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Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors
BACKGROUND: The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors. Activation profiles of most of these ligands at δ opioid receptors had not been previously characterized in vitro....
Autores principales: | , , , |
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Formato: | Texto |
Lenguaje: | English |
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BioMed Central
2002
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC137588/ https://www.ncbi.nlm.nih.gov/pubmed/12437765 http://dx.doi.org/10.1186/1471-2202-3-19 |
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author | Gharagozlou, Parham Demirci, Hasan Clark, J David Lameh, Jelveh |
author_facet | Gharagozlou, Parham Demirci, Hasan Clark, J David Lameh, Jelveh |
author_sort | Gharagozlou, Parham |
collection | PubMed |
description | BACKGROUND: The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors. Activation profiles of most of these ligands at δ opioid receptors had not been previously characterized in vitro. Receptor activation was assessed by measuring the inhibition of forskolin-stimulated cAMP production. RESULTS: Naltrexone and nalorphine were classified as antagonists at δ opioid receptor. The other ligands studied were agonists at δ opioid receptors and demonstrated IC(50 )values of 0.1 nM to 2 μM, maximal inhibition of 39–77% and receptor binding affinities of 0.5 to 243 nM. The rank order of efficacy of the ligands tested was metazocine = xorphanol ≥ fentanyl = SKF 10047 = etorphine = hydromorphone = butorphanol = lofentanil > WIN 44,441 = Nalbuphine = cyclazocine ≥ met-enkephalin >> morphine = dezocine. For the first time these data describe and compare the function and relative efficacy of several ligands at δ opioid receptors. CONCLUSIONS: The data produced from this study can lead to elucidation of the complete activation profiles of several opioid ligands, leading to clarification of the mechanisms involved in physiological effects of these ligands at δ opioid receptors. Furthermore, these data can be used as a basis for novel use of existing opioid ligands based on their pharmacology at δ opioid receptors. |
format | Text |
id | pubmed-137588 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2002 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
spelling | pubmed-1375882002-12-05 Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors Gharagozlou, Parham Demirci, Hasan Clark, J David Lameh, Jelveh BMC Neurosci Research Article BACKGROUND: The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors. Activation profiles of most of these ligands at δ opioid receptors had not been previously characterized in vitro. Receptor activation was assessed by measuring the inhibition of forskolin-stimulated cAMP production. RESULTS: Naltrexone and nalorphine were classified as antagonists at δ opioid receptor. The other ligands studied were agonists at δ opioid receptors and demonstrated IC(50 )values of 0.1 nM to 2 μM, maximal inhibition of 39–77% and receptor binding affinities of 0.5 to 243 nM. The rank order of efficacy of the ligands tested was metazocine = xorphanol ≥ fentanyl = SKF 10047 = etorphine = hydromorphone = butorphanol = lofentanil > WIN 44,441 = Nalbuphine = cyclazocine ≥ met-enkephalin >> morphine = dezocine. For the first time these data describe and compare the function and relative efficacy of several ligands at δ opioid receptors. CONCLUSIONS: The data produced from this study can lead to elucidation of the complete activation profiles of several opioid ligands, leading to clarification of the mechanisms involved in physiological effects of these ligands at δ opioid receptors. Furthermore, these data can be used as a basis for novel use of existing opioid ligands based on their pharmacology at δ opioid receptors. BioMed Central 2002-11-18 /pmc/articles/PMC137588/ /pubmed/12437765 http://dx.doi.org/10.1186/1471-2202-3-19 Text en Copyright © 2002 Gharagozlou et al; licensee BioMed Central Ltd. This is an Open Access article: verbatim copying and redistribution of this article are permitted in all media for any purpose, provided this notice is preserved along with the article's original URL. |
spellingShingle | Research Article Gharagozlou, Parham Demirci, Hasan Clark, J David Lameh, Jelveh Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors |
title | Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors |
title_full | Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors |
title_fullStr | Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors |
title_full_unstemmed | Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors |
title_short | Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors |
title_sort | activation profiles of opioid ligands in hek cells expressing δ opioid receptors |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC137588/ https://www.ncbi.nlm.nih.gov/pubmed/12437765 http://dx.doi.org/10.1186/1471-2202-3-19 |
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