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British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1998 Nov;125(5):949–952. doi: 10.1038/sj.bjp.0702188

Evidence that [Phe1 ψ(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord

Kate J Carpenter 1,*, Anthony H Dickenson 1
PMCID: PMC1565681  PMID: 9846631

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.

Keywords: nociceptin, spinal cord, ORL-1 receptor, antinociception

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