CHEMICAL IDENTIFICATION
-
RTECS NUMBER :
-
XH8680000
-
CHEMICAL NAME :
-
4-Thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((3-(2-chloro-6-fluorophenyl)- 5-methyl-4-isoxazolyl)carbonyl)amino)-3,3-dimethyl-7- oxo-, monosodium salt, (2S-(2-alpha,5-alpha,6-beta))-
-
CAS REGISTRY NUMBER :
-
1847-24-1
-
LAST UPDATED :
-
199603
-
DATA ITEMS CITED :
-
19
-
MOLECULAR FORMULA :
-
C19-H16-Cl-F-N3-O5-S.Na
-
MOLECULAR WEIGHT :
-
475.88
-
WISWESSER LINE NOTATION :
-
T45 ANV ESTJ F1 F1 GVO CMV- DT5NSJ C1 ER BG FF &-NA-
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
-
TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Human - woman
-
DOSE/DURATION :
-
120 mg/kg/3D-I
-
TOXIC EFFECTS :
-
Liver - jaundice, cholestatic
-
REFERENCE :
-
AJGAAR American Journal of Gastroenterology. (American College of Gastroenterology, Inc., 428 E. Preston St., Baltimore, MD 21202) V.21- 1954- Volume(issue)/page/year: 82,483,1987
-
TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Human - woman
-
DOSE/DURATION :
-
210 mg/kg/7D-I
-
TOXIC EFFECTS :
-
Liver - hepatitis (hepatocellular necrosis), zonal Liver - jaundice, cholestatic Skin and Appendages - dermatitis, other (after systemic exposure)
-
REFERENCE :
-
ANZJB8 Australian and New Zealand Journal of Medicine. (Modern Medicine of Australia Pty., Ltd., 100 Pacific Highway, North Sydney, 2060, Australia) V.1- 1971- Volume(issue)/page/year: 20,251,1990
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Rodent - rat
-
DOSE/DURATION :
-
11 gm/kg
-
TOXIC EFFECTS :
-
Details of toxic effects not reported other than lethal dose value
-
REFERENCE :
-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,697,1982
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Intraperitoneal
-
SPECIES OBSERVED :
-
Rodent - rat
-
DOSE/DURATION :
-
1100 mg/kg
-
TOXIC EFFECTS :
-
Details of toxic effects not reported other than lethal dose value
-
REFERENCE :
-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,697,1982
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Subcutaneous
-
SPECIES OBSERVED :
-
Rodent - rat
-
DOSE/DURATION :
-
2800 mg/kg
-
TOXIC EFFECTS :
-
Details of toxic effects not reported other than lethal dose value
-
REFERENCE :
-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,697,1982
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Intravenous
-
SPECIES OBSERVED :
-
Rodent - rat
-
DOSE/DURATION :
-
680 mg/kg
-
TOXIC EFFECTS :
-
Details of toxic effects not reported other than lethal dose value
-
REFERENCE :
-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,697,1982
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Rodent - mouse
-
DOSE/DURATION :
-
7600 mg/kg
-
TOXIC EFFECTS :
-
Details of toxic effects not reported other than lethal dose value
-
REFERENCE :
-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,697,1982
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Intraperitoneal
-
SPECIES OBSERVED :
-
Rodent - mouse
-
DOSE/DURATION :
-
1350 mg/kg
-
TOXIC EFFECTS :
-
Details of toxic effects not reported other than lethal dose value
-
REFERENCE :
-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,697,1982
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Subcutaneous
-
SPECIES OBSERVED :
-
Rodent - mouse
-
DOSE/DURATION :
-
1450 mg/kg
-
TOXIC EFFECTS :
-
Behavioral - convulsions or effect on seizure threshold Behavioral - muscle weakness
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Intravenous
-
SPECIES OBSERVED :
-
Rodent - mouse
-
DOSE/DURATION :
-
1360 mg/kg
-
TOXIC EFFECTS :
-
Details of toxic effects not reported other than lethal dose value
-
REFERENCE :
-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,697,1982
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Mammal - dog
-
DOSE/DURATION :
-
>10 gm/kg
-
TOXIC EFFECTS :
-
Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - nausea or vomiting
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Intravenous
-
SPECIES OBSERVED :
-
Mammal - dog
-
DOSE/DURATION :
-
670 mg/kg
-
TOXIC EFFECTS :
-
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - nausea or vomiting
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Rodent - rabbit
-
DOSE/DURATION :
-
>8 gm/kg
-
TOXIC EFFECTS :
-
Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic) Behavioral - somnolence (general depressed activity)
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
-
TYPE OF TEST :
-
LD50 - Lethal dose, 50 percent kill
-
ROUTE OF EXPOSURE :
-
Intravenous
-
SPECIES OBSERVED :
-
Rodent - rabbit
-
DOSE/DURATION :
-
710 mg/kg
-
TOXIC EFFECTS :
-
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969 ** OTHER MULTIPLE DOSE TOXICITY DATA **
-
TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Rodent - rat
-
DOSE/DURATION :
-
52 gm/kg/30D-I
-
TOXIC EFFECTS :
-
Gastrointestinal - hypermotility, diarrhea Liver - other changes Related to Chronic Data - death
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
-
TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Rodent - rat
-
DOSE/DURATION :
-
312 gm/kg/26W-I
-
TOXIC EFFECTS :
-
Lungs, Thorax, or Respiration - chronic pulmonary edema Gastrointestinal - changes in structure or function of salivary glands Related to Chronic Data - death
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969 ** REPRODUCTIVE DATA **
-
TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
DOSE :
-
6 gm/kg
-
SEX/DURATION :
-
female 9-14 day(s) after conception
-
TOXIC EFFECTS :
-
Reproductive - Effects on Embryo or Fetus - fetal death
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
-
TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
DOSE :
-
12 gm/kg
-
SEX/DURATION :
-
female 9-14 day(s) after conception
-
TOXIC EFFECTS :
-
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
-
TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
DOSE :
-
6 gm/kg
-
SEX/DURATION :
-
female 7-12 day(s) after conception
-
TOXIC EFFECTS :
-
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death
-
REFERENCE :
-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 17,1523,1969
|