Enantioselective kappa opioid binding sites on the macrophage cell line, P388d1

Academic Article


  • A kappa (κ{script}) opioid binding site has been characterized on the macrophage cell line, P388d1, using the kappa selective affinity ligand, [3H](1S,2S)-(-)-trans-2-isothiocyanato-N-methyl-N-[2-(1- pyrrolidinyl) cyclohexyl] benzeneacetamide (-)BD166). The kappa site has a relative molecular mass (Mr) of 38,000 under nonreducing conditions and 42,000 under reducing conditions. Moreover, it exhibits enantioselectivity in that 1S,2S-(-)-trans-3,4-dichloro- N-methyl-N-[2-1-pyrrolidinyl)cyclohexyl] benzeneacetamide ((-)- U-50,488) blocks [3H](5a, 7a, 8β)-(-)-N-methyl-N-[7-(1- pyrrolidinyl)- l-oxaspiro-(4,5)-dec-8-yl]benzeneacetamide (U-69,593) binding to P388d1 cells with an IC5 0 = 7.0 nM whereas IR,2R-(+)-trans-3,4- dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide ((+)U-50,488) blocks [3H]U-69,593 binding to P388d1 cells with an IC5 0 = 700 nM. © 1991.
  • Authors

    Published In

  • Life Sciences  Journal
  • Digital Object Identifier (doi)

    Pubmed Id

  • 19880745
  • Author List

  • Carr DJJ; DeCosta BR; Jacobson AE; Rice KC; Edwin Blalock J
  • Start Page

  • 45
  • End Page

  • 51
  • Volume

  • 49
  • Issue

  • 1