[Phe1phi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 acts as a partial agonist at ORL1 receptor endogenously expressed in mouse N1E-115 neuroblastoma cells.

Abstract

The nociceptin derivative [Phe1phi(CH2-NH)Gly2]-nociceptin-(1-13)-NH2 (Phe(phi)noc) has been reported to act either as a simple antagonist or as a full agonist at the opioid receptor-like (ORL1) receptor. In the present study, we identified the expression of the ORL1 receptor in murine N1E-115 neuroblastoma cells and used this neuronal system to investigate the pharmacological activity of Phe(phi)noc. Like nociceptin, Phe(phi)noc stimulated the binding of [35S]GTPgammaS (EC50 = 120 nM) and inhibited forskolin-stimulated [3H]cAMP formation (EC50 = 3.3 nM). However, Phe(phi)noc elicited maximal effects lower than those induced by nociceptin, and when combined with nociceptin potently antagonized the responses to the natural agonist (Ki = 0.9 nM). These data indicate that Phe(phi)noc acts as a partial agonist at the ORL1 receptor endogenously expressed in N1E-115 cells.

• Authors: M C Olianas, C Maullu, A Ingianni, P Onali
• Journal: Neuroreport (Neuroreport) Vol. 10 Issue 5 Pg. 1127-31 (Apr 06 1999) ISSN: 0959-4965 [Print] England
• PMID: 10321496 (Publication Type: Journal Article)

Chemical References

• Drug Combinations
• Opioid Peptides
• Peptide Fragments
• Receptors, Opioid
• nociceptin (1-13)-NH2, Phe(1)-psi(CH2-NH)-Gly(2)-
• Colforsin
• Guanosine 5'-O-(3-Thiotriphosphate)
• nociceptin
• Cyclic AMP
• Nociceptin Receptor
• Oprl1 protein, mouse

Topics

• Animals
• Colforsin (pharmacology)
• Cyclic AMP (antagonists & inhibitors, biosynthesis)
• Drug Combinations
• Guanosine 5'-O-(3-Thiotriphosphate) (metabolism)
• Mice
• Neuroblastoma (metabolism, pathology)
• Opioid Peptides (pharmacology)
• Peptide Fragments (pharmacology)
• Receptors, Opioid (agonists, metabolism)
• Tumor Cells, Cultured
• Nociceptin Receptor