Uses
XE-991 has been used as a KCNQ (Kv7.2/7.3) inhibitor to examine whether M-current inhibition affects oxytocin receptor (TGOT) mediated depolarization. It has also been used as an KCNQ inhibitor to study the ionic mechanism responsible for the overshoot/undershoot in membrane potential in mouse cholinergic interneurons (ChIs) in the presence of tetrodotoxin (TTX).
Biological Activity
Potent and selective blocker of KCNQ voltage-gated potassium channels. Blocks KCNQ2+3/M-currents (IC 50 = 0.6-0.98 μ M) and KCNQ1 homomeric channels (IC 50 = 0.75 μ M) but is less potent against KCNQ1/minK channels (IC 50 = 11.1 μ M). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo .
Biochem/physiol Actions
XE-991 is a KCNQ channel blocker; which is more potent than linopiridine (Cat. No. L-134).
storage
Room temperature (desiccate)