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异卡波肼

异卡波肼用途

Isocarboxazid 是一种非选择性的、不可逆的单胺氧化酶 monoamine oxidase 抑制剂,其在大鼠大脑中测得的 IC50 值为4.8 μM。

异卡波肼名称

[ CAS 号 ]:
59-63-2

[ 中文名 ]:
异卡波肼

[ 英文名 ]:
Isocarboxazid

[中文别名 ]:

异恶唑酰肼

[英文别名 ]:

isocarboxazide
Benazide
Marplan
Isocarboxazidum
N'-Benzyl-5-methylisoxazol-3-carbohydrazid
Isocarboxazida
N'-benzyl-5-méthylisoxazole-3-carbohydrazide
Isocarbonazid
Isocarboxazid
N'-benzyl-5-methylisoxazole-3-carbohydrazide

异卡波肼生物活性

[ 描述 ]:

Isocarboxazid 是一种非选择性的、不可逆的单胺氧化酶 monoamine oxidase 抑制剂,其在大鼠大脑中测得的 IC50 值为4.8 μM。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> 单胺氧化酶

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 4.8 μM (rat brain monoamine oxidase)[1].

[体内研究]

在小鼠中预处理Isocarboxazid(1,3 mg/kg,腹膜内注射,60分钟)显示5-HTP后15和30分钟时头部抽搐的数量显着增加[2]。与单独使用5-HTP的小鼠相比,小鼠中的Isocarboxazid(1,3 mg/kg,ip,60 min)处理与5-HTP一起施用导致43％的5-HT浓度增加和22％的5-HIAA降低[2]。动物模型：12只雄性小鼠dd株(20-25g)[2]剂量：0,0.3,1,3mg/kg给药：腹腔注射60分钟,静脉注射5-HTP结果：头部抽搐数量5-HTP增加后15和30分钟。 43％的5-HT浓度增加,22％的5-HIAA减少。

[参考文献]

[1]. MAXWELL DR, et al. Relative activity of some inhibitors of mono-amine oxidase in potentiating the action of tryptamine in vitro and in vivo. Br J Pharmacol Chemother. 1961 Dec;17:310-20.

异卡波肼物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
394.5±42.0 °C at 760 mmHg

[ 熔点 ]:
98-100ºC

[ 分子式 ]:
C₁₂H₁₃N₃O₂

[ 分子量 ]:
231.251

[ 闪点 ]:
192.4±27.9 °C

[ 精确质量 ]:
231.100784

[ PSA ]:
67.16000

[ LogP ]:
1.03

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.573

[ 储存条件 ]:
-20°C Freezer

异卡波肼毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NY2625000

CHEMICAL NAME :: 3-Isoxazolecarboxylic acid, 5-methyl-, 2-benzylhydrazide

CAS REGISTRY NUMBER :: 59-63-2

BEILSTEIN REFERENCE NO. :: 0201295

LAST UPDATED :: 199612

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C12-H13-N3-O2

MOLECULAR WEIGHT :: 231.28

WISWESSER LINE NOTATION :: T5NOJ C1 EVMM1R

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 4800 ug/kg/21W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - monoamine oxidase

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 280 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 :: 199 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 :: 193 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 :: 138 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 :: 150 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 :: Mammal - dog

DOSE/DURATION :: >40 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 160 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 :: 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 :: Intraperitoneal

DOSE :: 100 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: DNA damage

TYPE OF TEST :: DNA damage

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 49 mg/kg

REFERENCE :: JTEHD6 Journal of Toxicology and Environmental Health. (Hemisphere Pub., 1025 Vermont Ave., NW, Washington, DC 20005) V.1- 1975/76- Volume(issue)/page/year: 9,287,1982 *** 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 - X6269 No. of Facilities: 9 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 339 (estimated) No. of Female Employees: 170 (estimated)

异卡波肼安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 危险品运输编码 ]:
UN 3249

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2934999090

异卡波肼合成路线

详细合成路线

异卡波肼上下游产品

异卡波肼上游产品

异卡波肼下游产品

异卡波肼海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%