Remo Guerrini

Summary

Affiliation: University of Ferrara
Country: Italy

Publications

  1. doi request reprint Neurobiology, pharmacology, and medicinal chemistry of neuropeptide S and its receptor
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, Ferrara, Italy
    Med Res Rev 30:751-77. 2010
  2. ncbi request reprint Nociceptin/Orphanin FQ(1-13)NH2 analogues modified in the Phe1-Gly2 peptide bond
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, Via Fossato di Mortara, 17 19, 44100 Ferrara, Italy
    Bioorg Med Chem Lett 13:365-8. 2003
  3. pmc Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center and Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, National Institute of Neuroscience, Univ of Ferrara, Ferrara, Italy
    J Med Chem 52:4068-71. 2009
  4. pmc Synthesis and biological activity of human neuropeptide S analogues modified in position 5: identification of potent and pure neuropeptide S receptor antagonists
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center, Section of Pharmacology and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    J Med Chem 52:524-9. 2009
  5. pmc In vitro and in vivo studies on UFP-112, a novel potent and long lasting agonist selective for the nociceptin/orphanin FQ receptor
    Anna Rizzi
    Department of Experimental and Clinical Medicine, Section of Pharmacology and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 17, 44100 Ferrara, Italy
    Peptides 28:1240-51. 2007
  6. ncbi request reprint Structure-activity relationship study of position 4 in the urotensin-II receptor ligand U-II(4-11)
    Erika Marzola
    Department of Pharmaceutical Sciences and Biotechnology Center, Section of Pharmacology, University of Ferrara, 44100 Ferrara, Italy
    Peptides 29:674-9. 2008
  7. ncbi request reprint N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center and Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Centre, University of Ferrara, 44100 Ferrara, Italy
    J Med Chem 48:1421-7. 2005
  8. doi request reprint Structure-activity study at positions 3 and 4 of human neuropeptide S
    Valeria Camarda
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, Italy
    Bioorg Med Chem 16:8841-5. 2008
  9. doi request reprint Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide
    Claudio Trapella
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Bioorg Med Chem 17:5080-95. 2009
  10. ncbi request reprint Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids
    Marika Arduin
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, 44100 Ferrara, Italy
    Bioorg Med Chem 15:4434-43. 2007

Collaborators

Detail Information

Publications82

  1. doi request reprint Neurobiology, pharmacology, and medicinal chemistry of neuropeptide S and its receptor
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, Ferrara, Italy
    Med Res Rev 30:751-77. 2010
    ..The use in future studies of NPSR antagonists will be of paramount importance for understanding which biological functions are controlled by the NPS/NPSR system and for defining the therapeutic potential of selective NPSR ligands...
  2. ncbi request reprint Nociceptin/Orphanin FQ(1-13)NH2 analogues modified in the Phe1-Gly2 peptide bond
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, Via Fossato di Mortara, 17 19, 44100 Ferrara, Italy
    Bioorg Med Chem Lett 13:365-8. 2003
    ....
  3. pmc Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center and Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, National Institute of Neuroscience, Univ of Ferrara, Ferrara, Italy
    J Med Chem 52:4068-71. 2009
    ..The results confirmed that the [d-Xaa(5)] substitution promotes antagonist activity with potency inversely related to the side chain size and allowed identification of the novel potent NPSR peptide antagonist [(t)Bu-d-Gly(5)]NPS...
  4. pmc Synthesis and biological activity of human neuropeptide S analogues modified in position 5: identification of potent and pure neuropeptide S receptor antagonists
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center, Section of Pharmacology and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    J Med Chem 52:524-9. 2009
    ..56) among this series of peptides. The antagonist action of [D-Val5]NPS was confirmed in vivo in mice, where the peptide at a dose of 10 nmol completely blocked the stimulatory effect of 0.1 nmol NPS on locomotor activity...
  5. pmc In vitro and in vivo studies on UFP-112, a novel potent and long lasting agonist selective for the nociceptin/orphanin FQ receptor
    Anna Rizzi
    Department of Experimental and Clinical Medicine, Section of Pharmacology and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 17, 44100 Ferrara, Italy
    Peptides 28:1240-51. 2007
    ..Collectively, these findings demonstrate that UFP-112 behaves in vitro and in vivo as a highly potent and selective ligand able to produce full and long lasting activation of NOP receptors...
  6. ncbi request reprint Structure-activity relationship study of position 4 in the urotensin-II receptor ligand U-II(4-11)
    Erika Marzola
    Department of Pharmaceutical Sciences and Biotechnology Center, Section of Pharmacology, University of Ferrara, 44100 Ferrara, Italy
    Peptides 29:674-9. 2008
    ..Thus acylation of U-II(5-11) with small groups bearing nitrogen atoms could be instrumental in future studies for the identification of novel potent UT receptor ligands...
