Chemistry:Trapidil
Trapidil is used in the treatment of chronic stable angina pectoris. It is currently marketed in Japan under the brand name Rocornal.[1]
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]
References
- ↑ "ロコルナール錠100mg | 持田製薬株式会社". https://med.mochida.co.jp/index/rcr_100-h.html.
- ↑ "Trapidil and other 5-triazolo-(1, 5-alpha)-pyrimidine derivatives as calcium channel blockers in 108CC5 cells". Biomedica Biochimica Acta 44 (5): K37–K41. 1985. PMID 2415119.
- ↑ "Trapidil protects ischemic hearts from reperfusion injury by stimulating PKAII activity". Cardiovascular Research 58 (3): 602–610. June 2003. doi:10.1016/S0008-6363(03)00261-X. PMID 12798433.
- ↑ 4.0 4.1 4.2 "Antimitogenic effects of trapidil in coronary artery smooth muscle cells by direct activation of protein kinase A". Molecular Pharmacology 54 (2): 241–248. August 1998. doi:10.1124/mol.54.2.241. PMID 9687564.
- ↑ "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. December 1994. doi:10.1161/01.cir.90.6.2710. PMID 7994812.
- ↑ "Trapidil Professional Information (Summary of Product Characteristics/SPC)". January 2019. https://portal.dimdi.de/amguifree/am/docoutput/additionaldocs.xhtml?mpdidentifier=3000242.
- ↑ "Effect of trapidil, an antiplatelet and vasodilator agent on gentamicin-induced nephrotoxicity in rats". Pharmacological Research 44 (4): 321–328. October 2001. doi:10.1006/phrs.2001.0864. PMID 11592868.
- ↑ "Effect of trapidil in myocardial ischemia-reperfusion injury in rabbit". Indian Journal of Pharmacology 46 (2): 207–210. March–April 2014. doi:10.4103/0253-7613.129320. PMID 24741195.
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