氯苯氨啶

氯苯氨啶用途

Metoprine (BW 197U) 是一种有效的组胺 N-甲基转移酶 (HMT) 抑制剂。Metoprine 是一种二氨基嘧啶衍生物,可以透过血脑屏障,并通过抑制 HMT 增加脑组胺水平。Metoprine 是一种抗叶酸 (antifolate) 和抗肿瘤药。

氯苯氨啶名称

[ CAS 号 ]:
7761-45-7

[ 中文名 ]:
氯苯氨啶

[ 英文名 ]:
Metoprine

[英文别名 ]:

METOPRINE,METHODICHLOROPHEN
BW-197U
2aov
DDMP
METOPRINE
SK 5265
Methodichlorophen

氯苯氨啶生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 表观遗传学 >> 组蛋白甲基转移酶

信号通路 >> 细胞周期/DNA损伤 >> 叶酸

研究领域 >> 神经疾病

[体内研究]

美托普利(BW 197U；2-10mg/kg；IP)以剂量依赖性的方式改善基底大细胞(NBM)损伤引起的记忆障碍[2]。腹腔注射美托普利会产生各种行为效应,包括食物摄入减少和耗水量增加[1]。动物模型：雄性Sprague-dawley大鼠(200-280g)[2]剂量：2,5,10mg/kg给药：IP结果：大鼠基底核(NBM)损伤引起的记忆障碍呈剂量依赖性改善,高剂量10mg/kg可显著延长转移潜伏期。

[参考文献]

[1]. Junichi Kitanaka, et al. Brain Histamine N-Methyltransferase As a Possible Target of Treatment for Methamphetamine Overdose. Drug Target Insights. 2016 Mar 2;10:1-7.

[2]. Zhong Chen, et al. Effects of brain histamine on memory deficit induced by nucleus basalis-lesion in rats. Acta Pharmacol Sin. 2002 Jan;23(1):66-70.

[3]. John R Horton, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J Mol Biol. 2005 Oct 21;353(2):334-344.

氯苯氨啶物理化学性质

[ 密度 ]:
1.447g/cm3

[ 沸点 ]:
483.7ºC at 760 mmHg

[ 熔点 ]:
275-276ºC

[ 分子式 ]:
C₁₁H₁₀Cl₂N₄

[ 分子量 ]:
269.13000

[ 闪点 ]:
246.3ºC

[ 精确质量 ]:
268.02800

[ PSA ]:
77.82000

[ LogP ]:
4.08560

[ 折射率 ]:
1.678

[ 储存条件 ]:
2-8°C，干燥，密封

氯苯氨啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV8180000

CHEMICAL NAME :: Pyrimidine, 2,4-diamino-5-(3,4-dichlorophenyl)-6-methyl-

CAS REGISTRY NUMBER :: 7761-45-7

BEILSTEIN REFERENCE NO. :: 0223622

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C11-H10-Cl2-N4

MOLECULAR WEIGHT :: 269.15

WISWESSER LINE NOTATION :: T6N CNJ BZ DZ ER CG DG& F1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7 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 :: 50 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Tumorigenic - active as anti-cancer agent

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 40 mg/kg/21D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2500 ug/kg

SEX/DURATION :: female 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5 mg/kg

SEX/DURATION :: female 8-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7500 ug/kg

SEX/DURATION :: female 6-8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

MUTATION DATA

TEST SYSTEM :: Human

DOSE/DURATION :: 2800 ug/kg

REFERENCE :: RBBIAL Revista Brasileira de Biologia. Brazilian Review of Biology. (Academia Brasileira de Ciencias, Caixa Postal 229, ZC-00 Rio de Janeiro, Brazil) V.1- 1941- Volume(issue)/page/year: 25,145,1965

氯苯氨啶安全信息

[ 危害码 (欧洲) ]:
Xi