AChE-IN-14

AChE-IN-14 is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease[1].

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

AChE-IN-14 (compound 5) has a good affinity to human H3 receptor with a Ki value of 159.8 nM in HEK293 cells[1]. AChE-IN-14 (compound 5) has a high orally activity and cannot cross the blood-brain barrier[1]. AChE-IN-14 (compound 5) (10 μM, 5 min) inhibits hAChE with an IC50 value of 0.48 μM and represents the non-competitive type of eeAChE (Ki = 176 nM) and eqBuChE (Ki = 281 nM) inhibition[1].

[1]. Marek Bajda, et al. Search for new multi-target compounds against Alzheimer's disease among histamine H₃ receptor ligands. Eur J Med Chem. 2020 Jan 1;185:111785.