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for educational and safety purposes
Idalopirdine and Intepirdine both come up in the same conversations; they overlap on Serotonin and Acetylcholine. Idalopirdine: Idalopirdine is a potent, selective serotonin 5-HT6 receptor antagonist developed by H. Intepirdine: Intepirdine is a selective serotonin 5-HT6 receptor antagonist originally discovered at GlaxoSmithKline as SB-742457 and later licensed to Axovant Sciences as RVT-101 for Alzheimer's disease and dementia with Lewy bodies.
Idalopirdine is a potent, selective serotonin 5-HT6 receptor antagonist developed by H. Lundbeck (as Lu AE58054) as an adjunctive symptomatic treatment for Alzheimer's disease. By blocking 5-HT6 receptors, which are expressed almost exclusively in the central nervous system and concentrated in the hippocampus and cortex, it disinhibits cholinergic, glutamatergic and monoaminergic transmission relevant to memory. A phase 2 trial (LADDER) in donepezil-treated moderate Alzheimer's disease showed a significant cognitive benefit, but the larger phase 3 STARSHINE, STARBEAM and STARBRIGHT programme failed to replicate it. Idalopirdine is discontinued for cognition and is now referenced primarily as a pharmacological tool and cautionary case study.
Intepirdine is a selective serotonin 5-HT6 receptor antagonist originally discovered at GlaxoSmithKline as SB-742457 and later licensed to Axovant Sciences as RVT-101 for Alzheimer's disease and dementia with Lewy bodies. Like other compounds in its class it was intended to enhance cognition by disinhibiting cholinergic and glutamatergic signaling in cortex and hippocampus. A phase 2 study suggested a modest global and cognitive benefit, but the pivotal phase 3 MINDSET trial in mild-to-moderate Alzheimer's disease was clearly negative. Its high-profile failure in 2017 effectively ended enthusiasm for 5-HT6 antagonism as a standalone dementia strategy.
both fingerprints on one instrument; where the marks line up the two compounds work the same lever, where a slot goes dark only one of them touches it. read straight from each entry's affinity table; nothing here is invented.
Selective competitive antagonism / inverse agonism
Selective competitive antagonism
Secondary enhancement of acetylcholine release
Secondary acetylcholine enhancement
Reduces 5-HT6 mediated GABA release
Reduces food intake in preclinical obesity models
Reduces 5-HT6 mediated inhibition
strengths are the entries' qualitative ratings (strong / moderate / weak); Ki and EC50 figures appear where an entry records them.