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Genomes and Genes | Remo GuerriniSummaryAffiliation: University of Ferrara Country: Italy Publications
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Synthesis and biological activity of human neuropeptide S analogues modified in position 5: identification of potent and pure neuropeptide S receptor antagonistsRemo 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...
Nociceptin/Orphanin FQ(1-13)NH2 analogues modified in the Phe1-Gly2 peptide bondRemo 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....- Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonistsRemo 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... 
Neurobiology, pharmacology, and medicinal chemistry of neuropeptide S and its receptorRemo 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...- In vitro and in vivo studies on UFP-112, a novel potent and long lasting agonist selective for the nociceptin/orphanin FQ receptorAnna 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... - N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligandsRemo 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.... - 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... - Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamideClaudio 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... - Structure-activity study at positions 3 and 4 of human neuropeptide SValeria Camarda
Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, Italy
Bioorg Med Chem 16:8841-5. 2008.... - Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acidsMarika Arduin
Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, 44100 Ferrara, Italy
Bioorg Med Chem 15:4434-43. 2007.... - Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24Carmela 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... - Synthesis and biological activity of human neuropeptide S analogues modified in position 2Valeria 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.... - Anxiolytic- and antidepressant-like activities of H-Dmt-Tic-NH-CH(CH2-COOH)-Bid (UFP-512), a novel selective delta opioid receptor agonistRaffaella 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.... - 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... - Further studies on the pharmacological features of the nociceptin/orphanin FQ receptor ligand ZP120Carmela 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.... - UFP-101 antagonizes the spinal antinociceptive effects of nociceptin/orphanin FQ: behavioral and electrophysiological studies in miceCristiano 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... - Structure-activity relationship study on Tyr9 of urotensin-II(4-11): identification of a partial agonist of the UT receptorMadura 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... - Endogenous nociceptin/orphanin FQ signalling produces opposite spinal antinociceptive and supraspinal pronociceptive effects in the mouse formalin test: pharmacological and genetic evidencesAnna 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... - Further studies on the pharmacological profile of the neuropeptide S receptor antagonist SHA 68Chiara 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... - Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studiesRaffaella 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)... - UFP-112 a potent and long-lasting agonist selective for the Nociceptin/Orphanin FQ receptorGirolamo 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... - In vitro and in vivo pharmacological characterization of the neuropeptide s receptor antagonist [D-Cys(tBu)5]neuropeptide SValeria 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... - Structure-activity relationship study on human urotensin IIRemo 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... - Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptorsValeria 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... - [(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptorGiacomo 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... - In vitro and in vivo pharmacological characterization of the nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-olOzge 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... - Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonistClaudio 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... - Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)NH2 analogues. 2. In vivo studiesAnna 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... - Nociceptin/orphanin FQ modulates motor behavior and primary motor cortex output through receptors located in substantia nigra reticulataMatteo 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... - Pharmacological profile of NOP receptors coupled with calcium signaling via the chimeric protein G alpha qi5Valeria 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... - Blockade of nociceptin/orphanin FQ receptor signaling in rat substantia nigra pars reticulata stimulates nigrostriatal dopaminergic transmission and motor behaviorMatteo 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... - [Nphe1,Arg14,Lys15]nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptorGirolamo 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... - Blockade of nociceptin/orphanin FQ transmission attenuates symptoms and neurodegeneration associated with Parkinson's diseaseMatteo 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... - A new ligand for the urotensin II receptorValeria 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... - UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptorGirolamo 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.... - Urotensin II stimulates plasma extravasation in mice via UT receptor activationRaffaella 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... - Pharmacological profile of nociceptin/orphanin FQ receptorsGirolamo 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... - 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... - Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortexMatteo 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... - [Arg(14),Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studiesDaniela 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... - Urodynamic effects of intravesical nociceptin/orphanin FQ in neurogenic detrusor overactivity: a randomized, placebo-controlled, double-blind studyMassimo Lazzeri
Department of Urology, University of Ferrara, Ferrara, Italy
Urology 61:946-50. 2003..These findings apply nociceptin orphan peptide receptor agonists as potential novel drugs for the treatment of neurogenic urinary incontinence... - Anti-inflammatory and analgesic effects displayed by peptides derived from PKI55 protein, an endogenous protein kinase C inhibitorRita Selvatici
Department of Experimental and Diagnostic Medicine, Medical Genetics Section, University of Ferrara, Ferrara, Italy
