NS5806, widely used as a Kv4-selective activator, also activates TREK-1 and TREK-2 potassium channels.
This publication was recognised as the 'Most Impactful Safety Pharmacology Publication of the Year' by the Safety Pharmacology Society in 2024.
Brennan, R.J., Jenkinson, S., Brown, A. et al. The state of the art in secondary pharmacology and its impact on the safety of new medicines. Nat Rev Drug Discov 23, 525–545 (2024). https://doi.org/10.1038/s41573-024-00942-3.
PubMed: The state of the art in secondary pharmacology and its impact on the safety of new medicines.
NS5806, widely used as a Kv4-selective activator, also activates TREK-1 and TREK-2 potassium channels.
Nature Communications paper ‘The nucleobase guanine at the 3′-terminus of oligonucleotide RGLS4326 drives off-target AMPAR inhibition and CNS toxicity'