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丙咪嗪盐酸盐

丙咪嗪盐酸盐用途

Imipramine hydrochloride抑制血清素转运蛋白(serotonin),体内试验的IC50值为32 nM.

丙咪嗪盐酸盐名称

[ CAS 号 ]:
113-52-0

[ 中文名 ]:
盐酸丙咪嗪

[ 英文名 ]:
Imipramine hydrochloride

[中文别名 ]:

咪帕明

[英文别名 ]:

Janimine (hydrochloride)
Imipramine hydrochloride
MFCD00012669
EINECS 204-030-7
Melipramine hydrochloride
Melipramine HCl
Tofranil (hydrochloride)
Imipraminehydrochloride
Imipramine (hydrochloride)

丙咪嗪盐酸盐生物活性

[ 描述 ]:

Imipramine hydrochloride抑制血清素转运蛋白(serotonin),体内试验的IC50值为32 nM.

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> 5-羟色胺转运蛋白

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 32 nM (serotonin)[1]

[体外研究]

类似抑郁症的行为常常因慢性疼痛而复杂化。包括丙咪嗪在内的抗抑郁药被广泛用于治疗慢性疼痛,但其机制尚不完全清楚[2]。发现丙咪嗪(IC50 = 32 nM)和地昔帕明(IC50 = 160 nM)是人胎盘5-羟色胺转运蛋白的有效抑制剂[1]。

[体内研究]

丙咪嗪的施用逆转了社会回避行为,显着增加了交互时间。 RSD小鼠中24天的丙咪嗪治疗可显着降低脑小胶质细胞中应激诱导的IL-6 mRNA水平[3]。慢性轻度应激诱导前额皮质的长期改变基因表达谱,部分通过丙咪嗪治疗(10mg/kg,ip)恢复[4]。慢性丙咪嗪给药改变了大脑中的氨基酸动力学。在纹状体中,通过慢性丙咪嗪给药,天冬酰胺,谷氨酰胺和蛋氨酸的浓度显着增加。在丘脑和下丘脑中,慢性丙咪嗪给药显着降低了缬氨酸浓度[5]。丙咪嗪减轻疼痛相关的负性情绪而不影响疼痛,并且通过5-HT神经元的去神经支配和抗BDNF治疗减少了这种效应。丙咪嗪还使ERK/CREB偶联的紊乱正常化,这导致BDNF的诱导。这表明5-HT和BDNF之间可能存在相互作用[2]。丙咪嗪治疗抵消了皮质酮给药诱导的大鼠CA3海马回路对5-HT受体活化反应性的增加[6]。

[动物实验]

大鼠：Wistar（WIS）和Wistar Kyoto（WKY）大鼠分为四组：（1）对照WIS大鼠组，（2）丙咪嗪治疗的WIS大鼠组，（3）对照WKY大鼠组和（3） 4）丙咪嗪治疗的WKY大鼠组。口服给药蒸馏水（10mL / kg）或丙咪嗪溶液（10mg / 10mL / kg）28天，除了在旷场测试当天，没有给药以避免单次给药的急性效果在开放场测试[5]。小鼠：经历反复社交失败（RSD），家庭笼控制（HCC）的C57BL / 6小鼠随机选择成四组：RSD /丙咪嗪，RSD /媒介物，HCC /丙咪嗪和HCC /媒介物。在RSD的6个周期后，RSD /丙咪嗪中的小鼠每天腹膜内（ip）注射丙咪嗪（20mg / kg）24天。 HCC /丙咪嗪以相同剂量每日接受ip丙咪嗪，而RSD /载体和HCC /载体组在同一时间点腹膜内注射载体（氯化钠，0.9％）24天[3]。

[参考文献]

[1]. Balkovetz DF, et al. Evidence for an imipramine-sensitive serotonin transporter in human placental brush-border membranes. J Biol Chem. 1989 Feb 5;264(4):2195-8.

[2]. Yasuda S, et al. Imipramine ameliorates pain-related negative emotion via induction of brain-derived neurotrophic factor. Cell Mol Neurobiol. 2014 Nov;34(8):1199-208.

[3]. Ramirez K, et al. Imipramine attenuates neuroinflammatory signaling and reverses stress-induced social avoidance. Brain Behav Immun. 2015 May;46:212-20.

[4]. Erburu M, et al. Chronic mild stress and imipramine treatment elicit opposite changes in behavior and in gene expression in the mouse prefrontal cortex. Pharmacol BiochemBehav. 2015 Aug;135:227-36.

[5]. Nagasawa M, et al. Chronic imipramine treatment differentially alters the brain and plasma amino acid metabolism in Wistar and Wistar Kyoto rats. Eur J Pharmacol. 2015 Sep 5;762:127-35.

[6]. Tokarski K, et al. Imipramine counteracts corticosterone-induced alterations in the effects of the activation of 5-HT(7) receptors in rat hippocampus. J Physiol Pharmacol. 2009 Jun;60(2):83-8.

