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Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS

By Bencheva Leda Ivanova; De Matteo Marilenia; Ferrante Luca; Ferrara Marco; Prandi Adolfo; Randazzo Pietro; Ronzoni Silvano; Sinisi Roberta; Seneci Pierfausto; Di Fabio Romano; et al
From ACS medicinal chemistry letters (2019), 10(4), 627-632, Language: English, Database: MEDLINE

Acid-sensing ion channels (ASICs) are a family of ion channels permeable to cations and largely responsible for the onset of acid-evoked ion currents both in neurons and in different types of cancer cells, thus representing a potential target for drug discovery. Owing to the limited attention ASIC2 has received so far, an exploratory program was initiated to identify ASIC2 inhibitors using diminazene, a known pan-ASIC inhibitor, as a chemical starting point for structural elaboration. The performed exploration enabled the identification of a novel series of ASIC2 inhibitors. In particular, compound 2u is a brain penetrant ASIC2 inhibitor endowed with an optimal pharmacokinetic profile. This compound may represent a useful tool to validate in animal models in vivo the role of ASIC2 in different neurodegenerative central nervous system pathologies.

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