  7. ncbi request reprint N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Center and Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Centre, University of Ferrara, 44100 Ferrara, Italy
    J Med Chem 48:1421-7. 2005
    ....
  8. doi request reprint Structure-activity study at positions 3 and 4 of human neuropeptide S
    Valeria Camarda
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, Italy
    Bioorg Med Chem 16:8841-5. 2008
    ....
  9. doi request reprint Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide
    Claudio Trapella
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Bioorg Med Chem 17:5080-95. 2009
    ..However compound 35 was found inactive when challenged against N/OFQ in vivo in the mouse tail withdrawal assay. Thus, the usefulness of the novel NOP ligand compound 35 is limited to in vitro investigations...
  10. ncbi request reprint Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids
    Marika Arduin
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, 44100 Ferrara, Italy
    Bioorg Med Chem 15:4434-43. 2007
    ....
  11. doi request reprint Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24
    Carmela Fischetti
    Department Experimental and Clinical Medicine, University of Ferrara, Ferrara, Italy
    Eur J Pharmacol 614:50-7. 2009
    ..The present study demonstrated that Compound 24 is a pure, competitive, and highly potent non-peptide NOP receptor selective antagonist...
  12. ncbi request reprint Anxiolytic- and antidepressant-like activities of H-Dmt-Tic-NH-CH(CH2-COOH)-Bid (UFP-512), a novel selective delta opioid receptor agonist
    Raffaella Vergura
    Department of Experimental and Clinical Medicine, Section of Pharmacology, and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Peptides 29:93-103. 2008
    ....
  13. pmc In vitro and in vivo pharmacological characterization of the novel UT receptor ligand [Pen5,DTrp7,Dab8]urotensin II(4-11) (UFP-803)
    Valeria Camarda
    Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, Ferrara, Italy
    Br J Pharmacol 147:92-100. 2006
    ..While UFP-803 is less potent than urantide, it displayed reduced residual agonist activity and as such may be a useful pharmacological tool...
  14. doi request reprint Further studies on the pharmacological features of the nociceptin/orphanin FQ receptor ligand ZP120
    Carmela Fischetti
    Department Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, and National Institute of Neuroscience, Ferrara, Italy
    Peptides 30:248-55. 2009
    ....
  15. doi request reprint Synthesis and biological activity of human neuropeptide S analogues modified in position 2
    Valeria Camarda
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Italian Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 19, Ferrara, Italy
    J Med Chem 51:655-8. 2008
    ....
  16. doi request reprint Structure-activity relationship study on Tyr9 of urotensin-II(4-11): identification of a partial agonist of the UT receptor
    Madura Batuwangala
    Dept of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, Ferrara, Italy
    Peptides 30:1130-6. 2009
    ..This pharmacological activity of [3,5-diiodoTyr(9)]U-II(4-11) was confirmed in bioassay experiments performed using the rat thoracic aorta as a U-II sensitive preparation...
  17. ncbi request reprint Endogenous nociceptin/orphanin FQ signalling produces opposite spinal antinociceptive and supraspinal pronociceptive effects in the mouse formalin test: pharmacological and genetic evidences
    Anna Rizzi
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Pain 124:100-8. 2006
    ..The overall effect of blocking NOP receptor signalling, by either systemic pharmacological antagonism or genetic ablation, indicates that the spinal antinociceptive action prevails over supraspinal pronociceptive effects...
  18. ncbi request reprint UFP-101 antagonizes the spinal antinociceptive effects of nociceptin/orphanin FQ: behavioral and electrophysiological studies in mice
    Cristiano Nazzaro
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Peptides 28:663-9. 2007
    ..44). The present results demonstrate that N/OFQ-induced spinal antinociception in vivo and inhibition of spinal excitatory transmission in vitro are mediated by receptors of the NOP type...
  19. ncbi request reprint Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies
    Raffaella Bigoni
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, Via Fossato di Mortara 17 19, 44100 Ferrara, Italy
    Naunyn Schmiedebergs Arch Pharmacol 365:442-9. 2002
    ..Moreover, as part of this study, we have identified two novel, highly potent and selective agonists for the OP(4) receptor, [(pF)Phe(4)]NC(1-13)NH(2) and [(pNO(2))Phe(4)]NC(1-13)NH(2)...
  20. doi request reprint Further studies on the pharmacological profile of the neuropeptide S receptor antagonist SHA 68
    Chiara Ruzza
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Peptides 31:915-25. 2010
    ..However the usefulness of this research tool is limited by its poor pharmacokinetic properties...
