Emedastine

CAS No:
87233-61-2 Category:
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Product Details:

  • CAS No: 87233-61-2
  • AHFC code: 52:02.0
  • Synonyms: Emedastina [INN-Spanish] Emedastine difumarate Emedastinum [INN-Latin]
  • ATC Code: S01GX06
  • Chemical Formula: C20H24O2
  • Molecular Weight: 302.4145
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB01084 (APRD00946)
  • SMILES: CCOCCN1C(=NC2=CC=CC=C12)N1CCCN(C)CC1
  • InChl: KBUZBQVCBVDWKX-UHFFFAOYSA-N
  • PubChem: 3219
  • IUPAC: 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-1,3-benzodiazole

Additional Details

Indication:
For the temporary relief of the signs and symptoms of allergic conjunctivitis.
Pharmacodynamics:
Emedastine is a relatively selective H1-receptor antagonist.
Mode of Action:
Emedastine is a relatively selective, histamine H_ antagonist. In vitro examinations of emedastine's affinity for histamine receptors demonstrate relative selectivity for the H_ histamine receptor. In vivo studies have shown concentration-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva following topical ocular administration. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors.
Metabolism:
Two primary metabolites, 5-hydroxyemedastine and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5'-oxoanalogs of 5-hydroxyemedastine and 6-hydroxy-emedastine and the N-oxide are also formed as minor metabolites.
Toxicity:
Somnolence and malaise have been reported following daily oral administration.
General Reference:
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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