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Titolo:
TRANSPORT OF GABAPENTIN, A GAMMA-AMINO ACID DRUG, BY SYSTEM L-ALPHA-AMINO-ACID TRANSPORTERS - A COMPARATIVE-STUDY IN ASTROCYTES, SYNAPTOSOMES, AND CHO CELLS
Autore:
SU TZ; LUNNEY E; CAMPBELL G; OXENDER DL;
Indirizzi:
WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT BIOTECHNOL ANN ARBOR MI 00000 WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT BIOTECHNOL ANN ARBOR MI 00000 WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT CHEM ANN ARBOR MI 48105 WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT NEUROSCI PHARMACOL ANN ARBOR MI 00000
Titolo Testata:
Journal of neurochemistry
fascicolo: 5, volume: 64, anno: 1995,
pagine: 2125 - 2131
SICI:
0022-3042(1995)64:5<2125:TOGAGA>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
NA+-INDEPENDENT TRANSPORT; MOUSE BLASTOCYSTS; PLASMA-MEMBRANE; BRUSH-BORDER; RAT-BRAIN; METABOLISM; VESICLES; FLUXES;
Keywords:
GABAPENTIN; BIOLOGICAL TRANSPORT; SYSTEM L; ASTROCYTES; SYNAPTOSOMES; CHINESE HAMSTER OVARY CELLS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
T.Z. Su et al., "TRANSPORT OF GABAPENTIN, A GAMMA-AMINO ACID DRUG, BY SYSTEM L-ALPHA-AMINO-ACID TRANSPORTERS - A COMPARATIVE-STUDY IN ASTROCYTES, SYNAPTOSOMES, AND CHO CELLS", Journal of neurochemistry, 64(5), 1995, pp. 2125-2131

Abstract

The system L transporter is generally considered to be one of the major Na+-independent carriers for large neutral alpha-amino acids in mammalian cells. However, we found that cultured astrocytes from rat brain cortex accumulate gabapentin, a gamma-amino acid, predominately by this alpha-amino acid transport system. Uptake of gabapentin by system L transporter was also examined in synaptosomes and Chinese hamster ovary (CHO) cells. The inhibition pattern displayed by various amino acids on gabapentin uptake in astrocytes and synaptosomes corresponds closely to that observed for the system L transport activity in CHO cells. Gabapentin and leucine have K-m values that equal their K-i values for inhibition of each other, suggesting that leucine and gabapentin compete for the same system L transporter. By contrast, gabapentin exhibited no effect on uptake of GABA, glutamate, and arginine, indicating that these latter three types of brain transporters do not serve for uptake of gabapentin. A comparison of computer modeling analysis of gabapentin and L-leucine structures shows that although the former is a gamma-amino acid, it can assume a conformation that can resemble the L-form of a large neutral alpha-amino acid such as L-leucine. The steady-state kinetic study in astrocytes and CHO cells indicates that the intracellu[ar concentrations of gabapentin are about two to four times higher than that of leucine. The uptake levels of these two substrates are inversely related to their relative exodus rates. The concentrating ability by system L observed in astrocytes is consistent with the substantially high accumulation gradient of gabapentin in the brain tissue as determined by microdialysis.

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Documento generato il 28/01/21 alle ore 06:55:07