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马来酸三甲丙咪嗪

马来酸三甲丙咪嗪用途

Trimipramine maleate 是 5-HT 受体的拮抗剂,其对 5-HT1C,5-HT2 和 5-HT1A 受体的 pKi 值分别为 6.39,8.10,4.66。

马来酸三甲丙咪嗪名称

[ CAS 号 ]:
521-78-8

[ 中文名 ]:
马来酸三甲丙咪嗪

[ 英文名 ]:
Trimipramine maleate

[英文别名 ]:

UNII:269K6498LD
Trimipramine maleate
Trimipramine maleate salt
UNII:D28E1043W5
Trimipramine
UNII:I412286V22

马来酸三甲丙咪嗪生物活性

[ 描述 ]:

Trimipramine maleate 是 5-HT 受体的拮抗剂,其对 5-HT1C,5-HT2 和 5-HT1A 受体的 pKi 值分别为 6.39,8.10,4.66。

[ 相关类别 ]:

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

研究领域 >> 神经疾病

[ 靶点 ]

5-HT1C Receptor:6.39 (pKi)

5-HT2 Receptor:8.10 (pKi)

5-HT1A Receptor:4.66 (pKi)

[体外研究]

Trimipramine对5-HT2的亲和力高于对5-HT1C受体的亲和力[1]。

[体内研究]

由渗透微型泵在14天内递送的长效给予Trimipramine(5mg/kg /天)产生5-HT区域浓度的显着增加。额叶皮质和海马的增加最多,其次是嗅结节和下丘脑。 Trimipramine治疗也可使脑5-HIAA浓度显着增加,范围从海马中的63％到伏隔核中的25％,具有下丘脑,嗅结节,额叶皮质和伏隔核的中间值。 Trimipramine治疗使伏隔核,纹状体和嗅结节中的DA浓度显着增加,分别达到43％,21％和11％。 Trimipramine的慢性给药使额叶皮层5-HT2和纹状体DA D2受体的数量显着减少。长期服用Trimipramine会使大脑区域单胺和代谢物水平增加,表明DA和5-HT的合成率更高,与5-HT2和DA D2受体的适应性下调相一致[2]。

[动物实验]

大鼠[2]使用在实验开始时重220-250g的雄性Wistar大鼠。以6-8只为一组的动物可自由获取食物和水，并在一个温度下保持12小时光照/黑暗循环（在6a.m.开灯）。用戊巴比妥（50mg / kg ip）麻醉大鼠，并在背侧胸椎间区域皮下植入渗透性微型泵。每个泵输送5 mg / kg /天的Trimipramine或阿米替林。对照大鼠植入填充有0.9％盐水的泵。泵中溶液的总体积足以供药至少14天。植入后，切开并缝合切口，动物保持温暖直至从麻醉中恢复[2]。

[参考文献]

[1]. Jenck F, et al. Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs. Eur J Pharmacol. 1993 Feb 9;231(2):223-9.

[2]. Juorio AV, et al. The effects of chronic trimipramine treatment on biogenic amine metabolism and on dopamine D2, 5-HT2 and tryptamine binding sites in rat brain. Gen Pharmacol. 1990;21(5):759-62.

[相关活性小分子]

马来酸三甲丙咪嗪物理化学性质

[ 密度 ]:
1.029g/cm3

[ 沸点 ]:
411.8ºC at 760mmHg

[ 熔点 ]:
141-143ºC

[ 分子式 ]:
C₂₄H₃₀N₂O₄

[ 分子量 ]:
410.506

[ 闪点 ]:
183.3ºC

[ 精确质量 ]:
410.220551

[ PSA ]:
81.08000

[ LogP ]:
3.89780

[ 储存条件 ]:
2-8℃

马来酸三甲丙咪嗪MSDS

详细MSDS(安全技术说明书)

马来酸三甲丙咪嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HN9260000

CAS REGISTRY NUMBER :: 521-78-8

LAST UPDATED :: 199806

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C20-H26-N2.C4-H4-O4

MOLECULAR WEIGHT :: 410.56

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 :: 800 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 :: 150 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 308 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 :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 38 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 425 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,526,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 140 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 240 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 40 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 223 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,876,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 27 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 25,158,1965 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 85 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - Central Nervous System

REFERENCE :: DGDFA5 Development, Growth & Differentiation. (Japan Pub. Trading Co. (USA), 1255 Howard St., San Francisco, CA 94103) V.11- 1969- Volume(issue)/page/year: 22,61,1980

马来酸三甲丙咪嗪安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335-H361

[ 警示性声明 ]:
P280-P301 + P312 + P330-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn,T,F

[ 风险声明 (欧洲) ]:
22-36/37/38-63-36/38-23/25

[ 危险品运输编码 ]:
UN 3249

[ RTECS号 ]:
HN9260000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

马来酸三甲丙咪嗪文献

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