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Regulation of opioid receptors in rat sensory neurons in culture.
- Source :
-
Molecular pharmacology [Mol Pharmacol] 1997 Apr; Vol. 51 (4), pp. 666-73. - Publication Year :
- 1997
-
Abstract
- To determine whether opioid receptors in sensory neurons are regulated by chronic exposure to opioids, we assessed the binding of various opioid ligands to membranes derived from isolated rat dorsal root ganglia neurons grown in culture. Equilibrium binding of [3H]diprenorphine onto membranes from cells grown for 13-15 days revealed a saturable binding site with a Kd value of 0.3 +/- 0.2 nM and an approximate Bmax value of 1300 +/- 200 fmol/mg of protein. [3H]Diprenorphine binding increased 3-fold from 1-15 days in culture. The mu receptors represent approximately 70 +/- 11% of the [3H]diprenorphine binding sites, as indicated by saturation binding of [3H]DAMGO. The kappa and delta receptors represent approximately 10 +/- 3% and approximately 5 +/- 2% of the [3H]diprenorphine binding sites, respectively. Preexposure of neurons to 10 microM naloxone for 48 hr up-regulated the receptors by 40%, whereas incubation with 100 nM to 10 microM DAMGO for 48 hr resulted in a significant decrease in the Bmax value of opioid receptors, with a maximum reduction of 70%. The identification of a high level of opioid receptors expressed in isolated sensory neurons and their modulation by opioids demonstrates that cultured sensory neurons are an excellent model with which to study opioid receptor regulation.
- Subjects :
- Analgesics pharmacology
Animals
Cells, Cultured
Diprenorphine metabolism
Down-Regulation drug effects
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
Enkephalins pharmacology
Female
Kinetics
Naloxone pharmacology
Narcotic Antagonists pharmacology
Neurons, Afferent drug effects
Neurons, Afferent metabolism
Pregnancy
Rats
Rats, Sprague-Dawley
Receptors, Opioid classification
Receptors, Opioid drug effects
Receptors, Opioid, delta drug effects
Receptors, Opioid, delta metabolism
Receptors, Opioid, kappa drug effects
Receptors, Opioid, kappa metabolism
Receptors, Opioid, mu drug effects
Receptors, Opioid, mu metabolism
Tritium
Up-Regulation drug effects
Neurons, Afferent ultrastructure
Receptors, Opioid metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0026-895X
- Volume :
- 51
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Molecular pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 9106633
- Full Text :
- https://doi.org/10.1124/mol.51.4.666