Orphanin FQ/nociceptin and naloxone benzoylhydrazone activate distinct receptors in BE(2)-C human neuroblastoma cells Journal Article
| Authors: | Mathis, J. P.; Mandyam, C. D.; Altememi, G. F.; Pasternak, G. W.; Standifer, K. M. |
| Article Title: | Orphanin FQ/nociceptin and naloxone benzoylhydrazone activate distinct receptors in BE(2)-C human neuroblastoma cells |
| Abstract: | kappa (3) opioid receptors have a unique binding and analgesic profile, as originally defined by naloxone benzoylhydrazone (NalBzoH). Although antisense studies demonstrated the close relationship between kappa (3) opioid and Orphan opioid receptor-like receptor (ORL1) and implied they were generated from the same gene, these studies also revealed differences in the sensitivity profiles of NalBzoH and orphanin FQ/nociceptin (OFQ/N), indicating that they were not identical. To help define the relationship between kappa (3) and ORL1 receptors, we utilized BE(2)-C human neuroblastoma cells that natively express functional ORL1 and kappa (3) opioid receptors. I-125-[Tyr(14)]OFQ/N binds to a single population of receptors in BE(2)-C cells. Competition binding and adenylyl cyclase studies clearly illustrated marked selectivity differences between the ORL1 and the kappa (3) sites. Furthermore, antisense DNA targeting ORL1 blocked the inhibition of cAMP by OFQ/N, but not by NalBzoH. Thus, the receptor mechanisms mediating the activity of OFQ/N and NalBzoH in BE(2)-C cells are distinct. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved. |
| Keywords: | brain; opioid receptor; binding; receptors; nociceptin; pharmacological characterization; camp; fq; orphan opioid receptor-like receptor; homologous desensitization; kappa(3) opioid receptor; kappa(3)-opioid |
| Journal Title: | Neuroscience Letters |
| Volume: | 299 |
| Issue: | 3 |
| ISSN: | 0304-3940 |
| Publisher: | Elsevier Science, Inc. |
| Date Published: | 2001-02-23 |
| Start Page: | 173 |
| End Page: | 176 |
| Language: | English |
| ACCESSION: | WOS:000166912600002 |
| DOI: | 10.1016/s0304-3940(01)01524-5 |
| PROVIDER: | wos |
| PUBMED: | 11165763 |
| Notes: | Article -- Source: Wos |
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