Access the full text.
Sign up today, get DeepDyve free for 14 days.
Loading next page...
/lp/wiley/selective-rise-in-brain-dopamine-by-inhibition-of-extracerebral-tEiCEMNz6f
References (22)
-
G. Bartholini, A. Pletscher (1969)
Effect of various decarboxylase inhibitors on the cerebral metabolism of dihydroxyphenylalanineJournal of Pharmacy and Pharmacology, 21
-
Renin, dopamine and Parkinson's disease -
G. Bartholini, A. Pletscher (1968)
Cerebral accumulation and metabolism of C14-dopa after selective inhibition of peripheral decarboxylase.The Journal of pharmacology and experimental therapeutics, 161 1
-
S. Udenfriend, P. Zaltzman-Nirenberg, R. Gordon, S. Spector (1966)
Evaluation of the biochemical effects produced in vivo by inhibitors of the three enzymes involved in norepinephrine biosynthesis.Molecular pharmacology, 2 2
-
(1967)
Die Bedeutung des Monoamin . - Metabolismus fUr die Pathologie des extra - pyramidalen Systems , Ars . Medici -
G. Bartholini, M. Prada, A. Pletscher (1968)
Decrease of cerebral 5‐hydroxytryptamine by 3,4‐dihydroxyphenylalanine after inhibition of extracerebral decarboxylaseJournal of Pharmacy and Pharmacology, 20
-
C. Owman, E. Rosengren (1967)
DOPAMINE FORMATION IN BRAIN CAPILLARIES—AN ENZYMIC BLOOD–BRAIN BARRIER MECHANISMJournal of Neurochemistry, 14
-
Å. Bertler, B. Falck, E. Rosengren (2009)
THE DIRECT DEMONSTRATION OF A BARRIER MECHANISM IN THE BRAIN CAPILLARIES.Acta pharmacologica et toxicologica, 20
-
(1969)
ExperimenteIIe Ergebnisse liber die Kombinationsbehandlung des Parkinson-Syndroms mit L-DOPA und einem Decarboxylasehemmer -
(1967)
Die Bedeutung des Monoamin. -Metabolismus fUr die Pathologie des extrapyramidalen Systems -
(1969)
ExperimenteIIe Ergebnisse liber die Kombinationsbehandlung des Parkinson-Syndroms mit L-DOPA und einem Decarboxylasehemmer (Ro 4-4602) -
(1968)
Cerebral accumulation and metabolism of HC-dopa 352 Pletscher and Bartholini after selective inhibition of peripheral decarboxylase -
(1969)
Therapeutique du syndrome de Parkinson par la L-Dopa "per os" associee a un inhibiteur de la decarbosylase -
(1969)
ExperimenteIIe Ergebnisse liber die Kombinationsbehandlung des Parkinson - Syndroms mit L - DOPA und einem Decar - boxylasehemmer ( Ro 4 - 4602 ) , Wien -
R. Tissot, G. Bartholini, A. Pletscher (1969)
Drug-induced changes of extracerebral dopa metabolism in man.Archives of neurology, 20 2
-
(1967)
Die Bedeutung des Monoamin. -Metabolismus fUr die Pathologie des extrapyramidalen Systems, Ars -
A. Pletscher, K. Gey, W. Burkard (1966)
Inhibitors of monoamine oxidase and decarboxylase of aromatic amino acids -
C. Chouza, C. Marin, Sara Romero, J. Gomensoro (1970)
[Treatment of parkinsonism with L-dopa].Acta neurologica latinoamericana, 16 1
-
B. Hamberger (1967)
Reserpine-resistant uptake of catecholamines in isolated tissues of the rat. A histochemical study.Acta physiologica Scandinavica. Supplementum, 295
-
Å. Bertler, B. Falck, C. Owman, E. Rosengrenn (1966)
The localization of monoaminergic blood-brain barrier mechanisms.Pharmacological reviews, 18 1
-
(1969)
Thera - peutique du syndrome de Parkinson par la L - Dopa " per os " associee a un inhibiteur de la decarbosylase ( Ro IV 46 . 02 ) -
G. Bartholini, W. Burkard, A. Pletscher, H. Bates (1967)
Increase of Cerebral Catecholamines caused by 3,4-Dihydroxyphenylalanine after Inhibition of Peripheral DecarboxylaseNature, 215
- Publisher
- Wiley
- Copyright
- © American Society for Clinical Pharmacology and Therapeutic
- ISSN
- 0009-9236
- eISSN
- 1532-6535
- DOI
- 10.1002/cpt1971122part2344
- Publisher site
- See Article on Publisher Site
Abstract
The action of Ro 4‐4602 on decarboxylase of aromatic amino acids (DC) was studied in homogenates of both brain and heart to which the drug had been added and in intact rats after parenteral administration of the compound. Furthermore, investigations on the effect of Ro 4‐4602 on the metabolism of levodopa were carried out in extracerebral tissues as well as in brain of intact rats. In vivo, Ro 4‐4602 preferentially inhibits DC of extracerebral tissues including the brain capillaries. The inhibitor markedly enhances the accumulation of levodopa in the blood. As a consequence, increased amounts of levodopa penetrate through the brain capillaries into the cerebral parenchyma where decarboxylation to dopamine occurs. The newly formed amine is preferentially localized in the extrapyramidal brain centers. Concomitantly, the endogenous 5‐hydroxytryptamine (5‐HT) of the brain decreases. Potential advantages of the combination inhibitor plus levodopa over levodopa alone are: enhanced intestinal absorption of levodopa, decrease of the required levodopa dose, decrease of the peripheral side effects of levodopa, and enhanced selectivity of action of levodopa in the central nervous system.
Journal
Clinical Pharmacology & Therapeutics – Wiley
Published: Mar 1, 1971