Search

Your search keyword '"Calo’, Girolamo"' showing total 37 results
Start Over Author "Calo’, Girolamo" Publisher wiley
37 results on '"Calo’, Girolamo"'

5. Kallikrein–Kinin System

Author

Motta, Guacyara, primary, Tersariol, Ivarne LS, additional, Calo, Girolamo, additional, Gobeil, Fernand, additional, and Regoli, Domenico, additional

Published
2018
Full Text
View/download PDF

12. Pharmacological characterization of tachykinin tetrabranched derivatives

Author

Ruzza, Chiara, primary, Rizzi, Anna, additional, Malfacini, Davide, additional, Cerlesi, Maria Camilla, additional, Ferrari, Federica, additional, Marzola, Erika, additional, Ambrosio, Caterina, additional, Gro, Cristina, additional, Severo, Salvadori, additional, Costa, Tommaso, additional, Calo, Girolamo, additional, and Guerrini, Remo, additional

Published
2014
Full Text
View/download PDF

14. [Dmt1]N/OFQ(1‐13)‐NH2, a potent NOP/MOP receptor mixed agonist

Author

Calo’, Girolamo, primary, Molinari, Stefano, additional, Camarda, Valeria, additional, Rizzi, Anna, additional, Marzola, Giuliano, additional, Salvadori, Severo, additional, Marzola, Erika, additional, Molinari, Paola, additional, McDonald, John, additional, Ko, Mei-Chuan, additional, Lambert, David, additional, and Guerrini, Remo, additional

Published
2012
Full Text
View/download PDF

20. The peptidic urotensin-II receptor ligand GSK248451 possesses less intrinsic activity than the low-efficacy partial agonists SB-710411 and urantide in native mammalian tissues and recombinant cell systems

Author

Behm, David J, primary, Stankus, Gerald, additional, Doe, Christopher P A, additional, Willette, Robert N, additional, Sarau, Henry M, additional, Foley, James J, additional, Schmidt, Dulcie B, additional, Nuthulaganti, Parvathi, additional, Fornwald, James A, additional, Ames, Robert S, additional, Lambert, David G, additional, Calo', Girolamo, additional, Camarda, Valeria, additional, Aiyar, Nambi V, additional, and Douglas, Stephen A, additional

Published
2006
Full Text
View/download PDF

24. Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortex

Author

Marti, Matteo, primary, Stocchi, Sara, additional, Paganini, Francesca, additional, Mela, Flora, additional, Risi, Carmela De, additional, Calo', Girolamo, additional, Guerrini, Remo, additional, Barnes, Timothy A, additional, Lambert, David G, additional, Beani, Lorenzo, additional, Bianchi, Clementina, additional, and Morari, Michele, additional

Published
2003
Full Text
View/download PDF

27. [Nphe1 ,Arg14 ,Lys15 ]Nociceptin-NH2 , a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor

Author

Calo, Girolamo, primary, Rizzi, Anna, additional, Rizzi, Daniela, additional, Bigoni, Raffaella, additional, Guerrini, Remo, additional, Marzola, Giuliano, additional, Marti, Matteo, additional, McDonald, John, additional, Morari, Michele, additional, Lambert, David G, additional, Salvadori, Severo, additional, and Regoli, Domenico, additional

Published
2002
Full Text
View/download PDF

33. Comparison of the effects of [Phe1Ψ(CH2‐NH)Gly2]Nociceptin (1–13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors

Author

Okawa, Hirobumi, primary, Nicol, Beverley, additional, Bigoni, Raffaella, additional, Hirst, Robert A, additional, Calo', Girolamo, additional, Guerrini, Remo, additional, Rowbotham, David J, additional, Smart, Darren, additional, McKnight, Alexander T, additional, and Lambert, David G, additional

Published
1999
Full Text
View/download PDF

35. In vitro and in vivo study of butyrylfentanyl and 4-fluorobutyrylfentanyl in female and male mice: Role of the CRF 1 receptor in cardiorespiratory impairment.

