Biochemical evidence for orphanin FQ/nociceptin receptor heterogeneity in mouse brain Journal Article
| Authors: | Mathis, J. P.; Ryan-Moro, J.; Chang, A.; Hom, J. S. H.; Scheinberg, D. A.; Pasternak, G. W. |
| Article Title: | Biochemical evidence for orphanin FQ/nociceptin receptor heterogeneity in mouse brain |
| Abstract: | A recently identified novel peptide, orphanin FQ/nociceptin (OFQ/N), is an endogenous ligand for a unique member of the domed opioid receptor family. Saturation studies in mouse brain membranes reveal curvilinear Scatchard plots with both a higher (K(D) 3.8 pM, B(max) 31.6 fmol/mg protein) and a lower (K(D) 896 pM, B(max) 233 fmol/mg protein) affinity site in brain tissue, compared to only a single site in transfected CHO cells (K(D) 36 pM). Competition studies confirm the high affinity of OFQ/N for this site, but shallow Hill slopes suggest heterogeneity. Traditional opioids have poor affinity for this receptor and OFQ/N and its fragments do not label traditional opioid receptors. In brain homogenates, both OFQ/N and OFQ/N(1-11) inhibit forskolin-stimulated camp accumulation with IC50 values of 1 nM or less, an action which is readily reversed by opioid antagonists. OFQ/N(1-7) shows little activity. Together, these studies suggest the presence of heterogeneous, functionally active OFQ/N receptors in mouse brain. |
| Keywords: | controlled study; unclassified drug; nonhuman; mouse; animals; mice; animal tissue; opiate; transfection; animalia; kinetics; brain; recombinant proteins; cell membrane; cyclic amp; receptor affinity; receptor binding; binding competition; opiate receptor; cho cell; cho cells; cricetinae; opioid peptides; receptor subtype; scatchard plot; binding, competitive; opiate antagonist; forskolin; radioligand assay; opiate agonist; brain membrane; narcotics; receptors, opioid; dna transfection; priority journal; article; nociceptin receptor; enkephalins; dynorphins; brain receptor |
| Journal Title: | Biochemical and Biophysical Research Communications |
| Volume: | 230 |
| Issue: | 2 |
| ISSN: | 0006-291X |
| Publisher: | Elsevier Science, Inc. |
| Date Published: | 1997-01-13 |
| Start Page: | 462 |
| End Page: | 465 |
| Language: | English |
| DOI: | 10.1006/bbrc.1996.5867 |
| PUBMED: | 9016803 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 17 March 2017 -- Source: Scopus |
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499Scheinberg -
414Pasternak -
19Chang -
21
Mathis -
14
Ryan-Moro
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