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Current 

Molecular Medicine

Volume 3, Number 5, 2003

 

Contents

 

Recent Findings on the Pathologies of Schizophrenia and Bipolar

Disorder: Potential for Improved Therapeutic Strategies

Executive Editor: B. Dean

 

Schizophrenia and Bipolar Affective Disorder: Perspectives for the Development of Therapeutics Pp.393-407

S. Sundram , P.R. Joyce  and M.A. Kennedy

[Abstract]

 

From Pharmacotherapy to Pathophysiology: Emerging Mechanisms of Apolipoprotein D in Psychiatric Disorders Pp.408-418

E.A. Thomas , D.L. Copolov and J.G. Sutcliffe

[Abstract]

 

Muscarinic Receptors in Schizophrenia Pp.419-426

B. Dean , F.P. Bymaster  and E. Scarr

[Abstract]

 

Cellular Pathology in the Dorsolateral Prefrontal Cortex Distinguishes Schizophrenia from Bipolar Disorder Pp.427-436

L.D. Selemon  and G. Rajkowska

[Abstract]

 

The Use of Microarrays to Characterize Neuropsychiatric Disorders: Postmortem Studies of Substance Abuse and Schizophrenia Pp.437-446

E. Lehrmann , T.M. Hyde , M.P. Vawter , K.G. Becker , J.E. Kleinman  and W.J. Freed

[Abstract]

 

Proteomics in the Discovery of New Therapeutic Targets for Psychiatric Disease Pp.447-458

Hans Voshol , Marc J. Glucksman  and Jan van Oostrum

[Abstract]

 

Neurodevelopmental Animal Models of Schizophrenia: Effects on Prepulse Inhibition Pp.459-471

M. Van den Buuse , B. Garner  and M. Koch

[Abstract]

 

Neurodevelopment and Mood Stabilizers Pp.472-482

A.J. Harwood

[Abstract]

 

Abstracts

 

[Back to top] Schizophrenia and Bipolar Affective Disorder: Perspectives for the Development of Therapeutics

S. Sundram , P.R. Joyce  and M.A. Kennedy

 

Schizophrenia and bipolar disorder remain two of the most severe and difficult to treat psychotic disorders hampered by our poor understanding of their pathologies. The development of typical antipsychotic drugs opened an avenue of investigation through the dopamine D2 receptor in schizophrenia. With the reintroduction of the atypical antipsychotic clozapine came the development of a new generation of atypical agents and hypotheses challenging the centrality of this receptor in explaining antipsychotic effects. Evaluation of these competing theories does not provide sufficient evidence to displace the importance of the dopamine D2 receptor in antipsychotic efficacy, but does raise limitations of it as an explanatory hypothesis. Further, the treatment of other symptom domains in schizophrenia remains relatively neglected and open for the development of novel therapies. Similar to schizophrenia, bipolar disorder presents a diversity of clinical states but unlike schizophrenia, its mainstay of treatment, lithium, has not had a clear receptor target impeding understanding of the disorder's pathology and treatment. This has pushed investigation into other domains emphasising a number of intracellular signalling pathways and glial-neuronal interactions. The heavy genetic loading of bipolar disorder has allowed linkage analyses to identify a number of putative regions, however, the diversity of phenotypes complicates such studies. Polymorphisms of candidate genes have yielded potential leads such as dopamine beta hydroxylase in mood disorder and the serotonin transporter for treatment response. It is anticipated that combining the above approaches may hold promise for the development of more effective treatments.

 

[Back to top] From Pharmacotherapy to Pathophysiology: Emerging Mechanisms of Apolipoprotein D in Psychiatric Disorders

E.A. Thomas , D.L. Copolov and J.G. Sutcliffe

 

Apolipoprotein D (apoD) is an atypical plasma apolipoprotein and, based on its primary structure, it is a member of the lipocalin protein superfamily. Lipocalins have been extensively used as disease markers and, accordingly, apoD has become increasingly recognized as an important factor in the pathology of human neurodegenerative and neuropsychiatric disorders. ApoD expression is increased in the plasma and brains of subjects with schizophrenia and bipolar disorder, suggesting that it acts as a marker for disease pathology. ApoD also exhibits complex regulation by antipsychotic drug treatment and may represent a distinguishing mechanism of typical versus atypical drugs. The precise role of apoD in the CNS and disease remains to be elucidated, but recent findings have suggested that it plays an important role in the regulation of arachidonic acid signaling and metabolism providing further support for phospholipid membrane pathology in schizophrenia.

