CHEMICAL IDENTIFICATION
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RTECS NUMBER :
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RN6900000
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CHEMICAL NAME :
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5-Oxa-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(2-((difluoromethyl)thio)acetamido)- 3-(((1-(2-hydroxyethyl)-1H-tetrazol-5-yl)thio)methyl) -7-methoxy-8-oxo-, sodium salt, (6R,7R)-
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CAS REGISTRY NUMBER :
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92823-03-5
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LAST UPDATED :
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199706
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DATA ITEMS CITED :
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21
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MOLECULAR FORMULA :
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C15-H18-F2-N6-O7-S2.Na
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MOLECULAR WEIGHT :
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519.50
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
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TYPE OF TEST :
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LD50 - Lethal dose, 50 percent kill
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ROUTE OF EXPOSURE :
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Oral
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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>10 gm/kg
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TOXIC EFFECTS :
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Details of toxic effects not reported other than lethal dose value
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REFERENCE :
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IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,735,1988
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TYPE OF TEST :
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LD50 - Lethal dose, 50 percent kill
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ROUTE OF EXPOSURE :
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Subcutaneous
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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>10 gm/kg
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TOXIC EFFECTS :
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Details of toxic effects not reported other than lethal dose value
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REFERENCE :
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NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1055,1990
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TYPE OF TEST :
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LD50 - Lethal dose, 50 percent kill
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ROUTE OF EXPOSURE :
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Intravenous
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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6417 mg/kg
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TOXIC EFFECTS :
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Details of toxic effects not reported other than lethal dose value
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REFERENCE :
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NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1055,1990
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TYPE OF TEST :
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LD50 - Lethal dose, 50 percent kill
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ROUTE OF EXPOSURE :
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Oral
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SPECIES OBSERVED :
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Rodent - mouse
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DOSE/DURATION :
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>15 gm/kg
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TOXIC EFFECTS :
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Details of toxic effects not reported other than lethal dose value
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REFERENCE :
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IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,735,1988
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TYPE OF TEST :
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LD50 - Lethal dose, 50 percent kill
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ROUTE OF EXPOSURE :
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Subcutaneous
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SPECIES OBSERVED :
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Rodent - mouse
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DOSE/DURATION :
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13500 mg/kg
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TOXIC EFFECTS :
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Details of toxic effects not reported other than lethal dose value
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REFERENCE :
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IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,735,1988
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TYPE OF TEST :
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LD50 - Lethal dose, 50 percent kill
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ROUTE OF EXPOSURE :
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Intravenous
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SPECIES OBSERVED :
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Rodent - mouse
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DOSE/DURATION :
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8043 mg/kg
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TOXIC EFFECTS :
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Details of toxic effects not reported other than lethal dose value
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REFERENCE :
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IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,735,1988
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TYPE OF TEST :
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LD50 - Lethal dose, 50 percent kill
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ROUTE OF EXPOSURE :
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Intravenous
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SPECIES OBSERVED :
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Mammal - dog
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DOSE/DURATION :
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>5 gm/kg
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TOXIC EFFECTS :
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Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),226,1987 ** OTHER MULTIPLE DOSE TOXICITY DATA **
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Oral
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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90 gm/kg/30D-C
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TOXIC EFFECTS :
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Kidney, Ureter, Bladder - changes in bladder weight Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - changes in calcium
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 32(Suppl 3),199,1984
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Oral
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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273 gm/kg/26W-C
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TOXIC EFFECTS :
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Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - changes in testicular weight
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 32(Suppl 3),199,1984
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intraperitoneal
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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146 gm/kg/26W-I
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TOXIC EFFECTS :
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Gastrointestinal - other changes Kidney, Ureter, Bladder - changes in bladder weight Endocrine - changes in adrenal weight
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),270,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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90 mg/kg/30D-I
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TOXIC EFFECTS :
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Gastrointestinal - other changes Endocrine - changes in adrenal weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),207,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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SPECIES OBSERVED :
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Mammal - dog
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DOSE/DURATION :
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15 gm/kg/30D-I
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TOXIC EFFECTS :
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Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Biochemical - Metabolism (Intermediary) - lipids including transport
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),226,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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SPECIES OBSERVED :
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Mammal - dog
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DOSE/DURATION :
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36 gm/kg/13W-I
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TOXIC EFFECTS :
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Blood - change in clotting factors Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),251,1987 ** REPRODUCTIVE DATA **
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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DOSE :
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41600 mg/kg
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SEX/DURATION :
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female 17-22 day(s) after conception lactating female 20 day(s) post-birth
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TOXIC EFFECTS :
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Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),404,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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DOSE :
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10400 mg/kg
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SEX/DURATION :
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female 17-22 day(s) after conception lactating female 20 day(s) post-birth
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TOXIC EFFECTS :
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Reproductive - Maternal Effects - ovaries, fallopian tubes
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),404,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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DOSE :
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21 gm/kg
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SEX/DURATION :
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female 17-22 day(s) after conception lactating female 20 day(s) post-birth
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TOXIC EFFECTS :
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Reproductive - Maternal Effects - uterus, cervix, vagina
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),404,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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DOSE :
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8800 mg/kg
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SEX/DURATION :
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female 7-17 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
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REFERENCE :
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NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 35(Suppl 1),370,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Subcutaneous
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DOSE :
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2 gm/kg
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SEX/DURATION :
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female 6-15 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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REFERENCE :
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OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 34,335,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Subcutaneous
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DOSE :
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8 gm/kg
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SEX/DURATION :
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female 6-15 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - other effects to embryo
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REFERENCE :
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OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 34,335,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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DOSE :
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81 mg/kg
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SEX/DURATION :
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female 6-18 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Effects on Embryo or Fetus - fetal death
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REFERENCE :
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OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 34,475,1987
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TYPE OF TEST :
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TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Intravenous
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DOSE :
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19500 ug/kg
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SEX/DURATION :
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female 6-18 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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REFERENCE :
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OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 34,475,1987
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