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替马沙星

替马沙星用途

替马沙星(TMFX)是一种喹诺酮类抗菌剂,对革兰氏阳性菌、革兰氏阴性菌和厌氧菌具有广泛的抗菌谱[1][2]。

替马沙星名称

[ CAS 号 ]:
108319-06-8

[ 中文名 ]:
替马沙星

[ 英文名 ]:
temafloxacin

[中文别名 ]:

[英文别名 ]:

[14C]-Temafloxacin
Temafloxacina [Spanish]
Temafloxacina
Omniflox
Temafloxacinum [Latin]
Temafloxacine
Temafloxacinum
Temafloxacine [French]
Temafloxacin

替马沙星生物活性

[ 描述 ]:

替马沙星(TMFX)是一种喹诺酮类抗菌剂,对革兰氏阳性菌、革兰氏阴性菌和厌氧菌具有广泛的抗菌谱[1][2]。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[体外研究]

替莫沙星对革兰氏阳性菌和革兰氏阴性菌具有广泛的抗菌活性,包括对肺炎链球菌、人型支原体和厌氧菌(包括脆弱类杆菌)的体外抗菌活性提高[2]。

[体内研究]

替马沙星是一种氟喹诺酮类药物,半衰期为7-8小时,胃肠道吸收迅速。除中枢神经系统(CNS)外,替莫沙星具有良好的组织和体液渗透性和浓度[2]。

[参考文献]

[1]. S Matsuda, et al. Experimental and clinical studies of temafloxacin in the field of obstetrics and gynecology. Jpn J Antibiot. 1993 Jun;46(6):492-504.

[2]. G A Pankey. Temafloxacin: an overview. Am J Med. 1991 Dec 30;91(6A):166S-172S.

替马沙星物理化学性质

[ 密度 ]:
1.427g/cm3

[ 沸点 ]:
608.9ºC at 760mmHg

[ 分子式 ]:
C₂₁H₁₈F₃N₃O₃

[ 分子量 ]:
417.38100

[ 闪点 ]:
322.1ºC

[ 精确质量 ]:
417.13000

[ PSA ]:
74.57000

[ LogP ]:
3.29810

[ 蒸汽压 ]:
1.11E-15mmHg at 25°C

[ 折射率 ]:
1.603

[ 储存条件 ]:
2-8°C

替马沙星毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VB1999065

CHEMICAL NAME :: 3-Quinolinecarboxylic acid, 1,4-dihydro-1-(2,4-difluorophenyl)-6-fluoro-7- (3-methyl-1-piperazinyl)-4-oxo-

CAS REGISTRY NUMBER :: 108319-06-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C21-H18-F3-N3-O3

MOLECULAR WEIGHT :: 417.42

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 36400 mg/kg/26W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - changes in sodium

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 18200 mg/kg/26W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Musculoskeletal - joints Nutritional and Gross Metabolic - weight loss or decreased weight gain

MUTATION DATA

TYPE OF TEST :: DNA repair

TEST SYSTEM :: Bacteria - Bacillus subtilis

DOSE/DURATION :: 20 mg/L

REFERENCE :: AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 37,213,1993