PT  - JOURNAL ARTICLE
AU  - Bartholini, G.
AU  - Pletscher, A.
TI  - CEREBRAL ACCUMULATION AND METABOLISM OF C<sup>14</sup>-DOPA AFTER SELECTIVE INHIBITION OF PERIPHERAL DECARBOXYLASE
DP  - 1968 May 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 14--20
VI  - 161
IP  - 1
4099  - http://jpet.aspetjournals.org/content/161/1/14.short
4100  - http://jpet.aspetjournals.org/content/161/1/14.full
SO  - J Pharmacol Exp Ther1968 May 01; 161
AB  - The action of the dopa decarboxylase inhibitor Ro 4-4602 (N1-(DL-seryl)-N2-(2,3,4-trihydroxybenzyl) hydrazine) (50 mg/kg i.p.) on the metabolism of i.p. or p.o. administered C14-L-3,4-dihydroxyphenylalanine (dopa) has been investigated in brain, blood plasma and heart of rats. Thereby, the C14-amino acids (dopa and 3-O-methyldopa), the C14-catecholamines (dopamine and norepinephrine), as well as the C14-phenylcarboxylic acids (homovanillic and 3,4-dihydroxyphenylacetic acid), were determined. In the plasma and heart, Ro 4-4602 antagonizes the rise of C14-catecholamines and C14-phenylcarboxylic acids, but increases that of C14-amino acids. In the brain, the inhibitor enhances the C14-catecholamines (mainly C14-dopamine) as well as the C14-amino acids (mainly C14-dopa). The rise of C14-phenylcarboxylic acids is increased by Ro 4-4602 in the experiments with 16 mg/kg of C14-dopa but antagonized in those with 150 mg/kg of C14-dopa i.p. It is concluded that Ro 4-4602 inhibits the decarboxylation of C14-dopa in extracerebral tissues rather selectively. This probably leads to an increased penetration of C14-dopa from the blood into the brain, where it is then metabolized to C14-catecholamines. © 1968 by The Williams & Wilkins Company