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美托哌丙嗪

美托哌丙嗪用途

Metopimazine(EXP999)是一种吩噻嗪衍生物,用于预防化疗期间呕吐。Metopimazine属于抗多巴胺能抗呕吐药(ADA)类。Metopimazine可用于胃肠炎(GE)的研究[1]。

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美托哌丙嗪名称

[ CAS 号 ]:
14008-44-7

[ 中文名 ]:
美托哌丙嗪

[ 英文名 ]:
Metopimazine

[中文别名 ]:

[英文别名 ]:

RP 9965
Metopimazinum [INN-Latin]
EINECS 237-818-4
Vogalene
Metopimazina [INN-Spanish]
Metopimazine
EXP 999
Nortrip
Methopimazin

美托哌丙嗪生物活性

[ 描述 ]:

Metopimazine(EXP999)是一种吩噻嗪衍生物,用于预防化疗期间呕吐。Metopimazine属于抗多巴胺能抗呕吐药(ADA)类。Metopimazine可用于胃肠炎(GE)的研究[1]。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[参考文献]

[1]. Victoire Roussel, et al. Estimating the excess of inappropriate prescriptions of anti-dopaminergic anti-emetics during acute gastroenteritis epidemics in France. Pharmacoepidemiol Drug Saf. 2013 Oct;22(10):1080-5.

美托哌丙嗪物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
679.0±65.0 °C at 760 mmHg

[ 熔点 ]:
170.5℃

[ 分子式 ]:
C₂₂H₂₇N₃O₃S₂

[ 分子量 ]:
445.598

[ 闪点 ]:
364.4±34.3 °C

[ 精确质量 ]:
445.149384

[ PSA ]:
117.39000

[ LogP ]:
3.19

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.681

[ 储存条件 ]:
2-8°C，干燥，密闭

美托哌丙嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NS5075000

CHEMICAL NAME :: Isonipecotamide, 1-(3-(2-(methylsulfonyl)phenothiazin-10-yl)propyl)-

CAS REGISTRY NUMBER :: 14008-44-7

LAST UPDATED :: 199612

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C22-H27-N3-O3-S2

MOLECULAR WEIGHT :: 445.64

WISWESSER LINE NOTATION :: T C666 BN ISJ ESW1 B3- AT6NTJ DVZ

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 :: 976 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1080 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 800 mg/kg

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

REFERENCE :: CHDDAT Comptes Rendus des Seances de l'Academie des Sciences, Serie D: Sciences Naturelles. (Paris, France) V.262-291, 1966-80. For publisher information, see CRASEV. Volume(issue)/page/year: 266,2365,1968

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 78 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Olfaction) - change in sensation of smell Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,97,1967

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 :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,32,1972

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 64 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Olfaction) - change in sensation of smell Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,97,1967

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Behavioral - tremor Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,561,1976

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Behavioral - tremor Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,561,1976

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,561,1976

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 250 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,561,1976 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7500 mg/kg/30D-I

TOXIC EFFECTS :: Blood - changes in erythrocyte (RBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,97,1967

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美托哌丙嗪安全信息

[ 海关编码 ]:
2934300000

美托哌丙嗪合成路线

详细合成路线

美托哌丙嗪上下游产品

美托哌丙嗪上游产品

美托哌丙嗪下游产品

美托哌丙嗪海关

[ 海关编码 ]: 2934300000

[ 中文概述 ]:
2934300000. 含一个吩噻嗪环系的化合物(吩噻嗪环系不论是否氢化,化合物未经进一步稠合的 ). 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 ]:
2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%