14008-44-7

• 常用中文名：美托哌丙嗪
• 常用英文名：Metopimazine
• CAS号：14008-44-7
• 分子式：C₂₂H₂₇N₃O₃S₂
• 分子量：445.598
• 相关类别： 原料药 消化系统用药 止吐催吐药
• 发布时间：2018-03-31 08:00:00
• 更新时间：2024-01-02 15:23:00
• 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]。

名称

• 中文名: 美托哌丙嗪
• 英文名: 1-[3-(2-methylsulfonylphenothiazin-10-yl)propyl]piperidine-4-carboxamide
• 中文别名: 1-[3-[2-(甲基磺酰基)-10H-吩噻嗪-10-基]丙基]哌啶-4-甲酰胺
• 英文别名: 1-[3-[2-(Methylsulfonyl)phenothiazin-10-yl]propyl]isonipecotamide; RP 9965; Metopimazinum [INN-Latin]; EINECS 237-818-4; Vogalene; 1-[3-[2-(Methylsulfonyl)phenothiazin-10-yl]propyl]-4-piperidinecarboxamide; 1-(3-(2-(methylsulfonyl)-10-phenothiazinyl)propyl)piperidine-4-carboxamide; 1-{3-[2-(Methylsulfonyl)-10H-phenothiazin-10-yl]propyl}-4-piperidinecarboxamide; 4-Piperidinecarboxamide, 1-[3-[2-(methylsulfonyl)-10H-phenothiazin-10-yl]propyl]-; 1-{3-[2-(Methylsulfonyl)-10H-phenothiazin-10-yl]propyl}piperidine-4-carboxamide; Metopimazina [INN-Spanish]; 4-Piperidinecarboximidic acid, 1-[3-[2-(methylsulfonyl)-10H-phenothiazin-10-yl]propyl]-; 1-[3-[2-(Methylsulfonyl)-10H-phenothiazin-10-yl]propyl]-4-piperidinecarboxamide; 10-[3-(4-Carbamoylpiperidino)propyl]-2-(methanesulfonyl)phenothiazine; 1-{3-[2-(Methylsulfonyl)-10H-phenothiazin-10-yl]propyl}-4-piperidinecarboximidic acid; Metopimazine; EXP 999; Nortrip; Methopimazin

物化性质

• 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

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.

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

安全

• 海关编码: 2934300000

合成路线

129846-94-2 ~25% 14008-44-7

文献：Sindelar, Karel; Holubek, Jiri; Koruna, Ivan; Hrubantova, Marta Collection of Czechoslovak Chemical Communications, 1990 , vol. 55, # 6 p. 1586 - 1601

129846-91-9 ~% 14008-44-7

文献：Collection of Czechoslovak Chemical Communications, , vol. 55, # 6 p. 1586 - 1601

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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%