K_ATP channel openers in the trigeminovascular system

Abstract

K(ATP) channel openers do not interact with CGRP release or mast cell degranulation. Activation of these channels in the CNS is antinociceptive and therefore cannot explain the headache induced by K(ATP) channel openers. Thus, they are likely to induce headache by interaction with extracerebral K(ATP) channels, probably the SUR2B isoforms.

Neurologic and neuroimaging manifestations of Cantú syndrome

“…Prior pharmacologic studies using synthetic KATP channel openers include headache as an adverse side effect in clinical studies consistent with KATP channel opening being involved in migraine. 16 Again, underlying etiologies are unclear, but this does suggest that antagonists of the Kir6.1 and SUR2B subunits may be potential pharmacologic targets for migraine treatment. 17 Additionally, given the vascular anomalies and white matter changes observed in Cantú syndrome it may be prudent to obtain neuroimaging, particularly vascular imaging, in patients with Cantú syndrome who have migraines.…”

Levcromakalim, an Adenosine Triphosphate‐Sensitive Potassium Channel Opener, Dilates Extracerebral but not Cerebral Arteries

“…1 K ATP channels are expressed in the cranial arteries, trigeminal ganglion (TG) and trigeminal nucleus caudalis, [2][3][4][5][6][7] and several migraine triggering molecules activate and open K ATP channels. 1 K ATP channels are expressed in the cranial arteries, trigeminal ganglion (TG) and trigeminal nucleus caudalis, [2][3][4][5][6][7] and several migraine triggering molecules activate and open K ATP channels.…”

“…There has been a growing interest to redefine the role of adenosine 5′-triphosphate-sensitive potassium (K ATP ) channels in headache and migraine. 1 K ATP channels are expressed in the cranial arteries, trigeminal ganglion (TG) and trigeminal nucleus caudalis, [2][3][4][5][6][7] and several migraine triggering molecules activate and open K ATP channels. [8][9][10][11][12] In humans, intravenous infusion of synthetic K ATP channel openers, levcromakalim, and pinacidil, were associated with development of headache.…”

The KATP channel in migraine pathophysiology: a novel therapeutic target for migraine

“…Kir6.1, Kir6.2, SUR1 and SUR2 are expressed in the trigeminal ganglion and trigeminal nucleus caudalis [ 22 ] (Table 1 ). In trigeminal neurons Kir 6.1 and Kir 6.2 immunoreactivity were expressed in cells with all soma sizes in all three divisions of the trigeminal ganglion [ 23 ].…”