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Titolo:
Effects of the substituted (S)-3-phenylpiperidine (-)-OSU6162 on PET measurements of [C-11]SCH23390 and [C-11]raclopride binding in primate brains
Autore:
Ekesbo, A; Torstenson, R; Hartvig, P; Carlsson, A; Sonesson, C; Waters, N; Tedroff, J; Langstrom, B;
Indirizzi:
Univ Uppsala Hosp, Dept Neurosci, S-75185 Uppsala, Sweden Univ Uppsala Hosp Uppsala Sweden S-75185 urosci, S-75185 Uppsala, Sweden Univ Uppsala Hosp, Hosp Pharm, S-75185 Uppsala, Sweden Univ Uppsala Hosp Uppsala Sweden S-75185 Pharm, S-75185 Uppsala, Sweden Uppsalaweden, PET Ctr, Subfemtomole Biorecognit Project, S-75185 Uppsala, S Uppsala Univ Uppsala Sweden S-75185 recognit Project, S-75185 Uppsala, S Univ Gothenburg, Dept Pharmacol, Gothenburg, Sweden Univ Gothenburg Gothenburg Sweden g, Dept Pharmacol, Gothenburg, Sweden
Titolo Testata:
NEUROPHARMACOLOGY
fascicolo: 3, volume: 38, anno: 1999,
pagine: 331 - 338
SICI:
0028-3908(199903)38:3<331:EOTS((>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; LEVODOPA-INDUCED DYSKINESIA; PARKINSONS-DISEASE; INVIVO BINDING; L-DOPA; ENDOGENOUS DOPAMINE; RECEPTOR OCCUPANCY; SYNAPTIC DOPAMINE; N-METHYLSPIPERONE; STRIATAL BINDING;
Keywords:
[C-11]SCH23390; [C-11]raclopride; (-)-OSU6162; monkey; positron emission tomography;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
40
Recensione:
Indirizzi per estratti:
Indirizzo: Tedroff, J Univ Uppsala Hosp, Dept Neurosci, S-75185 Uppsala, Sweden Univ Uppsala Hosp Uppsala Sweden S-75185 5185 Uppsala, Sweden
Citazione:
A. Ekesbo et al., "Effects of the substituted (S)-3-phenylpiperidine (-)-OSU6162 on PET measurements of [C-11]SCH23390 and [C-11]raclopride binding in primate brains", NEUROPHARM, 38(3), 1999, pp. 331-338

Abstract

The substituted (S)-3-phenylpiperidine (-)-OSU6162 belongs to a novel class of functional modulators of dopaminergic systems. In vivo, (-)-OSU6162 has a unique stabilising profile on dopaminergic functions. In vitro this compound exhibits low affinity for the dopamine D2 receptor, but due to its similarity to neuroleptics on brain dopaminergic neurochemistry and differentpostsynaptic effects it has been characterised as a preferential dopamine autoreceptor antagonist. To further clarify the effects of(-)-OSU6162 on the postjunctional nigrostriatal dopaminergic system, dopamine receptor binding was measured in rhesus monkeys (Macaca mulatta) by positron emission tomography (PET) using the D1 and D2 dopamine receptor radioligands [C-11]SCH23390 and [C-11]raclopride respectively, before and during continuous intravenous infusions of(-)-OSU6162. Additionally, the test-retest variability ofsequential [C-11]SCH23390 scans was estimated. Following the administration of(-)-OSU6162, [C-11]raclopride binding in striatum was dose-dependently decreased with a 76% reduction occurring after 3.0 mg/kg per h continuous infusion. Whereas (-)-OSU6162 in the lower doses had no effect on [C-11]SCH23390 binding, the highest dose, 3.0 mg/kg per h, increased [C-11]SCH23390 binding, which may indicate a potentiating effect on D1 dopamine receptor mediated functions. Thus, in contrast to the conditions in vitro, (-)-OSU6162produces a high displacement of raclopride from D2 receptors in vivo. (C) 1999 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 06:07:56