  21. doi request reprint UFP-112 a potent and long-lasting agonist selective for the Nociceptin/Orphanin FQ receptor
    Girolamo Calo'
    Department Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, and National Institute of Neuroscience, Ferrara, Italy
    CNS Neurosci Ther 17:178-98. 2011
    ..Moreover, important biological actions and possible therapeutic indications of NOP receptor agonists are discussed based on the results obtained with UFP-112 and compared with other peptide and nonpeptide NOP receptor ligands...
  22. ncbi request reprint Structure-activity relationship study on human urotensin II
    Remo Guerrini
    Department of Pharmaceutical Sciences and Biotechnology Centre, University of Ferrara, 44100 Ferrara, Italy
    J Pept Sci 11:85-90. 2005
    ..Moreover, this study led to the identification of UT receptor partial agonists (compounds 23 and 24) which can be used as chemical templates for further investigations aimed at the identification of selective antagonists...
  23. ncbi request reprint Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptors
    Valeria Camarda
    Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, Via Fossato di Mortara, 19, 44100 Ferrara, Italy
    Eur J Pharmacol 498:83-6. 2004
    ..24), and pure antagonist in the rat aorta bioassay, while as an agonist (pEC50 8.11) in a calcium mobilization assay performed in CHO(hUT) cells. Urantide should be considered a low efficacy partial agonist...
  24. pmc In vitro and in vivo pharmacological characterization of the neuropeptide s receptor antagonist [D-Cys(tBu)5]neuropeptide S
    Valeria Camarda
    Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, Ferrara, Italy
    J Pharmacol Exp Ther 328:549-55. 2009
    ..Moreover, using this tool together with receptor knockout mice studies, we demonstrated that the arousal-promoting action of NPS is because of the selective activation of the NPSR protein...
  25. ncbi request reprint [(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor
    Giacomo Carrà
    Department of Experimental and Clinical Medicine, Section of Pharmacology, via Fossato di Mortara 19, 44100 Ferrara, Italy
    J Pharmacol Exp Ther 312:1114-23. 2005
    ..These effects were comparable with those evoked by N/OFQ at 5 nmol. Collectively, these findings demonstrate that UFP-102 behaves as a highly potent and selective NOP receptor agonist that produces long-lasting effects in vivo...
  26. ncbi request reprint In vitro and in vivo pharmacological characterization of the nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-ol
    Ozge Gunduz
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Eur J Pharmacol 539:39-48. 2006
    ..The high potency, selectivity of action, and in vivo effectiveness make Ac-RYYRIK-ol a useful pharmacological tool for future studies in the field of N/OFQ and its NOP receptor...
  27. doi request reprint Nociceptin/orphanin FQ modulates motor behavior and primary motor cortex output through receptors located in substantia nigra reticulata
    Matteo Marti
    Department of Experimental and Clinical Medicine, University of Ferrara, Ferrara, Italy
    Neuropsychopharmacology 34:341-55. 2009
    ..We conclude that N/OFQ receptors located in the substantia nigra reticulata mediate N/OFQ biphasic control over motor behavior, possibly through changes of primary motor cortex output...
  28. ncbi request reprint Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)NH2 analogues. 2. In vivo studies
    Anna Rizzi
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, Via Fossato di Mortara 17 19, 44100 Ferrara, Italy
    Naunyn Schmiedebergs Arch Pharmacol 365:450-6. 2002
    ..pF)Phe(4)]NC(1-13)NH(2) was more potent and its in vivo effects were longer lasting than those of NC(1-13)NH(2) and NC...
  29. ncbi request reprint Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist
    Claudio Trapella
    Department of Pharmaceutical Sciences, Biotechnology Center, University of Ferrara, 44100 Ferrara, Italy
    Bioorg Med Chem 14:692-704. 2006
    ..The compound coded as Trap-101, an achiral analogue of J-113397, combines a pharmacological profile similar to that of the parent compound with a practical, high-yielding preparation...
  30. doi request reprint Pharmacological profile of NOP receptors coupled with calcium signaling via the chimeric protein G alpha qi5
    Valeria Camarda
    Department Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, National Institute of Neuroscience, via Fossato di Mortara 19, 44100, Ferrara, Italy
    Naunyn Schmiedebergs Arch Pharmacol 379:599-607. 2009
    ..These results demonstrated that the FlexStation II-Galpha(qi5)-NOP receptor calcium assay represents an adequate and useful screening for NOP receptor ligands, particularly for antagonists...
