We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Pharmacological Characterization of the Nociceptin Receptor, ORL1.
- Authors
Chiou, Lih-Chu
- Abstract
A novel opioid receptor-like orphan receptor (ORL1) was cloned and identified to be homologous to classical opioid receptors but insensitive to traditional opioids. A heptadecapeptide, termed orphanin FQ or nociceptin (OFQ/N), was identified as its endogenous ligand. OFQ/N shares overlapping distribution sites in pain-processing areas and common cellular mechanisms with opioids but exerts diverse effects on nociceptive responses. Of the two reported ORL1 antagonists, [Phe[sup 1] ψ(CH[sub 2] -NH)- Gly[sup 2] ] nociceptin-(1–13)-NH[sub 2] (Pheψ) and naloxone benzoylhydrazone (NBZ), antagonisms were validated in the activation of inward rectifying K channels induced by OFQ/N, using the patch clamp technique in ventrolateral periaqueductal gray slices. Results showed that Pheψ acted as a partial agonist and NBZ was a weak nonselective antagonist of ORL1. It is comparable with most but not all of the findings from other tissues. Comparing all the reports supports the above inference for these two antagonists. The possible causes for the discrepancy were discussed. A brief review on the putative ORL1 antagonists, acetyl-RYYRIK-NH2, some σ-ligands and the functional antagonist, nocistatin, is also included. It indicates that a potent and selective ORL1 antagonist is expecting to elucidate the physiological role of OFQ/N.Copyright © 2000 National Science Council, ROC and S. Karger AG, Basel
- Subjects
OPIOID receptors; DRUG receptors; NALOXONE; PERIAQUEDUCTAL gray matter; PHARMACOLOGY
- Publication
Journal of Biomedical Science, 2000, Vol 7, Issue 3, p232
- ISSN
1021-7770
- Publication type
Article
- DOI
10.1007/BF02255471