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Titolo:
BINDING DOMAINS FOR BLOCKERS AND SUBSTRATES ON THE CLONED HUMAN DOPAMINE TRANSPORTER STUDIED BY PROTECTION AGAINST N-ETHYLMALEIMIDE-INDUCEDREDUCTION OF A-CARBOMETHOXY-3-BETA-(4-FLUOROPHENYL)[H-3]TROPANE ([H-3]WIN-35,428) BINDING
Autore:
REITH MEA; XU C; COFFEY LL;
Indirizzi:
UNIV ILLINOIS,COLL MED,DEPT BIOMED & THERAPEUT SCI,BOX 1649 PEORIA IL61656 ILLINOIS STATE UNIV,DEPT BIOL NORMAL IL 61790
Titolo Testata:
Biochemical pharmacology
fascicolo: 9, volume: 52, anno: 1996,
pagine: 1435 - 1446
SICI:
0006-2952(1996)52:9<1435:BDFBAS>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
BIOGENIC-AMINE TRANSPORTERS; H-3 WIN 35,428; RAT CAUDATE-NUCLEUS; COCAINE BINDING; NEURONAL CARRIER; MOUSE STRIATUM; UPTAKE SITES; NEUROTRANSMITTER TRANSPORTERS; )H-3>GBR-12935 BINDING; UPTAKE INHIBITORS;
Keywords:
WIN 35,428 BINDING; DOPAMINE BINDING; COCAINE BINDING; PROTEIN MODIFICATION; N-ETHYLMALEIMIDE; HUMAN DOPAMINE TRANSPORTER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
67
Recensione:
Indirizzi per estratti:
Citazione:
M.E.A. Reith et al., "BINDING DOMAINS FOR BLOCKERS AND SUBSTRATES ON THE CLONED HUMAN DOPAMINE TRANSPORTER STUDIED BY PROTECTION AGAINST N-ETHYLMALEIMIDE-INDUCEDREDUCTION OF A-CARBOMETHOXY-3-BETA-(4-FLUOROPHENYL)[H-3]TROPANE ([H-3]WIN-35,428) BINDING", Biochemical pharmacology, 52(9), 1996, pp. 1435-1446

Abstract

Binding sites for 2 beta-carbomethoxy-3 beta-(4-fluorophenyl)[H-3]tropane ([H-3]WIN 35,428) the human dopamine transporter expressed in C6 glioma cells were alkylated with N-ethylmaleimide (NEM), and the protective potency of the blockers cocaine, N[1-(2-benzo[b]thiophenyl)cyclohexyl]piperidine (BTCP), and benztropine, and of the substrates dopamine, d-amphetamine, and norepinephrine was measured. In general, the protective potency was lower (at least 4-5 times) than the potency in inhibiting [H-3]WIN 35,428 binding with the compounds present under the same experimental conditions used for the NEM alkylation. However, thedisparity was substantially greater for all substrates tested (23- to44-fold) than for the blockers (4- to 11-fold), especially cocaine (5-fold) and BTCP (4-fold). Benztropine took an intermediate place (11-fold) between cocaine (5-fold) and BTCP (4-fold), on the one hand, and dopamine (23-fold), on the other hand. [H-3]WIN 35,428 binding was best described by a one site model under the present conditions. The results are discussed in terms of models involving blocker-induced conformational charges and overlapping nonidentical binding domains for blockers and substrates. Copyright (C) 1996 Elsevier Science Inc.

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Documento generato il 05/07/20 alle ore 09:17:05