[Nphe1]NC(1-13)NH2 selectively antagonizes nociceptin/orphanin FQ- stimulated G-protein activation in rat brain

Journal of Pharmacology and Experimental Therapeutics

Volumn 294, Issue 2, 2000, Pages 428-433

  Berger, Hartmut ^a   Calo', Girolamo ^b   Albrecht, Erika ^a   Guerrini, Remo ^b   Bienert, Michael ^a  

^a LEIBNIZ INSTITUT FÜR MOLEKULARE PHARMAKOLOGIE   (Germany)

^b UNIVERSITY OF FERRARA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); GUANOSINE DIPHOSPHATE; GUANOSINE TRIPHOSPHATE; LIGAND; NOCICEPTIN; OPIATE RECEPTOR; PARTIAL AGONIST; PEPTIDE;

ANIMAL TISSUE; ARTICLE; BRAIN; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG EFFECT; MALE; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; RAT; RECEPTOR BINDING;

AMINO ACID SEQUENCE; ANIMALS; BINDING, COMPETITIVE; BRAIN; GTP-BINDING PROTEINS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); MALE; MEMBRANES; MICE; MICE, INBRED STRAINS; MOLECULAR SEQUENCE DATA; OPIOID PEPTIDES; PEPTIDE FRAGMENTS; RATS; RATS, WISTAR; RECEPTORS, OPIOID; STIMULATION, CHEMICAL; SUBSTRATE SPECIFICITY; SULFUR RADIOISOTOPES;

EID: 0033931478     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (37)

