Abstract
[Phe1 psi(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 psi(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 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, which was as potent as nociceptin itself.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics / pharmacology*
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Anesthesia
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Animals
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CHO Cells
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Cricetinae
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Humans
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Male
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Narcotic Antagonists*
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Neurons / drug effects
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Nociceptin
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Nociceptin Receptor
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Opioid Peptides / chemistry
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Opioid Peptides / pharmacology*
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Peptide Fragments / pharmacology*
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Peptides / pharmacology
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Rats
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Rats, Sprague-Dawley
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Receptors, Opioid / agonists*
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Spinal Cord / drug effects*
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Spinal Cord / metabolism
Substances
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Analgesics
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Narcotic Antagonists
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Opioid Peptides
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Peptide Fragments
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Peptides
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Receptors, Opioid
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nociceptin (1-13)-NH2, Phe(1)-psi(CH2-NH)-Gly(2)-
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Nociceptin Receptor