环己西林

环己西林用途

西拉西林(Wy-4508)是一种口服活性氨基青霉素抗生素,对多种革兰氏阳性和革兰氏阴性病原体具有抗菌活性[1]。

环己西林名称

[ 英文名 ]:
4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylicacid, 6-[[(1-aminocyclohexyl)carbonyl]amino]-3,3-dimethyl-7-oxo-, (2S,5R,6R)-

[中文别名 ]:

环青霉素

[英文别名 ]:

6-(1-aminocyclohexanecarboxamido)penicillanic acid
Vastcillin
Ultracillin
Cyclapen
CYCLACILLIN
Citosarin
Ciclacillin
Bastcillin
Calthor
Vipicil

环己西林生物活性

[ 描述 ]:

西拉西林(Wy-4508)是一种口服活性氨基青霉素抗生素,对多种革兰氏阳性和革兰氏阴性病原体具有抗菌活性[1]。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[体外研究]

环氯西林(0-125μg/mL)抑制各种病原体,克雷伯菌和肠杆菌除外,MIC值为0.24μg/mL至7.8μg/mL[1]。

[体内研究]

环氯西林(0-287 mg/kg；口服；单剂量)在小鼠中表现出口服活性,并拯救注射了革兰氏阳性和革兰氏阴性病原体的小鼠[1]。大鼠肠组织以相对低的浓度(小于1mg/mL)吸收了环氯西林(10mg/kg；静脉注射；单次剂量),仅遵循米氏动力学[2]。

环己西林物理化学性质

[ 密度 ]:
1.4g/cm3

[ 沸点 ]:
649.6ºC at 760mmHg

[ 熔点 ]:
182-183° (anhydrate) (Hou, Poole); mp 156-158° (dec) (Alburn et al.)

[ 分子式 ]:
C₁₅H₂₃N₃O₄S

[ 分子量 ]:
341.42600

[ 精确质量 ]:
341.14100

[ PSA ]:
138.03000

[ LogP ]:
1.30880

[ 折射率 ]:
1.631

环己西林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GT8450000

CHEMICAL NAME :: Cyclacillin

CAS REGISTRY NUMBER :: 3485-14-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C15-H23-N3-O4-S

MOLECULAR WEIGHT :: 341.47

WISWESSER LINE NOTATION :: T45 ANV ESTJ F1 F1 GVQ CMV- AL6TJ AZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 210 mg/kg/7D-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 22,154,1976

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5010 mg/kg

TOXIC EFFECTS :: Liver - other changes

REFERENCE :: CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 22,154,1976

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5010 mg/kg

TOXIC EFFECTS :: Liver - other changes

REFERENCE :: CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 22,154,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6500 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

REFERENCE :: TAKHAA Takeda Kenkyusho Ho. Journal of the Takeda Research Laboratories. (Takeda Yakuhin Kogyo K.K., 2-17-85 Jusohon-machi, Yodogawa-ku, Osaka 532, Japan) V.29- 1970- Volume(issue)/page/year: 29,117,1970

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5010 mg/kg

TOXIC EFFECTS :: Liver - other changes

REFERENCE :: CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 22,154,1976

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3776 mg/kg

TOXIC EFFECTS :: Liver - other changes

REFERENCE :: CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 22,154,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7500 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

REFERENCE :: TAKHAA Takeda Kenkyusho Ho. Journal of the Takeda Research Laboratories. (Takeda Yakuhin Kogyo K.K., 2-17-85 Jusohon-machi, Yodogawa-ku, Osaka 532, Japan) V.29- 1970- Volume(issue)/page/year: 29,117,1970

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2500 mg/kg

TOXIC EFFECTS :: Liver - other changes

REFERENCE :: CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 22,154,1976 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 87 gm/kg/26W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,1,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 108 gm/kg/30D-C

TOXIC EFFECTS :: Behavioral - food intake (animal) Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: TAKHAA Takeda Kenkyusho Ho. Journal of the Takeda Research Laboratories. (Takeda Yakuhin Kogyo K.K., 2-17-85 Jusohon-machi, Yodogawa-ku, Osaka 532, Japan) V.29- 1970- Volume(issue)/page/year: 29,117,1970 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X9351 No. of Facilities: 25 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 101 (estimated) No. of Female Employees: 51 (estimated)