Alomone Labs is pleased to offer the K+ Channel Antibodies for Pain Research Explorer Kit (#AK-390). This Explorer Kit includes K+ channel antibodies for pain research with their respective peptide control antigen. An ideal tool for screening purposes.
Four families of potassium channels with different structures, functional characteristics and pharmacological sensitivity, are distinguished in neurons: voltage-gated (KV), calcium-activated (KCa), inward rectifier (Kir) and two-pore (K2P) K+ channels. Studies have demonstrated that the opening of some of these K+ channels plays an important role in the antinociception induced by agonists of many G-protein-coupled receptors as well as by other antinociceptive drugs and natural products.
Agonists of µ- and δ-opioid receptors open inward rectifier K+ channels in neurons through the activation of Gi/o proteins indicating that potassium currents are involved in opioid induced anti-nociception. These currents are involved in both supraspinal and spinal pain relief. In addition, potassium currents are involved in local anti-nociception mediated by peripheral μ-opioid receptors. Local administration of potassium channel antagonists in animal models antagonizes the effect of morphine further ascertaining the involvement of potassium channels in anti-nociception.
NSAID’s anti-nociceptive effect is also partly mediated by potassium currents in the primary afferent nerve endings. Blockers of KATP channels such as sulfonylurea negate pain relief caused by ketorolac and diclofenac while KATP channel openers pinacidil and diazoxide also produce dose-dependent antinociception, blocked by sulfonylureas. Opening of the KV and KCa channels does not seem to be involved in NSAID’s antinociception in most cases.
Interestingly, Cannabinoid receptors are currently not known to be involved in potassium mediated anti-nociception. Anti-nociception induced by cannabinoid receptor agonists is not antagonized by K+ channel blockers such as glibenclamide or charybdotoxin suggesting that KATP and KV channels do not play a role in the supraspinal and spinal antinociception mediated by cannabinoid receptors1.
- Ocana, M. et al. (2004) Eur. J. Pharmacol. 500, 203.