alpha 2 Adrenoreceptor affinity of some inhibitors of norepinephrine N-methyltransferase |
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Authors: | R E Toomey J S Horng S K Hemrick-Luecke R W Fuller |
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Institution: | Lilly Research Laboratories, Eli Lilly and Company Indianapolis, Indiana 46285, U.S.A. |
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Abstract: | Because certain inhibitors of norepinephrine N-methyltransferase (NMT, the epinephrine-forming enzyme) are α2 adrenoreceptor blockers, we compared the ability of various compounds to inhibit rat brain NMT activity and the binding of tritiated clonidine to rat brain membranes . There was no correlation between potency of NMT inhibition and potency of α2 receptor antagonism (as measured by inhibition of tritiated clonidine binding) among NMT inhibitors representing several chemical classes or among members of a single class of compounds, l-aminoindans. In addition, several potent α2 blocking drugs were essentially inactive as NMT inhibitors. These findings indicate that NMT inhibition and α2 blockade are dissociable activities. Future development of NMT inhibitors should include this dissociation as a goal to increase the usefulness of NMT inhibitors as pharmacologic tools. |
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