Kappa2 opioid receptor subtype binding requires the presence of the DOR-1 gene

Michael A. Ansonoff, Ting Wen, John E. Pintar

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Over the past several years substantial evidence has documented that opioid receptor homo- and heterodimers form in cell lines expressing one or more of the opioid receptors. We used opioid receptor knockout mice to determine whether in vivo pharmacological characteristics of kappa1 and kappa 2 opioid receptors changed following knockout of specific opioid receptors. Using displacement of the general opioid ligand diprenorphine, we observed that occupancy or knockout of the DOR-1 gene increases the binding density of kappa1 receptors and eliminates kappa2 receptors in crude membrane preparations while the total density of kappa opioid binding sites is unchanged. Further, the analgesic potency of U69, 593 in cumulative dose response curves is enhanced in mice lacking the DOR-1 gene. These results demonstrate that the DOR-1 gene is required for the expression of the kappa2 opioid receptor subtype and are consistent with the possibility that a KOR-1/DOR-1 heterodimer mediates kappa2 pharmacology.

Original languageEnglish (US)
Pages (from-to)772-780
Number of pages9
JournalFrontiers in Bioscience - Scholar
Volume2 S
Issue number2
StatePublished - Jan 1 2010

Fingerprint

Opioid Receptors
Genes
Opioid Analgesics
Diprenorphine
Pharmacology
Knockout Mice
Analgesics
Binding Sites
Cells
Ligands
Membranes
Cell Line
kappa(2) opioid receptor

All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)
  • Immunology and Microbiology(all)

Keywords

  • Dimer
  • Intrathecal
  • Knockout
  • Opioid
  • U69

Cite this

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Kappa2 opioid receptor subtype binding requires the presence of the DOR-1 gene. / Ansonoff, Michael A.; Wen, Ting; Pintar, John E.

In: Frontiers in Bioscience - Scholar, Vol. 2 S, No. 2, 01.01.2010, p. 772-780.

Research output: Contribution to journalArticle

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