Evidence that [Phe1 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord.
[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.
Carpenter
K J
KJ
Department of Pharmacology, University College London.
Dickenson
A H
AH
D000700:Analgesics / Q000494:pharmacology*; D000758:Anesthesia; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D008297:Male; D009292:Narcotic Antagonists; D009474:Neurons / Q000187:drug effects; D018847:Opioid Peptides / Q000737:chemistry / Q000494:pharmacology*; D010446:Peptide Fragments / Q000494:pharmacology*; D010455:Peptides / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011957:Receptors, Opioid / Q000819:agonists*; D013116:Spinal Cord / Q000187:drug effects* / Q000378:metabolism; D000094942:Nociceptin Receptor; D000097629:Nociceptin
D000700:Analgesics; D009292:Narcotic Antagonists; D018847:Opioid Peptides; D010446:Peptide Fragments; D010455:Peptides; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor; D000097629:Nociceptin; C114149:nociceptin (1-13)-NH2, Phe(1)-psi(CH2-NH)-Gly(2)-