疟涤平
疟涤平用途
喹吖啶(Acriquine)是一种抗疟疾和抗癌药物。奎纳克林还抑制人醛氧化酶(IC50:3.3μM)。奎纳克林对核酸具有亲和力,并在固定细胞中染色DNA和RNA(Ex/Em:436/525nm)[1][2][3][4][7]。
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疟涤平名称
[ CAS 号 ]:
83-89-6
[ 中文名 ]:
米帕林
[ 英文名 ]:
Quinacrine Dihydrochloride Dihydrate
[中文别名 ]:
[英文别名 ]:
- Quinacrine Dihydrochloride Dihydrate
- 2-methoxy-6-(trifluoromethyl)nicotinic acid
疟涤平生物活性
[ 描述 ]:
喹吖啶(Acriquine)是一种抗疟疾和抗癌药物。奎纳克林还抑制人醛氧化酶(IC50:3.3μM)。奎纳克林对核酸具有亲和力,并在固定细胞中染色DNA和RNA(Ex/Em:436/525nm)[1][2][3][4][7]。
[ 相关类别 ]:
[体外研究]
奎纳克林抑制人和兔醛氧化酶,IC50分别为 3.3微米和 10微米[2]奎纳克林阻断电压依赖性钠通道 (IC50:3.3μM)[3]奎纳克林(100μM)也是一种 平面图2抑制剂[4] 奎纳克林(0-20μM,24小时)抑制 SGC-7901型细胞的生长,并诱导细胞凋亡[7] 细胞活力测定奎纳克林抑制人和兔醛氧化酶,IC50分别为 3.3微米和 10微米[2]细胞系:SGC-7901细胞浓度:0、5、10、15、20μM培养时间:24小时结果:抑制细胞生长,IC50值为16.18μM。
[体内研究]
奎纳克林(3-30mg/kg每日一次,连续三天) 对甘油诱导的大鼠急性肾损伤具有保护作用[5] 奎纳克林(2.5-10mg/kg每天一次,连续八周) 对环孢菌素引起的大鼠肾毒性具有保护作用[6] 动物模型:急性肾损伤大鼠模型[5]剂量:3-30mg/kg给药:腹腔注射结果:减弱的甘油诱导肾脏结构和功能变化。
[参考文献]
疟涤平物理化学性质
[ 密度 ]:
1.156 g/cm3
[ 沸点 ]:
557.1ºC at 760 mmHg
[ 熔点 ]:
247-250ºC
[ 分子式 ]:
C23H30ClN3O
[ 分子量 ]:
399.96
[ 闪点 ]:
290.7ºC
[ 精确质量 ]:
399.20800
[ PSA ]:
37.39000
[ LogP ]:
6.04540
[ 储存条件 ]:
通风低温干燥
疟涤平毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- AR7700000
- CHEMICAL NAME :
- Acridine, 6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2- methoxy-
- CAS REGISTRY NUMBER :
- 83-89-6
- LAST UPDATED :
- 199710
- DATA ITEMS CITED :
- 26
- MOLECULAR FORMULA :
- C23-H30-Cl-N3-O
- MOLECULAR WEIGHT :
- 400.01
- WISWESSER LINE NOTATION :
- T C666 BNJ EG IMY1&3N2&2 LO1
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1320 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 :
- 239 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 :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 50 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - cat
- DOSE/DURATION :
- 10 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 400 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 - rabbit
- DOSE/DURATION :
- 75 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 :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 8 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Bird - chicken
- DOSE/DURATION :
- 714 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - coma Lungs, Thorax, or Respiration - other changes
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intrauterine
- DOSE :
- 13600 ug/kg
- SEX/DURATION :
- female 1 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - uterus, cervix, vagina
- TYPE OF TEST :
- Specific locus test
MUTATION DATA
- TYPE OF TEST :
- Unscheduled DNA synthesis
- TEST SYSTEM :
- Mammal - species unspecified Lymphocyte
- DOSE/DURATION :
- 1 umol/L
- REFERENCE :
- CBINA8 Chemico-Biological Interactions. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1969- Volume(issue)/page/year: 8,113,1974 *** REVIEWS *** TOXICOLOGY REVIEW 32XPAD "Teratology," Berry, C.L., and D.E. Poswillo, eds., New York, Springer, 1975 Volume(issue)/page/year: -,49,1975 TOXICOLOGY REVIEW ARVPAX Annual Review of Pharmacology. (Palo Alto, CA) V.1-15, 1961-75. For publisher information, see ARPTDI. Volume(issue)/page/year: 5,447,1965
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疟涤平安全信息
[ 危害码 (欧洲) ]:
Xn: Harmful;
[ 风险声明 (欧洲) ]:
R36/37/38
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