PMID: 2888854Aug 1, 1987Paper

L-dopa esters as potential prodrugs: behavioural activity in experimental models of Parkinson's disease

The Journal of Pharmacy and Pharmacology
D R CooperC D Marsden

Abstract

Intraperitoneal administration of the 2-tetrahydropyranylmethyl, phenoxyethyl, ethyl, 2-hydroxypropyl and methyl ester prodrugs of L-dopa produced locomotor activity in reserpine-pretreated mice with equal intensity and duration to that observed following administration of L-dopa itself. Administration of the 2-(1-methoxy)propyl ester produced a more prolonged effect while the p-methoxyphenylethyl, n-propyl, phenylethyl, m-trifluoromethylbenzyl, cyclohexyl, p-chlorophenylethyl and benzyl ester prodrugs were less active than L-dopa itself. On oral administration, the ethyl and methyl ester prodrugs were more effective than L-dopa in reversing reserpine-induced akinesia in mice. The 2-tetrahydropyranylmethyl, 2-(1-methoxy)propyl, 2-hydroxypropyl, n-propyl, benzyl and phenoxyethyl ester prodrugs produced effects comparable with those of L-dopa. In contrast, the cyclohexyl, m-trifluoromethylbenzyl, phenylethyl, p-chlorophenylethyl and p-methoxyphenylethyl ester prodrugs were less effective than L-dopa on oral administration. Intraperitoneal administration of L-dopa and the ester prodrugs of L-dopa to rats with a prior 6-hydroxydopamine (6-OHDA) lesion of the medial forebrain bundle (MFB) produced contraversive circling responses. R...Continue Reading

References

Nov 1, 1977·Journal of Medicinal Chemistry·N BodorK Sasahara
Aug 1, 1987·The Journal of Pharmacy and Pharmacology·D R CooperC D Marsden
Mar 1, 1973·Journal of Pharmaceutical Sciences·C M Lai, W D Mason
Apr 1, 1974·Journal of Medicinal Chemistry·A M FelixH Sheppard
Jun 1, 1984·Brain : a Journal of Neurology·R J HardieG M Stern

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Citations

Jan 1, 1992·Movement Disorders : Official Journal of the Movement Disorder Society·F StocchiA Agnoli
Apr 4, 2007·Pharmaceutical Research·Nunzio DenoraGaetano Liso
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Apr 23, 2009·Expert Opinion on Drug Delivery·Antonio Di StefanoLaura Serafina Cerasa
Apr 13, 2012·Expert Opinion on Drug Discovery·Piera SozioAntonio Di Stefano
Jan 29, 2008·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Sanneke A M van VlietIngrid H C H M Philippens
Feb 9, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Antonio Di StefanoLaura Serafina Cerasa
Jan 4, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Fatma HaddadRafik Karaman
Oct 1, 1987·The Journal of Pharmacy and Pharmacology·D R CooperC D Marsden
Aug 1, 1987·The Journal of Pharmacy and Pharmacology·D R CooperC D Marsden

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