OXIDATION OF PHENETHYLAMINE DERIVATIVES BY AMINE OXIDASE

¹ Wellcome Research Laboratories, Tuckahoe, New York

1. The comparative rates of oxidation by amine oxidase in cat and guinea pig liver Brei of a series of primary, secondary and tertiary phenethylamines, unsubstituted or substituted inthe 2,3 and 4 positions with hydroxy and methoxy groups have been studied.

2. Tertiary amines were less rapidly oxidized than primary and secondary amines and quaternary salts were not oxidized. Secondary amines were usually oxidized at the same or greater rates than the primary amines.

3. 2-Hydroxyphenethylamines were oxidized less rapidly than the 3- and 4-position isomers.

4. 2-Methoxyphenethylamines were oxidized more rapidly than the 3- and 4-isomers. 2,3-Dimethoxyphenethylamines had the most rapid rates of the dimethoxy derivatives.

5. The -hydroxy group reduced the ease of oxidation.

6. The relationship of ease of oxidation by amine oxidase and pharmacological activity of the compounds was discussed.