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Trapidil

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Trapidil
Clinical data
Trade namesRocornal, Avantrin, Travisco
AHFS/Drugs.comInternational Drug Names
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Identifiers
  • N,N-Diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
ECHA InfoCard100.035.834Edit 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
 ☒NcheckY (what is this?)  (verify)

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

Ananalog was assigned the codename AR 12-456.[2]

Pharmacology

[edit]

Based on cell freein vitro activity assays, trapidil at therapeutic concentrations causes selective phosphorylation of cellular proteins through positive modulation of regulatory subunit RII(α/β) containingprotein 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 ofplatelet-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 includingvasodilation and inhibition of platelet aggregation[7][8]

References

[edit]
  1. ^"ロコルナール錠100mg | 持田製薬株式会社".med.mochida.co.jp. Retrieved2025-10-09.
  2. ^Hering S, Bodewei R, Schubert B, Krause EG, Wollenberger A (1985). "Trapidil and other 5-triazolo-(1, 5-alpha)-pyrimidine derivatives as calcium channel blockers in 108CC5 cells".Biomedica Biochimica Acta.44 (5):K37 –K41.PMID 2415119.
  3. ^Sichelschmidt OJ, Hahnefeld C, Hohlfeld T, Herberg FW, Schrör K (June 2003). "Trapidil protects ischemic hearts from reperfusion injury by stimulating PKAII activity".Cardiovascular Research.58 (3):602–610.doi:10.1016/S0008-6363(03)00261-X.PMID 12798433.
  4. ^abcBönisch D, Weber AA, Wittpoth M, Osinski M, Schrör K (August 1998). "Antimitogenic effects of trapidil in coronary artery smooth muscle cells by direct activation of protein kinase A".Molecular Pharmacology.54 (2):241–248.doi:10.1124/mol.54.2.241.PMID 9687564.
  5. ^Maresta A, Balducelli M, Cantini L, Casari A, Chioin R, Fabbri M, et al. (December 1994)."Trapidil (triazolopyrimidine), a platelet-derived growth factor antagonist, reduces restenosis after percutaneous transluminal coronary angioplasty. Results of the randomized, double-blind STARC study. Studio Trapidil versus Aspirin nella Restenosi Coronarica".Circulation.90 (6):2710–2715.doi:10.1161/01.cir.90.6.2710.PMID 7994812.
  6. ^"Trapidil Professional Information (Summary of Product Characteristics/SPC)".Federal Institute for Drugs and Medical Devices (German). January 2019. RetrievedOctober 9, 2025.
  7. ^Büyükafşar K, Yazar A, Düşmez D, Oztürk H, Polat G, Levent A (October 2001). "Effect of trapidil, an antiplatelet and vasodilator agent on gentamicin-induced nephrotoxicity in rats".Pharmacological Research.44 (4):321–328.doi:10.1006/phrs.2001.0864.PMID 11592868.
  8. ^Liu M, Sun Q, Wang Q, Wang X, Lin P, Yang M, et al. (March–April 2014)."Effect of trapidil in myocardial ischemia-reperfusion injury in rabbit".Indian Journal of Pharmacology.46 (2):207–210.doi:10.4103/0253-7613.129320.PMC 3987192.PMID 24741195.
Antiplatelet drugs
Glycoprotein IIb/IIIa inhibitors
ADP receptor/P2Y12inhibitors
Prostaglandin analogue (PGI2)
COX inhibitors
Thromboxane inhibitors
Phosphodiesterase inhibitors
Other
Anticoagulants
Vitamin K antagonists
(inhibitII,VII,IX,X)
Factor Xa inhibitors
(with some II inhibition)
Heparin group/
glycosaminoglycans/
(bindantithrombin)
Direct Xa inhibitors ("xabans")
Direct thrombin (IIa) inhibitors
Other
Thrombolytic drugs/
fibrinolytics
Non-medicinal
Nitrovasodilators
Quinolone vasodilators
Others
PDE1
PDE2
PDE3
PDE4
PDE5
PDE7
PDE9
PDE10
PDE11
Non-selective
Unsorted
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