Premium
A new selective antagonist of the nociceptin receptor
Author(s) -
Guerrini Remo,
Calo Girolamo,
Rizzi Anna,
Bigoni Raffaella,
Bianchi Clementina,
Salvadori Severo,
Regoli Domenico
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.0701640
Subject(s) - nociceptin receptor , vas deferens , agonist , medicine , ileum , endocrinology , antagonist , chemistry , guinea pig , receptor , antagonism , receptor antagonist , competitive antagonist , pharmacology , biology , opioid , opioid peptide
[Phe 1 Ψ(CH 2 ‐NH)Gly 2 ]NC(1‐13)NH 2 has been tested in the electrically stimulated guinea pig ileum and mouse vas deferens, two nociceptin sensitive preparations. The new compound showed per se little or no effect in the two tissues, but it displaced to the right the concentration‐response curves of nociceptin in a concentration‐dependent manner. Schild analyses of the data indicated a competitive type of antagonism and pA 2 values of 7.02 and 6.75 in the guinea‐pig ileum and the mouse vas deferens, respectively. At 10 μ M [Phe 1 Ψ(CH 2 ‐NH)Gly 2 ]NC(1‐13)NH 2 does not modify either the inhibitory effect of deltorphin I (the selective δ opioid receptor agonist) in the mouse vas deferens or that of dermorphine (the selective μ opioid receptor agonist) in the guinea‐pig ileum. The present findings indicate that [Phe 1 Ψ(CH 2 ‐NH)Gly 2 ]NC(1‐13)NH 2 is a selective antagonist of the nociceptin receptor. British Journal of Pharmacology (1998) 123 , 163–165; doi: 10.1038/sj.bjp.0701640