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    Trapidil

    ACTIVE PHARMA INGREDIENTS

    FINISHED DOSAGE FORMULATIONS

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    2D Structure
    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

    2D Structure

    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 Weight 205.26 g/mol
    Molecular Formula C10H15N5
    XLogP31.7
    Hydrogen Bond Donor Count0
    Hydrogen Bond Acceptor Count4
    Rotatable Bond Count3
    Exact Mass205.13274550 g/mol
    Monoisotopic Mass205.13274550 g/mol
    Topological Polar Surface Area46.3 Ų
    Heavy Atom Count15
    Formal Charge0
    Complexity206
    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

    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.