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Evidence that [Phe 1 ψ(CH 2 ‐NH)Gly 2 ]nociceptin‐(1‐13)‐NH 2 , a peripheral ORL‐1 receptor antagonist, acts as an agonist in the rat spinal cord
Author(s) -
Carpenter Kate J.,
Dickenson Anthony H.
Publication year - 1998
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0702188
Subject(s) - nociceptin receptor , agonist , antagonist , chemistry , electrophysiology , stereochemistry , receptor , opioid peptide , opioid , medicine , biochemistry
[Phe 1 ψ(CH 2 ‐NH)Gly 2 ]nociceptin‐(1‐13)‐NH 2 , a pseudopeptide analogue of nociceptin is an antagonist in peripheral assays. Here, using in vivo electrophysiological recordings of dorsal horn neurones, [Phe 1 ψ(CH 2 ‐NH)Gly 2 ]nociceptin‐(1‐13)‐NH 2 appears to have agonist activity after spinal administration. The noxious evoked activity of the neurones was inhibited by [Phe 1 ψ(CH 2 ‐NH)Gly 2 ]nociceptin‐(1‐13)‐NH 2 , which was as potent as nociceptin itself. British Journal of Pharmacology (1998) 125 , 949–952; doi: 10.1038/sj.bjp.0702188