*** CHEMICAL IDENTIFICATION *** RTECS NUMBER : VB2002000 CHEMICAL NAME : 3-Quinolinecarboxylic acid, 1,4-dihydro-1-ethyl-6-fluoro-7-(4-methyl-1-piperaziny l)-4-oxo- CAS REGISTRY NUMBER : 70458-92-3 BEILSTEIN REFERENCE NO. : 0567618 REFERENCE : 5-23-03-00135 (Beilstein Handbook Reference) LAST UPDATED : 199806 DATA ITEMS CITED : 9 MOLECULAR FORMULA : C17-H20-F-N3-O3 MOLECULAR WEIGHT : 333.40 WISWESSER LINE NOTATION : T66 BN VVJ B2 DVQ HF I- AT6N DNTJ D1 COMPOUND DESCRIPTOR : Drug Mutagen Reproductive Effector Human SYNONYMS/TRADE NAMES : * AM-725 * AM 725 * 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-methyl-1-piperazinyl)-3-quinolin ecarboxylic acid * Pefloxacin * Pefloxacine * 1584RB *** HEALTH HAZARD DATA *** ** ACUTE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 1714 mg/kg/21W-I TOXIC EFFECTS : Peripheral Nerve and Sensation - paresthesis Peripheral Nerve and Sensation - structural change in nerve or sheath REFERENCE : LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,126,1992 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 343 mg/kg/30D-I TOXIC EFFECTS : Musculoskeletal - joints Musculoskeletal - other changes REFERENCE : DRSAEA Drug Safety. (Adis International Ltd., Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand) V.5- 1990- Volume(issue)/page/year: 7,310,1992 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - woman DOSE/DURATION : 16 mg/kg TOXIC EFFECTS : Behavioral - hallucinations, distorted perceptions Behavioral - muscle contraction or spasticity REFERENCE : AMDIBO Annales de Medecine Interne. (Masson Abonnements, B.P.22, F-41354 Vineuil Cedex, France) V.120- 1969- Volume(issue)/page/year: 144,495,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >4 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4530930 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 225 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0047005 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >50 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4292317 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 7500 mg/kg/30D-C TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,475,1983 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE : 30 gm/kg SEX/DURATION : male 30 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,475,1983 ** MUTATION DATA ** TYPE OF TEST : Unscheduled DNA synthesis TEST SYSTEM : Rodent - rat Liver DOSE/DURATION : 780 umol/L REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 221,263,1989 *** END OF RECORD ***