*** CHEMICAL IDENTIFICATION ***

RTECS NUMBER            : VB1999050
CHEMICAL NAME           : 3-Quinolinecarboxylic acid,
                          1,4-dihydro-6,8-difluoro-1-(2-fluoroethyl)-7-(4-methy
                          l-1- piperazinyl)-4-oxo-
CAS REGISTRY NUMBER     : 79660-72-3
BEILSTEIN REFERENCE NO. : 4300996
LAST UPDATED            : 199612
DATA ITEMS CITED        : 16
MOLECULAR FORMULA       : C17-H18-F3-N3-O3
MOLECULAR WEIGHT        : 369.38
COMPOUND DESCRIPTOR     : Drug
                          Mutagen
                          Reproductive Effector
SYNONYMS/TRADE NAMES :
   * AM 833
   * Fleroxacin
   * Megalone
   * Ro 23-6240
   * Ro 23-6240/000
 
                       *** 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           : >4 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:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >1500 mg/kg
TOXIC EFFECTS :
   Sense Organs and Special Senses (Eye) - ptosis
   Behavioral - altered sleep time (including change in righting reflex)
   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:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >1500 mg/kg
TOXIC EFFECTS :
   Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
   NKRZAZ Chemotherapy (Tokyo).  (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
   Shinagawa-Ku, Tokyo 141, Japan)  V.1-    1953- Volume(issue)/page/year:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 20405 ug/kg
TOXIC EFFECTS :
   Sense Organs and Special Senses (Eye) - ptosis
   Behavioral - altered sleep time (including change in righting reflex)
   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:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >4 gm/kg
TOXIC EFFECTS :
   Sense Organs and Special Senses (Eye) - ptosis
   Behavioral - altered sleep time (including change in righting reflex)
   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:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >1500 mg/kg
TOXIC EFFECTS :
   Sense Organs and Special Senses (Eye) - ptosis
   Behavioral - altered sleep time (including change in righting reflex)
   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:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >1500 mg/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:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 21730 ug/kg
TOXIC EFFECTS :
   Sense Organs and Special Senses (Eye) - ptosis
   Behavioral - altered sleep time (including change in righting reflex)
   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:
   38(Suppl 2),135,1990
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >1 gm/kg
TOXIC EFFECTS :
   Gastrointestinal - nausea or vomiting
   Musculoskeletal - joints
REFERENCE :
   NKRZAZ Chemotherapy (Tokyo).  (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
   Shinagawa-Ku, Tokyo 141, Japan)  V.1-    1953- Volume(issue)/page/year:
   38(Suppl 2),135,1990
 
                 ** OTHER MULTIPLE DOSE TOXICITY DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 109 gm/kg/13W-I
TOXIC EFFECTS :
   Musculoskeletal - other changes
   Nutritional and Gross Metabolic - weight loss or decreased weight gain
   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:
   38(Suppl 2),145,1990
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 4550 mg/kg/13W-I
TOXIC EFFECTS :
   Behavioral - food intake (animal)
   Musculoskeletal - joints
   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:
   38(Suppl 2),175,1990
 
                          ** REPRODUCTIVE DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 26 gm/kg
SEX/DURATION            : male 61 day(s) pre-mating
                          female 2 week(s) pre-mating  - 7 day(s) after
                          conception
TOXIC EFFECTS :
   Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland,
   accessory glands
   Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
   number of implants per female; total number of implants per corpora lutea)
   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:
   38(Suppl 2),261,1990
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rabbit
DOSE                    : 1300 mg/kg
SEX/DURATION            : female 6-18 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Fertility - abortion
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
   NKRZAZ Chemotherapy (Tokyo).  (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
   Shinagawa-Ku, Tokyo 141, Japan)  V.1-    1953- Volume(issue)/page/year:
   38(Suppl 2),272,1990
 
                            ** MUTATION DATA **
 
TYPE OF TEST            : Mutation in microorganisms
TEST SYSTEM             : Bacteria - Salmonella typhimurium
DOSE/DURATION           : 100 ng/plate
REFERENCE :
   MUREAV Mutation Research.  (Elsevier Science Pub. B.V., POB 211, 1000 AE
   Amsterdam, Netherlands) V.1-    1964-  Volume(issue)/page/year: 248,135,1991
 
TYPE OF TEST            : Phage inhibition capacity
TEST SYSTEM             : Bacteria - Escherichia coli
DOSE/DURATION           : 30 ng/plate
REFERENCE :
   MUREAV Mutation Research.  (Elsevier Science Pub. B.V., POB 211, 1000 AE
   Amsterdam, Netherlands) V.1-    1964-  Volume(issue)/page/year: 248,135,1991
 
TYPE OF TEST            : DNA damage
TEST SYSTEM             : Bacteria - Bacillus subtilis
DOSE/DURATION           : 400 ng/disk
REFERENCE :
   NKRZAZ Chemotherapy (Tokyo).  (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki,
   Shinagawa-Ku, Tokyo 141, Japan)  V.1-    1953- Volume(issue)/page/year:
   38(Suppl 2),252,1990
 
                            *** END OF RECORD ***