INHIBITION OF CYCLIC-AMP SPLITTING NUCLEOTIDE HYDROLASE OF HEART-MUSCLE BY 5-METHYL-7-DIETHYLAMINO-S-TRIAZOLA-(1,5-ALPHA) PYRIMIDINE (ROCONAL)

  • 1 January 1976
    • journal article
    • research article
    • Vol. 35  (2) , 167-173
Abstract
5-Methyl-7-diethylamino-s-triazolo-(1,5-.alpha.)pyrimidine (Rocornal, trapidil), which has been introduced in clinical medicine as a coronary vasodilator, competitively inhibits the cyclic (c)AMP splitting nucleotide hydrolase (phosphodiesterase) from heart muscle [bovine]. The KI [inhibition constant] value for Rocornal is 0.14 .+-. 0.016 mM. Enzyme inhibition by this compound is abolished after an exchange of the diethylamino-group in C-7 position against dimethylamine and chloride. The proved triazolo-pyrimidines were without effect on myocardial [guinea-pig and rat] adenylate cyclase activity. The vasodilatory effect of Rocornal may be realized in smooth muscle cells by an inhibition of cAMP breakdown.

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