  31. ncbi request reprint Blockade of nociceptin/orphanin FQ receptor signaling in rat substantia nigra pars reticulata stimulates nigrostriatal dopaminergic transmission and motor behavior
    Matteo Marti
    Department of Experimental and Clinical Medicine, Section of Pharmacology, and Neuroscience Center, University of Ferrara, 44100 Ferrara, Italy
    J Neurosci 24:6659-66. 2004
    ..We conclude that NOP receptors in the substantia nigra pars reticulata, activated by endogenous N/OFQ, drive a physiologically inhibitory control on motor behavior, possibly via modulation of the nigrostriatal dopaminergic pathway...
  32. pmc [Nphe1,Arg14,Lys15]nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor
    Girolamo Calo
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, Via Fossato di Mortara, 17, 44100 Ferrara, Italy
    Br J Pharmacol 136:303-11. 2002
    ..5. UFP-101 is a novel, potent and selective NOP receptor antagonist which appears to be a useful tool for future investigations of the N/OFQ-NOP receptor system...
  33. ncbi request reprint Blockade of nociceptin/orphanin FQ transmission attenuates symptoms and neurodegeneration associated with Parkinson's disease
    Matteo Marti
    Department of Experimental and Clinical Medicine, Neuroscience Center, University of Ferrara, 44100 Ferrara, Italy
    J Neurosci 25:9591-601. 2005
    ..Based on these data, we propose that NOP receptor antagonists may represent a novel approach for combined (symptomatic and neuroprotective) therapy of Parkinson's disease...
  34. ncbi request reprint UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor
    Girolamo Calo
    Department Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Centre, University of Ferrara, Via Fossato di Mortara, 19, 44100 Ferrara, Italy
    CNS Drug Rev 11:97-112. 2005
    ....
  35. pmc A new ligand for the urotensin II receptor
    Valeria Camarda
    Department of Experimental and Clinical Medicine, Section of Pharmacology, Via Fossato di Mortara 17 19, Ferrara, 44100 Ferrara, Italy
    Br J Pharmacol 137:311-4. 2002
    ..56) showing however a small but consistent residual agonist activity. It is therefore proposed that [Orn(8)]U-II is a partial agonist at UT receptors...
  36. ncbi request reprint Pharmacological profile of nociceptin/orphanin FQ receptors
    Girolamo Calo'
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, Ferrara, Italy
    Clin Exp Pharmacol Physiol 29:223-8. 2002
    ..4. The results of these studies indicate that agents that selectively activate or block the OP4 receptor may represent new potential drugs for the treatment of human diseases...
  37. ncbi request reprint Urotensin II stimulates plasma extravasation in mice via UT receptor activation
    Raffaella Vergura
    Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Naunyn Schmiedebergs Arch Pharmacol 370:347-52. 2004
    ..The mouse plasma extravasation assay will be a useful tool in future studies aimed at characterizing the pharmacological features of novel UT receptor ligands in vivo...
  38. pmc Synthesis and separation of the enantiomers of the neuropeptide S receptor antagonist (9R/S)-3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide (SHA 68)
    Claudio Trapella
    Department of Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy
    J Med Chem 54:2738-44. 2011
    ..Calcium mobilization studies performed on cells expressing the recombinant NPSR demonstrated that compound 10 is the active enantiomer while the contribution of 10a to the NPSR antagonist properties of the racemic mixture is negligible...
  39. doi request reprint Anxiolytic- and panicolytic-like effects of Neuropeptide S in the mouse elevated T-maze
    Alice Pulga
    Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center and National Institute of Neuroscience, Ferrara, Italy
    Eur J Neurosci 36:3531-7. 2012
    ..In conclusion, this study demonstrated that NPS, via selective activation of the NPSR, promotes both anxiolytic- and panicolytic-like actions in the mouse ETM...
  40. pmc Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortex
    Matteo Marti
    Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, 44100 Ferrara, Italy
    Br J Pharmacol 138:91-8. 2003
    ..Nevertheless, they can be differentiated pharmacologically on the basis of responsiveness to [F/G]N/OFQ(1-13)NH(2) and time-dependent sensitivity towards non-peptide antagonists...
  41. ncbi request reprint [Arg(14),Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies
    Daniela Rizzi
    Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, Ferrara, Italy
    J Pharmacol Exp Ther 300:57-63. 2002
    ..Taken together, the present data demonstrate that [Arg(14),Lys(15)]NC behaves as a highly potent agonist of the OP(4) receptor and is able to produce long-lasting effects in vivo, compared with the natural ligand NC...
  42. ncbi request reprint Urodynamic effects of intravesical nociceptin/orphanin FQ in neurogenic detrusor overactivity: a randomized, placebo-controlled, double-blind study
    Massimo Lazzeri
    Department of Urology, University of Ferrara, Ferrara, Italy
    Urology 61:946-50. 2003
    ..To evaluate the acute urodynamic effects of the neuropeptide nociceptin/orphanin FQ (N/OFQ) in a selected group of patients with neurogenic detrusor overactivity incontinence in a randomized, placebo-controlled, double-blind study...
