Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
[H-3] WIN-35,428 ([H-3]CFT) BINDS TO MULTIPLE CHARGE-STATES OF THE SOLUBILIZED DOPAMINE TRANSPORTER IN PRIMATE STRIATUM
Autore:
GRACZ LM; MADRAS BK;
Indirizzi:
HARVARD UNIV,NEW ENGLAND REG PRIMATE RES CTR,SCH MED,DEPT PSYCHIAT,BOX 9102 SOUTHBOROUGH MA 01772 HARVARD UNIV,NEW ENGLAND REG PRIMATE RES CTR,SCH MED,DEPT PSYCHIAT SOUTHBOROUGH MA 01772 HARVARD UNIV,NEW ENGLAND REG PRIMATE RES CTR,SCH MED,DIV BEHAV BIOL SOUTHBOROUGH MA 01772
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 3, volume: 273, anno: 1995,
pagine: 1224 - 1234
SICI:
0022-3565(1995)273:3<1224:[W(BTM>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
COCAINE RECOGNITION SITES; RAT STRIATUM; NONHUMAN-PRIMATES; H-3 COCAINE; CAUDATE-PUTAMEN; HIGH-AFFINITY; I-125 RTI-55; MONKEY BRAIN; MOUSE-BRAIN; WIN 35,428;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
50
Recensione:
Indirizzi per estratti:
Citazione:
L.M. Gracz e B.K. Madras, "[H-3] WIN-35,428 ([H-3]CFT) BINDS TO MULTIPLE CHARGE-STATES OF THE SOLUBILIZED DOPAMINE TRANSPORTER IN PRIMATE STRIATUM", The Journal of pharmacology and experimental therapeutics, 273(3), 1995, pp. 1224-1234

Abstract

Caudate-putamen membranes of rhesus monkey were solubilized (1% digitonin; w/v) and [H-3]WIN 35,428 ([H-3]CFT: 2 beta-carbomethoxy-3 beta-(4-fluorophenyl)-N-[H-3]methyltropane) binding assayed. Saturation analysis revealed high- and low-affinity binding components (K-HIGH: 7.48 /- 2.77 nM; K-LOW: 292 +/- 788 nM; mean +/- SEM). Monoamine transportinhibitors and neurotransmitters had similar affinities for soluble and membrane [H-3]CFT binding sites (r, 0.998; P < .001). The rank order of potency of these compounds for inhibiting [H-3]CFT binding (Lu 19-005 > mazindol > CFT > GBR 12909 > (-)-cocaine > talsupram > dopamine> norepinephrine > citalopram) was consistent with [H-3]CFT labeling cocaine binding sites on the dopamine transporter. [H-3]CFT binding sites were separated into three protein fractions by anion-exchange chromatography, Monoamine transport inhibitors and neurotransmitters inhibited [H-3]CFT binding in each fraction with a rank order of potency consistent with binding to the dopamine transporter, Detection of multiple binding components for [H-3]CFT labeled sites by these drugs variedin each fraction. Size-exclusion chromatography indicated [H-3]CFT bound to a single protein in each fraction (apparent molecular weight, 170 kDa), Therefore, multiple binding components for cocaine reside solely on the dopamine transporter and exhibit different affinities for drugs depending on the charge-state of the transporter.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 07:16:54