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Fuller RW, Mills J, Marsh MM. 
“Inhibition of phenethanolamine N-methyl transferase by ring-substituted alpha-methylphenethylamines (amphetamines)”. 
J Med Chem. 1971 Apr 07;14(4):322-5.
Phenethanolamine N-methyl transferase (PNMT) transfers a Me group from S-adenosylmethionine to phenethylamines with an OH group β to the N. Phenethylamines (including a-methylphenethylamines) without such a β substitution combine with and inhibit the enzyme. Amphetamines with various aromatic substituents were studied as inhibitors: there was greater than a 1000-fold range in their inhihitor potency. The inhibitor activity of these compourids showed a correlation with the Hammett u arid T (a lipophilic parameter derived from the partition coefficient) associated with the aromatic substituent. The d isomers were more active as inhibitors than 2 isomers of amphetamines. d-3,4-Dichloroamphetamine was the most active inhibitor in the series and is the most potent inhibitor of PNMT reported to date; its inhibition was reversible and competitive. Inhibitors of PNMT that are effective in vivo should be of pharmacological importance.
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