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Titolo:
TRANSLOCATION OF DOPAMINE AND BINDING OF WIN-35,428 MEASURED UNDER IDENTICAL CONDITIONS IN CELLS EXPRESSING THE CLONED HUMAN DOPAMINE TRANSPORTER
Autore:
REITH MEA; XU C; ZHANG LA; COFFEY LL;
Indirizzi:
UNIV ILLINOIS,COLL MED,DEPT BIOMED & THERAPEUT SCI,BOX 1649 PEORIA IL61656
Titolo Testata:
Naunyn-Schmiedeberg's archives of pharmacology
fascicolo: 3, volume: 354, anno: 1996,
pagine: 295 - 304
SICI:
0028-1298(1996)354:3<295:TODABO>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
BIOGENIC-AMINE TRANSPORTERS; UPTAKE COMPLEX; NEUROTRANSMITTER TRANSPORTERS; UPTAKE INHIBITORS; COCAINE BINDING; NEURONAL CARRIER; MAZINDOL BINDING; PLASMA-MEMBRANE; LIGAND-BINDING; MOUSE STRIATUM;
Keywords:
HUMAN DOPAMINE TRANSPORTER; WIN 35,428 BINDING; DOPAMINE UPTAKE; COCAINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
65
Recensione:
Indirizzi per estratti:
Citazione:
M.E.A. Reith et al., "TRANSLOCATION OF DOPAMINE AND BINDING OF WIN-35,428 MEASURED UNDER IDENTICAL CONDITIONS IN CELLS EXPRESSING THE CLONED HUMAN DOPAMINE TRANSPORTER", Naunyn-Schmiedeberg's archives of pharmacology, 354(3), 1996, pp. 295-304

Abstract

Translocation of [H-3]dopamine and binding of [H-3]WIN 35, 428 were measured in intact C6 glioma cells expressing the cloned human dopaminetransporter (hDAT) under identical conditions of assay buffer (phosphate-Krebs) and temperature (25 degrees C) with uptake at initial velocity and binding at equilibrium. In the intact cells, [H-3]dopamine uptake was a one-component process; in contrast, [H-3]WIN 35,428 binding included both a high-affinity component, inhibitable by micromolar concentrations of dopamine, and a low-affinity component only partially inhibited by millimolar concentrations of dopamine. Binding (high-affinity) over uptake K-i ratios were on the average 2.3 for the inhibitorsWIN 35,428, cocaine, CBR 12909, and BTCP. The potency of dopamine in inhibiting its own translocation was close to that in inhibiting [H-3]WIN 35, 428 binding consonant with a more rapid reorientation step of the DAT in the C6-hDAT system than in rat striatal synaptosomes. The similarity in turnover values of the DAT estimated in the current experiments with the C6-hDAT system and in our previous study on rat striatal synaptosomes, performed under comparable conditions, suggest that all DAT's inserted into the C6 cell membrane are functionally active.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 22:15:41