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Titolo:
EFFECT OF CLOZAPINE AND RISPERIDONE ON 5-HT2 AND D-2-DOPAMINE RECEPTOR-BINDING IN THE POSTMORTEM HUMAN BRAIN - AN AUTORADIOGRAPHIC STUDY
Autore:
HALL H; HALLDIN C; NYBERG S; FARDE L; SEDVALL G;
Indirizzi:
KAROLINSKA HOSP & INST,DEPT CLIN NEUROSCI,PSYCHIAT & PSYCHOL SECT S-17176 STOCKHOLM SWEDEN
Titolo Testata:
European neuropsychopharmacology
fascicolo: 1, volume: 5, anno: 1995,
pagine: 19 - 25
SICI:
0924-977X(1995)5:1<19:EOCARO>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOPAMINE-RECEPTORS; RAT-BRAIN; SCHIZOPHRENIC-PATIENTS; ANTIPSYCHOTIC-DRUGS; SEROTONIN RECEPTORS; CEREBRAL-CORTEX; INVIVO BINDING; H-3 RACLOPRIDE; HIGH-AFFINITY; OCCUPANCY;
Keywords:
AUTORADIOGRAPHY; CLOZAPINE; D-2-DOPAMINE RECEPTOR; 5-HT2 RECEPTOR; HUMAN BRAIN; [H-3] N-METHYLSPIPERONE; RISPERIDONE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
H. Hall et al., "EFFECT OF CLOZAPINE AND RISPERIDONE ON 5-HT2 AND D-2-DOPAMINE RECEPTOR-BINDING IN THE POSTMORTEM HUMAN BRAIN - AN AUTORADIOGRAPHIC STUDY", European neuropsychopharmacology, 5(1), 1995, pp. 19-25

Abstract

Effects of the antipsychotics risperidone and clozapine on 5-HT2 and D-2-dopamine receptor binding were examined using [H-3]N-methylspiperone ([H-3]NMSP) and in vitro receptor autoradiography on human whole hemisphere cryosections. The 5-HT2 receptor antagonist ketanserin and the D-2-dopamine receptor antagonist raclopride were used as references.[H-3]NMSP binding was observed in caudate nucleus, putamen, and cerebral cortex indicating binding to D-2-dopamine and 5-HT2 receptors. Risperidone and clozapine counteracted the binding to both receptor types. This was in contrast to raclopride, which selectively blocked the D-2-dopamine receptors in the basal ganglia, and ketanserin, which selectively blocked the 5-HT2 receptors in the cerebral cortex. Risperidone(100 nM and 10 mu M) blocked up to 90% of [H-3]NMSP binding to both receptor types, whereas the blocking capacity of clozapine (10 mu M) was lower (approximately 60%). The lack of total blockade of D-2-dopamine receptors is in line with results obtained in with [C-11]raclopride and positron emission tomography studies of clozapine treated human subjects. However, autoradiographic studies of clozapine competition of [H-3]raclopride binding show total displacement of the binding at highclozapine concentrations, thus contradicting the PET results with [C-11]raclopride, as well as the autoradiographic results obtained with [H-3]NMSP. In conclusion it can be stated that pharmacological concentrations of the two drugs clozapine and risperidone block a large proportion of D-2-dopamine receptors and 5-HT2 receptors in the human brain. Moreover, the study shows the usefulness of human whole hemisphere autoradiography for the study of interaction of drugs with different central neurotransmitter receptors.

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Documento generato il 25/01/20 alle ore 19:19:25