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息顿

息顿用途

奥普拉莫(Ensidon)是一种非典型的三环抗抑郁药(TCA)。奥普拉莫主要作为西格玛(σ)受体激动剂,可以与Ki值为50nM的西格玛识别位点有效相互作用。奥普拉莫可用于广泛性焦虑症(GAD)的研究[1][2]。

息顿名称

[ CAS 号 ]:
315-72-0

[ 中文名 ]:
奥匹哌醇

[ 英文名 ]:
opipramol

[中文别名 ]:

息顿

[英文别名 ]:

Opipramol
Insidon
Opipramolum [INN-Latin]
opipramol hydrochloride
[3H]-Opipramol
EINECS 206-254-0
Opipramol [INN:BAN]
Opipramol G
Nisidana
UNII-D23ZXO613C

息顿生物活性

[ 描述 ]:

[ 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 >> Sigma Receptor

[ 靶点 ]

Ki: 50 nM (σ receptor); IC50: 5.5 μM ([3H] DA)[1].

[体外研究]

Opipramol可以有效地与Ki值为50nM的sigma识别位点相互作用[1]。奥普拉莫抑制粗突触体制剂中[3H]DA的摄取,IC50值为5.5μM[1]。

[体内研究]

奥普拉莫(i.p.；5-50 mg/kg)增加体内多巴胺释放[2]。动物模型：Sprague Dawley大鼠(雄性,150-l 80 g)[2]剂量：5-50 mg/kg给药：腹腔注射结果：增加了大鼠纹状体中DOPAC和HVA的水平,而没有改变DA的稳态水平。有效地增加了大大鼠纹状体、嗅结节和梨状皮质中多巴胺的代谢。大鼠血浆催乳素增加,剂量仅为50 mg/kg。

息顿物理化学性质

[ 密度 ]:
1.129 g/cm3

[ 沸点 ]:
555.1ºC at 760 mmHg

[ 熔点 ]:
100-101ºC

[ 分子式 ]:
C₂₃H₂₉N₃O

[ 分子量 ]:
363.49600

[ 闪点 ]:
290.5ºC

[ 精确质量 ]:
363.23100

[ PSA ]:
29.95000

[ LogP ]:
3.24930

[ 折射率 ]:
1.6500 (estimate)

[ 储存条件 ]:
-20°C Freezer

息顿毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TL8750000

CHEMICAL NAME :: 1-Piperazineethanol, 4-(3-(5H-dibenz(b,f)azepin-5-yl)propyl)-

CAS REGISTRY NUMBER :: 315-72-0

BEILSTEIN REFERENCE NO. :: 0627076

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C23-H29-N3-O

MOLECULAR WEIGHT :: 363.55

WISWESSER LINE NOTATION :: T C676 BNJ B3- AT6N DNTJ D2Q

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 :: 1110 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 :: 95 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,560,1964

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 497 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,560,1964

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 32 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,560,1964

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 181,68,1969

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,560,1964

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 315 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,560,1964

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,560,1964

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 11 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,560,1964

息顿安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H410

[ 警示性声明 ]:
P273-P501

[ 危害码 (欧洲) ]:
Xn,N

[ 风险声明 (欧洲) ]:
22-50/53

[ 安全声明 (欧洲) ]:
60-61

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ RTECS号 ]:
TL8750000

[ 海关编码 ]:
2933990090

息顿海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

息顿文献

Visuo-spatial memory deficits following medial temporal lobe damage: A comparison of three patient groups.

Neuropsychologia 81 , 168-79, (2016)

The contributions of the hippocampal formation and adjacent regions of the medial temporal lobe (MTL) to memory are still a matter of debate. It is currently unclear, to what extent discrepancies betw...

更多文献

息顿