CHEMICAL IDENTIFICATION
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RTECS NUMBER :
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NI2931000
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CHEMICAL NAME :
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Imidazo(4,5-d)(1,3)diazepin-8-ol, 3-(2-deoxy-beta-D-pentofuranosyl)-3,6,7,8-tetrahydro- , (R)-
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CAS REGISTRY NUMBER :
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53910-25-1
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LAST UPDATED :
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199703
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DATA ITEMS CITED :
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23
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MOLECULAR FORMULA :
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C11-H16-N4-O4
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MOLECULAR WEIGHT :
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268.31
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
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TYPE OF TEST :
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LDLo - Lowest published lethal dose
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ROUTE OF EXPOSURE :
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Unreported
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SPECIES OBSERVED :
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Human - woman
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DOSE/DURATION :
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390 mg/kg/3D-I
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TOXIC EFFECTS :
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Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - thrombocytopenia Blood - other hemolysis with or without anemia
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REFERENCE :
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IEDIEP Internal Medicine. (The Japanese Society of Internal Medicine, 34-3, 3-chome, Hongo, Bunkyo-ku, Tokyo 113, Japan) V.31- 1992- Volume(issue)/page/year: 34,593,1995
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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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227 mg/kg
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TOXIC EFFECTS :
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Kidney, Ureter, Bladder - hematuria Nutritional and Gross Metabolic - body temperature decrease
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,7888,1990
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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 - mouse
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DOSE/DURATION :
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122 mg/kg
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TOXIC EFFECTS :
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Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Nutritional and Gross Metabolic - weight loss or decreased weight gain
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REFERENCE :
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NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB84-211424
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TYPE OF TEST :
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LDLo - Lowest published lethal 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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360 mg/kg
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TOXIC EFFECTS :
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Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - nausea or vomiting
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,7888,1990 ** 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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Intravenous
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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650 mg/kg/26W-I
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TOXIC EFFECTS :
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Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Endocrine - other changes Blood - changes in bone marrow (not otherwise specified)
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REFERENCE :
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TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 22,519,1994
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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 - mouse
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DOSE/DURATION :
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80 mg/kg/4W-I
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TOXIC EFFECTS :
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Lungs, Thorax, or Respiration - changes in lung weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
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REFERENCE :
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CCPHDZ Cancer Chemotherapy and Pharmacology. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1978- Volume(issue)/page/year: 5,83,1980
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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 - mouse
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DOSE/DURATION :
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18200 ug/kg/26W-C
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TOXIC EFFECTS :
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Blood - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4277,1991
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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 - mouse
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DOSE/DURATION :
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28 mg/kg/4W-I
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TOXIC EFFECTS :
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Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in leukocyte (WBC) count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,1271,1991
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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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91 ug/kg/26W-C
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TOXIC EFFECTS :
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Blood - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4277,1991
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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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14 mg/kg/4W-I
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TOXIC EFFECTS :
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Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,1271,1991 ** 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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7500 ug/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 - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) 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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TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 44,325,1991
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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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7500 ug/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 Newborn - sex ratio
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REFERENCE :
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TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 44,325,1991
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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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DOSE :
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500 ug/kg
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SEX/DURATION :
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female 10 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 - blood and lymphatic systems (including spleen and marrow) Reproductive - Specific Developmental Abnormalities - immune and reticuloendothelial system
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REFERENCE :
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TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 25(2),36A,1982
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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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DOSE :
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5 mg/kg
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SEX/DURATION :
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female 8 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
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REFERENCE :
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TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 40,615,1989
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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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DOSE :
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1 mg/kg
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SEX/DURATION :
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female 7 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)
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REFERENCE :
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TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 45,91,1992
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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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DOSE :
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5 mg/kg
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SEX/DURATION :
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female 7 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system
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REFERENCE :
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TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 47,17,1993
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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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DOSE :
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5 mg/kg
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SEX/DURATION :
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female 7 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System
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REFERENCE :
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TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 47,17,1993
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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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5 mg/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)
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3977,1991
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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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8300 ug/kg
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SEX/DURATION :
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male 9 week(s) pre-mating female 2 week(s) pre-mating - 6 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Maternal Effects - other 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)
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3965,1991
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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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8300 ug/kg
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SEX/DURATION :
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male 9 week(s) pre-mating female 2 week(s) pre-mating - 6 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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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3965,1991
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TYPE OF TEST :
-
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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28 ug/kg
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SEX/DURATION :
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female 15-21 day(s) after conception lactating female 21 day(s) post-birth
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TOXIC EFFECTS :
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Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4329,1991
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
-
Intravenous
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DOSE :
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28 ug/kg
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SEX/DURATION :
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female 15-21 day(s) after conception lactating female 21 day(s) post-birth
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TOXIC EFFECTS :
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Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4329,1991
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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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1300 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 - Maternal Effects - other effects Reproductive - Fertility - abortion Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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REFERENCE :
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KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4319,1991
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