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.
Export Options
About this article
Cite this article as:
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 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Psychopharmacological Interventions for Adolescents with Eating Disorders
Adolescent Psychiatry Adenosine Receptor Ligands in Clinical Trials
Current Topics in Medicinal Chemistry Neuroregeneration in Parkinson’s Disease: From Proteins to Small Molecules
Current Neuropharmacology Magnetic Resonance Imaging of Iron in Parkinsons Disease
Current Medical Imaging The Use of Stem Cells in Regenerative Medicine for Parkinson’s and Huntington’s Diseases
Current Medicinal Chemistry Role of Catechol-O-Methyltransferase (COMT)-Dependent Processes in Parkinson’s Disease and L-DOPA Treatment
CNS & Neurological Disorders - Drug Targets Imaging Endogenous Neurotransmitters In Vivo with Positron Emission Tomography Displacement Studies
Current Psychopharmacology 5'-Nucleotidases, Nucleosides and their Distribution in the Brain: Pathological and Therapeutic Implications
Current Medicinal Chemistry Blocking Striatal Adenosine A2A Receptors: A New Strategy for Basal Ganglia Disorders
Recent Patents on CNS Drug Discovery (Discontinued) From Treatment Adherence to Advanced Shared Decision Making: New Professional Strategies and Attitudes in Mental Health Care
Current Clinical Pharmacology Oxidative Stress in the Early Stage of Psychosis
Current Topics in Medicinal Chemistry Mitochondrial Disturbances, Tryptophan Metabolites and Neurodegeneration: Medicinal Chemistry Aspects
Current Medicinal Chemistry Functional MRI of the Pancreaticobiliary System
Current Medical Imaging Omega-3 Fatty Acids: Role in the Prevention and Treatment of Psychiatric Disorders
Current Psychiatry Reviews Advances in Lentiviral Vectors: A Patent Review
Recent Patents on DNA & Gene Sequences Effects of Yokukansan, a Japanese Kampo Medicine for Symptoms Associated Autism Spectrum Disorder
CNS & Neurological Disorders - Drug Targets The NMDA/D1 Receptor Complex as a New Target in Drug Development
Current Topics in Medicinal Chemistry Selected Natural and Synthetic Agents Effective against Parkinson’s Disease with Diverse Mechanisms
Current Topics in Medicinal Chemistry Novel Kynurenic Acid Analogues in the Treatment of Migraine and Neurodegenerative Disorders: Preclinical Studies and Pharmaceutical Design
Current Pharmaceutical Design Evaluation of the Antipsychotic Effects of 2-(dimethylamino)- and 2-(methylamino)-7H-naphtho[1,2,3-de]quinolin-7-one Derivatives in Experimental Model of Psychosis in Mice
Current Topics in Medicinal Chemistry