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Authordc.contributor.authorDajas-Bailador, Federico A. 
Authordc.contributor.authorAsencio, Marcelo es_CL
Authordc.contributor.authorBonilla, Carolina es_CL
Authordc.contributor.authorScorza, Ma. Cecilia es_CL
Authordc.contributor.authorEcheverry, Carolina es_CL
Authordc.contributor.authorReyes Parada, Miguel es_CL
Authordc.contributor.authorSilveira, Rodolfo es_CL
Authordc.contributor.authorProtais, Philippe es_CL
Authordc.contributor.authorRussell, Graeme es_CL
Authordc.contributor.authorCassels Niven, Bruce es_CL
Authordc.contributor.authorDajas, Federico es_CL
Admission datedc.date.accessioned2012-05-25T19:30:35Z
Available datedc.date.available2012-05-25T19:30:35Z
Publication datedc.date.issued1998-07-07
Cita de ítemdc.identifier.citationGeneral Pharmacology , Vol. 32, p. 373–379, 1999.es_CL
Identifierdc.identifier.issn. 0306-3623
Identifierdc.identifier.urihttps://repositorio.uchile.cl/handle/2250/119422
Abstractdc.description.abstractThe dopaminergic and antioxidant properties of pukateine [(R)-11-hydroxy-1,2-methylenedioxyaporphine, PUK], a natural aporphine derivative, were analyzed in the rat central nervous system. At dopamine (DA) D1 ([3H]-SCH 23390) and D2 ([3H]- raclopride) binding sites, PUK showed IC50 values in the submicromolar range (0.4 and 0.6 mM, respectively). When the uptake of tritiated dopamine was assayed by using a synaptosomal preparation, PUK showed an IC50 5 46 mM. In 6-hydroxydopamine unilaterally denervated rats, PUK (8 mg/kg but not 4 mg/kg) elicited a significant contralateral circling, a behavior classically associated with a dopaminergic agonist action. When perfused through a microdialysis probe inserted into the striatum, PUK (340 mM) induced a significant increase in dopamine levels. In vitro experiments with a crude rat brain mitochondrial suspension showed that PUK did not affect monoamine oxidase activities, at concentrations as high as 100 mM. PUK potently (IC50 5 15 mM) and dose-dependently inhibited the basal lipid peroxidation of a rat brain membrane preparation. As a whole, PUK showed a unique profile of action, comprising an increase in extracellular DA, an agonist-like interaction with DA receptors, and antioxidant activity. Thus, PUK may be taken as a lead compound for the development of novel therapeutic strategies for Parkinson disease.es_CL
Patrocinadordc.description.sponsorshipThis work was supported by an IDB-CONICYT Program (Grant No. FINTEC 013/F), Celsius S.A. and Dispert S.A. in Uruguay, by an ECOS (France)-CONICYT (Chile) exchange program, and by the Presidential Chair in Science (Chile).es_CL
Lenguagedc.language.isoenes_CL
Publisherdc.publisherElsevier Science Inc.es_CL
Keywordsdc.subjectPukateinees_CL
Títulodc.titleDopaminergic pharmacology and antioxidant properties of pukateine, a natural product lead for the design of agents increasing dopamine neurotransmissiones_CL
Document typedc.typeArtículo de revistaes_CL


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