Abstract

High affinity and saturable nociceptin (orphanin FQ) receptors were detected and characterized in adult rat and human fetal hypothalamic membranes, utilizing [ 125I]Tyr 12-nociceptin as ligand. Nociceptin bound with picomolar affinity, dynorphin A with nanomolar affinity, naloxone and dynorphan A(1–8) with micromolar while des-Tyr 1-dynorphin (dynorphin A(2–17)), several other opioids, morphine and benzomorphans failed to compete for binding at 1–10 μM. Gpp(NH)p together with sodium ion markedly decreased binding, consistent with involvement of a G protein-linked receptor.

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