Epinastine

Pair of enantiomers
  • C
Routes of
administrationEye dropsATC code
  • R06AX24 (WHO) S01GX10 (WHO)
Pharmacokinetic dataProtein binding64%Elimination half-life12 hoursIdentifiers
  • (RS)-3-amino-9,13b-dihydro-1H-dibenz(c,f)imidazo(1,5-a)azepine
CAS Number
  • 80012-43-7 checkY
PubChem CID
  • 3241
IUPHAR/BPS
  • 7176
DrugBank
  • DB00751 checkY
ChemSpider
  • 3128 checkY
UNII
  • Q13WX941EF
KEGG
  • D07900 checkY
ChEBI
  • CHEBI:51032 checkY
ChEMBL
  • ChEMBL1106 checkY
CompTox Dashboard (EPA)
  • DTXSID2048371 Edit this at Wikidata
ECHA InfoCard100.120.187 Edit this at WikidataChemical and physical dataFormulaC16H15N3Molar mass249.317 g·mol−13D model (JSmol)
  • Interactive image
  • N\4=C(\N3c1c(cccc1)Cc2c(cccc2)C3C/4)N
  • InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18) checkY
  • Key:WHWZLSFABNNENI-UHFFFAOYSA-N checkY
  (verify)

Epinastine (brand names Alesion, Elestat, Purivist, Relestat) is a second-generation antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis. It is produced by Allergan and marketed by Inspire in the United States.[1] It is highly selective for the H1 receptor and does not cross the blood-brain-barrier.[2]

It was patented in 1980 and came into medical use in 1994.[3]

References

  1. ^ Pradhan S, Abhishek K, Mah F (September 2009). "Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects". Expert Opinion on Drug Metabolism & Toxicology. 5 (9): 1135–1140. doi:10.1517/17425250903117284. PMID 19630694. S2CID 207490591.
  2. ^ Walther G, Daniel H, Bechtel WD, Brandt K (April 1990). "New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine". Arzneimittel-Forschung. 40 (4): 440–446. PMID 1972625.
  3. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 549. ISBN 9783527607495.
  • v
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Benzimidazoles (*)DiarylmethanesEthylenediaminesTricyclicsOthers
For topical use
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H1
Agonists
Antagonists
  • Unknown/unsorted: Azanator
  • Belarizine
  • Elbanizine
  • Flotrenizine
  • GSK1004723
  • Napactadine
  • Tagorizine
  • Trelnarizine
  • Trenizine
H2
Agonists
Antagonists
H3
Agonists
Antagonists
H4
Agonists
Antagonists
See also
Receptor/signaling modulators
Monoamine metabolism modulators
Monoamine reuptake inhibitors
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Classes
Antidepressants
(Tricyclic antidepressants (TCAs))
Antihistamines
Antipsychotics
Anticonvulsants
Anticholinergics
Others
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