Functional blockade of opioid analgesia by orphanin FQ/nociceptin Journal Article
| Authors: | King, M.; Chang, A.; Pasternak, G. W. |
| Article Title: | Functional blockade of opioid analgesia by orphanin FQ/nociceptin |
| Abstract: | Orphanin FQ/nociceptin (OFQ/N) is a recently identified neuropeptide with high affinity for the orphan opioid receptor. OFQ/N blocked morphine analgesia in mice in a dose-dependent manner, as well as the analgesic actions of [D-Pen2, D-Pen5]enkephalin (DPDPE), morphine-6β-glucuronide, trans-3,4-dichloro-N-[2(1-pyrrolindinyl)-cyclohexyl]-benzeneacetamide, methane sulfonate hydrate (U50,488H) and naloxone benzoylhydrazone. These actions are anti-analgesic, because OFQ/N also blocked clonidine analgesia and OFQ/N was inactive against the inhibition of gastrointestinal transit by morphine. Although OFQ/N was quite potent in these paradigms, two truncated forms, OFQ/N(1-11) and OFQ/N(1-7), were inactive. An antisense oligodeoxynucleotide targeting the first coding exon of KOR-3, the mouse homolog of the orphan opioid receptor, effectively prevented the anti-opioid actions of OFQ/N, confirming the importance of the orphan opioid receptor in this action. |
| Keywords: | drug activity; nonhuman; animals; mice; nerve tissue proteins; drug effect; drug receptor binding; drug antagonism; drug mechanism; peptide fragments; receptor blocking; morphine; analgesics, opioid; analgesia; hyperalgesia; naloxone; opiate receptor; enkephalin[2,5 dextro penicillamine]; oligonucleotides, antisense; opioid receptor; opioid peptides; cerebral ventricles; injections, intraventricular; opiate antagonist; nociceptin; morphine derivative; opiate agonist; morphine derivatives; receptors, opioid; male; priority journal; article; receptors, opioid, kappa; enkephalins; anti-opioid; enkephalin, d-penicillamine (2,5)-; kor-3; 3,4 dichloro n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide; mesylic acid |
| Journal Title: | Biochemical Pharmacology |
| Volume: | 55 |
| Issue: | 9 |
| ISSN: | 0006-2952 |
| Publisher: | Elsevier Inc. |
| Date Published: | 1998-05-01 |
| Start Page: | 1537 |
| End Page: | 1540 |
| Language: | English |
| DOI: | 10.1016/s0006-2952(98)00023-9 |
| PUBMED: | 10076548 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 12 December 2016 -- Source: Scopus |
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