Pharmacological evidence for the activation of K(+) channels by diclofenac

Eur J Pharmacol. 2002 Mar 1;438(1-2):85-91. doi: 10.1016/s0014-2999(02)01288-8.

Abstract

The involvement of K(+) channels in the antinociceptive action of diclofenac was assessed in the formalin test. Local administration of diclofenac produced a dose-dependent antinociceptive effect due to a local action because drug administration in the contralateral paw was ineffective. Pretreatment of the injured paw with glibenclamide and tolbutamide (ATP-sensitive K(+) channel inhibitors), charybdotoxin and apamin (large- and small-conductance Ca(2+)-activated K(+) channel blockers, respectively), 4-aminopyridine or tetraethylammonium (voltage-dependent K(+) channel inhibitors) prevented diclofenac-induced antinociception. Given alone, K(+) channel inhibitors did not modify formalin-induced nociceptive behavior. Pinacidil (an ATP-sensitive K(+) channel opener) also produced antinociception which was blocked by glibenclamide. The peripheral antinociceptive effect of morphine (positive control) was blocked by glibenclamide and 4-aminopyridine but not by charybdotoxin or apamin. The results suggest that the peripheral antinociceptive effect of diclofenac may result from the activation of several types of K(+) channels, which may cause hyperpolarization of peripheral terminals of primary afferents.

MeSH terms

  • 4-Aminopyridine / pharmacology
  • Analgesics / pharmacology
  • Analgesics, Opioid / pharmacology
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Apamin / pharmacology
  • Behavior, Animal / drug effects
  • Charybdotoxin / pharmacology
  • Diclofenac / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • Formaldehyde / administration & dosage
  • Glyburide / pharmacology
  • Hindlimb / drug effects
  • Hindlimb / physiopathology
  • Morphine / pharmacology
  • Pain / etiology
  • Pain / prevention & control
  • Pinacidil / pharmacology
  • Potassium Channel Blockers / pharmacology
  • Potassium Channels / drug effects*
  • Potassium Channels / physiology
  • Rats
  • Rats, Wistar
  • Tetraethylammonium / pharmacology
  • Tolbutamide / pharmacology

Substances

  • Analgesics
  • Analgesics, Opioid
  • Anti-Inflammatory Agents, Non-Steroidal
  • Potassium Channel Blockers
  • Potassium Channels
  • Charybdotoxin
  • Diclofenac
  • Formaldehyde
  • Apamin
  • Tetraethylammonium
  • Morphine
  • Pinacidil
  • Tolbutamide
  • 4-Aminopyridine
  • Glyburide