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Titolo:
Evaluation of, dopamine D-2 receptor occupancy by clozapine, risperidone, and haloperidol in vivo in the rodent and nonhuman primate brain using F-18-fallypride
Autore:
Mukherjee, J; Christian, BT; Narayanan, TK; Shi, BH; Mantil, J;
Indirizzi:
Wright State Univ, Kettering Med Ctr, Dept Internal Med Nucl Med, Dayton, OH 45435 USA Wright State Univ Dayton OH USA 45435 Med Nucl Med, Dayton, OH 45435 USA
Titolo Testata:
NEUROPSYCHOPHARMACOLOGY
fascicolo: 4, volume: 25, anno: 2001,
pagine: 476 - 488
SICI:
0893-133X(200110)25:4<476:EODDRO>2.0.ZU;2-J
Fonte:
ISI
Lingua:
ENG
Soggetto:
EXTRASTRIATAL D-2-DOPAMINE RECEPTORS; POSITRON-EMISSION-TOMOGRAPHY; ANTIPSYCHOTIC-DRUGS; TREATED PATIENTS; F-18 FALLYPRIDE; GRAPHICAL ANALYSIS; I-125 EPIDEPRIDE; HIGH-AFFINITY; IN-VIVO; BINDING;
Keywords:
dopamine D-2 receptors; occupancy; neuroleptics; F-18-fallypride; PET;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
41
Recensione:
Indirizzi per estratti:
Indirizzo: Mukherjee, J Univ Calif Irvine, Brain Imaging Ctr, 163 Irvine Hall, Irvine, CA 92697 USA Univ Calif Irvine 163 Irvine Hall Irvine CA USA 92697 697 USA
Citazione:
J. Mukherjee et al., "Evaluation of, dopamine D-2 receptor occupancy by clozapine, risperidone, and haloperidol in vivo in the rodent and nonhuman primate brain using F-18-fallypride", NEUROPSYCH, 25(4), 2001, pp. 476-488

Abstract

We have used the high-affinity dopamine D-2 receptor radioligand, F-18-fallypride for evaluating receptor occupancy by the antipsychotic drugs, clozapine, risperidone, and haloperidol in rodents and nonhuman primates. In rodents, clozapine (0.1 mg/kg to 100 mg/kg) competed with F-18-fallypride at all the doses administered. At doses over 40 mg/kg, clozapine was able to displace all the administered F-18-fallypride, A pseudobiphasic profile of receptor occupancy by clozapine was observed. This behavior was compared withsuch other neuroleptics as risperidone and haloperidol that exhibited over90% receptor occupancy at doses over 0.1 mg/kg and did not exhibit a biphasic nature. Dopamine D-2 receptor occupancy in the monkeys was studied using positron emission tomography (PET) after acute subcutaneous doses of the various drugs. At therapeutically relevant doses, clozapine, risperidone, and haloperidol were able to compete significantly with the binding of F-18-fallypride in all brain regions in rhesus monkeys, and our analyses indicate that these drugs (clozapine, risperidone, and haloperidol) do not discriminate between the striatal (caudate and putamen) and the extrastriatal (thalamus and cortical regions) dopamine receptors. The following extent of D-2receptor occupancies were measured in the monkey brain using PET: clozapine approximate to 70% (dose of 9.7 mg/kg), risperidone approximate to 75% (0.05 mg/kg), and haloperidol approximate to 90% (0.05 mg/kg).

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Documento generato il 20/11/19 alle ore 03:27:02