Dimerization of morphine and orphanin FQ/nociceptin receptors: Generation of a novel opioid receptor subtype Journal Article
| Authors: | Pan, Y. X.; Bolan, E.; Pasternak, G. W. |
| Article Title: | Dimerization of morphine and orphanin FQ/nociceptin receptors: Generation of a novel opioid receptor subtype |
| Abstract: | Although orphanin FQ/nociceptin (OFQ/N) receptors are a member of the opioid receptor family of receptors, they bind traditional opioids with very poor affinity. We now demonstrate that mu opioid receptors can physically associate with OFQ/N receptors, resulting in a complex with a unique binding selectivity profile. Immunoprecipitation of epitope-tagged OFQ/N receptors co-precipitates mu receptors. When the two receptors were co-expressed in CHO cells, [3H]OFQ/N retained its high binding affinity for its receptor. However, co-expression of the two receptors increased by up to 250-fold the affinity of a series of opioids in [3H]OFQ/N binding assays. This enhanced affinity was limited to agonists with high affinity for mu receptors. Selective κ1 and δ opioids did not lower binding. Despite the dramatic increase in affinity for the opioid agonists in co-expressing cells, the opioid antagonists naloxone and diprenorphine failed to compete [3H]OFQ/N binding. © 2002 Elsevier Science (USA). All rights reserved. |
| Keywords: | controlled study; protein expression; unclassified drug; nonhuman; binding affinity; polymerase chain reaction; animal cell; animals; protein protein interaction; genetic vectors; cloning, molecular; recombinant proteins; epitope; cell membrane; immunoprecipitation; dimerization; morphine; protein family; mu opiate receptor; receptors, opioid, mu; drug protein binding; binding competition; naloxone; fentanyl; opiate receptor; enkephalin[2,5 dextro penicillamine]; tritium; opioid receptor; cho cell; cho cells; cricetinae; dimer; receptor subtype; binding, competitive; enkephalin, ala(2)-mephe(4)-gly(5)-; 3,4 dichloro n methyl n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate; naloxone benzoylhydrazone; binding assay; dynorphin a; kappa opiate receptor; nociceptin; restriction mapping; enkephalin[2 dextro alanine 4 methylphenylalanine 5 glycine]; opiate agonist; receptors, opioid; priority journal; article; diprenorphine; nociceptin receptor; κ3 receptor; ofq; orl1; enkephalin[2 dextro alanine 5 dextro leucine]; nociceptin derivative; nociceptin[1-11] |
| Journal Title: | Biochemical and Biophysical Research Communications |
| Volume: | 297 |
| Issue: | 3 |
| ISSN: | 0006-291X |
| Publisher: | Elsevier Science, Inc. |
| Date Published: | 2002-09-27 |
| Start Page: | 659 |
| End Page: | 663 |
| Language: | English |
| DOI: | 10.1016/s0006-291x(02)02258-1 |
| PUBMED: | 12270145 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Erratum/Corrigendum issued, see DOI: 10.1016/s0006-291x(02)02479-8 -- Export Date: 14 November 2014 -- Source: Scopus |
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