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Effects of Deuterium Substitution on the Catabolism of β‐Phenylethylamine: An In Vivo Study
Author(s) -
Dyck L. E.,
Burden D. A.,
Boulton A. A.
Publication year - 1986
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1986.tb12982.x
Subject(s) - chemistry , in vivo , pargyline , catabolism , deuterium , monoamine oxidase , hydrochloride , endocrinology , biochemistry , metabolism , enzyme , biology , physics , microbiology and biotechnology , quantum mechanics
β‐Phenylethylamine (PE) hydrochloride injected intraperitoneally into rats was distributed evenly throughout the various regions of rat brain. Similarly, when a mixture of PE and α, α, β, β‐deuterated PE ([ 2 H 4 ]PE) was injected, no regional differences were observed in the ratios of the amounts of [ 2 H 4 ]PE and PE present; however, significantly more [ 2 H 4 ]PE than PE was present, although a 1:1 mixture had been administered. Further experiments in which the amounts of [ 2 H 4 ]PE and PE in whole rat brain, liver, and plasma were quantified confirmed this finding. The maximum [ 2 H 4 ]PE‐to‐PE ratios observed were 67 in whole brain 1 h after injection and 8 in liver and in plasma 45 min after injection. The whole brain [ 2 H 4 ]PE‐to‐PE ratios were decreased by pargyline pretreatment. Subsequent experiments showed that more α, α‐[ 2 H 4 ]PE than PE was present in whole brain, liver, and plasma of rats injected with an equimolar mixture of α, α‐[ 2 H 4 ]PE and PE. In contrast, β, β‐[ 2 H 4 ]PE was not enriched in comparison to PE under the same experimental conditions. We concluded that the basis for the enrichment of [ 2 H 4 ]PE and α, α‐[ 2 H 4 ]PE compared to PE was due to protection of the deuterated analogs from the actions of monoamine oxidase and perhaps aldehyde dehydrogenase; this protection led to pronounced deuterium substitution effects in vivo especially in the brain.