  43. doi request reprint Anti-inflammatory and analgesic effects displayed by peptides derived from PKI55 protein, an endogenous protein kinase C inhibitor
    Rita Selvatici
    Department of Experimental and Diagnostic Medicine, Medical Genetics Section, University of Ferrara, Ferrara, Italy
    Naunyn Schmiedebergs Arch Pharmacol 382:193-9. 2010
    ....
  44. doi request reprint Study of synthetic peptides derived from the PKI55 protein, a protein kinase C modulator, in human neutrophils stimulated by the methyl ester derivative of the hydrophobic N-formyl tripeptide for-Met-Leu-Phe-OH
    Rita Selvatici
    Dipartimento di Medicina Sperimentale e Diagnostica, Sezione Genetica Medica, Universita degli Studi di Ferrara, Italy
    FEBS J 275:449-57. 2008
    ..Western blotting experiments also demonstrated a selective reduction in the levels of the protein kinase C beta(1) isoform, which was previously demonstrated to be associated with the polymorphonuclear leukocyte chemotactic response...
  45. doi request reprint Unexpected impact of the number of glutamine residues on metal complex stability
    Nadine M Chiera
    Department of Chemical and Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy
    Metallomics 5:214-21. 2013
    ..This peculiar finding allows one to look at polyglutamine sequences, not only the ones present in some bacterial chaperones but also those involved in several neurodegenerative diseases, from a new perspective...
  46. ncbi request reprint Copper binding to the neurotoxic peptide PrP106-126: thermodynamic and structural studies
    Barbara Belosi
    Dipartimento di Chimica, Universita di Ferrara, Via L Borsari 46, 44100 Ferrara, Italy
    Chembiochem 5:349-59. 2004
    ..Solution structures for the main complexes are suggested...
  47. ncbi request reprint Modeling of overloaded gradient elution of nociceptin/orphanin FQ in reversed-phase liquid chromatography
    Nicola Marchetti
    Department of Chemistry, University of Ferrara Via L Borsari 46, 44100 Ferrara, Italy
    J Chromatogr A 1079:162-72. 2005
    ..The agreement between theoretical calculations and experimental overloaded band profiles appeared reasonably accurate...
  48. pmc Proteinase-activated receptor-1 (PAR-1) activation contracts the isolated human renal artery in vitro
    Michele Tognetto
    Department of Experimental and Clinical Medicine, Pharmacology Unit, University of Ferrara, S Anna Hospital, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Br J Pharmacol 139:21-7. 2003
    ..5. In agreement with the motor function data immunohistochemistry showed specific staining patterns for PAR-1 in the human renal artery. 6. Combined, these studies would suggest a possible role for PAR-1 in renal vascular homeostasis...
  49. ncbi request reprint [Nphe(1)]N/OFQ-(1-13)-NH(2) is a competitive and selective antagonist at nociceptin/orphanin FQ receptors mediating K(+) channel activation in rat periaqueductal gray slices
    Lih Chu Chiou
    Department of Pharmacology, College of Medicine, National Taiwan University, No 1, Jen Ai Rd, Section 1, Taipei 100, Taiwan
    Neuropharmacology 42:246-52. 2002
    ..It is concluded that Nphe acts as a pure, selective and competitive antagonist at native NOP receptors of ventrolateral PAG neurons...
  50. ncbi request reprint Nociceptin/orphanin FQ prevents gastric damage induced by cold-restraint stress in the rat by acting in the periphery
    Daniela Grandi
    Department of Human Anatomy, Pharmacology and Forensic Medicine, University of Parma, Via Volturno 39, I 43100 Parma, Italy
    Peptides 28:1572-9. 2007
    ..These results suggest that N/OFQ counteracts acute stress-induced gastric mucosal damage by interacting with NOP receptor and by influencing mucous cell activity...
  51. ncbi request reprint Pharmacological characterization of the nociceptin receptor which mediates reduction of alcohol drinking in rats
    Roberto Ciccocioppo
    Department of Pharmacological Sciences and Experimental Medicine, University of Camerino, 62032, Camerino, Italy
    Peptides 23:117-25. 2002
    ....
  52. ncbi request reprint Characterization of nociceptin/orphanin FQ binding sites in dog brain membranes
    Emma E Johnson
    University Department of Anaesthesia, Critical Care and Pain Management, Leicester Royal Infirmary, Leicester, United Kingdom
    Anesth Analg 97:741-7. 2003
    ..We have demonstrated a low density of NOP receptors, measured with two radioligands, in dog, and these receptors display a high degree of pharmacological similarity with those natively expressed in the rat...
