Interaction of opioid peptides and other drugs with multiple kappa receptors in rat and human brain. Evidence for species differences

Richard B. Rothman, Victor Bykov, B. G. Xue, Heng Xu, Brian R. De Costa, Arthur E. Jacobson, Kenner C. Rice, Joel E. Kleinman, Linda S. Brady

Research output: Contribution to journalArticle

Abstract

Previous experiments resolved four κ binding sites in guinea pig brain termed κ1a, κ1b, κ2a, and κ2b. The present study was undertaken to examine the occurrence of κ receptor sybtypes in rat and human brain. [3H]U69,593 and [3H]bremazocine were used to label κ1 and κ2 binding sites, respectively, present in brain membranes depleted of μ and δ binding sites by pretreatment with the irreversible ligands, BIT and FIT. Low levels of [3H]U69,593 binding precluded a detailed quantitative study of κ1 binding sites in these species. Quantitative examination of [3H]bremazocine binding resolved two κ2 binding sites in both rat and human brain whose ligand selectivity patterns differed from that of the guinea pig. These observations suggest that there may be considerable variation in the ligand recognition site of κ receptor subtypes among mammalian species.

Original languageEnglish (US)
Pages (from-to)977-987
Number of pages11
JournalPeptides
Volume13
Issue number5
DOIs
StatePublished - Jan 1 1992
Externally publishedYes

Keywords

  • Autoradiography
  • Kappa receptors
  • Ligand binding studies
  • Opioid receptors
  • U69,593

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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    Rothman, R. B., Bykov, V., Xue, B. G., Xu, H., De Costa, B. R., Jacobson, A. E., Rice, K. C., Kleinman, J. E., & Brady, L. S. (1992). Interaction of opioid peptides and other drugs with multiple kappa receptors in rat and human brain. Evidence for species differences. Peptides, 13(5), 977-987. https://doi.org/10.1016/0196-9781(92)90059-C