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Titolo:
Positron emission tomography of radioligand binding in porcine striatum invivo: Haloperidol inhibition linked to endogenous ligand release
Autore:
Ishizu, K; Smith, DF; Bender, D; Danielsen, E; Hansen, SB; Wong, DF; Cumming, P; Gjedde, A;
Indirizzi:
Aarhus Gen Hosp, PET Ctr, DK-8000 Aarhus C, Denmark Aarhus Gen Hosp Aarhus Denmark C osp, PET Ctr, DK-8000 Aarhus C, Denmark Aarhus Univ Hosp, Aarhus Psychiat Hosp, Dept Biol Psychiat, Inst Basic ResPsychiat, DK-8000 Aarhus, Denmark Aarhus Univ Hosp Aarhus Denmark DK-8000sychiat, DK-8000 Aarhus, Denmark Johns Hopkins Univ, Inst Med, Dept Radiol, Div Nucl Med, Baltimore, MD USAJohns Hopkins Univ Baltimore MD USA iol, Div Nucl Med, Baltimore, MD USA
Titolo Testata:
SYNAPSE
fascicolo: 1, volume: 38, anno: 2000,
pagine: 87 - 101
SICI:
0887-4476(200010)38:1<87:PETORB>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
LIVING HUMAN-BRAIN; DOPAMINE-RECEPTOR-BINDING; MEDIAL PREFRONTAL CORTEX; C-11 RACLOPRIDE; IN-VIVO; SEROTONIN RECEPTORS; RAT-BRAIN; SYNAPTIC DOPAMINE; PET; INVIVO;
Keywords:
3-N-[C-11]methylspiperone; dopamine; PET; haloperidol; receptor binding; pig brain;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
51
Recensione:
Indirizzi per estratti:
Indirizzo: Gjedde, A Aarhus Gen Hosp, PET Ctr, Norrebrogade 44, DK-8000 Aarhus C, Denmark Aarhus Gen Hosp Norrebrogade 44 Aarhus Denmark C hus C, Denmark
Citazione:
K. Ishizu et al., "Positron emission tomography of radioligand binding in porcine striatum invivo: Haloperidol inhibition linked to endogenous ligand release", SYNAPSE, 38(1), 2000, pp. 87-101

Abstract

The ligands N-methylspiperone and haloperidol both bind to D-2-live dopamine receptors. The competitive nature of the binding over a wide range of haloperidol concentrations and the effect on dopamine release have never beentested in vivo. We determined the competitive interaction between 3-N-[C-11] methylspiperone ([C-11]NMSP) and haloperidol binding to striatal dopamine D-2-like receptors with positron emission tomography (PET) of pig brain. [C-11]NMSP tomography was performed with haloperidol at five different plasma concentrations maintained constant by programmed infusion. Kinetic parameters of ligand competition for binding in the striatum were determined by deconvolving time-activity curves of the striatum and cerebellum from metabolite-corrected arterial plasma [C-11]NMSP and haloperidol concentrations. Two types of [C-11]NMSP-binding sites were evident in the striatum, both saturable by haloperidol administration. The preponderant or primary sites bound [C-11]NMSP irreversibly, as dopamine DB-like receptors, while the secondary sites bound [C-11]NMSP reversibly, as do serotonin S2 receptors. Woolf-Hanes plots revealed the predicted approximately linear relationships between the binding indices and the haloperidol plasma concentration. For the irreversible binding sites, this relationship indicated a 50% inhibitory concentration of haloperidol of 2 nM in plasma and a maximum binding capacity of 64 pmol cm(-3) in striatum. For the reversible binding sites, the relationship indicated a 50% inhibitory plasma concentration of haloperidol of 1 nM and a maximum binding capacity of 4.5 pmol cm(-3). Second-order polynomial Eadie-Hofstee-Scatchard plots were consistent with increased competitionfrom an endogenous ligand of the irreversibly binding sites only with increasing doses of haloperidol. At the highest haloperidol dose, this hypothetical endogenous ligand had risen 6-7-fold. We contend that this reveals therelease of dopamine by high concentrations of haloperidol. Synapse 38:87-101, 2000, (C) 2000 Wiley Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 17:05:10