[相关活性小分子]

丙咪嗪盐酸盐物理化学性质

[ 密度 ]:
1.041g/cm3

[ 沸点 ]:
403.1ºC at 760mmHg

[ 熔点 ]:
168-1700C

[ 分子式 ]:
C₁₉H₂₅ClN₂

[ 分子量 ]:
316.868

[ 闪点 ]:
179.7ºC

[ 精确质量 ]:
316.170624

[ PSA ]:
6.48000

[ LogP ]:
4.74200

[ 外观性状 ]:
crystalline | white

[ 蒸汽压 ]:
6.6E-06mmHg at 25°C

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: 50 mg/mL

丙咪嗪盐酸盐MSDS

详细MSDS(安全技术说明书)

丙咪嗪盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HO1925000

CHEMICAL NAME :: 5H-Dibenz(b,f)azepine, 5-(3-(dimethylamino)propyl)-10,11-dihydro-, monohydrochloride

CAS REGISTRY NUMBER :: 113-52-0

LAST UPDATED :: 199706

DATA ITEMS CITED :: 41

MOLECULAR FORMULA :: C19-H24-N2.Cl-H

MOLECULAR WEIGHT :: 316.91

WISWESSER LINE NOTATION :: T C676 BN&T&J B3N1&1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 2143 ug/kg/2D-I

TOXIC EFFECTS :: Behavioral - tremor

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Behavioral - sleep Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 15 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Cardiac - other changes Kidney, Ureter, Bladder - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 27 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle contraction or spasticity Kidney, Ureter, Bladder - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 70 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - paresthesis Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 305 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 72 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 217 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 275 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 104 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 189 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 27 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Vascular - BP lowering not characterized in autonomic section

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 14 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 85 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 190 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 78 mg/kg

TOXIC EFFECTS :: Cardiac - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1575 mg/kg/15W-C

TOXIC EFFECTS :: Brain and Coverings - changes in brain weight Lungs, Thorax, or Respiration - other changes Biochemical - Metabolism (Intermediary) - other proteins

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 285 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating - 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 200 mg/kg

SEX/DURATION :: female 7-16 day(s) after conception

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 :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 800 mg/kg

SEX/DURATION :: female 1-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 gm/kg

SEX/DURATION :: female 7-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 180 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 225 mg/kg

SEX/DURATION :: female 23 day(s) pre-mating female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 210 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 65 mg/kg

SEX/DURATION :: female 8-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Effects on Newborn - biochemical and metabolic

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 130 mg/kg

SEX/DURATION :: female 8-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 65 mg/kg

SEX/DURATION :: female 8-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - biochemical and metabolic Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 9700 mg/kg

SEX/DURATION :: female 75 day(s) pre-mating female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 9200 mg/kg

SEX/DURATION :: female 10 week(s) pre-mating female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 125 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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 165 mg/kg

SEX/DURATION :: female 3-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 35 mg/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: DNA inhibition

MUTATION DATA

TEST SYSTEM :: Insect - not otherwise specified

DOSE/DURATION :: 10 gm/L

REFERENCE :: JCLBA3 Journal of Cell Biology. (Rockefeller Univ. Press, 1230 York Ave., New York, NY 10003) V.12- 1962- Volume(issue)/page/year: 47,182a,1970 *** REVIEWS *** TOXICOLOGY REVIEW IDPYAK Industrial Pharmacology. (Mount Kisco, NY) V.1-3, 1974-79. Discontinued. Volume(issue)/page/year: 2,209,1975 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5236 No. of Facilities: 123 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 2577 (estimated) No. of Female Employees: 1421 (estimated)

丙咪嗪盐酸盐安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R23/25

[ 安全声明 (欧洲) ]:
7-16-24-33-45-36-26

[ 危险品运输编码 ]:
UN 1230 3/PG 2

[ WGK德国 ]:
3

[ RTECS号 ]:
HO1925000

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丙咪嗪盐酸盐上游产品

丙咪嗪盐酸盐下游产品

丙咪嗪盐酸盐制备

10，11-二氢-5-二苯并[b，f]氮杂卓（见14230）与甲苯、钠氨一起加热回流1h，冷至40 -50 ℃ ，滴加1-氯-3-二甲氨基丙烷，再回流16h。冷却，过滤，滤液水洗层，取甲苯层减压蒸馏，回收甲苯后，收集210 -230 ℃ （0.67kPa）馏分，得米帕明碱，最后经成盐而得成品。

丙咪嗪盐酸盐文献

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Biochem. Pharmacol. 95 , 311-23, (2015)

Different lines of evidence indicate that the lysophosphatidic acid (LPA) receptor LPA1 is involved in neurogenesis, synaptic plasticity and anxiety-related behavior, but little is known on whether th...

Developing structure-activity relationships for the prediction of hepatotoxicity.

Chem. Res. Toxicol. 23 , 1215-22, (2010)

Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals ...

A predictive ligand-based Bayesian model for human drug-induced liver injury.

Drug Metab. Dispos. 38 , 2302-8, (2010)

Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...

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