COMPARISON OF SOME CONFORMATIONALLY RIGID BENZYLAMINE ANALOGS AS SUBSTRATES FOR RABBIT LUNG N-METHYLTRANSFERASE

  • 1 January 1980
    • journal article
    • research article
    • Vol. 30  (3) , 401-408
Abstract
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline hydrochloride (SK&F 64139) and 8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine hydrochloride (LY134046) were excellent substrates for rabbit lung N-methyltransferase using S-adenosyl-L-methionine-methyl-14C as the methyl donor. These conformationally rigid analogs of benzylamine and Km values lower than, and Vmax values at least as high as, those of the physiologically occurring amines usually considered as the best substrates for the enzyme (tryptamine, N-methyltryptamine and serotonin). As LY134046 and SK&F 64139 have high affinity as competitive inhibitors of norepinephrine N-methyltransferase, some similarity in the active sites of these 2 enzymes is suggested.

This publication has 1 reference indexed in Scilit: