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Titolo:
EVALUATION OF 5-[F-18]FLUOROPROPYLEPIDEPRIDE AS A POTENTIAL PET RADIOLIGAND FOR IMAGING DOPAMINE D2 RECEPTORS
Autore:
KESSLER RM; VOTAW JR; DEPAULIS T; BINGHAM DR; ANSARI MS; MASON NS; HOLBURN G; SCHMIDT DE; VOTAW DB; MANNING RG; EBERT MH;
Indirizzi:
VANDERBILT UNIV,SCH MED,DEPT RADIOL NASHVILLE TN 37232 VANDERBILT UNIV,SCH MED,DEPT CHEM NASHVILLE TN 37232 VANDERBILT UNIV,SCH MED,DEPT PSYCHIAT NASHVILLE TN 37232 VANDERBILT UNIV,SCH MED,DEPT PHYS NASHVILLE TN 37232
Titolo Testata:
Synapse
fascicolo: 3, volume: 15, anno: 1993,
pagine: 169 - 176
SICI:
0887-4476(1993)15:3<169:EO5AAP>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; F-18 N-METHYLSPIROPERIDOL; LIVING HUMAN-BRAIN; HIGH-AFFINITY; ENDOGENOUS DOPAMINE; H-3 RACLOPRIDE; INVITRO BINDING; RAT-BRAIN; BENZAMIDES; LIGANDS;
Keywords:
POSITRON TOMOGRAPHY; SUBSTITUTED BENZAMIDE; F-18;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
39
Recensione:
Indirizzi per estratti:
Citazione:
R.M. Kessler et al., "EVALUATION OF 5-[F-18]FLUOROPROPYLEPIDEPRIDE AS A POTENTIAL PET RADIOLIGAND FOR IMAGING DOPAMINE D2 RECEPTORS", Synapse, 15(3), 1993, pp. 169-176

Abstract

This study evaluated the utility of l]-5-(3-[F-18]fluoropropyl)-2,3-dimethoxybenzamide ([F-18]fluoropropylepidepride), [F-18]5-FPrEpid, as a ligand for PET studies of cerebral dopamine D2 receptors. The in vitro affinity for the rat striatal dopamine D2 receptor, K-D 138 pM, wasdetermined by Scatchard analysis of in vitro binding to rat striatal homogenate. The apparent lipophilicity, log k(w) 1.6, was measured with reverse phase HPLC at pH 7.5. The receptor specificity was determined by competitive displacement of [F-18]5-FPrEpid by a variety of neurotransmitter ligands. Only dopamine D2 ligands displaced [F-18]5-FPrEpid with high affinity. Positron tomographic imaging studies in primatesof[F-18]5-FPrEpid demonstrated a stable striatal uptake of 0.02% injected dose/ml for up to 5 h after injection. The striatal: cerebellar ratio increased from 2 at 15 min, to 7 at 200 min, and to 10 at 300 min. Striatal uptake was displaceable by haloperidol (1 mg/kg) or raclopride (2.5 mg/kg) to cerebellar levels with a t(1/2) of washout of 9 or 15 min. Striatal uptake was mildly susceptible to displacement by d-amphetamine (1-2 mg/kg) released endogenous dopamine; d-amphetamine administration produced a 10%h increase in the rate of striatal washout. Although uptake in the striatum is reversible, an equilibrium between receptor bound [F-18]5-FPrEpid in striatum and [F-18]5-FPrEpid in plasma is not reached within 5 h postinjection. (c) 1993 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 07:04:11