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Titolo:
Blood-brain barrier transport studies of organic guanidino cations using an in situ brain perfusion technique
Autore:
Doan, KMM; Lakhman, SS; Boje, KMK;
Indirizzi:
SUNY Buffalo, Sch Pharm, Dept Pharmaceut, Buffalo, NY 14260 USA SUNY Buffalo Buffalo NY USA 14260 Dept Pharmaceut, Buffalo, NY 14260 USA
Titolo Testata:
BRAIN RESEARCH
fascicolo: 1-2, volume: 876, anno: 2000,
pagine: 141 - 147
SICI:
0006-8993(20000908)876:1-2<141:BBTSOO>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
AMINO-ACID TRANSPORTER; OXIDE SYNTHASE INHIBITORS; BRUSH-BORDER MEMBRANES; P-GLYCOPROTEIN; TISSUE DISTRIBUTION; MOUSE BLASTOCYSTS; ANIMAL-CELLS; SYSTEM; RAT; EXPRESSION;
Keywords:
aminoguanidine; blood-brain barrier; cationic amino acids; in situ brain perfusion; organic cation; transport;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
44
Recensione:
Indirizzi per estratti:
Indirizzo: Boje, KMK SUNY Buffalo, Sch Pharm, Dept Pharmaceut, H517 Cooke Hochstetter, Buffalo,NY 14260 USA SUNY Buffalo H517 Cooke Hochstetter Buffalo NY USA 14260 260 USA
Citazione:
K.M.M. Doan et al., "Blood-brain barrier transport studies of organic guanidino cations using an in situ brain perfusion technique", BRAIN RES, 876(1-2), 2000, pp. 141-147

Abstract

Blood-brain barrier (BBB) transport of essential polar substrates is mediated by specific, carrier-mediated transport proteins. The BBB transport mechanisms for polar compounds with terminal guanidino functional groups (R-NHC(NH)NH2) are not well defined. The goal of the present work was to investigate the BBB transport mechanism(s) for terminal guanidino substrates usingan in situ brain perfusion technique. Brain region radiotracer influx clearance (Cii,) was calculated for representative guanidino substrates, [C-14]L-arginine, [C-14]aminoguanidine and [C-14]guanidine, in the presence or absence of excess terminal guanidino analogues. The Cl-in for [C-14]L-arginine (0.21+/-0.0094 cm(3)/min/g wet brain weight, mean+/-S.E.M., n=four rats) was significantly decreased by 1000X concentrations of unlabeled L-arginine, N-G-methyl-L-arginine, N-G-,N-G-dimethyl-L-arginine and N-G-amino-L-arginine by similar to 83% (P<0.01; n=4-5), whereas 1000x concentrations of niuo-L-arginine, aminoguanidine and guanidine were without effect. In contrast,the respective Cl-in of [C-14]aminoguanidine and [C-14]guanidine (0.0085+/-0.00039 and 0.015+/-0.0015 cm(3)/min/g, n=4, respectively) were not significantly decreased by 1000X concentrations of unlabeled aminoguanidine or guanidine. The Cl-in values for all [C-14]guanidino probes were significantlygreater (P<0.05) from that of [H-3]inulin, a marker of cerebrovascular blood volume. These data suggest that the hydrophilic guanidino cations aminoguanidine and guanidine penetrate the BBB by a minor diffusional process with no appreciable transport via saturable processes. In contrast, BBB penetration of L-arginine occurs via the saturable basic amino acid transporter that has specificity for amino acid analogues possessing cationic terminal guanidino groups. (C) 2000 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/10/20 alle ore 02:08:51