*** CHEMICAL IDENTIFICATION ***

RTECS NUMBER            : UU8815300
CHEMICAL NAME           : 7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic
                          acid, 2,3-dihydro-10-(1-aminocyclopropyl)-9-
                          fluoro-3-methyl-7-oxo-, (S)-
CAS REGISTRY NUMBER     : 127045-41-4
LAST UPDATED            : 199801
DATA ITEMS CITED        : 14
MOLECULAR FORMULA       : C16-H15-F-N2-O4
MOLECULAR WEIGHT        : 318.33
COMPOUND DESCRIPTOR     : Drug
                          Reproductive Effector
SYNONYMS/TRADE NAMES :
   * Pazufloxacin
   * T 3761
 
                       *** HEALTH HAZARD DATA ***
 
                        ** ACUTE TOXICITY DATA **
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NKRZAZ Chemotherapy (Tokyo).  (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
   Shinagawa-Ku, Tokyo 141, Japan)  V.1-    1953- Volume(issue)/page/year:
   43(Suppl 2),132,1995
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,754,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 341 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,754,1995
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,754,1995
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,754,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 783 mg/kg
TOXIC EFFECTS :
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - dyspnea
   Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,754,1995
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >2 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,754,1995
 
TYPE OF TEST            : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 400 mg/kg
TOXIC EFFECTS :
   Behavioral - convulsions or effect on seizure threshold
   Gastrointestinal - nausea or vomiting
   Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,754,1995
 
                 ** OTHER MULTIPLE DOSE TOXICITY DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 36400 mg/kg/13W-I
TOXIC EFFECTS :
   Gastrointestinal - other changes
   Musculoskeletal - joints
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,790,1995
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 16800 mg/kg/4W-I
TOXIC EFFECTS :
   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:
   43(Suppl 2),132,1995
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 2730 mg/kg/13W-I
TOXIC EFFECTS :
   Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
   Musculoskeletal - joints
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,790,1995
 
                          ** REPRODUCTIVE DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 125 gm/kg
SEX/DURATION            : male 9 week(s) pre-mating
                          female 2 week(s) pre-mating  - 7 day(s) after
                          conception
TOXIC EFFECTS :
   Reproductive - Paternal Effects - testes, epididymis, sperm duct
   Reproductive - Maternal Effects - other effects
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,832,1995
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 16500 mg/kg
SEX/DURATION            : female 7-17 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Maternal Effects - other effects
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
   Reproductive - Specific Developmental Abnormalities - cardiovascular
   (circulatory) system
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,832,1995
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 39 gm/kg
SEX/DURATION            : female 17-21 day(s) after conception
                          lactating female 21 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Maternal Effects - parturition
   Reproductive - Maternal Effects - other effects
REFERENCE :
   JJANAX Japanese Journal of Antibiotics.  (Japan Antibiotics Research Assoc.,
   2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan)  V.21-    1968-
   Volume(issue)/page/year: 48,832,1995
 
                            *** END OF RECORD ***