*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : DE8025500
CHEMICAL NAME : 11H-Benzo(5,6)cyclohepta(1,2-b)pyridine,
5,6-dihydro-11-(1-methyl-4-piperidylidene)-,
dimaleate
CAS REGISTRY NUMBER : 3978-86-7
LAST UPDATED : 199604
DATA ITEMS CITED : 11
MOLECULAR FORMULA : C20-H22-N2.2C4-H4-O4
MOLECULAR WEIGHT : 522.60
WISWESSER LINE NOTATION : T C676 DN&T&J B1- AT6N CUTJ &QV1U1VQ 2
COMPOUND DESCRIPTOR : Drug
Human
SYNONYMS/TRADE NAMES :
* Azatadine dimaleate
* Azatadine maleate
* 6,11-Dihydro-11-(1-methyl-4-piperidylidene)5H-benzo(5,6)cyclohepta(1,2-b
)pyridine dimaleate
* Idulian
* Optimine
* Sch 10649
* Zadine
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 286 mg/kg/24H-I
TOXIC EFFECTS :
Behavioral - muscle contraction or spasticity
REFERENCE :
MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd.,
71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914-
Volume(issue)/page/year: 141,449,1984
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 440 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year:
18,185,1971
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 166 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 :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
1,173,1975
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 1 gm/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 :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
1,173,1975
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 165 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AGACBH Agents and Actions, A Swiss Journal of Pharmacology. (Birkhaeuser
Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1969/70-
Volume(issue)/page/year: 4,264,1974
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 105 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 :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
1,173,1975
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 178 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 :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
1,173,1975
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 50 mg/kg
TOXIC EFFECTS :
Behavioral - tremor
Gastrointestinal - nausea or vomiting
Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
1,79,1975
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - guinea pig
DOSE/DURATION : 356 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AGACBH Agents and Actions, A Swiss Journal of Pharmacology. (Birkhaeuser
Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1969/70-
Volume(issue)/page/year: 4,264,1974
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 8400 mg/kg/4W-I
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of endocrine pancreas
Liver - fatty liver degeneration
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
1,173,1975
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 27300 mg/kg/26W-I
TOXIC EFFECTS :
Liver - fatty liver degeneration
Musculoskeletal - other changes
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
1,173,1975
*** END OF RECORD ***