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Technical details about Flurinol, learn more about the structure, uses, toxicity, action, side effects and more

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2D Structure
1. Also known as: Epinastine hcl, 108929-04-0, Alesion, Elestat, Wal-801cl, 80012-44-8
Molecular Formula
C16H16ClN3
Molecular Weight
285.77  g/mol
InChI Key
VKXSGUIOOQPGAF-UHFFFAOYSA-N
FDA UNII
GFM415S5XL

Epinastine Hydrochloride is an histamine H1 receptor antagonist without sedative activity. Epinastine hydrochloride blocks the histamine H1 receptor and inhibits the release of histamine from mast cells. This prevents the typical allergic symptoms that are caused by histamine activity on capillaries, skin, mucous membranes, and on gastrointestinal and bronchial smooth muscles. Typical histamine activities include vasodilation, bronchoconstriction, increased vascular permeability, pain, itching, and spasmodic contractions of gastrointestinal smooth muscles. Epinastine also has affinity for the histamine H2, 5-HT2, and the alpha-1, alpha-2 adrenergic receptors.
1 2D Structure

2D Structure

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2,4-diazatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine;hydrochloride
2.1.2 InChI
InChI=1S/C16H15N3.ClH/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);1H
2.1.3 InChI Key
VKXSGUIOOQPGAF-UHFFFAOYSA-N
2.1.4 Canonical SMILES
C1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N.Cl
2.2 Other Identifiers
2.2.1 UNII
GFM415S5XL
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 3-amino-9,13b-dihydro-1h-benz(c,f)imidazo(1,5a)azepine

2. Epinastine

3. Flurinol

4. Wal 80

5. Wal 801

6. Wal 801 Cl

7. Wal 801cl

8. Wal-80 Cl

2.3.2 Depositor-Supplied Synonyms

1. Epinastine Hcl

2. 108929-04-0

3. Alesion

4. Elestat

5. Wal-801cl

6. 80012-44-8

7. Wal 801 Cl

8. Epinastine Hydrochloride [jan]

9. De-114

10. Epinastine (hydrochloride)

11. Epinastinehydrochloride

12. Gfm415s5xl

13. Wal-802-cl

14. Wal801

15. Relestat

16. 3-amino-9,13b-dihydro-1h-dibenzo[c,f]imidazo[1,5-a]azepine Hydrochloride

17. 9,13b-dihydro-1h-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine Hydrochloride

18. Dsstox_cid_26502

19. Dsstox_rid_81671

20. Dsstox_gsid_46502

21. Epinastine Hydrochloride (jan)

22. Epinastine Monohydrochloride

23. Chebi:51037

24. Cas-108929-04-0

25. Ncgc00165791-02

26. Unii-gfm415s5xl

27. Flurinol

28. (13brs)-9,13b-dihydro-1h-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine Hydrochloride

29. Alesion (tn)

30. Elestat (tn)

31. Mfcd00933434

32. Epinastin Hydrochloride

33. 9,13b-dihydro-1h-dibenz[cf]imidazo[1,5-a]azepine Hydrochloride

34. Wal-801cl Hcl

35. 3-amino-9,13b-dihydro-1h-dibenz(c,f)imidazo(1,5-a)azepine Monohydrochloride

36. Schembl122749

37. Chembl1200491

38. Dtxsid1046502

39. Epinastine For System Suitability

40. Hy-b0640a

41. Hms3652n21

42. Hms3885b15

43. Bcp12119

44. Ex-a1004

45. Tox21_112263

46. Tox21_500501

47. Epinastine Hydrochloride [mi]

48. S4253

49. Akos015967222

50. Tox21_112263_1

51. Ac-1491

52. Ccg-221805

53. Ks-1159

54. Lp00501

55. Epinastine Hydrochloride [mart.]

56. Ih-dibenz(c,f)imidazo(1,5-a)azepin-3-amine, 9,13b-dihydro-, Monohydrochloride

57. Epinastine Hydrochloride [usp-rs]

58. Epinastine Hydrochloride [who-dd]

59. Ncgc00165791-04

60. Ncgc00261186-01

61. 2,4-diazatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine;hydrochloride

