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Trapidil

Chemical compound From Wikipedia, the free encyclopedia

Trapidil is used in the treatment of chronic stable angina pectoris. It is currently marketed in Japan under the brand name Rocornal.[1]

Trade namesRocornal, Avantrin, Travisco
ATC code
Quick facts Clinical data, Trade names ...
Trapidil
Clinical data
Trade namesRocornal, Avantrin, Travisco
AHFS/Drugs.comInternational Drug Names
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • US: Not approved
  • In general: ℞ (Prescription only)
Identifiers
  • N,N-Diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
ECHA InfoCard100.035.834 Edit this at Wikidata
Chemical and physical data
FormulaC10H15N5
Molar mass205.265 g·mol−1
3D model (JSmol)
  • CCN(CC)c1cc(nc2n1ncn2)C
  • 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 ☒N
  • Key:GSNOZLZNQMLSKJ-UHFFFAOYSA-N ☒N
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An analog was assigned the codename AR 12-456.[2]

Pharmacology

Based on cell free in vitro activity assays, trapidil at therapeutic concentrations causes selective phosphorylation of cellular proteins through positive modulation of regulatory subunit RII(α/β) containing protein kinase A (PKA).[3][4] At higher, non-physiologically relevant concentrations, which are generally not achieved after administration of therapeutic doses, non-selective inhibition of phosphodiesterases occurs.[4] Further, the previous documented activities as an antagonist of platelet-derived growth factor[5] are abolished when a PKA inhibitor is administered, suggesting that these noted activities are PKA mediated.[4] At these higher concentrations,[6] additional effects have been noted including vasodilation and inhibition of platelet aggregation[7][8]

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