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Tasosartan

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Also known as: 145733-36-4, Ana-756, Way-ana-756, 2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one, Chembl432162, 48g92v856h

Molecular Formula

C₂₃H₂₁N₇O

Molecular Weight

411.5 g/mol

InChI Key

ADXGNEYLLLSOAR-UHFFFAOYSA-N

FDA UNII

48G92V856H

Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Its long duration of action has been attributed to its active metabolite enoltasosartan. It is used to treat patients with essential hypertension.

1 2D Structure

Tasosartan

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

2,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one

2.1.2 InChI

InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29)

2.1.3 InChI Key

ADXGNEYLLLSOAR-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CC1=C2CCC(=O)N(C2=NC(=N1)C)CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5

2.2 Other Identifiers

2.2.1 UNII

48G92V856H

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)pyrido(2,3-d)pyrimidin-7(6h)-one

2. Ana 756

3. Ana-756

4. Ana756

5. Taso-sartan

2.3.2 Depositor-Supplied Synonyms

1. 145733-36-4

2. Ana-756

3. Way-ana-756

4. 2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one

5. Chembl432162

6. 48g92v856h

7. Verdia

8. 2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[6,5-d]pyrimidin-7-one

9. 5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)pyrido(2,3-d)pyrimidin-7(6h)-one

10. Taso-sartan

11. 8-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6h)-one

12. Ana756

13. Tasosartan (usan/inn)

14. Tasosartan [usan:inn:ban]

15. Unii-48g92v856h

16. Ana 756

17. Way-126756

18. Ethylglycidylether

19. Tasosartan [mi]

20. Tasosartan [inn]

21. Tasosartan [usan]

22. Tasosartan [mart.]

23. Tasosartan [who-dd]

24. Schembl49626

25. Way-ana 756

26. Gtpl6898

27. Dtxsid40163148

28. Ex-a082

29. Chebi:135666

30. Act06754

31. Amy31168

32. Bcp06091

33. Hy-a0250

34. Bdbm50040439

35. Mfcd00865905

36. Zinc13444037

37. Akos000278114

38. Db01349

39. Ds-6574

40. Ncgc00390218-01

41. 5,8-dihydro-2,4-dimethyl-8-(p-(o-1h-tetrazol-5-ylphenyl)benzyl)pyrido(2,3-d)pyrimidin-7(6h)-one

42. Ac-35374

43. Db-042802

44. Cs-0017594

45. Ft-0631174

46. D06010

47. 733t364

48. A846571

49. L001443

50. J-524315

51. Q1317131

52. 2,4-dimethyl-8-({4-[2-(2h-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-5h,6h,7h,8h-pyrido[2,3-d]pyrimidin-7-one

53. 2,4-dimethyl-8-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one

54. 2,4-dimethyl-8-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one

55. 2,4-dimethyl-8-[2'-(1h-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one

56. 2,4-dimethyl-8-{[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6h)-one

57. 5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-pyrido[2,3-d]pyrimidin-7(6h)-one

58. 5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]pyrido[2,3-d]pyrimidin-7(6h)-one

59. 8-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,6-dihydropyrido[2,3-d]pyrimidin-7(8h)-one

60. 8-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-2,4-dimethyl-5,6-dihydropyrido[2,3-d]pyrimidin-7(8h)-one

61. Pyrido(2,3-d)pyrimidin-7(6h)-one, 5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-

62. Pyrido[2,3-d]pyrimidin-7(6h)-one, 5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-

2.4 Create Date

2005-08-08

3 Chemical and Physical Properties

Molecular Formula	C₂₃H₂₁N₇O
Molecular Weight	411.5 g/mol
XLogP3	3
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	4
Exact Mass	411.18075832 g/mol
Monoisotopic Mass	411.18075832 g/mol
Topological Polar Surface Area	101 Å²
Heavy Atom Count	31
Formal Charge	0
Complexity	625
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

Tasosartan is infrequently in the treatment of hypertension and heart failure.

5 Pharmacology and Biochemistry

5.1 Pharmacology

By blocking the angiotensin II (AT1) receptor, the drug ultimately causes vasodilation, reduced secretion of vasopressin (ADH), reduced production and secretion of aldosterone, amongst other actions leading to the combined effect of a reduction of blood pressure.

5.2 MeSH Pharmacological Classification

Angiotensin II Type 1 Receptor Blockers

Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS. (See all compounds classified as Angiotensin II Type 1 Receptor Blockers.)

5.3 ATC Code

C - Cardiovascular system

C09 - Agents acting on the renin-angiotensin system

C09C - Angiotensin ii receptor blockers (arbs), plain

C09CA - Angiotensin ii receptor blockers (arbs), plain

C09CA05 - Tasosartan

5.4 Metabolism/Metabolites

Tasosartan has known human metabolites that include enoltasosartan.

S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560

5.5 Mechanism of Action

Tasosartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. AT1 receptor antagonists avoid the nonspecificity of the Ang I converting enzyme (ACE) inhibitors.

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