ITI-002 is a unique, orally available, investigational drug being developed for the treatment of motor and non-motor impairments accompanying Parkinson's disease and other neurologic and neuropsychiatric disorders, including schizophrenia and Alzheimer's disease.
ITI-002 potently inhibits the PDE1 enzyme in a competitive manner with sub-nanomolar affinity for this subfamily. This compound is very selective for the PDE1 subfamily relative to other PDE subfamilies. ITI-002 has no significant off target activities at other enzymes, receptor or ion channels.
PDE Type I – PDE enzymes hydrolyze and inactivate cyclic nucleotides (cAMP and cGMP) in the brain. Eleven classes of PDE enzymes with distinct tissue distributions, cyclic nucleotide selectivity, and regulatory factors are known. The PDE1 family of enzymes, including PDE1A, PDE1B, and PDE1C isoforms, are calcium/calmodulin-dependent, dual-function (cAMP/cGMP) PDEs that are expressed at high levels in mammalian brain. This enzyme subfamily has little influence on basal nucleotide activity and only becomes active under stimulated conditions. This "on demand" character distinguishes PDE1 from all other PDE family members. PDE1 is enriched in the striatal medium spiny neurons that lose dopamine input in Parkinson's disease and controls the responsiveness of striatal neurons to dopamine. Intra-Cellular Therapies has shown that orally available, small molecule inhibitors of PDE1 restore dopamine signaling in striatal neurons and potentiate the level of motor correction in Parkinson's disease.
About Parkinson's Disease - Parkinson's disease is a progressive, neurodegenerative disease. The prevalence of Parkinson's disease increases with a
|SOURCE Intra-Cellular Therapies, Inc.|
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