Kappa binding sites in guinea-pig brain membranes: evidence for a dynorphin-resistant subtype

Life Sci. 1983:33 Suppl 1:179-82. doi: 10.1016/0024-3205(83)90472-1.

Abstract

Using [3H]ethylketocyclazocine after suppression of mu, delta and sigma binding by 100 nM DAGO + 100 nM DADLE + 10 microM phencyclidine we showed the existence of a subclass of kappa sites insensitive to dynorphins 1-9 and 1-17, and alpha and beta neoendorphins, but sensitive to the non-peptidic opiates. The dynorphin-sensitive site probably corresponds to the "standard" kappa site while the importance of the dynorphin-resistant site remains to be established.

MeSH terms

  • Analgesics, Opioid / metabolism
  • Animals
  • Binding, Competitive
  • Brain / metabolism*
  • Cell Membrane / metabolism
  • Cyclazocine / analogs & derivatives
  • Cyclazocine / metabolism
  • Ethylketocyclazocine
  • Guinea Pigs
  • Male
  • Phencyclidine / pharmacology
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / metabolism*
  • Receptors, Opioid, kappa

Substances

  • Analgesics, Opioid
  • Receptors, Opioid
  • Receptors, Opioid, kappa
  • Ethylketocyclazocine
  • Phencyclidine
  • Cyclazocine