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去甲丙咪嗪盐酸盐

去甲丙咪嗪盐酸盐用途

Desipramine hydrochloride 是去甲肾上腺素转运蛋白 (NET), 5-羟色胺转运体 (SERT) 和多巴胺转运 (DAT) 的抑制剂,其 Ki 值分别为 4, 61 和 78,720 nM。

去甲丙咪嗪盐酸盐名称

[ CAS 号 ]:
58-28-6

[ 中文名 ]:
3-氟茴香硫醚

[ 英文名 ]:
Desipramine hydrochloride

[中文别名 ]:

[英文别名 ]:

T C676 BN&T&J B3M1 &&HCl
Desipramine hydrochloride
Desimipramine Hydrochloride
MFCD00058108
irene
EINECS 200-373-1
Desipramine HCl
N-(g-Methylaminopropyl)iminodibenzyl Hydrochloride
RMI 9384A
N-(γ-Methylaminopropyl)iminodibenzyl hydrochloride

去甲丙咪嗪盐酸盐生物活性

[ 描述 ]:

Desipramine hydrochloride 是去甲肾上腺素转运蛋白 (NET), 5-羟色胺转运体 (SERT) 和多巴胺转运 (DAT) 的抑制剂,其 Ki 值分别为 4, 61 和 78,720 nM。

[ 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

信号通路 >> 神经信号通路 >> 多巴胺转运蛋白

研究领域 >> 神经疾病

[ 靶点 ]

Ki: 4 nM (NET), 61 nM (SERT), 78720 nM (DAT)[1]

[体内研究]

用盐酸地昔帕明治疗大鼠14天可以剂量依赖的方式减少去甲肾上腺素转运蛋白(NET)的表达,这表明大脑皮层制剂中3H-尼索西汀与NET的特异性结合减少(F(3,16) )= 4.33,p <0.05)和海马(F(3,16)= 4.34,p <0.05)。在停用慢性盐酸地昔帕明治疗2天后观察到这种NET下调,此时盐酸地昔帕明和去甲基地昔帕明的血浆和脑浓度检测不到(即低于25 ng检测限)[2]。

[动物实验]

用氯胺酮（100mg / kg）和甲苯噻嗪（10mg / kg）麻醉大鼠并皮下植入预先加载载体（50％盐水，40％DMSO和10％乙醇）或盐酸地昔帕明的渗透微泵，其浓度为每天递送5,10或15mg / kg游离碱。 14天后，在麻醉下取出微型泵。在泵取出和停用盐酸地昔帕明治疗后2至8天，在强迫游泳试验中测试大鼠的抗抑郁样行为。在完成行为测试后，通过断头处死大鼠，取出大脑，解剖大脑皮层和海马进行神经化学分析[2]。

[参考文献]

[1]. Torres GE, et al. Plasma membrane monoamine transporters: structure, regulation and function. Nat Rev Neurosci. 2003 Jan;4(1):13-25.

[2]. Zhao Z, et al. Norepinephrine transporter regulation mediates the long-term behavioral effects of the antidepressant desipramine. Neuropsychopharmacology. 2008 Dec;33(13):3190-200.

[相关活性小分子]

去甲丙咪嗪盐酸盐物理化学性质

[ 沸点 ]:
407.4ºC at 760 mmHg

[ 熔点 ]:
214-216ºC

[ 分子式 ]:
C₁₈H₂₃ClN₂

[ 分子量 ]:
302.842

[ 闪点 ]:
160.5ºC

[ 精确质量 ]:
302.154968

[ PSA ]:
15.27000

[ LogP ]:
4.79070

[ 外观性状 ]:
白色至灰白色粉末

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: 50 mg/mL

去甲丙咪嗪盐酸盐MSDS

详细MSDS(安全技术说明书)

去甲丙咪嗪盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HO0525000

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

CAS REGISTRY NUMBER :: 58-28-6

LAST UPDATED :: 199709

DATA ITEMS CITED :: 20

MOLECULAR FORMULA :: C18-H22-N2.Cl-H

MOLECULAR WEIGHT :: 302.88

WISWESSER LINE NOTATION :: T C676 BN&T&J B3M1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 45 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - acute pulmonary edema

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 36 mg/kg/6D-I

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - hallucinations, distorted perceptions Gastrointestinal - decreased motility or constipation

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5 mg/kg/5D-I

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 70 mg/kg/4W-I

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 490 ug/kg

TOXIC EFFECTS :: Behavioral - sleep

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 14 mg/kg/1W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume decreased Nutritional and Gross Metabolic - changes in sodium Nutritional and Gross Metabolic - changes in chlorine

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 871 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 :: 55 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 :: 19 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 :: 315 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 :: 88 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 :: 37 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - rigidity (including catalepsy) Nutritional and Gross Metabolic - body temperature decrease

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 25 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 :: 55 mg/kg

TOXIC EFFECTS :: Cardiac - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 130 mg/kg

SEX/DURATION :: female 10-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 90 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - Central Nervous System

TYPE OF TEST :: Specific locus test

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 - X5341 No. of Facilities: 62 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 1952 (estimated) No. of Female Employees: 1089 (estimated)

去甲丙咪嗪盐酸盐安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;F: Flammable;T: Toxic;

[ 风险声明 (欧洲) ]:
R22;R36/37/38;R42/43;R48/23/24/25;R11

[ 安全声明 (欧洲) ]:
S7-S16-S36/37-S45-S26-S24-S22

[ 危险品运输编码 ]:
UN 1230 3/PG 2

[ WGK德国 ]:
3

[ RTECS号 ]:
HO0525000

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由二苯并氮杂卓为原料制得。

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