Intra-Cellular’s schizophrenia drugs found effective in preclinical trials

In vitro, ITI-007 was shown to be a potent, sub-nanomolar, antagonist at 5HT2A receptors with a 60-fold higher affinity for 5HT2A receptors over D2 receptors. In vivo, ITI-007 produced an intracellular protein phosphorylation pattern consistent with the activity of a partial agonist at pre-synaptic D2 receptors. This pre-synaptic partial agonist activity preserves normal dopamine metabolism rather than causing a dramatic increase as seen with other antipsychotic therapies.

ITI-002 was shown to be an orally active and a potent inhibitor of a novel intracellular target and was designed to amplify but not supplant ongoing activity of D1 receptive neurons, primarily in the prefrontal cortex. In behavioral studies, ITI-002 displayed acute and chronic activity as a cognitive enhancing agent in rodent models. ITI-002 has been shown to be safe in all preliminary evaluations and is advancing to preclinical development.