29216-28-2

• 常用中文名：美喹他嗪
• 常用英文名：Mequitazine
• CAS号：29216-28-2
• 分子式：C₂₀H₂₂N₂S
• 分子量：322.467
• 相关类别： 原料药 抗变态反应药 抗组胺药
• 发布时间：2018-08-08 18:10:57
• 更新时间：2024-01-04 17:13:18
• Mequitazine是一种有效的,非依赖性和长效的组胺H1拮抗剂。

名称

• 中文名: 美喹他嗪
• 英文名: Mequitazine
• 中文别名: 甲喹吩嗪; 10-(1-氮杂双环[2.2.2]辛烷-3-基甲基)-10H-吩噻嗪
• 英文别名: EINECS 249-521-7; Mequitazine; Butix; UNII:Y463242LY2; 10H-Phenothiazine, 10- (1-azabicyclo[2.2.2]oct-3-ylmethyl)-; 10H-Phenothiazine, 10-(1-azabicyclo[2.2.2]oct-3-ylmethyl)-; Zesulan; Phenothiazine, 10- (3-quinuclidinylmethyl)-; 10-(1-Azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine; MFCD01706743

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 469.4±24.0 °C at 760 mmHg
• 熔点: 143-145ºC
• 分子式: C₂₀H₂₂N₂S
• 分子量: 322.467
• 闪点: 237.7±22.9 °C
• 精确质量: 322.150360
• PSA: 31.78000
• LogP: 5.38
• 外观性状: 白色固体
• 蒸汽压: 0.0±1.2 mmHg at 25°C
• 折射率: 1.707
• 储存条件: Refrigerator
• 水溶解性: 水溶性：不溶；易溶于：甲醇；可溶于：乙醇

生物活性

• 描述: Mequitazine是一种有效的,非依赖性和长效的组胺H1拮抗剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
• 体外研究: 美喹他嗪是一种有效的H1受体选择性抗组胺药,被广泛研究并用于过敏性疾病,如花粉症和荨麻疹[1]。美喹他嗪对所有测试的临床分离株(包括Ps)表现出显着的杀菌作用。铜绿假单胞菌。它对革兰氏阳性菌株的作用更明显[2]。
• 体内研究: 美喹他嗪和克立咪唑竞争性地拮抗组胺对豚鼠回肠的作用。在107处的美喹他嗪产生剂量-反应曲线与大鼠十二指肠中的乙酰胆碱的平行移动。最高浓度的美喹他嗪显示出抗胆碱能活性[3]。美喹他嗪抑制大鼠主动脉对KCl,去氧肾上腺素(PE),5-羟色胺(5-HT)和Ca2 +的收缩反应[4]。
• 参考文献:

  [1]. Gonnot V, et al. Expedient synthesis of mequitazine an antihistaminic drug by palladium catalyzed allylic alkylation of sodium phenothiazinate. Chem Pharm Bull (Tokyo). 2009 Nov;57(11):1300-2.

  [2]. El-Nakeeb MA, et a. In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates. Braz J Microbiol. 2011 Jul;42(3):980-91.

  [3]. Martinez-Mir I, et al. Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole. J Pharm Pharmacol. 1988 Sep;40(9):655-6.

  [4]. Satake N, et al. Possible mechanisms of vasoinhibitory effects of mequitazine, an antiallergic agent, on the contractions of isolated rat aorta induced by K+, phenylephrine, 5-hydroxytryptamine, and Ca2+. J Cardiovasc Pharmacol. 1994 Apr;23(4):669-73.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : SP5080000 CHEMICAL NAME : Phenothiazine, 10-(3-quinuclidinylmethyl)- CAS REGISTRY NUMBER : 29216-28-2 LAST UPDATED : 199612 DATA ITEMS CITED : 15 MOLECULAR FORMULA : C20-H22-N2-S MOLECULAR WEIGHT : 322.50 WISWESSER LINE NOTATION : T C666 BN ISJ B1- AT66 A B CNTJ 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 : 245 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,491,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 54 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,491,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 690 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,491,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 210 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,491,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 54 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,491,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 278 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,491,1981 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 360 mg/kg/30D-C TOXIC EFFECTS : Liver - changes in liver weight Endocrine - changes in thymus weight Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,491,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3240 mg/kg/26W-C TOXIC EFFECTS : Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in erythrocyte (RBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 22,507,1981 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 13750 ug/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - behavioral REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,867,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 55 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,867,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 220 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,867,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 101 mg/kg SEX/DURATION : male 8 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Fertility - other measures of fertility REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,855,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 65 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - urogenital system REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,893,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 325 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - sex ratio REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,893,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1625 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,893,1981

安全

• 海关编码: 2934300000

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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%