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

Peptides. Sep-Oct 1992;13(5):977-87. doi: 10.1016/0196-9781(92)90059-c.


Previous experiments resolved four kappa binding sites in guinea pig brain termed kappa 1a, kappa 1b, and kappa 2b. The present study was undertaken to examine the occurrence of kappa receptor subtypes in rat and human brain. [3H]U69,593 and [3H]bremazocine were used to label kappa 1 and kappa 2 binding sites, respectively, present in brain membranes depleted of mu and delta binding sites by pretreatment with the irreversible ligands, BIT and FIT. Low levels of [3H]U69,593 binding precluded a detailed quantitative study of kappa 1 binding sites in these species. Quantitative examination of [3H]bremazocine binding resolved two kappa 2 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 kappa receptor subtypes among mammalian species.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • Animals
  • Benzeneacetamides*
  • Benzomorphans / metabolism
  • Brain / drug effects
  • Brain / metabolism*
  • Endorphins / metabolism*
  • Guanylyl Imidodiphosphate / pharmacology
  • Humans
  • Kinetics
  • Male
  • Pyrrolidines / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Opioid, kappa / classification
  • Receptors, Opioid, kappa / drug effects
  • Receptors, Opioid, kappa / metabolism*
  • Species Specificity
  • Structure-Activity Relationship


  • Benzeneacetamides
  • Benzomorphans
  • Endorphins
  • Pyrrolidines
  • Receptors, Opioid, kappa
  • Guanylyl Imidodiphosphate
  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • bremazocine
  • U 69593