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Pharmacological Profile of Antipsychotics at Monoamine Receptors: Atypicality Beyond 5-HT2A Receptor Blockade

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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; binding; function; monoamine receptors; pharmacology

Document Type: Research Article


Affiliations: GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AD, UK.

Publication date: 2006-08-01

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  • CNS & Neurological Disorders - Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular targets involved in neurological and central nervous system (CNS) disorders e.g. disease specific proteins, receptors, enzymes, genes. Each issue of the journal will contain a series of timely in-depth reviews written by leaders in the field covering a range of current topics on drug targets involved in neurological and CNS disorders. As the discovery, identification, characterization and validation of novel human drug targets for neurological and CNS drug discovery continues to grow; this journal will be essential reading for all pharmaceutical scientists involved in drug discovery and development.
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