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Trapidil

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Chemistry

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Also known as: 15421-84-8, Rocornal, Trapymin, Avantrin, Trapymine, N,n-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine

Molecular Formula

C₁₀H₁₅N₅

Molecular Weight

205.26 g/mol

InChI Key

GSNOZLZNQMLSKJ-UHFFFAOYSA-N

FDA UNII

EYG5Y6355E

A coronary vasodilator agent.

1 2D Structure

Trapidil

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

N,N-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine

2.1.2 InChI

InChI=1S/C10H15N5/c1-4-14(5-2)9-6-8(3)13-10-11-7-12-15(9)10/h6-7H,4-5H2,1-3H3

2.1.3 InChI Key

GSNOZLZNQMLSKJ-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CCN(CC)C1=CC(=NC2=NC=NN12)C

2.2 Other Identifiers

2.2.1 UNII

EYG5Y6355E

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Rocornal

2. Trapymin

2.3.2 Depositor-Supplied Synonyms

1. 15421-84-8

2. Rocornal

3. Trapymin

4. Avantrin

5. Trapymine

6. N,n-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine

7. Ar 12008

8. Ar-12008

9. (1,2,4)triazolo(1,5-a)pyrimidin-7-amine, N,n-diethyl-5-methyl-

10. [1,2,4]triazolo[1,5-a]pyrimidin-7-amine,n,n-diethyl-5-methyl-

11. 7-diethylamino-5-methyl-s-triazolo(1,5-a)pyrimidine

12. Mls000567667

13. Eyg5y6355e

14. N,n-diethyl-5-methyl-(1,2,4)triazolo(1,5-a)pyrimidine-7-amine

15. Ncgc00016715-01

16. S-triazolo(1,5-a)pyrimidin-7-amine, N,n-diethyl-5-methyl-

17. Smr000154170

18. Cas-15421-84-8

19. Dsstox_cid_25416

20. Dsstox_rid_80865

21. Dsstox_gsid_45416

22. 7-(diethylamino)-5-methyl-s-triazolo(1,5-a)pyrimidine

23. Trapidilum

24. Trapidilum [inn-latin]

25. [1,2,4]triazolo[1,5-a]pyrimidin-7-amine, N,n-diethyl-5-methyl-

26. Einecs 239-434-2

27. Trapidil [inn:ban:jan]

28. Brn 0186842

29. Unii-eyg5y6355e

30. 7-(diethylamino)-5-methyl-s-triazolo[1,5-a]pyrimidine

31. Rocornal (tn)

32. Trapidil,(s)

33. Mfcd00193104

34. 5-methyl-7-diethylamino-s-triazolo-(1,5-a)-pyrimidine

35. Opera_id_461

36. 5-methyl-7-diaethylamino-s-triazolo(1.5-a)pyrimidin [german]

37. Trapidil [inn]

38. Trapidil [jan]

39. Trapidil [mi]

40. Prestwick0_001012

41. Prestwick1_001012

42. Prestwick2_001012

43. Prestwick3_001012

44. Trapidil (jp17/inn)

45. Trapidil [mart.]

46. Trapidil [who-dd]

47. Schembl33563

48. Bspbio_001163

49. Mls000881142

50. Spbio_003034

51. 5-methyl-7-diaethylamino-s-triazolo(1.5-a)pyrimidin

52. Bpbio1_001281

53. Chembl132767

54. Zinc2202

55. Trapidil [ep Monograph]

56. Trapidil, >=98% (hplc)

57. Dtxsid0045416

58. Chebi:32254

59. Hms1571k05

60. Hms1735k19

61. Hms2098k05

62. Hms2231g07

63. Hms3372j09

64. Hms3715k05

65. Bcp09350

66. Hy-b1016

67. Tox21_110578

68. S4736

69. Akos001093408

70. Tox21_110578_1

71. Ccg-221012

72. Cs-4529

73. Db09283

74. Hs-0048

75. N,n-diethyl-4-methyl-1,5,7,9-tetrazabicyclo[4.3.0]nona-2,4,6,8-tetraen-2-amine

76. Ncgc00016715-02

77. Ncgc00016715-03

78. Ncgc00016715-04

79. Ac-32565

80. Ab00457635

81. Ft-0763046

82. D01220

83. F31376

84. Ab00457635-12

85. 421t848

86. A927178

87. Sr-01000673280

88. Q2449982

89. Sr-01000673280-3

90. 5-methyl-7-diethylamino-s-triazolo(1,5-a)pyrimidine

91. Brd-k95763993-001-03-7

92. Z56791867

93. 5-methyl-7-(diethylamino)-s-triazolo[1,5-a]pyrimidine

94. 7-(diethylamino)-5-methyl-2-triazolo[1,5-a]pyrimidine

95. Trapidil, European Pharmacopoeia (ep) Reference Standard

96. 7-(diethylamino)-5-methyl-s-triazolo(1,5-a)pyrimidine.

97. Diethyl-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)amine

98. N,n-diethyl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine #

99. N,n-diethyl-n-(5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)amine

2.4 Create Date

2005-03-25

3 Chemical and Physical Properties

Molecular Formula	C₁₀H₁₅N₅
Molecular Weight	205.26 g/mol
XLogP3	1.7
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Exact Mass	205.13274550 g/mol
Monoisotopic Mass	205.13274550 g/mol
Topological Polar Surface Area	46.3 Å²
Heavy Atom Count	15
Formal Charge	0
Complexity	206
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

Used in the treatment of chronic stable angina.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Trapidil exerts vasodilatory and antiplatelet effects. It also inhibits the activity of platelet derived growth factor (PDGF).

5.2 MeSH Pharmacological Classification

Vasodilator Agents

Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

Platelet Aggregation Inhibitors

Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. (See all compounds classified as Platelet Aggregation Inhibitors.)

Phosphodiesterase Inhibitors

Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases. (See all compounds classified as Phosphodiesterase Inhibitors.)

5.3 ATC Code

C - Cardiovascular system

C01 - Cardiac therapy

C01D - Vasodilators used in cardiac diseases

C01DX - Other vasodilators used in cardiac diseases

C01DX11 - Trapidil

5.4 Absorption, Distribution and Excretion

Absorption

Trapidil has a Tmax of 1 h.

Clearance

The apparent clearance is 179 mL/min for a single dose and 273 mL/min for steady state dosing.

5.5 Biological Half-Life

The half life of elimination is 1.31 h for a single dose and 1.14 h for steady state dosing.

5.6 Mechanism of Action

Trapidil is thought to inhibit cyclic adenosine monophosphate (cAMP) phosphodiesterase enzymes. The resultant increase in cAMP potentiates the inhibition of platelets by adenosine. The reduction in platelet activation is likely responsible for the decrease in thromboxane A2 generation seen with trapidil. The increase in cAMP is also likely responsible for the vasdilatory action of trapidil. The increase in protein kinase A activity due to increased cAMP activated L-type calcium channels in the heart leading to increased depolarization and a positive inotropic effect. Lastly, PKA inactivates Raf-1, an activator of mitogen activated protein kinase (MAPK), which leads to a reduction in MAPK activation. This reduction in MAPK prevents mitogenesis due to PDGF binding to PDGF receptors.

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