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Titolo:
RELATIONSHIPS BETWEEN THE CATECHOL SUBSTRATE-BINDING SITE AND AMPHETAMINE, COCAINE, AND MAZINDOL BINDING-SITES IN A KINETIC-MODEL OF THE STRIATAL TRANSPORTER OF DOPAMINE IN-VITRO
Autore:
WAYMENT H; MEIERGERD SM; SCHENK JO;
Indirizzi:
WASHINGTON STATE UNIV,DEPT CHEM PULLMAN WA 99164 WASHINGTON STATE UNIV,DEPT CHEM PULLMAN WA 99164 WASHINGTON STATE UNIV,DEPT BIOPHYS & BIOCHEM PULLMAN WA 99164 WASHINGTON STATE UNIV,PROGRAM PHARMACOL TOXICOL PULLMAN WA 99164 WASHINGTON STATE UNIV,PROGRAM NEUROSCI PULLMAN WA 99164
Titolo Testata:
Journal of neurochemistry
fascicolo: 5, volume: 70, anno: 1998,
pagine: 1941 - 1949
SICI:
0022-3042(1998)70:5<1941:RBTCSS>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
VESICULAR TRANSMITTER STORES; RAT-BRAIN SYNAPTOSOMES; INDUCED RELEASE; ACETYLCHOLINE NEUROTRANSMISSION; SYNTHESIS INHIBITORS; CORPUS STRIATUM; H-3 AMPHETAMINE; MECHANISM; GBR-12935; SYSTEMS;
Keywords:
STRIATAL DOPAMINE TRANSPORTER; COCAINE BINDING SITE; AMPHETAMINE BINDING SITE; MAZINDOL BINDING SITE; ROTATING DISK ELECTRODE VOLTAMMETRY; M-TYRAMINE; CATECHOL SUBSTRATE BINDING SITE; PHENETHYLAMINES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
37
Recensione:
Indirizzi per estratti:
Citazione:
H. Wayment et al., "RELATIONSHIPS BETWEEN THE CATECHOL SUBSTRATE-BINDING SITE AND AMPHETAMINE, COCAINE, AND MAZINDOL BINDING-SITES IN A KINETIC-MODEL OF THE STRIATAL TRANSPORTER OF DOPAMINE IN-VITRO", Journal of neurochemistry, 70(5), 1998, pp. 1941-1949

Abstract

Experiments were conducted to determine how (-)-cocaine and S(+)-amphetamine binding sites relate to each other and to the catechol substrate site on the striatal dopamine transporter (sDAT). In controls, m-tyramine and S(+)-amphetamine caused release of dopamine from intracellular stores at concentrations greater than or equal to 12-fold those observed to inhibit inwardly directed sDAT activity for dopamine. In preparations from animals pretreated with reserpine, m-tyramine and S(+)-amphetamine caused release of preloaded dopamine at concentrations similar to those that inhibit inwardly directed sDAT activity. S(+)-Amphetamine and m-tyramine inhibited sDAT activity for dopamine by competing for a common binding site with dopamine and each other, suggesting that phenethylamines are substrate analogues at the plasmalemmal sDAT. (-)-Cocaine inhibited sDAT at a site separate from that for substrate analogues. This site is mutually interactive with the substrate site (K-int = 583 nM). Mazindol competitively inhibited sDAT at the substrate analogue binding site. The results with (-)-cocaine suggest that the(-)-cocaine binding site on sDAT is distinct from that of hydroxyphenethylamine substrates, reinforcing the notion that an antagonist for (-)-cocaine binding may be developed to block(-)-cocaine binding with minimal effects on dopamine transporter activity. However, a strategy of how to antagonize drugs of abuse acting as substrate analogues is still elusive.

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Documento generato il 08/04/20 alle ore 22:32:14