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Titolo:
Uptake and efflux of the peptidic delta-opioid receptor agonist [D-penicillamine(2,5)]-enkephalin at the murine blood-brain barrier by in situ perfusion
Autore:
Dagenais, C; Ducharme, J; Pollack, GM;
Indirizzi:
Univ N Carolina, Sch Pharm, Div Drug Delivery & Disposit, Chapel Hill, NC 27599 USA Univ N Carolina Chapel Hill NC USA 27599 posit, Chapel Hill, NC 27599 USA AstraZeneca R&D Montreal, Ville St Laurent, PQ H4S 1Z9, Canada AstraZenecaR&D Montreal Ville St Laurent PQ Canada H4S 1Z9 S 1Z9, Canada Univ Montreal, Fac Pharm, Montreal, PQ H3C 3J7, Canada Univ Montreal Montreal PQ Canada H3C 3J7 rm, Montreal, PQ H3C 3J7, Canada Univ Montreal, Dept Anesthesiol, Montreal, PQ H3C 3J7, Canada Univ Montreal Montreal PQ Canada H3C 3J7 ol, Montreal, PQ H3C 3J7, Canada
Titolo Testata:
NEUROSCIENCE LETTERS
fascicolo: 3, volume: 301, anno: 2001,
pagine: 155 - 158
SICI:
0304-3940(20010406)301:3<155:UAEOTP>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRANSPORTING POLYPEPTIDE-2 OATP2; CENTRAL-NERVOUS-SYSTEM; P-GLYCOPROTEIN; ORGANIC ANION; D-PENICILLAMINE(2,5) ENKEPHALIN; CELLULAR UPTAKE; RAT-BRAIN; MODEL; MICE; ANTINOCICEPTION;
Keywords:
delta opioid-receptor agonist; blood-brain barrier; uptake; efflux; inhibitors; P-glycoprotein; organic anion-transporting polypeptide;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
20
Recensione:
Indirizzi per estratti:
Indirizzo: Pollack, GM Univ N Carolina, Sch Pharm, Div Drug Delivery & Disposit, Beard Hall CB 7360, Chapel Hill, NC 27599 USA Univ N Carolina Beard Hall CB 7360 Chapel Hill NC USA 27599 SA
Citazione:
C. Dagenais et al., "Uptake and efflux of the peptidic delta-opioid receptor agonist [D-penicillamine(2,5)]-enkephalin at the murine blood-brain barrier by in situ perfusion", NEUROSCI L, 301(3), 2001, pp. 155-158

Abstract

P-glycoprotein IP-gp) and organic anion transporting polypeptides (Oatp) are expressed at the blood-brain barrier (BBB), There is little functional evidence for Oatp-mediated transport at the BBB. The peptidic delta opioid-receptor agonist [D-penicillamine(2,5)]-enkephalin (DPDPE) is a substrate ofmdr1aP-gp and Oatp2. The present study evaluated the influence of these transporters on brain uptake of DPDPE by in situ perfusion in mice. Brain uptake was increased similar to 12-fold in mice lacking P-gp in the BBB, but the P-gp inhibitor dexverapamil did not increase uptake in P-gp-competent mice. In P-gp-deficient mice, DPDPE uptake was saturable (K-m similar to 24 mM), and was inhibited by dexverapamil and the Oatp2 substrates digoxin, estradiol-17 beta -glucuronide and fexofenadine. These results confirm P-gp-mediated efflux of DPDPE, and suggest functional uptake transport of DPDPE byOatp, at the murine BBB. (C) 2001 Elsevier Science Ireland Ltd. All rightsreserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 22:38:12