  53. ncbi request reprint Effects of [(pF)Phe(4)]nociceptin/orphanin FQ-(1-13)NH(2) on GTPgamma(35)S binding and cAMP formation in Chinese hamster ovary cells expressing the human nociceptin/orphanin FQ receptor
    John McDonald
    University Department of Anaesthesia, Critical Care and Pain Management, Leicester Royal Infirmary, Leicester LE1 5WW, UK
    Eur J Pharmacol 443:7-12. 2002
    ..89-8.53) and III-BTD (pA(2)/pK(B) values 7.27-7.96). [(pF)Phe(4)] is therefore a potent full agonist at NOP receptors that will be useful as pharmacological tool for defining the role of N/OFQ-NOP system in health and disease...
  54. ncbi request reprint Effects of nociceptin/orphanin FQ receptor ligands on blood pressure, heart rate, and plasma catecholamine concentrations in guinea pigs
    Eiji Hashiba
    Department of Anesthesiology, University of Hirosaki School of Medicine, 036 8562 Hirosaki, Japan
    Naunyn Schmiedebergs Arch Pharmacol 367:342-7. 2003
    ....
  55. ncbi request reprint Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09126 Cagliari, Italy
    J Med Chem 45:5556-63. 2002
    ....
  56. ncbi request reprint The SH3 domain of nebulin binds selectively to type II peptides: theoretical prediction and experimental validation
    Anastasia S Politou
    Laboratory of Biological Chemistry, Medical School, University of Ioannina, Ioannina 45110, Greece
    J Mol Biol 316:305-15. 2002
    ..The strategy outlined here is of more general applicability and may provide a valuable tool to identify potential partners of SH3 domains and of other peptide-binding modules...
  57. ncbi request reprint Effects of chronic nociceptin/orphanin FQ exposure on cAMP accumulation and receptor density in Chinese hamster ovary cells expressing human nociceptin/orphanin FQ receptors
    Yoshio Hashimoto
    University Department of Anaesthesia, Critical Care and Pain Management, Leicester Royal Infirmary, Leicester, LE1 5WW, UK
    Eur J Pharmacol 449:17-22. 2002
    ..There was a positive correlation between pEC(50) for cAMP inhibition and B(max). The lack of effect on maximum cAMP response probably results from receptor overexpression and the creation of a receptor reserve...
  58. ncbi request reprint Intrathecal [Nphe1]nociceptin( 1-13)NH2 selectively reduces the spinal inhibitory effect of nociceptin
    Isabella S Xu
    Department of Medical Laboratory Sciences and Technology, Karolinska Institutet, Huddinge University Hospital, Sweden
    Life Sci 70:1151-7. 2002
    ..It can be further suggested that the spinal inhibitory effect of nociceptin may be tonically active...
  59. ncbi request reprint Proinflammatory and vasodilator effects of nociceptin/orphanin FQ in the rat mesenteric microcirculation are mediated by histamine
    Zoe L S Brookes
    University of Sheffield, Academic Anaesthesia Unit and Microcirculation Research Group, Royal Hallamshire Hospital, Sheffield S10 2JF, UK
    Am J Physiol Heart Circ Physiol 293:H2977-85. 2007
    ..Therefore, N/OFQ-NOP has an important role in microvascular inflammation, and this may be targeted during disease, particularly as we have proven that UFP-101 is an effective antagonist of microvascular responses in vivo...
  60. ncbi request reprint Peripheral mechanisms involved in gastric mucosal protection by intracerebroventricular and intraperitoneal nociceptin in rats
    Carlo Polidori
    Department of Experimental Medicine and Public Health, University of Camerino, Italy
    Endocrinology 146:3861-7. 2005
    ..The study provides evidence that N/OFQ contributes to neurally mediated gastric mucosal protection...
  61. ncbi request reprint Functional selectivity of nociceptin/orphanin FQ peptide receptor partial agonists on cardiovascular and renal function
    Daniel R Kapusta
    Department of Pharmacology and Experimental Therapeutics, Louisiana State University Health Sciences Center, 1901 Perdido St, New Orleans, LA 70112, USA
    J Pharmacol Exp Ther 314:643-51. 2005
    ..c.v., cardiovascular depressor; i.c.v. and i.v., water diuresis), partial agonist (i.v., submaximal hypotension) to antagonist (i.v., blockade of N/OFQ-evoked bradycardia and hypotension) behavior...
