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Titolo:
[H-3] GABAPENTIN MAY LABEL A SYSTEM-L-LIKE NEUTRAL AMINO-ACID CARRIERIN BRAIN
Autore:
THURLOW RJ; BROWN JP; GEE NS; HILL DR; WOODRUFF GN;
Indirizzi:
PARKE DAVIS & CO,NEUROSCI RES CTR,ADDENBROOKES HOSP SITE,HILLS RD CAMBRIDGE CB2 2QB ENGLAND PARKE DAVIS & CO,NEUROSCI RES CTR,ADDENBROOKES HOSP SITE,HILLS RD CAMBRIDGE CB2 2QB ENGLAND
Titolo Testata:
European journal of pharmacology. Molecular pharmacology section
fascicolo: 3, volume: 247, anno: 1993,
pagine: 341 - 345
SICI:
0922-4106(1993)247:3<341:[GMLAS>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRANSPORT; ASTROCYTES; GABAPENTIN;
Keywords:
GABAPENTIN; ANTICONVULSANT; L-AMINO ACIDS; SYSTEM-L; TRANSPORTER; BRAIN;
Tipo documento:
Note
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
R.J. Thurlow et al., "[H-3] GABAPENTIN MAY LABEL A SYSTEM-L-LIKE NEUTRAL AMINO-ACID CARRIERIN BRAIN", European journal of pharmacology. Molecular pharmacology section, 247(3), 1993, pp. 341-345

Abstract

The ability of large neutral amino acids to interact with a site in mouse and pig brain labelled by [H-3]gabapentin was examined. As previously described for rat tissue, [H-3]gabapentin bound to synaptic plasma membranes prepared from mouse or pig cerebral cortex with high affinity (Kinetically derived K(D) = 14 and 17 nM for mouse and pig, respectively). Equilibrium binding in each species was inhibited by gabapentin and a range of large neutral amino acids. L-leucine (IC50 = 80 nM),L-isoleucine (IC50 = 72 nM), L-norleucine (IC50 = 40 nM) and L-methionine (IC50 = 50 nM) were the most potent of those tested. Binding was also inhibited by L-phenylalanine (IC50 = 380 nM), L-valine (IC50 = 310 nM) and the selective system-L substrate 2-amino-2-carboxy-bicycloheptane (IC50 = 420 nM) but not by the sodium-dependent System-A substrate methylaminoisobutyric acid. The presence of a submaximal concentration of leucine reduced [H-3]gabapentin binding affinity but did not affect the maximum number of binding sites, suggesting a competitive interaction between leucine and the binding protein. The results suggest [H-3]gabapentin may label a site in brain that resembles the large neutral amino acid transporter described in other tissues.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/01/21 alle ore 06:24:55