By accurately defining the drug exposure levels that affect QRS duration, researchers can establish safety margins, prioritise lower-risk compounds, and reduce the chance of late-stage failures due to cardiac toxicity
A new paper co-authored by Eddy Stevens PhD, CSO and Tony Rush PhD, Director of Neuroscience, Metrion Biosciences reports that NS5806, widely used as a Kv4-selective activator, also activates TREK-1 and TREK-2 potassium ion channels. NS5806 was shown to hyperpolarize resting membrane potential in trigeminal neurons and activate heterologously expressed TREK-1 and TREK-2 (both highly expressed in sensory neurons). These findings should be considered when using NS5806 to study Kv4 channel physiology.
The paper is co-authored with Emma Veale and Alistair Mathie (Universities of Kent and Greenwich) and published in Pharmacology Research & Perspectives.¹
Veale et al., Pharmacol Res Perspect 14(3):e70264 (2026). https://doi.org/10.1002/prp2.70264
By accurately defining the drug exposure levels that affect QRS duration, researchers can establish safety margins, prioritise lower-risk compounds, and reduce the chance of late-stage failures due to cardiac toxicity
By accurately defining the drug exposure levels that affect QRS duration, researchers can establish safety margins, prioritise lower-risk compounds, and reduce the chance of late-stage failures due to cardiac toxicity