*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : XI0335000
CHEMICAL NAME : 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic
acid, 7-((amino-1,4-cyclohexadien-1-
ylacetyl)amino)-3-methoxy-8-oxo-,
(6R-(6-alpha,7-beta(R*)))-
CAS REGISTRY NUMBER : 51762-05-1
OTHER CAS REGISTRY NOS. : 109945-75-7
BEILSTEIN REFERENCE NO. : 0587499
LAST UPDATED : 199806
DATA ITEMS CITED : 17
MOLECULAR FORMULA : C16-H19-N3-O5-S
MOLECULAR WEIGHT : 365.44
WISWESSER LINE NOTATION : T46 ANV ES GUTJ GO1 HVQ CMV1- AL6U DUTJ BZ
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
SYNONYMS/TRADE NAMES :
* 7-(D-2-Amino-2-(1,4-cyclohexadienyl)acetamide)-3-methoxy-3-cephem-4-carb
oxylic acid
* Antibiotic CGP 9000
* Cefroxadin
* Cefroxadine
* CGP 9000
* CXD
* Oraspor
*** 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 : >22500 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - somnolence (general depressed activity)
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),98,1980
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 6 gm/kg
TOXIC EFFECTS :
Behavioral - ataxia
Gastrointestinal - hypermotility, diarrhea
Skin and Appendages - hair
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),98,1980
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >15 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation)
Behavioral - altered sleep time (including change in righting reflex)
Skin and Appendages - hair
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),98,1980
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >13500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),98,1980
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 7090 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8
Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968-
Volume(issue)/page/year: 29,653,1976
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 13500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),98,1980
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >1 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: -,689,1995
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : 10 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,APP-11,1982
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : >4 gm/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - structural or functional changes in ureter
Kidney, Ureter, Bladder - other changes
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),98,1980
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 56 gm/kg/28D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased
Kidney, Ureter, Bladder - changes in bladder weight
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),131,1980
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 182 gm/kg/13W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition
Blood - normocytic anemia
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),103,1980
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 27800 mg/kg/26W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased
Endocrine - changes in adrenal weight
Endocrine - changes in spleen weight
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),116,1980
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 455 gm/kg/13W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in bladder weight
Endocrine - changes in adrenal weight
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:
28(Suppl 3),103,1980
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : 2500 mg/kg/5D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased
Kidney, Ureter, Bladder - changes in bladder weight
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year:
28(Suppl 3),131,1980
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 27 gm/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
number of implants per female; total number of implants per corpora lutea)
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
Reproductive - Specific Developmental Abnormalities - urogenital system
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,615,1980
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 27 gm/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,615,1980
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 2700 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - weaning or lactation index (e.g., #
alive at weaning per # alive at day 4)
Reproductive - Effects on Newborn - delayed effects
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,615,1980
*** END OF RECORD ***