  62. ncbi request reprint The interaction of highly helical structural mutants with the NOP receptor discloses the role of the address domain of nociceptin/orphanin FQ
    Teodorico Tancredi
    Istituto di Chimica Biomolecolare, CNR, Via Campi Flegrei 34, 80078 Pozzuoli, Italy
    Chemistry 11:2061-70. 2005
    ..This hypothesis is also consistent with previous data on this hinge region obtained by systematic substitution of Thr, Gly, and Ala with Pro...
  63. pmc Activation of the nociceptin/orphanin FQ receptor reduces bronchoconstriction and microvascular leakage in a rabbit model of gastroesophageal reflux
    Bruno D'Agostino
    Department of Experimental Medicine Section of Pharmacology, Faculty of Medicine and Surgery, 2nd University of Naples, Via Constantinopoli 16, 80138 Naples, Italy
    Br J Pharmacol 144:813-20. 2005
    ..7. These results suggest that bronchoconstriction and airway plasma extravasation induced by i.oe. HCl instillation are inhibited by activation of prejunctional NOP receptors...
  64. ncbi request reprint Structural and dynamic characterization of copper(II) binding of the human prion protein outside the octarepeat region
    Francesco Berti
    Faculty of Chemistry, University of Wroclaw, F Joliot Curie 15, 50383 Wroclaw, Poland
    Chemistry 13:1991-2001. 2007
    ....
  65. ncbi request reprint Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I 09126 Cagliary, Italy
    J Med Chem 47:4066-71. 2004
    ....
  66. ncbi request reprint Gastrointestinal effects of intracerebroventricularly injected nociceptin/orphaninFQ in rats
    Maria Broccardo
    Department of Human Physiology and Pharmacology, University La Sapienza Ple A Moro 5 00185, Rome, Italy
    Peptides 25:1013-20. 2004
    ..These results indicate that N/OFQ activates via NOP receptor stimulation a central inhibitory pathway modulating gastrointestinal propulsive activity and gastric acid secretion in rats...
  67. ncbi request reprint Functional coupling of the nociceptin/orphanin FQ receptor in dog brain membranes
    Emma E Johnson
    University Department of Anaesthesia, Critical Care and Pain Management, Leicester Royal Infirmary, Leicester, LE15WW, UK
    Brain Res 1003:18-25. 2004
    ..33+/-0.02 was obtained). Despite relatively low receptor density, we were able to detect functional activity of native dog NOP, with pharmacology consistent with reports for other species...
  68. ncbi request reprint Nociceptin/orphanin FQ inhibits electrically induced contractions of the human bronchus via NOP receptor activation
    Marco Basso
    UPRES EA 220 Pharmacology, University of Versailles and UFR Biomédicale des Saint Péres, 45 Rue des Saints Peres, F 75006 Paris, France
    Peptides 26:1492-6. 2005
    ..In conclusion, the present data demonstrate that N/OFQ inhibited acetylcholine (ACh) release in the human bronchi via NOP receptor activation. This effect may involve stimulation of potassium currents...
  69. ncbi request reprint Blockade of nociceptin/orphanin FQ transmission in rat substantia nigra reverses haloperidol-induced akinesia and normalizes nigral glutamate release
    Matteo Marti
    Department of Experimental and Clinical Medicine, Section of Pharmacology, Neuroscience Center, University of Ferrera, Ferrera, Italy
    J Neurochem 91:1501-4. 2004
    ..NOP receptor antagonists may be beneficial in the symptomatic therapy of parkinsonism, via normalization of subthalamonigral glutamatergic transmission...
  70. pmc Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1)
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124, Cagliari, Italy
    J Med Chem 48:8112-4. 2005
    ..44-1.42 nM). Only delta antagonism (pA(2)=8.52-10.14) was observed; micro agonism (IC(50)=30-450 nM) was not correlated with changes in alkylating agent or delta antagonism, and some compounds yielded mixed delta antagonism/micro agonism...
  71. ncbi request reprint [Nphe1,Arg14,Lys15]N/OFQ-NH2 is a competitive antagonist of NOP receptors in the periaqueductal gray
    Lih Chu Chiou
    Department of Pharmacology, College of Medicine, National Taiwan University, No 1, Jen Ai Rd, Section 1, Taipei 100, Taiwan
    Eur J Pharmacol 515:47-53. 2005
    ..It is concluded that UFP-101 is a potent and competitive peptide antagonist of NOP receptors that mediate GIRK channel activation in ventrolateral periaqueductal gray neurons...
  72. ncbi request reprint Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I09126 Cagliary, Italy
    J Med Chem 45:713-20. 2002
    ....
