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Titolo:
Quantification of neuroreceptors in living human brain. V. Endogenous neurotransmitter inhibition of haloperidol binding in psychosis
Autore:
Gjedde, A; Wong, DF;
Indirizzi:
Johns Hopkins Med Inst, Dept Radiol, Baltimore, MD 21205 USA Johns HopkinsMed Inst Baltimore MD USA 21205 ol, Baltimore, MD 21205 USA Aarhus Univ Hosp, Positron Emiss Tomog Ctr, DK-8000 Aarhus, Denmark AarhusUniv Hosp Aarhus Denmark DK-8000 mog Ctr, DK-8000 Aarhus, Denmark
Titolo Testata:
JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
fascicolo: 8, volume: 21, anno: 2001,
pagine: 982 - 994
SICI:
0271-678X(200108)21:8<982:QONILH>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON-EMISSION-TOMOGRAPHY; D2 DOPAMINE-RECEPTORS; TERNARY COMPLEX MODEL; SEROTONIN RECEPTORS; N-METHYLSPIPERONE; C-11 RACLOPRIDE; LIGAND-BINDING; IN-VIVO; SCHIZOPHRENIA; DENSITY;
Keywords:
dopamine; neuroleptics; neuroreceptors; positron emission tomography;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
44
Recensione:
Indirizzi per estratti:
Indirizzo: Gjedde, A Aarhus Gen Hosp, PET Ctr, 44 Norrebrogade, DK-8000 Aarhus C, Denmark Aarhus Gen Hosp 44 Norrebrogade Aarhus Denmark C hus C, Denmark
Citazione:
A. Gjedde e D.F. Wong, "Quantification of neuroreceptors in living human brain. V. Endogenous neurotransmitter inhibition of haloperidol binding in psychosis", J CEREBR B, 21(8), 2001, pp. 982-994

Abstract

The half-inhibition concentration (IC50) of a drug indicates its ability to inhibit the binding of other ligands of a receptor. The authors used positron emission tomography to test the hypothesis that haloperidol's IC50 toward the binding of tracer N-[C-11]methylspiperone ([C-11]NMSP) in brain must be increased in patients in whom more dopamine is bound to receptors thanin healthy volunteers. The IC50 of haloperidol was significantly elevated from 1.5 nmol/L in healthy volunteers and patients with bipolar disease without psychosis to 4.5 nmol/L in patients with schizophrenia or bipolar disease with psychosis. The higher IC50 values in psychosis are consistent withan 8-fold increased binding of dopamine and a 16-fold elevated concentration of synaptic dopamine in psychosis. At the 80% haloperidol blockade of the receptors, the calculated amount of neurotransmitter bound in the patients with psychosis declined to twice the value estimated in the nonpsychotic subjects, that is, 5 pmol cm(-3).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 18:24:38