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Titolo:
IN-VITRO AND IN-VIVO CHARACTERIZATION OF R(-FIDA2 - A DOPAMINE D2-LIKE IMAGING AGENT())
Autore:
VESSOTSKIE JM; KUNG MP; CHUMPRADIT S; ROMANIELLO G; MCELGIN W; FREDERICK D; MALISON RT; KUNG HF;
Indirizzi:
UNIV PENN,DEPT PHARMACOL,3700 MARKET ST,ROOM 305 PHILADELPHIA PA 19104 UNIV PENN,DEPT PSYCHIAT PHILADELPHIA PA 19104 UNIV PENN,DEPT RADIOL PHILADELPHIA PA 19104
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 7, volume: 36, anno: 1995,
pagine: 1282 - 1288
SICI:
0161-5505(1995)36:7<1282:IAICOR>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; HIGH-AFFINITY; HUMAN-BRAIN; RAT-BRAIN; RECEPTOR RADIOLIGANDS; I-125 EPIDEPRIDE; SUBSTITUTED BENZAMIDE; ANTIPSYCHOTIC AGENTS; SEROTONIN RECEPTORS; INVIVO BINDING;
Keywords:
R(T)-FIDA2; DOPAMINE DE-LIKE RECEPTORS; SINGLE-PHOTON EMISSION COMPUTED TOMOGRAPHY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
45
Recensione:
Indirizzi per estratti:
Citazione:
J.M. Vessotskie et al., "IN-VITRO AND IN-VIVO CHARACTERIZATION OF R(-FIDA2 - A DOPAMINE D2-LIKE IMAGING AGENT())", The Journal of nuclear medicine, 36(7), 1995, pp. 1282-1288

Abstract

R(+)-FIDA2, 4'-fluorobenzyl)-2-pyrrolidinyl)-methyl]benzamide, is a new dopamine D2-like receptor imaging agent that can be labeled with either I-123 or F-18 for SPECT or PET imaging. The purpose of this studywas to characterize its in vitro and in vivo binding properties. Methods: In vitro binding studies using [I-125]R(+)-FIDA2 were performed in Sf9 cells expressing dopamine D2 or D3 receptors and in rat basal forebrain homogenates, which contain a high density of dopamine D2-like receptors. A series of in vivo SPECT imaging studies in nonhuman primates (cynomologous monkeys) were performed by intravenously injecting 7.1 +/- 1.0 mCi of [I-123]R(+)-FIDA2. At least one control study and one displacement experiment, in which a cold compound was injected intravenously 90 min after tracer injection, was performed in each monkey. Data were acquired in 10-min frames for 180 min, and the activity in regions of interest (basal ganglia and cerebellum) were plotted versus time. Results: iodine-125-R(+)-FIDA2 displayed K-d values for D2 and D3 receptor subtypes expressed in Sf9 cells of 0.11 and 0.04 nM, respectively. As expected, SPECT images of monkey brain (transaxial sections, 2 mm) showed that the radioactivity was localized in the area of thebasal ganglia and reached peak concentrations in 11.5 +/- 5.8 min postinjection. An injection of R(+)7-OH-PIPAT, a new ligand that is selective for dopamine D3 receptors and the high affinity state of dopamineD2 receptors, did not show significant displacement of [I-123]R(+)-FIDA2 binding in the basal ganglia. Conclusion: These studies indicate that R(+)-FIDA2 may be a useful ligand for in vitro pharmacological characterization and in vivo imaging of CNS dopamine D2-like receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/12/19 alle ore 01:35:53