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161967-81-3

161967-81-3结构式
161967-81-3结构式
  • 常用中文名：盐酸格帕沙星
  • 常用英文名：Grepafloxacin hydrochloride
  • CAS号：161967-81-3
  • 分子式：C19H23ClFN3O3
  • 分子量：395.85600
  • 相关类别： 原料药 人工合成抗感染类药 喹诺酮类药
  • 发布时间：2018-02-10 08:00:00
  • 更新时间：2024-01-03 19:30:20
  • 盐酸格列帕沙星(OPC-17116)是一种口服活性氟喹诺酮类抗生素,对包括肺炎链球菌在内的社区获得性呼吸道病原体具有有效活性。盐酸格列帕沙星具有高组织渗透性和良好的药效学特性[1][2][3][4]。

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中文名 盐酸格帕沙星
英文名 1-Cyclopropyl-6-fluoro-5-methyl-7-(3-methyl-1-piperazinyl)-4-oxo- 1,4-dihydro-3-quinolinecarboxylic acid hydrochloride (1:1)
英文别名 4-Cyclohexene-1,3-dione,5-hydroxy-2,2,6,6-tetramethyl-4-(1-oxo-3-phenylpropyl)
Grepafloxacin hydrochloride
grandiflorone
5-Hydroxy-2,2,6,6-tetramethyl-4-(1-oxo-3-phenylpropyl)-4-cyclohexene-1,3-dione
描述 盐酸格列帕沙星(OPC-17116)是一种口服活性氟喹诺酮类抗生素,对包括肺炎链球菌在内的社区获得性呼吸道病原体具有有效活性。盐酸格列帕沙星具有高组织渗透性和良好的药效学特性[1][2][3][4]。
相关类别
体外研究 盐酸格列帕沙星(OPC-17116；0-1 mg/L；14-21 d)具有抗生素活性,MIC值为≤ 大肠杆菌菌株为0.006 mg/L[1]。盐酸格列帕沙星(0-1 mg/L；3 h)对巨噬细胞中的分枝杆菌具有抗菌活性,对禽分枝杆菌的MIC值为0.5 mg/L[1]。盐酸格列帕沙星对革兰氏阳性细菌(如肺炎链球菌)表现出强大的体外抗菌活性,对由所测试的革兰氏阴性和阳性细菌引起的实验性全身感染具有较高的体内疗效[4]。
体内研究 盐酸格列帕沙星(OPC-17116；200 mg/kg；口服；Balb/c小鼠)在光毒性方面表现出良好的安全性[2]。盐酸格列帕沙星(25-200 mg/kg；口服；每周5天,持续4周；雌性C57BL6/J-Lyst bg-J/小鼠/米色小鼠)在鼻内(in)感染和静脉内(IV)禽分枝杆菌感染模型中均具有适度活性[3]。
沸点 626.7ºC at 760mmHg
分子式 C19H23ClFN3O3
分子量 395.85600
闪点 332.8ºC
精确质量 395.14100
PSA 74.57000
LogP 3.47600
蒸汽压 1.43E-16mmHg at 25°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VB1993790
CHEMICAL NAME :
3-Quinolinecarboxylic acid, 1,4-dihydro-1-cyclopropyl-6-fluoro-5-methyl-7-(3-meth yl- piperazinyl)-4-oxo-, monohydrochloride, (+-)-
CAS REGISTRY NUMBER :
161967-81-3
LAST UPDATED :
199706
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C19-H22-F-N3-O3.Cl-H
MOLECULAR WEIGHT :
395.90

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 :
3029 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
152 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3900 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - tremor
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
69200 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>100 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,464,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
27300 mg/kg/13W-I
TOXIC EFFECTS :
Nutritional and Gross Metabolic - changes in sodium Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Metabolism (Intermediary) - other proteins
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,413,1995
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
9100 mg/kg/13W-I
TOXIC EFFECTS :
Blood - normocytic anemia Blood - changes in bone marrow (not otherwise specified) Related to Chronic Data - death
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,438,1995 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
550 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - behavioral
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,4515,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1650 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - delayed effects
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,4515,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1300 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,4539,1994

海关编码 2933990090
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%

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