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- W2065074021 abstract "The metabolic fate in vivo of the antihypertensive agent α-methyldopa (α-MD) has been examined in rat brain tissues with the aid of 13C- and 2H-labeled compounds and chemical ionization mass spectrometry. After intraperitoneal administration of (S)-α-MD, endogenous catecholamines in the caudate nucleus and hypothalamus were replaced by the corresponding α-methylated compounds. In contrast to these results, brain catecholamines were unaffected when (R)-α-MD was given. Transport of the amino acids into the brain was found to be highly stereoselective for the (S)-enantiomer. After direct administration of (S)- or (R)-α-MD into rat brain (third ventricle), evidence of metabolism was obtained only for the pharmacologically active (S)-enantiomer. These results are consistent with the hypothesis that the centrally mediated antihypertensive properties of (S)-α-MD are dependent on its metabolic conversion in the brain to α-methyldopamine and/or α-methylnorepinephrine." @default.
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- W2065074021 date "1977-10-01" @default.
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- W2065074021 title "Stereochemical course in vivo of alpha-methyldopa decarboxylation in rat brains" @default.
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- W2065074021 doi "https://doi.org/10.1016/0006-2952(77)90342-2" @default.
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