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Chemistry

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Also known as: 65847-85-0, Up 164, Flomax;up 164, 2-morpholin-4-ylethyl 2-[3-(trifluoromethyl)anilino]pyridine-3-carboxylate, R133mwh7x1, 2-morpholinoethyl 2-((3-(trifluoromethyl)phenyl)amino)nicotinate
Molecular Formula
C19H20F3N3O3
Molecular Weight
395.4  g/mol
InChI Key
LDXSPUSKBDTEKA-UHFFFAOYSA-N
FDA UNII
R133MWH7X1

Morniflumate
Morniflumate is a non-steroidal anti-inflammatory drug with antipyretic properties. It is the morpholinoethyl ester of niflumic acid. In one study, post morniflumate ingestion, physical examination and clinical symptoms of those with bronchitis showed improvement.
1 2D Structure

Morniflumate

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-morpholin-4-ylethyl 2-[3-(trifluoromethyl)anilino]pyridine-3-carboxylate
2.1.2 InChI
InChI=1S/C19H20F3N3O3/c20-19(21,22)14-3-1-4-15(13-14)24-17-16(5-2-6-23-17)18(26)28-12-9-25-7-10-27-11-8-25/h1-6,13H,7-12H2,(H,23,24)
2.1.3 InChI Key
LDXSPUSKBDTEKA-UHFFFAOYSA-N
2.1.4 Canonical SMILES
C1COCCN1CCOC(=O)C2=C(N=CC=C2)NC3=CC=CC(=C3)C(F)(F)F
2.2 Other Identifiers
2.2.1 UNII
R133MWH7X1
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Beta-morpholinoethyl Niflumate

2. Niflumic Acid Beta-morpholinoethyl Ester

2.3.2 Depositor-Supplied Synonyms

1. 65847-85-0

2. Up 164

3. Flomax;up 164

4. 2-morpholin-4-ylethyl 2-[3-(trifluoromethyl)anilino]pyridine-3-carboxylate

5. R133mwh7x1

6. 2-morpholinoethyl 2-((3-(trifluoromethyl)phenyl)amino)nicotinate

7. Up-164

8. Morniflumate (usan)

9. Morniflumatum

10. Morniflumate [usan]

11. Morniflumato

12. 2-(morpholin-4-yl)ethyl 2-{[3-(trifluoromethyl)phenyl]amino}pyridine-3-carboxylate

13. 3-pyridinecarboxylic Acid, 2-((3-(trifluoromethyl)phenyl)amino)-, 2-(4-morpholinylethyl) Ester

14. Morniflumate [usan:inn]

15. Morniflumatum [inn-latin]

16. Morniflumato [inn-spanish]

17. Unii-r133mwh7x1

18. Nifluminsaeure 2-morpholinoethylester

19. Niflumic Acid Beta-morpholinoethyl Ester

20. Morniflumate [inn]

21. Dsstox_cid_31587

22. Dsstox_rid_97471

23. Dsstox_gsid_57798

24. Schembl50683

25. Morniflumate [mart.]

26. Morniflumate [who-dd]

27. 2-morpholinoethyl 2-(3-trifluoromethylanilino)nicotinat

28. Chembl2105059

29. Dtxsid6057798

30. Chebi:136018

31. Tox21_113913

32. Zinc21999791

33. 2-morpholinoethyl 2-(alpha,alpha,alpha-trifluoro-m-toluidino)nicotinate

34. Akos015918126

35. Db09285

36. Ncgc00262915-01

37. As-15259

38. Hy-17488

39. Cas-65847-85-0

40. Db-054848

41. Cs-0009223

42. Ft-0628990

43. D05078

44. 847m850

45. A835248

46. Niflumic Acid .beta.-morpholinoethyl Ester

47. 2,4-dimethyl-thiazole-5-carboxylicacidamide

48. Q-201412

49. Q6912761

50. Niflumic Acid .beta.-morpholinoethyl Ester [mi]

51. 2-morpholinoethyl 2-(3-(trifluoromethyl)phenylamino)nicotinate

52. 2-morpholinoethyl2-((3-(trifluoromethyl)phenyl)amino)nicotinate

53. 2-morpholinoethyl 2-(a,a,a-trifluoro-m-toluidino)nicotinate

54. 2-[3-(trifluoromethyl)anilino]-3-pyridinecarboxylic Acid 2-(4-morpholinyl)ethyl Ester

