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Titolo:
IN-VIVO KINETICS OF [F-18] (N-METHYL)BENPERIDOL - A NOVEL PET TRACER FOR ASSESSMENT OF DOPAMINERGIC D2-LIKE RECEPTOR-BINDING
Autore:
MOERLEIN SM; PERLMUTTER JS; MARKHAM J; WELCH MJ;
Indirizzi:
WASHINGTON UNIV,SCH MED,EDWARD MALLINCKRODT INST RADIOL,510 S KINGSHIGHWAY BLVD ST LOUIS MO 63110 WASHINGTON UNIV,SCH MED,DEPT BIOCHEM & MOL BIOPHYS ST LOUIS MO 63110 WASHINGTON UNIV,SCH MED,DEPT NEUROL & NEUROSURG ST LOUIS MO 63110 WASHINGTON UNIV,SCH MED,INST BIOMED COMP ST LOUIS MO 63110
Titolo Testata:
Journal of cerebral blood flow and metabolism
fascicolo: 8, volume: 17, anno: 1997,
pagine: 833 - 845
SICI:
0271-678X(1997)17:8<833:IKO[(->2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; STEADY-STATE MEASUREMENT; EARLY PARKINSONS-DISEASE; LIVING HUMAN-BRAIN; C-11 RACLOPRIDE; H-3 RACLOPRIDE; SEROTONIN RECEPTORS; INVIVO ASSESSMENT; INVITRO BINDING; D-2 RECEPTORS;
Keywords:
DOPAMINERGIC D2 RECEPTORS; POSITRON EMISSION TOMOGRAPHY; [F-18] (N-METHYL)BENPERIDOL; IMAGING; BENPERIDOL; NEURORECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
81
Recensione:
Indirizzi per estratti:
Citazione:
S.M. Moerlein et al., "IN-VIVO KINETICS OF [F-18] (N-METHYL)BENPERIDOL - A NOVEL PET TRACER FOR ASSESSMENT OF DOPAMINERGIC D2-LIKE RECEPTOR-BINDING", Journal of cerebral blood flow and metabolism, 17(8), 1997, pp. 833-845

Abstract

A novel D2-like receptor-binding radioligand, [F-18](N-methyl)benperidol ([F-18]NMB), was evaluated via positron emission tomographic (PET)imaging studies of baboons. [F-18]NMB rapidly localized in vivo within dopaminergic receptor-rich cerebral tissues, and striatum-to-cerebellum ratios as high as 35 were achieved after 3 hours. Pretreatment of an animal with unlabeled receptor-specific antagonists before injection of [F-18]NMB confirmed that the radioligand bound specifically to central D2-like receptors in vivo, and not to S2- or D1-like receptors. Unlabeled eticlopride displaced striatal [F-18]NMB in vivo, showing that D2-like binding is reversible. Receptor-binding by the radioligand was resistant to competitive displacement by synaptic dopamine, as illustrated by the lack of effect of intravenous d-amphetamine on the in vivo localization of [F-18]NMB. Studies involving sequential intravenous administration of [F-18]NMB, d-amphetamine, and eticlopride show that the radioligand does not undergo agonist-mediated internalization with subsequent trapping. The feasibility of applying a three-compartment non-steady state model for quantification of [F-18]NMB receptor binding was demonstrated. These in vivo characteristics give [F-18]NMB distinct advantages over the PET radiopharmaceuticals currently used forclinical investigation of D2-like receptor binding.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/02/20 alle ore 04:49:49