Naunyn Schmiedebergs Arch Pharmacol 382:193-9. 2010.... - 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-OHRita 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... - Anxiolytic- and panicolytic-like effects of Neuropeptide S in the mouse elevated T-mazeAlice 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... - Modeling of overloaded gradient elution of nociceptin/orphanin FQ in reversed-phase liquid chromatographyNicola 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... - Copper binding to the neurotoxic peptide PrP106-126: thermodynamic and structural studiesBarbara 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... - Unexpected impact of the number of glutamine residues on metal complex stabilityNadine 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... - Proteinase-activated receptor-1 (PAR-1) activation contracts the isolated human renal artery in vitroMichele 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... - Effects of nociceptin/orphanin FQ receptor ligands on blood pressure, heart rate, and plasma catecholamine concentrations in guinea pigsEiji Hashiba
Department of Anesthesiology, University of Hirosaki School of Medicine, 036 8562 Hirosaki, Japan
Naunyn Schmiedebergs Arch Pharmacol 367:342-7. 2003.... - Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophoreGianfranco Balboni
Department of Toxicology, University of Cagliari, I-09126 Cagliari, Italy
J Med Chem 45:5556-63. 2002.... - Pharmacological characterization of the nociceptin receptor which mediates reduction of alcohol drinking in ratsRoberto Ciccocioppo
Department of Pharmacological Sciences and Experimental Medicine, University of Camerino, 62032, Camerino, Italy
Peptides 23:117-25. 2002.... - Effects of chronic nociceptin/orphanin FQ exposure on cAMP accumulation and receptor density in Chinese hamster ovary cells expressing human nociceptin/orphanin FQ receptorsYoshio 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... - 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 receptorJohn 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... - The SH3 domain of nebulin binds selectively to type II peptides: theoretical prediction and experimental validationAnastasia 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... - Intrathecal [Nphe1]nociceptin( 1-13)NH2 selectively reduces the spinal inhibitory effect of nociceptinIsabella 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... - Activation of the nociceptin/orphanin FQ receptor reduces bronchoconstriction and microvascular leakage in a rabbit model of gastroesophageal refluxBruno 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... - [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 slicesLih 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... - Characterization of nociceptin/orphanin FQ binding sites in dog brain membranesEmma 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... - Proinflammatory and vasodilator effects of nociceptin/orphanin FQ in the rat mesenteric microcirculation are mediated by histamineZoe 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... - Peripheral mechanisms involved in gastric mucosal protection by intracerebroventricular and intraperitoneal nociceptin in ratsCarlo 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... - Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonismGianfranco Balboni
Department of Toxicology, University of Cagliary, I-09126 Cagliary, Italy
J Med Chem 47:4066-71. 2004.... - The interaction of highly helical structural mutants with the NOP receptor discloses the role of the address domain of nociceptin/orphanin FQTeodorico 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... - Structural and dynamic characterization of copper(II) binding of the human prion protein outside the octarepeat regionFrancesco Berti
Faculty of Chemistry, University of Wroclaw, F Joliot Curie 15, 50383 Wroclaw, Poland
Chemistry 13:1991-2001. 2007.... - Functional selectivity of nociceptin/orphanin FQ peptide receptor partial agonists on cardiovascular and renal functionDaniel 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... - Gastrointestinal effects of intracerebroventricularly injected nociceptin/orphaninFQ in ratsMaria 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... - Functional coupling of the nociceptin/orphanin FQ receptor in dog brain membranesEmma 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... - Nociceptin/orphanin FQ prevents gastric damage induced by cold-restraint stress in the rat by acting in the peripheryDaniela 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... - Nociceptin/orphanin FQ inhibits electrically induced contractions of the human bronchus via NOP receptor activationMarco Basso
UPRES EA 220-Pharmacology, , , 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... - Blockade of nociceptin/orphanin FQ transmission in rat substantia nigra reverses haloperidol-induced akinesia and normalizes nigral glutamate releaseMatteo 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... - Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed propertiesGianfranco Balboni
Department of Toxicology, University of Cagliary, I09126 Cagliary, Italy
J Med Chem 45:713-20. 2002.... - 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... - 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 seedingSimona Tomaselli
Dipartimento di Chimica, , 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... - [Nphe1,Arg14,Lys15]N/OFQ-NH2 is a competitive antagonist of NOP receptors in the periaqueductal grayLih 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... - New approaches to high-throughput structure characterization of SH3 complexes: the example of Myosin-3 and Myosin-5 SH3 domains from S. cerevisiaeValeria 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... - Solution structure of nociceptin peptidesPietro 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... - Solution structure of the Alzheimer amyloid beta-peptide (1-42) in an apolar microenvironment. Similarity with a virus fusion domainOrlando Crescenzi
Dipartimento di Chimica, , 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... - Crystal structures of dipeptides containing the Dmt-Tic pharmacophoreSharon 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... - Chronic intracerebroventricular infusion of nociceptin/orphanin FQ increases food and ethanol intake in alcohol-preferring ratsCarlo 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... - Synthesis and antimicrobial activity of dermaseptin S1 analoguesDianella 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... - Conformation-activity relationship of neuropeptide S and some structural mutants: helicity affects their interaction with the receptorTeodorico 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... - Quantitative study of [(pF)Phe4,Arg14,Lys15]nociceptin/orphanin FQ-NH2 (UFP-102) at NOP receptors in rat periaqueductal gray slicesChia 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... - Synthesis and opioid activity of N,N-dimethyl-Dmt-Tic-NH-CH(R)-R' analogues: acquisition of potent delta antagonismGianfranco 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...