Azatadine dimaleate

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Names

[ Name ]:
Azatadine dimaleate

[Synonym ]:
11-(1-methyl-piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
11-(1-methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (2Z)-but-2-enedioate (1:2)
Azatadinum [INN-Latin]
Azatadina [INN-Spanish]
11-(1-methylpiperidin-4-ylidene)-5,6-dihydrobenzo[1,2]cyclohepta[3,4-b]pyridine
Azatadina
Optimine
Idulian
Azatadinum
Azatidine
5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-, (2Z)-2-butenedioate (1:2)
11-(1-Methyl-4-piperidinylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (2Z)-2-butenedioate (1:2)
Azatadine [INN:BAN]
6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Azatadine dimaleate
6,11--dihydro-11-(N-methyl-4-piperidylidene)-5H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridine
Azatadine maleate
(Z)-but-2-enedioic acid,11-(1-methylpiperidin-4-ylidene)-5,6-dihydrobenzo[1,2]cyclohepta[3,4-b]pyridine
Zadine
Azatadin maleate
AZATADINE
EINECS 223-615-8
Azatadine (dimaleate)

Chemical & Physical Properties

[ Boiling Point ]:
450.1ºC at 760 mmHg

[ Melting Point ]:
152-154°

[ Molecular Formula ]:
C₂₈H₃₀N₂O₈

[ Molecular Weight ]:
522.546

[ Flash Point ]:
226ºC

[ Exact Mass ]:
522.200195

[ PSA ]:
165.33000

[ LogP ]:
3.06920

Toxicological Information

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

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

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H336

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

Azatadine
Thiethylperazine dimaleate
Zolantidine dimaleate
Mifanertinib dimaleate
trifluoperazine dimaleate
(E)-but-2-enedioic acid,2-[2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethoxy]ethanol
1-{6-[4-(4-Benzylphthalazin-1-yl)piperazin-1-yl]pyridin-3-yl}ethanol
1-(2-hydroxyethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4,5,7-tetrone
3-(Dimethylamino)-1-(4-(hexylsulfonyl)-2,6-dimethylphenyl)propan-1-one
N-(3-carbamoyl-5,6-dihydro-4H-cyclopenta[b]thiophen-2-yl)-1-((4-chlorophenyl)sulfonyl)piperidine-4-carboxamide
N-(4-(benzo[d]oxazol-2-yl)phenyl)-1-((4-chlorophenyl)sulfonyl)piperidine-4-carboxamide
N-(4-methoxy-4-methylpentan-2-yl)aniline
N-(5-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-1,3,4-oxadiazol-2-yl)-2,2-diphenylacetamide
2,2,2-trifluoro-N-(2-methoxy-3,5-dinitrophenethyl)acetamide
methyl (1S,3S)-1-amino-3-(4-bromophenyl)cyclopentane-1-carboxylate
Ethyl 1-(2-(2-benzamidothiazol-4-yl)acetyl)piperidine-4-carboxylate

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