Cholecystokinin octapeptide reverses mu-opioid-receptor-mediated inhibition of calcium current in rat dorsal root ganglion neurons

J Pharmacol Exp Ther. 1995 Dec;275(3):1293-9.

Abstract

Cholecystokinin octapeptide (CCK-8) is reported to antagonize the analgesic effect produced by mu- and kappa- but not delta-opioid agonist in spinal cord. However, the mechanisms of interaction remain obscure. In the present study, whole-cell patch-clamp recording was performed on acutely isolated rat dorsal root ganglion (DRG) neurons to evaluate the effects of the highly specific mu-opioid agonist ohmefentanyl and the delta-opioid agonist DPDPE on voltage-gated calcium channels and the possible interaction between CCK-8 receptor and mu- or delta-opioid receptor. The results indicated that ohmefentanyl, but not DPDPE, can suppress the voltage-gated calcium currents elicited in DRG neurons, an effect readily reversed by naloxone or by the antiopioid peptide CCK-8. The effect of CCK-8 can in turn be abolished by the CCK-B receptor antagonist L365,260. CCK-8 used by itself has no enhancing effect, but rather a depressant effect, on calcium currents. However, used simultaneously with ohmefentanyl, CCK-8 shows a clear-cut reversal of depression of the mu-opioid. We conclude that the depressant effect produced by mu-opioid on voltage-gated calcium current in DRG neurons can be antagonized by CCK-8 through CCK-B receptor located in the same neuron. The delta-opioid DPDPE has no direct effect on the voltage-gated calcium current in DRG neurons.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Enkephalin, D-Penicillamine (2,5)-
  • Enkephalins / pharmacology
  • Fentanyl / analogs & derivatives
  • Fentanyl / pharmacology
  • Ganglia, Spinal / cytology
  • Ganglia, Spinal / drug effects*
  • Ganglia, Spinal / metabolism
  • Ion Channel Gating
  • Male
  • Neurons / drug effects*
  • Neurons / metabolism
  • Rats
  • Rats, Wistar
  • Receptors, Opioid, delta / agonists
  • Receptors, Opioid, mu / antagonists & inhibitors*
  • Receptors, Opioid, mu / physiology
  • Sincalide / pharmacology*

Substances

  • Calcium Channel Blockers
  • Enkephalins
  • Receptors, Opioid, delta
  • Receptors, Opioid, mu
  • F 7302
  • Enkephalin, D-Penicillamine (2,5)-
  • Sincalide
  • Fentanyl