Member"The antispasmodic effect of aryl-substituted α- pyrones from the kava-root have previously been reported, although it was not known that these effects were due to the property of potassium channel activation. It has now been confirmed that kawain is indeed a potassium channel activating substance. All of the kava pyrones have a bulky aromatic group. It has unexpectedly been found that the substitution of a lower alkyl group for the more bulky aromatic group enhances the potassium channel activation effects of the compounds."
"While the kava pyrones were known to have anti¬ convulsant and anti-spasmodic properties, it was not known that they had potassium channel activation effects, and therefore it would not have been obvious from their known anti-convulsive and anti-spasmodic effect that they could also be used for the treatment of hypertension or the treatment of addiction withdrawal symptoms, or any of the other effects of potassium channel activation which do not involve the anti-convulsant or anti-spasmodic effects of the compounds."
"Kava's action as a voltage-dependent ion channel modulator may be a more important part of its pharmacology than action at any GABA allosteric site. I think the similarity of effect to the benzodiazepines may have lead people to jump to conclusions about its mode of action. In effect, kava acts as a combined sodium and calcium channel blocker, as well as a potentiator of potassium channels."
Potassium channel activating compounds and methods of use thereof
http://www.google.com/patents/WO1993008800A1?cl=en
3-substituted oxindole derivatives as potassium channel modulators
https://www.google.com/patents/US5565483
Diphenyl triazoles as potassium channel modulators
http://www.google.co.ug/patents/US6077861
"While the kava pyrones were known to have anti¬ convulsant and anti-spasmodic properties, it was not known that they had potassium channel activation effects, and therefore it would not have been obvious from their known anti-convulsive and anti-spasmodic effect that they could also be used for the treatment of hypertension or the treatment of addiction withdrawal symptoms, or any of the other effects of potassium channel activation which do not involve the anti-convulsant or anti-spasmodic effects of the compounds."
"Kava's action as a voltage-dependent ion channel modulator may be a more important part of its pharmacology than action at any GABA allosteric site. I think the similarity of effect to the benzodiazepines may have lead people to jump to conclusions about its mode of action. In effect, kava acts as a combined sodium and calcium channel blocker, as well as a potentiator of potassium channels."
Potassium channel activating compounds and methods of use thereof
http://www.google.com/patents/WO1993008800A1?cl=en
3-substituted oxindole derivatives as potassium channel modulators
https://www.google.com/patents/US5565483
Diphenyl triazoles as potassium channel modulators
http://www.google.co.ug/patents/US6077861
Potassium Channels and Neurodegenerative Diseases
"The classes of drugs that need to be explored include potassium channel openers of the ATP-sensitive, high-conductance calcium-sensitive, and inward rectifier or leakage types. Selective openers for inward rectifier potassium channels are currently not available, although activation of 5-HT1A receptors results in the induction of an inwardly rectifying potassium current. Potent neuroprotective properties have been described for different 5-HT1A agonists in models of focal and global ischemia. Retigabine, a leakage-current potassium channel opener, has been shown to have neuroprotective effects in animal models of neurodegeneration. Of the currently available potassium channel openers, retigabine and BAY-X-3702 are active at nontoxic doses. Further research is needed to develop selective, well-tolerated potassium channel openers."
"The classes of drugs that need to be explored include potassium channel openers of the ATP-sensitive, high-conductance calcium-sensitive, and inward rectifier or leakage types. Selective openers for inward rectifier potassium channels are currently not available, although activation of 5-HT1A receptors results in the induction of an inwardly rectifying potassium current. Potent neuroprotective properties have been described for different 5-HT1A agonists in models of focal and global ischemia. Retigabine, a leakage-current potassium channel opener, has been shown to have neuroprotective effects in animal models of neurodegeneration. Of the currently available potassium channel openers, retigabine and BAY-X-3702 are active at nontoxic doses. Further research is needed to develop selective, well-tolerated potassium channel openers."
Very useful resource:
Tuning the Brain: Principles and Practice of Neurosomatic Medicine
