1,720,993 research outputs found
Design and synthesis of multifunctional drugs: a strategy to improve the treatment of Parkinson’s disease
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Novel O-palmitoylscleroglucan-coated liposomes as drug carriers: Development, characterization and interation with leuprolide
No full textIn vivo anti-apoptotic effect of compound 4 in rats infused with Aβ (1-40), as a model of Alzheimer’s disease
No full textMaleic- and Fumaric-diamides of (O,O-diacetyl)-L-Dopa-methylester as anti-Parkinson prodrugs in liposomal formulation
No full textThe maleic and fumaric diamides preparation of (O,O-diacetyl)-L-Dopa-methylester [(+)-4, (+)-5] are reported; they were synthesized in order to attenuate marked fluctuations of L-DOPA (LD) plasma levels and to overcome the problem of low bioavailability of LD. The new compounds were characterized evaluating solubility, chemical stability, apparent partition coefficient (log P) and comparing neostriatum dopamine (DA) levels in freely moving rats after i.p. administration of prodrugs [(+)-4, (+)-5 ] with prodrugs in liposomal formulations [(+)-4,(+)-5 Lip]. All the new compounds showed chemical stability in aqueous buffer solutions (pH 1.3 and 7.4). A relatively slow release of LD in human plasma was observed. Among the studied products, prodrug was able to induce sustained delivery of DA in rat striatal dialysate with respect to equimolar i.p admistration of LD. Furthermore, neostriatum DA concentration after administration of the synthesized prodrugs vs. prodrugs in liposomal formulations was compared (+)-4Lip. (+)-5 Lip). The results suggest that cis dimeric prodrug (+)-4 and (+)-4 Lip can improve the release of DA in rat brain and demonstrate the potential of these formulations for controlled delivery of antiparkinson agents
Effect of choline-containing phospholipids on brain cholinergic transporters in the rat.
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Sintesi di trans-2-ammino-1-fenil-5-fluoro-6-idrossi (e 6-fluoro-5-idrossi)-2,3-diidro-1H-indeni quali potenziali ligandi per i recettori dopaminergici
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