  73. ncbi request reprint The alpha-to-beta conformational transition of Alzheimer's Abeta-(1-42) peptide in aqueous media is reversible: a step by step conformational analysis suggests the location of beta conformation seeding
    Simona Tomaselli
    Dipartimento di Chimica, Universita Federico II di Napoli, Via Cintia, 80126 Napoli, Italy
    Chembiochem 7:257-67. 2006
    ..The structures obtained might help to find regions that are more affected by environmental conditions in vivo. This could in turn aid the design of molecules able to inhibit fibril deposition or revert oligomerization processes...
  74. pmc New approaches to high-throughput structure characterization of SH3 complexes: the example of Myosin-3 and Myosin-5 SH3 domains from S. cerevisiae
    Valeria Musi
    National Institute for Medical Research, London NW71AA, United Kingdom
    Protein Sci 15:795-807. 2006
    ..From our study, we propose a consensus sequence that may provide a useful guideline to identify new natural partners and suggest a strategy of more general applicability that may be of use in other structural proteomic studies...
  75. ncbi request reprint Solution structure of nociceptin peptides
    Pietro Amodeo
    Istituto di Chimica Biomolecolare del CNR, Pozzuoli, Italy
    J Pept Sci 8:497-509. 2002
    ..None of the structural investigations yielded a completely reliable bioactive conformation, but the global conformation of the peptides in biomimetic environments can shed light on their interaction with receptors...
  76. ncbi request reprint Solution structure of the Alzheimer amyloid beta-peptide (1-42) in an apolar microenvironment. Similarity with a virus fusion domain
    Orlando Crescenzi
    Dipartimento di Chimica, Universita degli Studi di Napoli Federico II, Italy
    Eur J Biochem 269:5642-8. 2002
    ..The surprising similarity of this structure, as well as the sequence of the C-terminal moiety, with those of the fusion domain of influenza hemagglutinin suggests a direct mechanism of neurotoxicity...
  77. ncbi request reprint Crystal structures of dipeptides containing the Dmt-Tic pharmacophore
    Sharon D Bryant
    Peptide Neurochemistry, LCBRA, National Institute of Environmental Health Sciences, P O Box 12233, Mail Drop C3 04, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 45:5506-13. 2002
    ..Furthermore, the structural results support the hypothesis that expanded dimensions between aromatic nuclei is important for acquiring mu-agonism...
  78. ncbi request reprint Chronic intracerebroventricular infusion of nociceptin/orphanin FQ increases food and ethanol intake in alcohol-preferring rats
    Carlo Cifani
    Department of Experimental Medicine and Public Health, University of Camerino, Via Scalzino 5, 62032 Camerino MC, Italy
    Peptides 27:2803-10. 2006
    ..Moreover, the data suggest that continuous activation of the opioidergic N/OFQ receptor is not a suitable way to reduce alcohol abuse...
  79. ncbi request reprint Synthesis and opioid activity of N,N-dimethyl-Dmt-Tic-NH-CH(R)-R' analogues: acquisition of potent delta antagonism
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I 09126, Cagliary, Italy
    Bioorg Med Chem 11:5435-41. 2003
    ..With the exception of compound 1', the change in the hydrophobic environment at the N-terminus and formation of a tertiary amine by N,N-dimethylation in analogues of the Dmt-Tic pharmacophore produced potent delta-selective antagonists...
  80. doi request reprint Synthesis and antimicrobial activity of dermaseptin S1 analogues
    Dianella Savoia
    Department of Clinical and Biological Sciences, University of Torino, S Luigi Gonzaga Hospital, Regione Gonzole 10, 10143 Orbassano, Torino, Italy
    Bioorg Med Chem 16:8205-9. 2008
    ..Our data showed a dose-dependent killing effect by most DS1 derivatives. Maximal antibacterial activity was displayed by a 16-mer peptide that was more active than native DS1...
  81. ncbi request reprint Quantitative study of [(pF)Phe4,Arg14,Lys15]nociceptin/orphanin FQ-NH2 (UFP-102) at NOP receptors in rat periaqueductal gray slices
    Chia Ju Kuo
    Institute of Pharmacology, College of Medicine, National Taiwan University, Taipei, Taiwan
    Eur J Pharmacol 579:110-5. 2008
    ..7. These results suggest that UFP-102 is a full agonist at the postsynaptic NOP receptors of the midbrain of rats and is 5 fold more potent than N/OFQ...
  82. ncbi request reprint Conformation-activity relationship of neuropeptide S and some structural mutants: helicity affects their interaction with the receptor
    Teodorico Tancredi
    Istituto di Chimica Biomolecolare, CNR, Via Campi Flegrei 34, I 80078 Pozzuoli, Italy
    J Med Chem 50:4501-8. 2007
    ..The identification of hNPSR partial agonists heralds the possibility of designing pure NPS receptor antagonists...