Abstract
Antipsychotic drugs (APD) are widely prescribed for the treatment of schizophrenia. The APD are differentiated into typical and atypical based on the lower incidence of extra-pyramidal side-effects associated with the newer atypical APD. It was suggested that atypicality may arise from an interaction with the 5-hydroxytryptamine (5-HT)2 receptor and specifically on the 5-HT2:dopamine D2 affinity ratio. It is now realised that multiple subtypes of these receptors exist and that in addition, atypical APD interact with many monoamine receptors. The aim of the present study was to characterise the interaction of APD with a variety of monoamine receptors in terms of both affinity and efficacy. The data produced has highlighted that the atypical profile of APD such as olanzapine and clozapine may reflect antagonism of the 5-HT2A and 5-HT2C receptors, whilst that of, ziprasidone and quetiapine may reflect partial agonist activity at the 5-HT1A receptor, and that of aripiprazole may reflect partial agonist activity at the 5-HT1A receptor as well as is its claimed partial agonist activity at the dopamine D2 receptor.
Keywords: Antipsychotic, pharmacology, monoamine receptors, function, binding
CNS & Neurological Disorders - Drug Targets
Title: Pharmacological Profile of Antipsychotics at Monoamine Receptors: Atypicality Beyond 5-HT2A Receptor Blockade
Volume: 5 Issue: 4
Author(s): Martyn D. Wood, Claire Scott, Kirsten Clarke, Katherine J. Cato, Nisha Patel, Jennie Heath, Angela Worby, Laurie Gordon, Lorraine Campbell, Graham Riley, Ceri H. Davies, Andrew Gribble and Declan N.C. Jones
Affiliation:
Keywords: Antipsychotic, pharmacology, monoamine receptors, function, binding
Abstract: Antipsychotic drugs (APD) are widely prescribed for the treatment of schizophrenia. The APD are differentiated into typical and atypical based on the lower incidence of extra-pyramidal side-effects associated with the newer atypical APD. It was suggested that atypicality may arise from an interaction with the 5-hydroxytryptamine (5-HT)2 receptor and specifically on the 5-HT2:dopamine D2 affinity ratio. It is now realised that multiple subtypes of these receptors exist and that in addition, atypical APD interact with many monoamine receptors. The aim of the present study was to characterise the interaction of APD with a variety of monoamine receptors in terms of both affinity and efficacy. The data produced has highlighted that the atypical profile of APD such as olanzapine and clozapine may reflect antagonism of the 5-HT2A and 5-HT2C receptors, whilst that of, ziprasidone and quetiapine may reflect partial agonist activity at the 5-HT1A receptor, and that of aripiprazole may reflect partial agonist activity at the 5-HT1A receptor as well as is its claimed partial agonist activity at the dopamine D2 receptor.
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Wood D. Martyn, Scott Claire, Clarke Kirsten, Cato J. Katherine, Patel Nisha, Heath Jennie, Worby Angela, Gordon Laurie, Campbell Lorraine, Riley Graham, Davies H. Ceri, Gribble Andrew and Jones N.C. Declan, Pharmacological Profile of Antipsychotics at Monoamine Receptors: Atypicality Beyond 5-HT2A Receptor Blockade, CNS & Neurological Disorders - Drug Targets 2006; 5 (4) . https://dx.doi.org/10.2174/187152706777950693
DOI https://dx.doi.org/10.2174/187152706777950693 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
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