CHEMICAL IDENTIFICATION
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RTECS NUMBER :
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HP1750000
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CHEMICAL NAME :
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5H-Dibenzo(b,e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)-
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CAS REGISTRY NUMBER :
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5786-21-0
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BEILSTEIN REFERENCE NO. :
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0764984
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LAST UPDATED :
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199807
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DATA ITEMS CITED :
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33
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MOLECULAR FORMULA :
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C18-H19-Cl-N4
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MOLECULAR WEIGHT :
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326.86
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WISWESSER LINE NOTATION :
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T C676 BM INJ FG J- AT6N DNTJ D1
HEALTH HAZARD DATA
ACUTE 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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Human - man
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DOSE/DURATION :
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3280 mg/kg/82W-I
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TOXIC EFFECTS :
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Blood - agranulocytosis
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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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Human - child
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DOSE/DURATION :
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4762 ug/kg
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TOXIC EFFECTS :
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Behavioral - ataxia Behavioral - muscle contraction or spasticity Behavioral - antipsychotic
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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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Human - man
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DOSE/DURATION :
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5357 ug/kg/5D-I
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TOXIC EFFECTS :
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Behavioral - hallucinations, distorted perceptions Behavioral - antipsychotic Cardiac - pulse rate increase, without fall in BP
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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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Human - man
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DOSE/DURATION :
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429 mg/kg/60D-I
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TOXIC EFFECTS :
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Behavioral - muscle contraction or spasticity
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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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Human - woman
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DOSE/DURATION :
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20 mg/kg
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TOXIC EFFECTS :
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Behavioral - coma Gastrointestinal - changes in structure or function of endocrine pancreas Blood - leukopenia
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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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Human - woman
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DOSE/DURATION :
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280 mg/kg/5W-I
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TOXIC EFFECTS :
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Liver - hepatitis (hepatocellular necrosis), diffuse Blood - eosinophilia
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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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Human - man
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DOSE/DURATION :
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27 mg/kg/13D-I
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TOXIC EFFECTS :
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Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic) Behavioral - hallucinations, distorted perceptions Behavioral - ataxia
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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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Human
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DOSE/DURATION :
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5 mg/kg/7D-I
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TOXIC EFFECTS :
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Cardiac - pulse rate increase, without fall in BP
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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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Human - man
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DOSE/DURATION :
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4286 ug/kg/11D-I
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TOXIC EFFECTS :
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Gastrointestinal - hypermotility, diarrhea Blood - changes in cell count (unspecified) Nutritional and Gross Metabolic - body temperature increase
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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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Human - woman
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DOSE/DURATION :
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28 mg/kg/2W-I
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TOXIC EFFECTS :
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Gastrointestinal - changes in structure or function of endocrine pancreas
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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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Human - man
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DOSE/DURATION :
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2211 mg/kg/37W-I
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TOXIC EFFECTS :
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Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes
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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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Human - man
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DOSE/DURATION :
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270 mg/kg/6W-I
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TOXIC EFFECTS :
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Lungs, Thorax, or Respiration - structural or functional change in trachea or bronchi Gastrointestinal - hypermotility, diarrhea Blood - agranulocytosis
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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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251 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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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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240 mg/kg
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TOXIC EFFECTS :
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Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression
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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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41600 ug/kg
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TOXIC EFFECTS :
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Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression
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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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Intramuscular
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SPECIES OBSERVED :
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Rodent - rat
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DOSE/DURATION :
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210 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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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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150 mg/kg
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TOXIC EFFECTS :
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Nutritional and Gross Metabolic - body temperature decrease
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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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Intraperitoneal
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SPECIES OBSERVED :
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Rodent - mouse
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DOSE/DURATION :
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90 mg/kg
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TOXIC EFFECTS :
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Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea
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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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194 mg/kg
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TOXIC EFFECTS :
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Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - excitement
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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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36500 ug/kg
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TOXIC EFFECTS :
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Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression
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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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Mammal - dog
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DOSE/DURATION :
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145 mg/kg
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TOXIC EFFECTS :
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Gastrointestinal - nausea or vomiting
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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 - guinea pig
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DOSE/DURATION :
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510 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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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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900 mg/kg/30D-I
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TOXIC EFFECTS :
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Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
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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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3650 mg/kg/1Y-I
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TOXIC EFFECTS :
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Behavioral - somnolence (general depressed activity) Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain
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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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Mammal - dog
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DOSE/DURATION :
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6320 mg/kg/52W-I
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TOXIC EFFECTS :
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Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Gastrointestinal - changes in structure or function of salivary glands
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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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Primate - monkey
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DOSE/DURATION :
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14560 mg/kg/2Y-I
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TOXIC EFFECTS :
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Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Cardiac - other changes
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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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DOSE :
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1080 mg/kg
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SEX/DURATION :
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female 16-22 day(s) after conception lactating female 20 day(s) post-birth
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TOXIC EFFECTS :
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Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) 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)
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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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DOSE :
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24 mg/kg
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SEX/DURATION :
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female 9-14 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
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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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DOSE :
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96 mg/kg
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SEX/DURATION :
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female 9-14 day(s) after conception
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TOXIC EFFECTS :
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Reproductive - Effects on Newborn - live birth index (measured after birth)
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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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DOSE :
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48 mg/kg
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SEX/DURATION :
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female 7-12 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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TYPE OF TEST :
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Sex chromosome loss and nondisjunction
MUTATION DATA
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TYPE OF TEST :
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Cytogenetic analysis
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TEST SYSTEM :
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Human Lymphocyte
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DOSE/DURATION :
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10 mg/L
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REFERENCE :
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HUGEDQ Human Genetics. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.31- 1976- Volume(issue)/page/year: 38,77,1977 *** REVIEWS *** TOXICOLOGY REVIEW PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 1,1,1977
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