55. 2-morpholin-4-ylethyl 2-[[3-(trifluoromethyl)phenyl]amino]pyridine-3-carboxylate

2.4 Create Date
2005-08-08
3 Chemical and Physical Properties
Molecular Weight 395.4 g/mol
Molecular Formula C19H20F3N3O3
XLogP33.7
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count9
Rotatable Bond Count7
Exact Mass395.14567599 g/mol
Monoisotopic Mass395.14567599 g/mol
Topological Polar Surface Area63.7 Ų
Heavy Atom Count28
Formal Charge0
Complexity501
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Morniflumate is indicated for the treatment of inflammatory conditions affecting the airways, ENT system, urogenital tract and bone and joint systems in adults. In Italy, morniflumate is also indicated for the treatment of pain associated with ear, nose, throat (ENT) and gastrointestinal inflammatory conditions in children. Morniflumate is a well established NSAID that has been in use for over three decades in Italy (particularly for the treatment of upper respiratory tract infections in children), France, Belgium, Austria, Switzerland, Spain and Portugal; it has a generally favorable tolerability profile.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Morniflumate, given at therapeutic dosages to healthy human volunteers, on leukotriene B4 (LTB4) and thromboxane (TXB2) synthesis, both in purified PMNs (polymorphnuclear neutrophils) and in whole blood. In whole blood experiments, morniflumate reduced blood leukotriene B4 (LTB4) synthesis induced by Ca-ionophore A23187 Bx approximately 50%, both after a single dose and at steady state; the level of inhibition showed a pattern similar to the plasma levels of the bioactive metabolite of morniflumate (M1). The inhibition of serum thromboxane B2 (TXB2) levels was higher than 85%. Hence, morniflumate is demonstrated to reduce arachidonic acid metabolism, by exerting its effects on cyclooxygenase and 5-lipoxygenase. This characteristic might provide a better approach for anti-inflammatory therapy. In several animal models orally administered morniflumate, the beta-morpholinoethyl ester of niflumic acid, proved almost equal to the parent compound in anti-inflammatory, analgesic and antipyretic activity with the absence of gastric irritating/ulcerogenic effects of its acidic parent compound.


5.2 ATC Code

M - Musculo-skeletal system

M01 - Antiinflammatory and antirheumatic products

M01A - Antiinflammatory and antirheumatic products, non-steroids

M01AX - Other antiinflammatory and antirheumatic agents, non-steroids

M01AX22 - Morniflumate


5.3 Absorption, Distribution and Excretion

Route of Elimination

0.12 L /kg on average


Clearance

45 ml/min


5.4 Metabolism/Metabolites

The pharmacokinetic availability of niflumic acid in two different pharmaceutical preparations have been studied in 12 subjects after oral administration. Bioavailability and pharmacokinetics studies after oral and intravenous (IV) administration demonstrate that morniflumate is absorbed as from the gastrointestinal tract, followed by rapid hydrolysis in the plasma, releasing the free acidic form, the molecule responsible for its anti-inflammatory effects. The ester displays gastroprotective effect against the ulcerogenic effects of niflumic acid.


5.5 Biological Half-Life

2h


5.6 Mechanism of Action

The primary mechanism of niflumic acid and its ester is action is inhibition of enzymes involved in the synthesis of inflammatory prostaglandins. This medication inhibits cyclooxygenase and 5-lipoxygenase pathways, which lead to fever and inflammation. Niflumic acid, a calcium-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of inflammatory conditions. Niflumic acid does directly inhibit calcium channels or activate potassium channels. Niflumic acid selectively reduces noradrenaline- and 5-HT-induced pressor responses by inhibiting a mechanism which leads to the opening of voltage-gated calcium channels. Niflumic acid (NFA) produces biphasic behavior on human CLC-K channels that suggests the presence of two functionally different binding sites: an activating site and a blocking site.


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