62. Db-040850

63. Cs-0013220

64. E0799

65. Ft-0631049

66. Ft-0700527

67. Sw220223-1

68. Epinastine Hydrochloride [orange Book]

69. D01713

70. Epinastine Hydrochloride [ep Monograph]

71. F17420

72. Epinastine Hydrochloride, >=98% (hplc), Solid

73. A857231

74. J-002209

75. Q27122286

76. Epinastine Hydrochloride, European Pharmacopoeia (ep) Reference Standard

77. 1h-dibenz(c,f)imidazo(1,5-a)azepin-3-amine, 9,13b-dihydro-, Hydrochloride (1:1)

78. 3-amino-9,13b-dihydro-1h-dibenz(c,f)imidazo(1,5-a)azepine Hydrochloride, Dl-

79. Epinastine Hydrochloride, United States Pharmacopeia (usp) Reference Standard

80. 2,4-diazatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine;hydron;chloride

81. Epinastine Hydrochloride For System Suitability, European Pharmacopoeia (ep) Reference Standard

2.4 Create Date
2005-06-24
3 Chemical and Physical Properties
Molecular Weight 285.77 g/mol
Molecular Formula C16H16ClN3
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count1
Rotatable Bond Count0
Exact Mass285.1032752 g/mol
Monoisotopic Mass285.1032752 g/mol
Topological Polar Surface Area41.6 Ų
Heavy Atom Count20
Formal Charge0
Complexity378
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count1
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count2
4 Drug and Medication Information
4.1 Drug Information
1 of 4  
Drug NameElestat
PubMed HealthEpinastine (Into the eye)
Drug ClassesOphthalmologic Agent
Drug LabelELESTAT (epinastine HCl ophthalmic solution) 0.05% is a clear, colorless, sterile isotonic solution containing epinastine HCl, an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinast...
Active IngredientEpinastine hydrochloride
Dosage FormSolution/drops
RouteOphthalmic
Strength0.05%
Market StatusPrescription
CompanyAllergan

2 of 4  
Drug NameEpinastine hydrochloride
Drug LabelEpinastine HCl ophthalmic solution, 0.05% is a clear, colorless, sterile isotonic solution containing epinastine HCl, an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes.Epinastine HCl is r...
Active IngredientEpinastine hydrochloride
Dosage FormSolution/drops; Solution
Routeophthalmic; Ophthalmic
Strength0.05%
Market StatusTentative Approval; Prescription
CompanyTesa Pharms; Breckenridge Pharm; Apotex; Sun Pharm Inds; Sandoz

3 of 4  
Drug NameElestat
PubMed HealthEpinastine (Into the eye)
Drug ClassesOphthalmologic Agent
Drug LabelELESTAT (epinastine HCl ophthalmic solution) 0.05% is a clear, colorless, sterile isotonic solution containing epinastine HCl, an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinast...
Active IngredientEpinastine hydrochloride
Dosage FormSolution/drops
RouteOphthalmic
Strength0.05%
Market StatusPrescription
CompanyAllergan

4 of 4  
Drug NameEpinastine hydrochloride
Drug LabelEpinastine HCl ophthalmic solution, 0.05% is a clear, colorless, sterile isotonic solution containing epinastine HCl, an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes.Epinastine HCl is r...
Active IngredientEpinastine hydrochloride
Dosage FormSolution/drops; Solution
Routeophthalmic; Ophthalmic
Strength0.05%
Market StatusTentative Approval; Prescription
CompanyTesa Pharms; Breckenridge Pharm; Apotex; Sun Pharm Inds; Sandoz

5 Pharmacology and Biochemistry
5.1 MeSH Pharmacological Classification

Histamine H1 Antagonists

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)


5.2 FDA Pharmacological Classification
5.2.1 Pharmacological Classes
Adrenergic Receptor Agonist [EPC]; Decreased Histamine Release [PE]; Histamine H1 Receptor Antagonists [MoA]; Histamine-1 Receptor Inhibitor [EPC]; Adrenergic Agonists [MoA]
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