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In contrast, the hydroxy- and N-methyltransferase activities of rat brain are strongly dependent on Mg2+, and the overall activity is greater than that of the mouse brain homogenates. Hydroxy-methylation is the predominant reaction, but N-methylation can also occur. No N-methyltransferase activity was detected in the rat heart. A specific inhibitor of N-methyltransferase, kojic acid, has been shown to be a very potent inhibitor of the rat brain enzyme (Ki = 3 X 10(-7) M) but has no inhibitory effect on the mouse brain enzyme (Ki greater than or equal to 10(-4) M). 3-Hydroxy-N-methylphenethylamine (3-HMPEA), the metabolic precursor of PEA, was also a potent inhibitor of rat brain and liver N-methyltransferase. 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