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Rat central ORL-1 receptor uncouples from adenylyl cyclase during membrane preparation
- Source :
- Neuroscience Letters. 246:49-52
- Publication Year :
- 1998
- Publisher :
- Elsevier BV, 1998.
-
Abstract
- Nociceptin/orphanin FQ is the endogenous agonist of the orphan receptor ORL-1. In this study, we sought to examine any possible regional differences of nociceptin binding using [ 125 I]Tyr 14 -nociceptin, and of agonist induced inhibition of cAMP formation in membranes prepared from cerebrocortex, cerebellum and brainstem. The binding of [ 125 I]Tyr 14 -nociceptin was concentration-dependent and saturable, with B max and p K d (pM) values of 179.7±15.3 fmol/mg protein and 10.26±0.09 (60.0), 12.4±1.8 fmol/mg protein and 10.44±0.07 (37.0), 52.3±0.8 fmol/mg protein and 10.16±0.08 (74.0) in cerebrocortical, cerebella and brainstem membranes, respectively. In all preparations, nociceptin up to 1 μ M failed to inhibit basal and forskolin stimulated cAMP formation. In all tissues forskolin stimulated and nabilone (acting at the central cannabinoid receptor) inhibited cAMP formation. Collectively these data report regional differences in ORL-1 receptor expression and that these receptors uncouple during membrane preparation.
- Subjects :
- Agonist
medicine.medical_specialty
medicine.drug_class
Receptor expression
Nociceptin Receptor
Iodine Radioisotopes
Adenylyl cyclase
chemistry.chemical_compound
Piperidines
Cerebellum
Internal medicine
Cyclic AMP
medicine
Animals
Dronabinol
Rats, Wistar
Receptor
Cerebral Cortex
Orphan receptor
Forskolin
Cannabinoids
Chemistry
General Neuroscience
Cell Membrane
Colforsin
Rats
Nociceptin receptor
Endocrinology
Opioid Peptides
Receptors, Opioid
Pyrazoles
Female
Rimonabant
Endogenous agonist
Brain Stem
Subjects
Details
- ISSN :
- 03043940
- Volume :
- 246
- Database :
- OpenAIRE
- Journal :
- Neuroscience Letters
- Accession number :
- edsair.doi.dedup.....818c6770960dadff3179c3725e8b4422