*** CHEMICAL IDENTIFICATION ***

RTECS NUMBER            : TH9203800
CHEMICAL NAME           : 1(2H)-Phthalazinone,
                          4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-a
                          zepin-4-yl)-
CAS REGISTRY NUMBER     : 58581-89-8
BEILSTEIN REFERENCE NO. : 0900747
LAST UPDATED            : 199612
DATA ITEMS CITED        : 12
MOLECULAR FORMULA       : C22-H24-Cl-N3-O
MOLECULAR WEIGHT        : 381.94
WISWESSER LINE NOTATION : T66 BVNNJ E1R DG& C- DT7NTJ A1
COMPOUND DESCRIPTOR     : Drug
SYNONYMS/TRADE NAMES :
   * Azelastine
   *   4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalaz
     inone
 
                       *** 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           : 310 mg/kg
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - flaccid paralysis without anesthesia
   (usually neuromuscular blockage)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - other changes
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 43200 ug/kg
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - flaccid paralysis without anesthesia
   (usually neuromuscular blockage)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - other changes
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 59600 ug/kg
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - flaccid paralysis without anesthesia
   (usually neuromuscular blockage)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - other changes
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 26900 ug/kg
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - flaccid paralysis without anesthesia
   (usually neuromuscular blockage)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - other changes
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intramuscular
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 115 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   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: 17,1106,1986
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 124 mg/kg
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - flaccid paralysis without anesthesia
   (usually neuromuscular blockage)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - other changes
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 42800 ug/kg
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - flaccid paralysis without anesthesia
   (usually neuromuscular blockage)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - other changes
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 54200 ug/kg
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - flaccid paralysis without anesthesia
   (usually neuromuscular blockage)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - other changes
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 25400 ug/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   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: 17,1106,1986
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intramuscular
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 59700 ug/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   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: 17,1106,1986
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 51300 ug/kg
TOXIC EFFECTS :
   Behavioral - convulsions or effect on seizure threshold
   Behavioral - changes in motor activity (specific assay)
   Gastrointestinal - nausea or vomiting
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 13700 ug/kg
TOXIC EFFECTS :
   Behavioral - convulsions or effect on seizure threshold
   Behavioral - changes in motor activity (specific assay)
   Gastrointestinal - nausea or vomiting
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 31,1184,1981
 
                            *** END OF RECORD ***