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Titolo:
IDENTIFICATION OF D-3 AND SIGMA-RECEPTORS IN THE RAT STRIATUM AND NUCLEUS-ACCUMBENS USING (+ -)-7-HYDROXY-N,N-DI-N-[H-3] PROPYL-2-AMINOTETRALIN AND CARBETAPENTANE/
Autore:
WALLACE DR; BOOZE RM;
Indirizzi:
UNIV KENTUCKY,COLL MED,DEPT PHARMACOL,MS-305,UKMC LEXINGTON KY 00000 UNIV KENTUCKY,COLL MED,DEPT PHARMACOL LEXINGTON KY 00000
Titolo Testata:
Journal of neurochemistry
fascicolo: 2, volume: 64, anno: 1995,
pagine: 700 - 710
SICI:
0022-3042(1995)64:2<700:IODASI>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
BINDING-SITES; DOPAMINE-D3 RECEPTOR; INVITRO BINDING; H-3 RACLOPRIDE; GUINEA-PIG; LIGAND; COCAINE; BRAIN; LOCALIZATION; SUBTYPES;
Keywords:
DOPAMINERGIC SYSTEM; NUCLEUS ACCUMBENS; STRIATUM; AUTORADIOGRAPHY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
40
Recensione:
Indirizzi per estratti:
Citazione:
D.R. Wallace e R.M. Booze, "IDENTIFICATION OF D-3 AND SIGMA-RECEPTORS IN THE RAT STRIATUM AND NUCLEUS-ACCUMBENS USING (+ -)-7-HYDROXY-N,N-DI-N-[H-3] PROPYL-2-AMINOTETRALIN AND CARBETAPENTANE/", Journal of neurochemistry, 64(2), 1995, pp. 700-710

Abstract

Cross-reactions between dopamine D-3 and sigma receptor ligands were investigated using (+/-)-7-hydroxy-N,N-di-n-[H-3] propyl-2-aminotetralin [(+/-)-7-OH-[3H]-DPAT], a putative D-3-selective radioligand, in conjunction with the unlabeled sigma ligands 1,3-di(2-tolyl)guanidine (DTG), carbetapentane, and R(-)-N-(3-phenyl-1-propyl)-1-phenyl-2-aminopropane [R(-)-PPAP]. In transfected CCL1.3 mouse fibroblasts expressing the human D-3 receptor, neither DTG nor carbetapentane (0.1 mu M) displaced (+/-)-7-OH-[H-3]DPAT binding. R(-)-PPAP (0.1 mu M) displaced 39.6 +/- 1.0% of total (+/-)-7-OH-[H-3]DPAT binding. In striatal and nucleus accumbens homogenates, (+/-)-7-OH-[H-3]DPAT labeled a single site (15-20 fmol/mg of protein) with high (1 nM) affinity. Competition analysis with carbetapentane defined both high- and low-affinity sites in striatal (35 and 65%, respectively) and nucleus accumbens (59 and 41%,respectively) tissue, yet R(-)-PPAP identified two sites in equal proportion. Carbetapentane and R(-)-PPAP (0.1 mu M) displaced similar to 20-50% of total (+/-)-7-OH-[H-3]DPAT binding in striatum, nucleus accumbens, and olfactory tubercle in autoradiographic studies, with the nucleus accumbens shell subregion exhibiting the greatest displacement. To determine directly (+)-7-OH-[H-3]DPAT binding to sigma receptors, saturation analysis was performed in the cerebellum while masking D-3 receptors with 1 mu M dopamine. Under these conditions (+)-7-OH-[3H]DPAT labeled sigma receptors with an affinity of 24 nM. These results suggest that (a) (+/-)7-OH-[H-3]DPAT binds D-3 receptors with high affinity in rat brain and (b) a significant proportion of (+/-)-7-OH-[H-3]DPAT binding consists of sigma(1) sites and the percentages of these sites differ among the subregions of the striatum and nucleus accumbens.

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Documento generato il 25/01/20 alle ore 09:25:21