene-N,N-dimethyl-, (3E)- 11-(3-Dimethylamino-propyliden)-6,11-dihydro-dibenzo<b.e>thiepin Methiaden Dothiepin Dolsulepine Dosulepin Prothiadene Dosulepine 11-(3-Dimethylaminopropylidene)-6,11-dihydrodibenzo(b,e)thiepin (3E)-3-(Dibenzo[b,e]thiepin-11(6H)-ylidene)-N,N-dimethyl-1-propanamine досулепин iz914 Dothep trans-dothiepin Prothiaden 11(16H)-(3-[dimethylamino]propylidene)dibenz[b,e]thiopine EINECS 204-031-2

描述	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]。
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.

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
分子结构	1、摩尔折射率：95.07 2、摩尔体积（cm³/mol）：257.2 3、等张比容（90.2K）：687.4 4、表面张力（dyne/cm）：50.9 5、极化率（10-24cm3）：37.68

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

危险品运输编码	UN 3249
包装等级	III
危险类别	6.1(b)

1531-85-7结构式

1531-85-7

~%

113-53-1结构式

113-53-1

文献：WO2007/136743 A2, ; Page/Page column 20-21 ;

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