 

[Back to top] Muscarinic Receptors in Schizophrenia

B. Dean , F.P. Bymaster  and E. Scarr

 

An increasing body of evidence suggests that the muscarinic receptors may present a potential therapeutic target for the treatment of schizophrenia. This argument is supported by studies using postmortem CNS tissue and a neuroimaging study that have shown there are regionally specific decreases in selective muscarinic receptors in the CNS of subjects with schizophrenia. This raises the possibility that drugs specific to individual muscarinic receptors could have beneficial effects on the symptoms of schizophrenia, a posit supported by studies in receptor knockout/knockdown mice where it has been shown that specific behaviours affected by schizophrenia are also abnormal in mice lacking a single muscarinic receptor. Moreover, drugs have been synthesised that are partial agonists at muscarinic receptors and these drugs have been shown to improve the behavioural deficits in humans which are modulated by the muscarinic receptor family. The widespread distribution of muscarinic receptors in the human CNS and the receptor specific changes identified in postmortem CNS from subjects with schizophrenia would suggest that drugs targeting specific muscarinic receptors would also need to partition into selected CNS regions to achieve optimal responses. Some existing compounds show regional selectivity for the same muscarinic receptor in different CNS regions, suggesting that this characteristic could be engineered into muscarinic receptor targeting drugs. This review presents data from diverse areas of research to argue that it is now imperative that the therapeutic potential of manipulating the activity of muscarinic receptors for the treatment of schizophrenia is fully explored.

 

[Back to top] Cellular Pathology in the Dorsolateral Prefrontal Cortex Distinguishes Schizophrenia from Bipolar Disorder

L.D. Selemon  and G. Rajkowska

 

The classification of schizophrenia and bipolar disorder as two separate disease entities has been hotly debated almost from the moment of its inception with Kraepelin’s descriptions of “dementia praecox” and “manic-depressive insanity” in 1896. Kraepelin’s nosologic distinction was based on clinical observation of symptomatology and outcome, and even today, despite major advances in science and technology, differential diagnosis of psychosis relies on the clinical course of illness. However, new evidence from diverse fields, e.g., genetics, neuropsychology, and brain imaging, have refueled the debate about whether or not schizophrenia and bipolar disorder represent distinct diseases, leading some to postulate that schizophrenia and bipolar disorder represent different manifestations of psychosis along a continuum with schizoaffective disorder representing an intermediate subtype. To this discourse, we add our own recent postmortem anatomic findings indicating that cellular pathology in the dorsolateral prefrontal cortex in schizophrenia and bipolar disorder differs not just in magnitude but also in direction, in laminar scope, and in relative involvement of neuronal and glial cell types. Thus, distinct morphometric alterations in the dorsolateral prefrontal cortex underlie what appear on neuroimaging analysis to be similar abnormalities in structural and metabolic function in the prefrontal cortex, and the diverse cellular pathology in the dorsolateral prefrontal cortex in these two disorders may account for the greater deficit in schizophrenia on cognitive tasks involving memory, problem solving and abstraction.

 

[Back to top] The Use of Microarrays to Characterize Neuropsychiatric Disorders: Postmortem Studies of Substance Abuse and Schizophrenia

E. Lehrmann , T.M. Hyde , M.P. Vawter , K.G. Becker , J.E. Kleinman  and W.J. Freed

 

Neuropsychiatric disorders are generally diagnosed based on a classification of behavioral and, in some cases, specific neurological deficits. The lack of distinct quantitative and qualitative biological descriptors at the anatomical and cellular level complicates the search for and understanding of the neurobiology of these disorders. The advent of microarray technology has enabled large-scale profiling of transcriptional activity, allowing a comprehensive characterization of transcriptional patterns relating to the pathophysiology of neuropsychiatric disorders. We review some of the unique methodological constraints related to the use of human postmortem brain tissue in addition to the generally applicable requirements for microarray experiments. Microarray studies undertaken in neuropsychiatric disorders such as schizophrenia and substance abuse by the use of postmortem brain tissue indicate that transcriptional changes relating to synaptic function and plasticity, cytoskeletal function, energy metabolism, oligodendrocytes, and distinct intracellular signaling pathways are generally present. These have been supported by microarray studies in experimental models, and have produced multiple avenues to be explored at the functional level. The quality and specificity of information obtained from human postmortem tissue is rapidly increasing with the maturation and refinement of array-related methodologies and analysis tools, and with the use of focused cell populations. The development of experimental models of gene regulation in these disorders will serve as the initial step towards a comprehensive genome-linked analysis of the brain and associated disorders, and help characterize the integration and coordinate regulation of complex functions within the CNS.

