Drug Discovery Opinion

It has been estimated that as many as 50 million people worldwide suffer from schizophrenia and many of these will be treated with antipsychotic medicines. The so-called typical antipsychotics have been available since the mid-1950s and a number of newer agents, the atypical antipsychotics, have been introduced since 1990. Increased dopaminergic activity is thought to be a contributory factor in schizophrenia and all of the antipsychotic medicines interact with the dopamine D2 receptor although they have different affinities and modulate the receptor in different ways.

A new study has shown that, regardless of their effect on G-protein coupled signalling via the D2 receptor, antipsychotic drugs potently antagonize the dopamine-mediated interaction of the D2 receptor with β-arrestin-2.

Arrestins are proteins that were initially found to regulate signal transduction by silencing GPCRs, although they have recently been shown to directly activate signalling pathways. The new results suggest that selective targeting of the interaction of D2 with β-arrestin-2 may provide a new opportunity for the development of antipsychotic medicines. More generally, targeting β-arrestin signalling pathways may open opportunities in other therapeutic areas.

Bookmark It

Hide Sites

Related posts:

1. New Study Casts Light on Anti-Cancer Mechanism A new study describes a high affinity interaction between siramesine and phosphatidic acid, a component of cell membranes that also...
2. Study Casts New Light on Prozac Mechanism Selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine (Prozac®) have been used to treat depression for more than three decades...
3. Mechanism of PPAR-γ Activators in Tumour Suppression Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that play essential roles in the regulation of cellular differentiation, development and metabolism....
4. GlyT-1 Inhibitor Helps Negative Symptoms of Schizophrenia Last week, Roche reported data from a 320 patient phase II proof-of-concept study with its first-in-class investigational glycine transporter-1 (GlyT-1)...
5. New Approach to Treatment of Schizophrenia Schizophrenia is a complex disorder, generally believed to arise from dysregulation of dopamine and glutamate neurotransmission pathways. Current front-line treatment...

Related posts brought to you by Yet Another Related Posts Plugin.

 Email This Post

This entry was posted on Tuesday, September 16th, 2008 at 12:14 pm and is filed under News. You can follow any responses to this entry through the RSS 2.0 feed. You can leave a response, or trackback from your own site.