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词条 Epinastine
释义

  1. References

  2. External links

{{Drugbox
| verifiedrevid = 461094015
| IUPAC_name = (RS)-3-amino-9,13b-dihydro-1H-dibenz(c,f)imidazo(1,5-a)azepine
| image = Epinastine.svg
| image2 = Epinastine-3D-balls.png
| tradename = Alesion, Elestat, Purivist, Relestat
| Drugs.com = {{drugs.com|monograph|epinastine-hydrochloride}}
| MedlinePlus = a604011
| pregnancy_category = C
| legal_status =
| routes_of_administration = Eye drops
| bioavailability =
| protein_bound = 64%
| metabolism =
| elimination_half-life = 12 hours
| IUPHAR_ligand = 7176
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 80012-43-7
| ATC_prefix = R06
| ATC_suffix = AX24
| ATC_supplemental = {{ATC|S01|GX10}}
| PubChem = 3241
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00751
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 3128
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = Q13WX941EF
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D07900
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 51032
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 1106
| C=16 | H=15 | N=3
| molecular_weight = 249.311 g/mol
| smiles = N\\4=C(\3c1c(cccc1)Cc2c(cccc2)C3C/4)N
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = WHWZLSFABNNENI-UHFFFAOYSA-N
}}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. ^{{cite journal|pmid=19630694|year=2009|last1=Pradhan|first1=S|last2=Abhishek|first2=K|last3=Mah|first3=F|title=Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects|volume=5|issue=9|pages=1135–40|doi=10.1517/17425250903117284|journal=Expert opinion on drug metabolism & toxicology}}
2. ^{{cite journal |vauthors=Walther G, Daniel H, Bechtel WD, Brandt K | title = New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine | journal = Arzneimittel-Forschung | volume = 40 | issue = 4 | pages = 440–6 |date=April 1990 | pmid = 1972625 | doi = | url = }}
3. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=549 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA549 |language=en}}

External links

  • Official U.S. website of Elestat
{{Antihistamines}}{{Histamine receptor modulators}}{{Tricyclics}}{{respiratory-system-drug-stub}}

5 : Azepanes|H1 receptor antagonists|Guanidines|Mast cell stabilizers|Peripherally selective drugs

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