 

[Back to top] Proteomics in the Discovery of New Therapeutic Targets for Psychiatric Disease

Hans Voshol , Marc J. Glucksman  and Jan van Oostrum

 

In terms of impact on and cost to society psychiatric disorders are among the most important health problems of today. Current estimates from the US suggest that the collective cost of psychiatric diseases could amount to one-third of the total health care budget with a cumulative lifetime prevalence of 30%. While undoubtedly improvements have been made in the diagnosis and treatment of at least the symptoms of mental illness, there has been frustratingly little progress in elucidating the molecular mechanisms. However, a fundamentally different approach to study molecular mechanisms of psychiatric diseases is emerging as a result of technological advances in expression profiling methods. This comprises the investigation of the expressed disease ‘phenotypes’, developing from the differential gene and protein expression in the central nervous system as a result of the complex interaction between genetic predisposition and environmental modulation. This paper will focus on proteomics, expression profiling at the protein level, reviewing some of the available tools and their application in the molecular analysis of psychiatric disease.

 

[Back to top] Neurodevelopmental Animal Models of Schizophrenia: Effects on Prepulse Inhibition

M. Van den Buuse , B. Garner  and M. Koch

 

Epidemiological studies have shown increased incidence of schizophrenia in patients subjected to different forms of pre- or perinatal stress. However, as the onset of schizophrenic illness does not usually occur until adolescence or early adulthood, it is not yet fully understood how disruption of early brain development may ultimately lead to malfunction years later. In order to elucidate a possible role for neurodevelopmental factors in the pathogenesis of schizophrenia and to highlight potential new treatments, animal models are needed. Prepulse inhibition (PPI) is a model of sensorimotor gating mechanisms in the brain. It is disrupted in schizophrenia patients and the disruption can be reversed with atypical antipsychotics. It has been widely used in animal studies to explore central mechanisms possibly involved in schizophrenia. There has been a recent surge of behavioural and neurochemical animal studies on neurodevelopmental models, particularly on the effects of postweaning isolation, maternal separation and neonatal lesions of the hippocampus. In these models, long lasting alterations in behaviour and/or molecular changes in specific brain regions are observed, comparable to those seen in schizophrenia. The aim of this article is to critically review the available literature on such neurodevelopmental animal models with special focus on the effects on PPI and brain regions that are putatively involved in regulation of PPI.

 

[Back to top] Neurodevelopment and Mood Stabilizers

A.J. Harwood

 

Mood disorders and schizophrenia share a number of common properties, including: genetic susceptibility; differences in brain structure and drug based therapy. Some genetic loci may even confer susceptibility for bipolar mood disorder and schizophrenia, and some atypical antipsychotic drugs are used as mood stabilizers. As schizophrenia is associated with aberrant neurodevelopment, could this also be true for mood disorders? Such changes could arise pre- or post-natal, however the recent interest in neurogenesis in the adult brain has suggested involvement of these later processes in the origins of mood disorders. Interestingly, the common mood stabilizing drugs, lithium, valproic acid (VPA) and carbamazepine, are teratogens, affecting a number of aspects of animal development. Recent work has shown that lithium and VPA interfere with normal cell development, and all three drugs affect neuronal morphology. The molecular basis for mood stabilizer action in the treatment of mood is unknown, however these studies have suggested both targets and potential mechanisms.

 

Lithium directly inhibits two evolutionarily conserved signal transduction pathways: the protein kinase Glycogen Synthase Kinase-3 (GSK-3) and inositol signaling. VPA can up-regulate gene expression through inhibition of histone deacetylase (HDAC) and indirectly reduce GSK-3 activity. VPA effects are not conserved between cell types, and carbamazepine has no effect on the GSK-3 pathway. All three mood stabilizers suppress inositol signaling, results further supported by studies on the enzyme prolyl oligopeptidase (PO) and the sodium myo-inositol transporter (SMIT). Despite these intriguing observations, it remains unclear whether GSK-3, inositol signaling or both underlie the origins of bipolar disorder.