Trapidil

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

Trapidil

Clinical data
Trade names	Rocornal, Avantrin, Travisco
AHFS/Drugs.com	International Drug Names
Routes of administration	By mouth
ATC code	C01DX11 (WHO)
Legal status
Legal status	US: Not approved In general: ℞ (Prescription only)
Identifiers
IUPAC name N,N-Diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
CAS Number	15421-84-8 N
PubChem CID	5531
ChemSpider	5330 N
UNII	EYG5Y6355E
CompTox Dashboard (EPA)	DTXSID0045416
ECHA InfoCard	100.035.834
Chemical and physical data
Formula	C10H15N5
Molar mass	205.265 g·mol−1
3D model (JSmol)	Interactive image
SMILES CCN(CC)c1cc(nc2n1ncn2)C
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 N Key:GSNOZLZNQMLSKJ-UHFFFAOYSA-N N
NY (what is this?)  (verify)

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]