Characterization of [3H]-etorphine binding in guinea-pig striatum after blockade of mu and delta sites.
The guinea-pig striatum contains an apparent homogenous population of [3H]-etorphine high affinity sites (KD = 0.56 +/- 0.12 nM; Bmax = 267 +/- 47 fmoles/mg protein). The specific binding is completely abolished by 5 microM (D-Ala2, D-Leu5) enkephalin whereas an important residual binding is still present after the blockade of mu and delta sites. The binding properties of these residual sites are very similar to those of the benzomorphan sites characterized in rat brain and spinal cord. From the different binding properties of kappa and benzomorphan sites, the subdivision into kappa1 (kappa sites) and kappa2 (benzomorphan sites) is discussed.
D000818:Animals; D001575:Benzomorphans / Q000494:pharmacology; D001665:Binding Sites; D003342:Corpus Striatum / Q000187:drug effects; D004745:Enkephalins / Q000494:pharmacology; D005048:Etorphine / Q000378:metabolism*; D006168:Guinea Pigs; D008297:Male; D009019:Morphinans / Q000378:metabolism*; D011957:Receptors, Opioid / Q000502:physiology*; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D014316:Tritium
D001575:Benzomorphans; D004745:Enkephalins; D009019:Morphinans; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D014316:Tritium; D005048:Etorphine