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Internalization of mu-opioid receptors in rat spinal cord slices.
- Source :
-
Neuroreport [Neuroreport] 1999 Aug 02; Vol. 10 (11), pp. 2329-34. - Publication Year :
- 1999
-
Abstract
- Cells immunoreactive for the mu-opioid receptor (MOR) in laminae I-II of the spinal cord were identified as small neurons with rostro-caudal dendrites. In spinal cord slices, [D-Ala2,MePhe4-Gly-ol5]enkephalin (DAMGO) or etorphine (1 microM) caused naloxone-sensitive MOR endocytosis in 100% of these neurons, whereas the selective delta- and kappa-opioid agonists [D-Pen2,5]enkephalin (DPDPE) and spiradoline mesylate (U-62,066), respectively, produced negligible internalization at 1 microM. The EC50 for DAMGO was 30 nM, similar to its potency to inhibit cAMP accumulation and to increase [gamma-35S]GTP binding. MOR internalization followed an exponential timecourse with a half-life of 1.7 min. MOR internalization in spinal cord slices was faster and occurred at lower agonist concentrations than in MOR-transfected cells, suggesting that spinal cord neurons have a more effective coupling of MORs to intracellular components mediating endocytosis.
- Subjects :
- Animals
Dose-Response Relationship, Drug
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
Enkephalins pharmacology
Immunohistochemistry
In Vitro Techniques
Kinetics
Rats
Receptors, Opioid, mu agonists
Spinal Cord drug effects
Spinal Cord physiology
Tissue Distribution physiology
Endocytosis physiology
Receptors, Opioid, mu metabolism
Spinal Cord metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0959-4965
- Volume :
- 10
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Neuroreport
- Publication Type :
- Academic Journal
- Accession number :
- 10439458
- Full Text :
- https://doi.org/10.1097/00001756-199908020-00020