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Intra-Cellular Therapies Presents Preclinical Data From Schizophrenia and Sleep Maintenance Programs
Date:12/19/2007

nlike some atypical antipsychotics, ITI- 007 does not exhibit significant potency for a variety of other targets that have been implicated in a range of dose-limiting side effects of antipsychotic drugs. ITI-007 does not interact with muscarinic or histaminergic receptors and has a reduced affinity for adrenergic receptors relative to other antipsychotic drugs and relative to its potency at 5HT2A receptors.

About ITI-007

ITI-007 is an orally available compound that combines potent 5HT2A receptor antagonism with cell-type-specific modulation of phosphoprotein pathways downstream of dopamine receptors. As a dopamine receptor protein phosphorylation 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 by simple dose adjustments using a single drug. 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 and the treatment of bipolar disorders.

ITI-007 has a much lower propensity than several currently marketed antipsychotic drugs to interact with receptors that mediate deleterious cardiovascular events, sedation, and rapid and significant weight gain.

About Schizophrenia

Schizophrenia is a major neuropsychiatric disorder that affects over 1% of the world population with an illness that begins in late adolesc
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SOURCE Intra-Cellular Therapies, Inc.
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