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Idalopirdine is an orally available small molecule drug that acts as a selective antagonist of the serotonin 6 (5-HT6) receptor, which is primarily expressed in the brain regions involved in cognition such as the cerebral cortex and hippocampus. By blocking this receptor, idalopirdine is thought to enhance cholinergic, glutamatergic, noradrenergic, and dopaminergic neurotransmission. It was developed mainly as an adjunctive therapy to acetylcholinesterase inhibitors for symptomatic treatment of cognitive impairment in Alzheimer's disease and has also been studied for schizophrenia. The drug was originally discovered by Eli Lilly and later developed by Lundbeck (after acquiring Saegis), with Otsuka Pharmaceutical also involved in development. Despite reaching phase III clinical trials for Alzheimer's disease and being investigated for cognitive impairment associated with schizophrenia, its development has been discontinued for these indications[1][2][3][4][5].
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