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Intra-Cellular Therapies Announces the Discovery of Potent Antidepressant Activity in ITI-007
Date:4/9/2008

phoprotein modulator (DPPM), ITI-007 has dual properties; it acts as a post-synaptic antagonist and as a pre-synaptic partial agonist. The combination of ITI-007's high-potency blockade of 5HT2A receptors and unique dopamine receptor activity will make it possible for the first time, to select a clinical dose capable of saturating 5HT2A receptors while permitting the "dialing in" of an optimal amount of dopamine receptor modulation. The ability to optimize the level of dopamine receptor modulation holds promise for the reduction of psychotic symptoms without incurring high levels of dopamine antagonism that cause motor disturbances and other deleterious side effects. In addition, the wide separation of affinity at 5HT2A and D2 receptors may allow for administration of the appropriate amount of dopamine modulation for antipsychotic maintenance therapy in the treatment of bipolar disorders. ITI-007 also has nanomolar affinity for the serotonin transporter (SERT). ITI-007 has a much lower propensity than several currently marketed antipsychotic drugs to bind receptors that mediate deleterious cardiovascular events, sedation and rapid and significant weight gain.

About ITI-722

A low-dose formulation of ITI-007, called ITI-722, is being developed simultaneously for the treatment of sleep maintenance insomnia in the general population. Due to the unique separation of D2 and 5HT2A receptor affinities, at low doses, ITI-722 acts primarily as a 5HT2A receptor antagonist. Additionally, its profile suggests the compound may be appropriate for the treatment of sleep disorders that accompany neurodegenerative disorders, such as Parkinson's disease.

About Depression

Depression is a common psychiatric disorder affecting approximately 20 million people in the United States. It is characterized by a pervasive low mood, loss of interest in usual activities and diminished ability to experience pleasure. Although the term "depression" is commonly used to des
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SOURCE Intra-Cellular Therapies, Inc.
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