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PMID: 6313900 Published · ppublish English Journal Article Research Support, U.S. Gov't, Non-P.H.S. Research Support, U.S. Gov't, P.H.S.

Opioid peptides with differential affinity for mu and delta receptors decrease sensory neuron calcium-dependent action potentials.

The Journal of pharmacology and experimental therapeutics ·Vol. 227 ·No. 2 ·1983-11-00 ·Pages 394-402

Werz MA, Macdonald RL

Abstract

Previously, it has been reported that opioid peptides decrease the calcium component of action potentials in a dose-dependent and naloxone-reversible manner consistent with mediation by opiate receptors. To clarify the relation of mu and delta opiate receptors to decreases of somatic calcium-dependent action potential duration, we investigated the potency of two opioid peptides which have different affinities for mu and delta opiate receptors, Leu-enkephalin and morphiceptin. We predicted that Leu-enkephalin would be about 1000-fold more potent than morphiceptin on dorsal root ganglion (DRG) neurons if delta receptors mediated decreases of DRG neuron somatic calcium-dependent action potentials, but that these ligands would be approximately equipotent if mu receptors mediated opiate actions. Additionally, because naloxone has been reported to have a higher affinity for mu receptors in comparison with delta receptors, we investigated agonist sensitivity to naloxone antagonism. When morphiceptin and Leu-enkephalin were tested at equimolar concentrations on individual DRG neurons, a heterogeneous pattern of response to the two opioid peptides was obtained. The response pattern ranged from Leu-enkephalin and morphiceptin producing equal effects to Leu-enkephalin, but not morphiceptin, decreasing action potential duration. DRG neurons that responded only to Leu-enkephalin were approximately 100-fold less sensitive to naloxone antagonism than DRG neurons that responded equally well to both opioid peptides. DRG neurons that responded to both opioid peptides but better to Leu-enkephalin were intermediate in sensitivity to naloxone antagonism. Our results suggest that both mu and delta opiate receptors mediate decreases in somatic calcium-dependent action potentials of DRG neurons.(ABSTRACT TRUNCATED AT 250 WORDS)

MeSH Terms
Action Potentials/drug effects Animals Calcium/physiology Cells, Cultured Endorphins/pharmacology Enkephalin, Leucine/pharmacology Ganglia, Spinal/cytology In Vitro Techniques Mice Naloxone/pharmacology Neurons, Afferent/drug effects Receptors, Opioid/drug effects,physiology Receptors, Opioid, delta Receptors, Opioid, mu Time Factors
Chemicals
Endorphins Receptors, Opioid Receptors, Opioid, delta Receptors, Opioid, mu Naloxone Enkephalin, Leucine morphiceptin Calcium
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Werz M A
Macdonald R L
Article Info
Journal
The Journal of pharmacology and experimental therapeutics
Abbr.
J Pharmacol Exp Ther
ISSN
0022-3565
Published
1983-11-00
Pages
394-402
Language
English
Region
United States
NLM ID
0376362
Subset
IM
Grants
PHS HHS · 12479 · United States
NIDA NIH HHS · DA 5244 · United States
NINDS NIH HHS · NS00481 · United States
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