Small conductance calcium-activated potassium (SK, KCa2) channels represent interesting and challenging targets in medicinal chemistry. So far, the reference ligand is apamin, a peptide including the [125I] analog for binding studies. Nonpeptidic ligands with high affinity have been developed for several years. Currently, different questions remain to be solved since no selective and brain-penetrating agent is available. In addition, replacing [125I]apamin in binding experiments would be also interesting.

Researchers at CIRM have developed different series of compounds exhibiting significant affinity for SK channels.

These new compounds may act as SK channels blockers or may interact selectively with one of the three subtypes (i.e. SK1, SK2, SK3) offering a novel approach to the treatment of CNS diseases (i.e. Alzheimer’s disease, Parkinson’s disease, neurodegenerative disorders, psychotic disorders, cognitive dysfunction, alcohol and drug addiction, depression…).

Interested in these projects? Drop us an email []. We are looking forward collaborating with you!