PMID: 8935801Mar 1, 1996

Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding

Psychopharmacology
A SchotteJ E Leysen

Abstract

Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). An ex vivo autoradiography technique was applied to determine the receptor occupancy by the drugs administered in vivo. Of particular interest are the central 5HT2A receptors and D2-type receptors. Predominant 5HT2A receptor antagonism is supposed to add to an atypical profile of the antipsychotics (treatment of the negative symptoms, low incidence of extrapyramidal side effects). D2 antagonism is required the treatment of positive symptoms. A contribution of the new dopamine receptor subtypes D3 and in particular D4 receptors has been proposed. In vitro, all compounds, except the 'typical' antipsychotics haloperidol and fluspirilene, showed higher affinity for 5HT2A than for D2 receptors. Subnanomolar affinity for human...Continue Reading

References

Mar 26, 1999·Movement Disorders : Official Journal of the Movement Disorder Society·V G EvidenteC H Alder
Dec 17, 2002·Pharmazie in unserer Zeit·Walter E Müller
Mar 20, 2004·Irish Journal of Medical Science·J V Lucey, S E Libretto
Sep 2, 2006·Naunyn-Schmiedeberg's Archives of Pharmacology·Marie-Bernadette AssiéAdrian Newman-Tancredi
Feb 15, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Georges VauquelinPhilip Seeman
Jul 8, 2005·Psychopharmacology·Charles H LargeDonald C Goff
Feb 19, 2005·Psychopharmacology·James M StoneLyn S Pilowsky
Feb 26, 2008·Psychopharmacology·Frank I TaraziMohammed Shahid
May 23, 2009·Psychopharmacology·Hugh M MarstonMohammed Shahid
Aug 19, 2009·Psychopharmacology·Shona L KirkGavin P Reynolds
Aug 21, 2012·Psychopharmacology·Masaaki OgasaJohn Guarino
Jun 24, 2006·Wiener klinische Wochenschrift·Julia EnglChristoph Ebenbichler
Dec 25, 2010·Journal of Computer-aided Molecular Design·Sébastien Dilly, Jean-François Liégeois
May 3, 2007·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Jesper EkelundMarc Laruelle
Nov 19, 2013·Clinical Drug Investigation·Alfonso Rodríguez-Martínez, Carlos Guzmán Quilo

Citations

Sep 12, 1979·Biochemical and Biophysical Research Communications·J S KarlinerC T Dollery
Apr 15, 1978·European Journal of Pharmacology·R S ChangS H Snyder
Feb 1, 1979·Journal of Neurochemistry·P M LaduronJ E Leysen
Jun 24, 1976·Nature·Philip SeemanK Wong
Jan 1, 1975·Pharmacology, Biochemistry, and Behavior·J MajB Przewlocka
Aug 6, 1992·European Journal of Pharmacology·A SchotteJ E Leysen
Sep 1, 1992·Proceedings of the National Academy of Sciences of the United States of America·D LévesqueP Sokoloff
Nov 1, 1991·The American Journal of Psychiatry·K L DavisM Davidson
Sep 1, 1990·Pharmacopsychiatry·Y G GeldersP F Janssen
Jan 25, 1991·Science·R M SniderR W Spencer
Jan 1, 1989·Psychopharmacology·R GrohmannL G Schmidt
Feb 26, 1985·European Journal of Pharmacology·R A LahtiP F Von Voigtlander
Jul 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·R S Chang, V J Lotti
Aug 1, 1986·Naunyn-Schmiedeberg's Archives of Pharmacology·A SchotteP M Laduron
Dec 15, 1986·Biochemical Pharmacology·S B Hwang, M H Lam
May 1, 1987·British Journal of Pharmacology·P V HalushkaD E Mais
Jan 1, 1987·Computers in Biology and Medicine·E G Oestreicher, G F Pinto
Jun 1, 1985·Archives of General Psychiatry·G AndrewsD Silove
Jan 1, 1985·Schizophrenia Bulletin·W HallD Silove
Aug 1, 1973·Archives of General Psychiatry·J R Stevens
Aug 1, 1984·Proceedings of the National Academy of Sciences of the United States of America·B L LargentS H Snyder
Jan 12, 1980·British Medical Journal·T J Crow

Related Concepts

Antipsychotic Effect
Receptors, Histamine H1
Tissue Membrane
Assay OF Haloperidol
Olanzapine
Seroquel
Schizophrenia
Cavia
Paliperidone
Clozapine

Related Feeds

Antipsychotic Drugs

Antipsychotic drugs are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. Discover the latest research on antipsychotic drugs here

Blood And Marrow Transplantation

The use of hematopoietic stem cell transplantation or blood and marrow transplantation (bmt) is on the increase worldwide. BMT is used to replace damaged or destroyed bone marrow with healthy bone marrow stem cells. Here is the latest research on bone and marrow transplantation.