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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]。

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 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 癌症

研究领域 >> 感染

研究领域 >> 神经疾病

[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]

[1]. Vogtherr M, et al. Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. J Med Chem. 2003 Aug 14;46(17):3563-4.

[2]. Pryde DC, et al. Aldehyde oxidase: an enzyme of emerging importance in drug discovery. J Med Chem. 2010 Dec 23;53(24):8441-60.

[3]. McNeal ET, et al. [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. J Med Chem. 1985 Mar;28(3):381-8.

[4]. Caro AA,et al. Role of phospholipase A2 activation and calcium in CYP2E1-dependent toxicity in HepG2 cells. J Biol Chem. 2003 Sep 5;278(36):33866-77.

[5]. Al Asmari AK, et al. Protective effect of quinacrine against glycerol-induced acute kidney injury in rats. BMC Nephrol. 2017 Jan 28;18(1):41.

[6]. al Khader A, et al. Quinacrine attenuates cyclosporine-induced nephrotoxicity in rats. Transplantation. 1996 Aug 27;62(4):427-35.

[7]. Wu X, et al. Quinacrine Inhibits Cell Growth and Induces Apoptosis in Human Gastric Cancer Cell Line SGC-7901. Curr Ther Res Clin Exp. 2012 Feb;73(1-2):52-64.

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

疟涤平安全信息

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R36/37/38

疟涤平