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Substance Name: Azelastine [INN:BAN]
RN: 58581-89-8
UNII: ZQI909440X
InChIKey: MBUVEWMHONZEQD-UHFFFAOYSA-N

Note

  • Azeptin is azelastine hydrochloride; eye drop formulation effective in relieving symptoms of allergic conjunctivitis.

Molecular Formula

  • C22-H24-Cl-N3-O

Molecular Weight

  • 381.905
 

Classification Codes

  • Anti-Allergic Agents
  • Anti-Asthmatic Agents
  • Autonomic Agents
  • Bronchodilator Agents
  • Drug / Therapeutic Agent
  • Enzyme Inhibitors
  • Histamine Agents
  • Histamine Antagonists
  • Histamine H1 Antagonists
  • Histamine H1 Antagonists, Non-Sedating
  • Lipoxygenase Inhibitors
  • Neurotransmitter Agents
  • Peripheral Nervous System Agents
  • Respiratory System Agents

Names and Synonyms

Name of Substance

  • Azelastine
  • Azelastine [INN:BAN]

Synonyms

  • (+-)-Azelastine
  • 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalazinone
  • Azelastina
  • Azelastina [INN-Spanish]
  • Azelastine
  • Azelastinum
  • Azelastinum [INN-Latin]
  • BRN 0900747
  • HSDB 7991
  • UNII-ZQI909440X

Systematic Names

  • 1(2H)-Phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-
  • 4-((4-Chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone hydrochloride

Registry Numbers

CAS Registry Number

  • 58581-89-8

FDA UNII

  • ZQI909440X

Other Registry Number

  • 153483-42-2

Related Registry Numbers

  • 37932-96-0 (unspecified hydrochloride)
  • 79307-93-0 (hydrochloride)

System Generated Number

  • 0058581898

Structure Descriptors

InChI

1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3

InChIKey

MBUVEWMHONZEQD-UHFFFAOYSA-N

Smiles

C1C[C@@H](CCC[N@@]1C)n1nc(c2ccccc2c1=O)Cc1ccc(cc1)Cl

Toxicity

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
dog LD50 intravenous 13700ug/kg (13.7mg/kg) BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

GASTROINTESTINAL: NAUSEA OR VOMITING
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
dog LD50 oral 51300ug/kg (51.3mg/kg) GASTROINTESTINAL: NAUSEA OR VOMITING

BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
mouse LD50 intramuscular 59700ug/kg (59.7mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 17, Pg. 1106, 1986.
mouse LD50 intraperitoneal 42800ug/kg (42.8mg/kg) LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
mouse LD50 intravenous 25400ug/kg (25.4mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 17, Pg. 1106, 1986.
mouse LD50 oral 124mg/kg (124mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
mouse LD50 subcutaneous 54200ug/kg (54.2mg/kg) LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 intramuscular 115mg/kg (115mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 17, Pg. 1106, 1986.
rat LD50 intraperitoneal 43200ug/kg (43.2mg/kg) LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 intravenous 26900ug/kg (26.9mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 oral 310mg/kg (310mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 subcutaneous 59600ug/kg (59.6mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)
Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.