The 'glibenclamide-shift' of centrally-acting antinociceptive agents in mice

Brain Res. 1995 Apr 24;677(2):277-82. doi: 10.1016/0006-8993(95)00164-l.

Abstract

Morphine-induced antinociception is antagonized by the K(+)-channel blocker glibenclamide (glyburide; Glib), implicating ATP-sensitive (KATP) K+ channels in the analgesic effect of opioids. The present study examined the generality of this conclusion by measuring the effect of Glib on supraspinal (intracerebroventricular; i.c.v.) antinociception produced by representative mu-opioids and the non-opioids pilocarpine and two alpha 2-adrenoceptor agonists (clonidine and tizanidine) using the mouse tail-flick test. Concurrent administration of Glib (40 micrograms, i.c.v.) produced a significant rightward shift of the dose-response curve of morphine, levorphanol, methadone, pilocarpine, clonidine and tizanidine; a modest, but not statistically significant, rightward shift of the dose-response curves of the mu-selective peptides DAMGO ([D-Ala2,N-Me-Phe4,Gly-ol5]-enkephalin) and PL017 ([N-Me-Phe3,D-Pro4]-morphiceptin); and no shift of the dose-response curves of alfentanil, carfentanil, fentanyl, sufentanil, or beta-endorphin. Glib produced a leftward shift of the dose-response curve of etorphine. These data support the involvement of KATP-type K+ channels in mediation of supraspinal antinociception, differentiate Glib-sensitive and Glib-insensitive opioid agonists, and reveal fundamental differences among antinociceptive agents in the extent of demonstrable utilization of this transduction pathway.

MeSH terms

  • Analgesics / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Glyburide / pharmacology*
  • Male
  • Methadone / pharmacology
  • Mice
  • Mice, Inbred ICR
  • Morphine / pharmacology
  • Potassium Channels / drug effects

Substances

  • Analgesics
  • Potassium Channels
  • Morphine
  • Glyburide
  • Methadone