50335-55-2

• 常用中文名：Mezilamine
• 常用英文名：Mezilamine
• CAS号：50335-55-2
• 分子式：C₁₁H₁₈ClN₅S
• 分子量：287.81200
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 肾上腺素能受体
• 发布时间：2017-11-17 23:03:43
• 更新时间：2024-01-02 11:20:09
• Mezilamine是一种强效的抗多巴胺药物。Mezilamine诱导大鼠皮质切片电刺激3H-去甲肾上腺素溢出的浓度依赖性增加,而不影响基础溢出。Mezilamine作为突触前α肾上腺素受体拮抗剂和突触后α肾上腺素受体激动剂[1]。

名称

• 英文名: Mezilamine
• 英文别名: 4-Chloro-2-methylamino-5-methylthio-6-(4-methyl-1-piperazinyl)pyrimidine; [4-chloro-6-(4-methyl-piperazin-1-yl)-5-methylsulfanyl-pyrimidin-2-yl]-methyl-amine; N-Methyl-4-chloro-5-(methylthio)-6-(4-methylpiperazino)pyrimidine-2-amine; 4-Chloro-N-methyl-6-(4-methylpiperazin-1-yl)-5-(methylthio)pyrimidin-2-amine; 2-Methylamino-4-(4-methylpiperazino)-5-methylmercapto-6-chlorpyrimidin

物化性质

• 密度: 1.32g/cm3
• 沸点: 440.2ºC at 760 mmHg
• 分子式: C₁₁H₁₈ClN₅S
• 分子量: 287.81200
• 闪点: 220ºC
• 精确质量: 287.09700
• PSA: 69.59000
• LogP: 1.72130
• 折射率: 1.627

生物活性

• 描述: Mezilamine是一种强效的抗多巴胺药物。Mezilamine诱导大鼠皮质切片电刺激3H-去甲肾上腺素溢出的浓度依赖性增加,而不影响基础溢出。Mezilamine作为突触前α肾上腺素受体拮抗剂和突触后α肾上腺素受体激动剂[1]。
• 相关类别:
  研究领域 >> 内分泌
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
  研究领域 >> 神经疾病
• 体外研究: 夹层胺(1、5、10μM)导致 3小时刺激的溢出浓度依赖性增加,而不影响皮质切片的自发流出[1]。
• 参考文献:

  [1]. G Le Fur, et al. Mezilamine, a new dopamine antagonist, blocks presynaptic but stimulates postsynaptic alpha-adrenoceptors. Eur J Pharmacol. 1979 Oct 15;58(4):359-67.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UV8126000 CHEMICAL NAME : Pyrimidine, 4-chloro-2-(methylamino)-5-(methylthio)-6-(4-methyl-1 -piperazinyl)- CAS REGISTRY NUMBER : 50335-55-2 BEILSTEIN REFERENCE NO. : 0666978 LAST UPDATED : 199612 DATA ITEMS CITED : 4 MOLECULAR FORMULA : C11-H18-Cl-N5-S MOLECULAR WEIGHT : 287.85 WISWESSER LINE NOTATION : T6N DNTJ A1 D- DT6N CNJ BM1 ES1 FG 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 : 800 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 21 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 330 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 35 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977

安全

• 海关编码: 2933990090

合成路线

109-01-3 40765-72-8 ~% 50335-55-2

文献：Gueremy, Claude; Audiau, Francois; Uzan, Andre; Fur, Gerard Le; Leger, Jean-Michel; Carpy, Alain Journal of Medicinal Chemistry, 1982 , vol. 25, # 12 p. 1459 - 1465

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海关

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%