Demonstration of κ3‐opioid receptors in the SH‐SY5Y human neuroblastoma cell line Journal Article
| Authors: | Cheng, J.; Standifer, K. M.; Tublin, P. R.; Su, W.; Pasternak, G. W. |
| Article Title: | Demonstration of κ3‐opioid receptors in the SH‐SY5Y human neuroblastoma cell line |
| Abstract: | Abstract: In addition to the μ‐ and δ‐opioid receptors previously reported, the SH‐SY5Y human neuroblastoma cell line has high levels of κ3 receptors, accounting for 40% of total opioid binding, as measured with [3H]‐diprenorphine binding. Competition studies reveal binding profiles for all three receptor classes that are similar to those observed in brain membranes. Differentiation with retinoic acid increases the levels of opioid receptor binding in the cell line, with the largest elevations in κ3 binding. Fully 75% of the increased binding corresponds to κ3 sites, which represent 50% of total opioid receptor binding in differentiated cells. Morphine inhibits forskolin‐stimulated cyclic AMP accumulation, and this effect is readily blocked by the μ antagonist d‐Phe‐Cys‐Tyr‐d‐Trp‐Arg‐Thr‐Pen‐Thr‐NH2 (CTAP). Naloxone benzoylhydrazone, a κ3 agonist, inhibits forskolin‐stimulated cyclic AMP accumulation more potently than morphine and is not reversed by CTAP. These studies indicate that SH‐SY5Y cells contain high levels of functional κ3 receptors. Copyright © 1995, Wiley Blackwell. All rights reserved |
| Keywords: | controlled study; unclassified drug; human cell; cell differentiation; cancer cell culture; tumor cells, cultured; drug receptor binding; neuroblastoma; neuroblastoma cell; cyclic amp; binding sites; morphine; nerve cell culture; naloxone; differentiation; enkephalin[2,5 dextro penicillamine]; naltrindole; tissue culture; receptor subtype; binding, competitive; opiate antagonist; tretinoin; naloxone benzoylhydrazone; kappa opiate receptor; enkephalin[2 dextro alanine 4 methylphenylalanine 5 glycine]; opiate agonist; human; priority journal; article; diprenorphine; receptors, opioid, kappa; support, u.s. gov't, p.h.s.; n methyl n [7 (1 pyrrolidinyl) 1 oxaspiro[4.5]dec 8 yl]benzeneacetamide; bremazocine; μ receptors; dextro phenylalanylcysteinyltyrosyl dextro tryptophylarginylthreonylpenicillaminylthreoninamide |
| Journal Title: | Journal of Neurochemistry |
| Volume: | 65 |
| Issue: | 1 |
| ISSN: | 0022-3042 |
| Publisher: | Wiley Blackwell |
| Date Published: | 1995-07-01 |
| Start Page: | 170 |
| End Page: | 175 |
| Language: | English |
| DOI: | 10.1046/j.1471-4159.1995.65010170.x |
| PUBMED: | 7790858 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 28 August 2018 -- Source: Scopus |
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