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Titolo:
SLOW DELIVERY OF THE SELECTIVE CHOLECYSTOKININ AGONIST PBC-264 INTO THE RAT NUCLEUS-ACCUMBENS USING MICROSPHERES
Autore:
BLANCOPRIETO MJ; DURIEUX C; DAUGE V; FATTAL E; COUVREUR P; ROQUES BP;
Indirizzi:
UNIV PARIS 05,DEPT PHARMACOCHIM MOL & STRUCT,U266 INSERM,URA D 1500 CNRS F-75270 PARIS 06 FRANCE UNIV PARIS 05,DEPT PHARMACOCHIM MOL & STRUCT,U266 INSERM,URA D 1500 CNRS F-75270 PARIS 06 FRANCE UNIV PARIS 11,FAC PHARM,URA CNRS 1218,LAB PHYSICOCHIM PHARMACOTECH BIOPHARM F-92290 CHATENAY MALABRY FRANCE
Titolo Testata:
Journal of neurochemistry
fascicolo: 6, volume: 67, anno: 1996,
pagine: 2417 - 2424
SICI:
0022-3042(1996)67:6<2417:SDOTSC>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
CCK-B AGONIST; CONTROLLED RELEASE; CENTRAL RECEPTORS; TISSUE REACTION; DRUG DELIVERY; BRAIN-TUMORS; DOPAMINE; ANTAGONIST; POLYMERS; MEMORY;
Keywords:
POLY(LACTIDE-CO-GLYCOLIDE) MICROSPHERES; STEREOTAXIC IMPLANTATION; RAT BRAIN DELIVERY; SELECTIVE CHOLECYSTOKININ; B AGONIST; PBC 264; OPEN-FIELD TEST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
41
Recensione:
Indirizzi per estratti:
Citazione:
M.J. Blancoprieto et al., "SLOW DELIVERY OF THE SELECTIVE CHOLECYSTOKININ AGONIST PBC-264 INTO THE RAT NUCLEUS-ACCUMBENS USING MICROSPHERES", Journal of neurochemistry, 67(6), 1996, pp. 2417-2424

Abstract

Neuropeptides have been shown to play a critical role in adaptationalprocesses, probably by long-term modulation of neuronal pathways. It could therefore be interesting to study behavioral changes induced by chronic local stimulation of neuropeptide receptors. With this aim poly(lactide-co-glycolide) microspheres loaded with a highly potent, peptidase-resistant, cholecystokinin (CCK)-B-selective CCK peptidomimetic agonist (pBC 264) were prepared by a water in oil in water emulsion solvent evaporation method and stereotaxically implanted into the anterior part of the rat nucleus accumbens. Two different kinds of loaded polymeric microspheres differing only by the stabilizing agent [ovalbumin (OVA) or Pluronic F 68] added to the inner emulsion were used. The histological and behavioral studies done 24 h and 8 days after implantation of nonloaded microspheres in the nucleus accumbens indicated thatthe microspheres were well tolerated. The in vivo release of the selective CCK-B agonist pBC 264 (associated with a tracer dose of [H-3] pBC 264) from microspheres prepared with OVA was very fast (92% after 6 h), whereas only 26% (88 pmol) of pBC 264 was released from the formulation with Pluronic F 68 after 24 h. Eight days after implantation 36%of pBC 264 had diffused from the microspheres, and 8% (similar to 30 pmol) was still present in the brain concentrated around the site of administration. In all cases the released material was found to correspond to intact pBC 264, thus demonstrating the possibility of obtaininga slow controlled release of peptide in vivo. This method opens up interesting perspectives to study the long-term effects of neuropeptides.

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Documento generato il 15/07/20 alle ore 08:24:22