Evidence that [Phe1ψ(CH2‐NH)Gly2]nociceptin‐(1‐13)‐NH2, a peripheral ORL‐1 receptor antagonist, acts as an agonist in the rat spinal cord

Abstract
[Phe1 ψ(CH2‐NH)Gly2]nociceptin‐(1‐13)‐NH2, a pseudopeptide analogue of nociceptin is an antagonist in peripheral assays. Here, using in vivo electrophysiological recordings of dorsal horn neurones, [Phe1 ψ(CH2‐NH)Gly2]nociceptin‐(1‐13)‐NH2 appears to have agonist activity after spinal administration. The noxious evoked activity of the neurones was inhibited by [Phe1 ψ(CH2‐NH)Gly2]nociceptin‐(1‐13)‐NH2, which was as potent as nociceptin itself.British Journal of Pharmacology (1998) 125, 949–952; doi:10.1038/sj.bjp.0702188