1. Adapa ID and Toll L (1997) Relationship between binding affinity and functional activity of nociceptin/orphanin FQ. Neuropeptides 31:403-408.
2. Albrecht E, Samovilova NN, Oswald S, Baeger I and Berger H (1998) Nociceptin (orphanin FQ): High-affinity and high-capacity binding site coupled to low-potency stimulation of guanylyl-5́-O-(γ-thio)-triphosphate binding in rat brain membranes. J Pharmacol Exp Ther 286:896-902.
3. 2 of G protein activation in rat brain preparations and of chronotropic effect on rat cardiomyocytes evoked by nociceptin/orphanin FQ. Br J Pharmacol 126:555-558.
4. 2, a nociceptin/orphanin FQ (noc/OFQ) receptor ligand, exhibits properties of an antagonist and agonist as well. Regul Pept 80:122.
5. Breivogel CS, Selley DE and Childers SR (1998) Cannabinoid receptor agonist efficacy for stimulating [S-35]GTP gamma S binding to rat cerebellar membranes correlates with agonist-induced decreases in GDP affinity. J Biol Chem 273: 16865-16873.
6. 2 N-terminal tetrapeptide and discovery of a nociceptin receptor antagonist. J Med Chem 41:3360-3366.
7. 2, a new selective nociceptin receptor antagonist. Br J Pharmacol 129:1183-1193.
8. Calo G, Rizzi A, Marzola G, Guerrini R, Salvadori S, Beani L, Regoli D and Bianchi C (1998b) Pharmacological characterization of the nociceptin receptor mediating hyperalgeaia in the mouse tail withdrawal assay. Br J Pharmacol 125:373-378.
9. 2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord. Br J Pharmacol 125:949-951.
10. 2 activation of an inward rectifier as a partial agonist of ORL1 receptors in rat periaqueductal gray. Br J Pharmacol 128:103-107.
11. Chu XP, Xu NS, Li P and Wang JQ (1999) The nociceptin receptor-mediated inhibition of the rat rostral ventrolateral medulla neurons in vitro. Eur J Pharmacol 364:49-53.
12. Darland T, Heinricher MM and Grandy DK (1998) Orphanin FQ/nociceptin: A role in pain and analgesia, but so much more. Trends Neurosci 21:215-221.
13. Dooley CT, Spaeth CG, Berzeteigurske IP, Craymer K, Adapa ID, Brandt SR, Houghten RA and Toll L (1997) Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. J Pharmacol Exp Ther 283:735-741.
14. Griffin G, Wray EJ, Rorrer WK, Cracker PJ, Ryan WJ, Saha B, Razdan RK, Martin BR and Abood ME (1999) An investigation into the structural determinants of cannabinoid receptor ligand efficacy. Br J Pharmacol 126:1575-1584.
15. 2 acts as an agonist of the orphanin FQ/nociceptin receptor in vivo. Eur J Pharmacol 357:R1-R3.
16. Guerrini R, Calo G, Rizzi A, Bigoni R, Bianchi C, Salvadori S and Regoli D (1998) A new selective antagonist of the nociceptin receptor. Br J Pharmacol 123:163-165.
17. 2 on nociceptin receptor mediated inhibition of cAMP formation in Chinese ovary cells stably expressing the recombinant human nociceptin receptor. Neurosci Lett 278:109-112.
18. 2 and orphanin FQ/nociceptin (OFQ/N) produce similar cardiovascular and renal responses in conscious rats. J Pharmacol Exp Ther 289:173-180.
19. Madeddu P, Salis MB, Milia AF, Emanueli C, Guerrini R, Regoli D and Calo G (1999) Cardiovascular effects of nociceptin in unanesthetized mice. Hypertension 33:914-919.
20. Meis S and Pape HC (1998) Postsynaptic mechanisms underlying responsiveness of amygdaloid neurons to nociceptin/orphanin FQ. J Neurosci 18:8133-8144.
21. Meunier JC, Mollereau C, Toll L, Suaudeau C, Moisand C, Alvinerie P, Butour JL, Guillemot JC, Ferrara P, Monsarrat B, Mazarguil H, Vassart G, Parmentier M and Costentin J (1995) Isolation and structure of the endogenous agonist of opioid receptor-like ORL(1) receptor. Nature (Lond) 377:532-535.
22. Newman-Tancredi A, Conte C, Chaput C, Verriele L and Millan MJ (1997) Agonist and inverse agonist efficacy at human recombinant serotonin 5-HT1A receptors as a function of receptor: G-protein stoichiometry. Neuropharmacology 36:451-459.
23. 2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors. Br J Pharmacol 127:123-130.
24. Polidori C, Calo G, Ciccocioppo R, Guerrini R, Regoli D and Massi M (2000) Pharmacological characterization of the nociceptin receptor mediating hyperphagia: Identification of a selective antagonist. Psychopharmacology 148:430-437.
25. Reinscheid RK, Nothacker HP, Bourson A, Ardati A, Henningsen RA, Bunzow JR, Grandy DK, Langen H, Monsma FJ and Civelli O (1995) Orphanin FQ: A neuropeptide that activates an opioidlike G protein-coupled receptor. Science (Wash DC) 270:792-794.
26. 2 antagonizes nociceptin effects in the mouse colon. Eur J Pharmacol 385:R3-R5.
27. Schlicker E, Werthwein S, Kathmann M and Bauer U (1998) Nociceptin inhibits noradrenaline release in the mouse brain cortex via presynaptic ORL1 receptors. Naunyn-Schmiedeberg's Arch Pharmacol 358:418-422.
28. Selley DE, Liu QX and Childers SR (1998) Signal transduction correlates of mu opioid agonist intrinsic efficacy: Receptor-stimulated [S-35]GTPgammaS binding in mMOR-CHO cells and rat thalamus. J Pharmacol Exp Ther 285:496-505.
29. Selley DE, Sim LJ, Xiao RY, Liu QX and Childers SR (1997) mu-Opioid receptor-stimulated guanosine-5′-O-lgamma-thio)-triphosphate binding in rat thalamus and cultured cell lines: Signal transduction mechanisms underlying agonist efficacy. Mol Pharmacol 51:87-96.
30. Shimonira I, Tokuyama S, Himeno A, Niwa M and Ueda H (1997) Characterization of nociceptin-stimulated in situ [S-35]GTP gamma S binding in comparison with opioid agonist-stimulated ones in brain regions of the mice. Neurosci Lett 237:113-116.
31. Sim LJ, Selley DE and Childers SR (1995) In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5′-[gamma-[S-35]thio]triphosphate binding. Proc Natl Acad Sci USA 92:7242-7246.
32. Sim LJ, Xiao RY and Childers SR (1996) Identification of opioid receptor-like (ORL1) peptide-stimulated [S-35]GTP gamma S binding in rat brain. Neuroreport 7:729-733.
33. Taylor F and Dickenson A (1998) Nociceptin/orphanin FQ. A new opioid, a new analgesic? Neuroreport 9:R65-R70.
34. Toll L, Burnside J and Berzetei-Gurske I (1998) Agonist activity of ORL1 antagonists is dependent upon receptor number. Abstracts of 29th International Narcotic Research Conference; July 20-25; Garmisch-Partenkirchen, Germany; 81.
35. Traynor JR and Nahorski SR (1995) Modulation by mu-opioid agonists of guanosine-5′-O-(3-[S-35]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells. Mol Pharmacol 47:848-854.
36. 2, a proposed antagonist of the nociceptin receptor, is a potent and stable agonist in the rat spinal cord. Neurosci Lett 249:127-130.
37. Yakimova KS and Pierau FK (1999) Nociceptin orphanin FQ: Effects on thermoregulation in rats. Methods Find Exp Clin Pharmacol 21:345-352.