(R)-tacrine(10)-hupyridone

(R)-tacrine(10)-hupyridone is an experimental small molecule designed as a multitarget-directed ligand for neurodegenerative diseases. It is a dimeric hybrid of tacrine and a huperzine A fragment. The compound acts primarily as a dual-binding acetylcholinesterase inhibitor with higher potency than either parent compound. In preclinical studies it has demonstrated the ability to inhibit acetylcholinesterase activity in the brain and cross the blood-brain barrier. Additionally, it activates brain-derived neurotrophic factor (BDNF) signaling via TrkB/Akt pathways and disrupts β‑amyloid aggregation and deposition. These combined actions result in improved cognitive performance in animal models of Alzheimer’s disease and post-operative cognitive dysfunction without significant hepatotoxicity at high concentrations[3][5][7]. The drug also alleviates neuroinflammation and enhances cholinergic neurotransmission.

Other names

(5R)-5-((10-((1,2,3,4-tetrahydroacridin-9-yl)amino)decyl)amino)-1,2,5,6,7,8-hexahydroquinolin-2-one(5R)-5-{[10-(1,2,3,4-TETRAHYDROACRIDIN-9-YLAMINO)DECYL]AMINO}-5,6,7,8-TETRAHYDROQUINOLIN-2(1H)-ONE