Author

Bilel S, Azevedo Neto J, Tirri M, Corli G, Bassi M, Fantinati A, Serpelloni G, Malfacini D, Trapella C, Calo' G, and Marti M

Subjects
Animals, Male, Female, Mice, beta-Arrestin 2 metabolism, Receptors, Opioid, mu agonists, Receptors, Opioid, mu metabolism, Receptors, Opioid, mu antagonists & inhibitors, Humans, beta-Arrestins metabolism, CRF Receptor, Type 1, Fentanyl pharmacology, Fentanyl analogs & derivatives, Receptors, Corticotropin-Releasing Hormone antagonists & inhibitors, Receptors, Corticotropin-Releasing Hormone metabolism, Receptors, Corticotropin-Releasing Hormone agonists, Analgesics, Opioid pharmacology
Abstract

Background and Purpose: Fentanyl analogues have been implicated in many cases of intoxication and death with overdose worldwide. The aim of this study is to investigate the pharmaco-toxicology of two fentanyl analogues: butyrylfentanyl (BUF) and 4-fluorobutyrylfentanyl (4F-BUF)., Experimental Approach: In vitro, we measured agonist opioid receptor efficacy, potency, and selectivity and ability to promote interaction of the μ receptor with G protein and β-arrestin 2. In vivo, we evaluated thermal antinociception, stimulated motor activity and cardiorespiratory changes in female and male CD-1 mice injected with BUF or 4F-BUF (0.1-6 mg·kg -1 ). Opioid receptor specificity was investigated using naloxone (6 mg·kg -1 ). We investigated the possible role of stress in increasing cardiorespiratory toxicity using the corticotropin-releasing factor 1 (CRF 1 ) antagonist antalarmin (10 mg·kg -1 )., Key Results: Agonists displayed the following rank of potency at μ receptors: fentanyl > 4F-BUF > BUF. Fentanyl and BUF behaved as partial agonists for the β-arrestin 2 pathway, whereas 4F-BUF did not promote β-arrestin 2 recruitment. In vivo, we revealed sex differences in motor and cardiorespiratory impairments but not antinociception induced by BUF and 4F-BUF. Antalarmin alone was effective in blocking respiratory impairment induced by BUF in both sexes but not 4F-BUF. The combination of naloxone and antalarmin significantly enhanced naloxone reversal of the cardiorespiratory impairments induced by BUF and 4F-BUF in mice., Conclusion and Implications: In this study, we have uncovered a novel mechanism by which synthetic opioids induce respiratory depression, shedding new light on the role of CRF 1 receptors in cardiorespiratory impairments by μ agonists., (© 2024 The Author(s). British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.)

Published
2025
Full Text
View/download PDF

36. Neurobiology, pharmacology, and medicinal chemistry of neuropeptide S and its receptor.

Author

Guerrini R, Salvadori S, Rizzi A, Regoli D, and Calo' G

Subjects
Amino Acid Sequence, Animals, Humans, Ligands, Molecular Sequence Data, Neuropeptides chemistry, Chemistry, Pharmaceutical, Neurobiology, Neuropeptides metabolism, Neuropeptides pharmacology, Receptors, Neuropeptide chemistry, Receptors, Neuropeptide metabolism
Abstract

Neuropeptide S (NPS) is the last neuropeptide identified via reverse pharmacology techniques. NPS selectively binds and activates a previous orphan GPCR, now named NPSR, producing intracellular calcium mobilization and increases in cAMP levels. Biological functions modulated by the NPS/NPSR system include anxiety, arousal, locomotion, food intake, memory, and drug addiction. The primary sequence of NPS (in humans SFRNGVGTGMKKTSFQRAKS) is highly conserved among vertebrates especially at the N-terminus. Ala- and D-scan studies demonstrated that this part of the molecule is crucial for biological activity. Focused structure-activity studies performed on Phe(2), Arg(3), and Asn(4) confirmed this indication and revealed the chemical requirements of these positions for NPSR binding and activation. The sequence Gly(5)-Val(6)-Gly(7) seems to be important for shaping the bioactive conformation of the peptide. Structure-activity studies on Gly(5) enabled identification of the first generation of peptidergic NPSR pure antagonists including [D-Cys(tBu)(5)]NPS and [D-Val(5)]NPS whose antagonist properties were confirmed in vivo. Finally, the pharmacological features of substituted bicyclic piperazine molecules (e.g. SHA 68 (3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide) were recently published making available the first generation of nonpeptide NPSR antagonists. 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., ((c) 2009 Wiley Periodicals, Inc.)

Published
2010
Full Text
View/download PDF

37. [Nphe1,Arg14,Lys15]nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor.

Author

Calo G, Rizzi A, Rizzi D, Bigoni R, Guerrini R, Marzola G, Marti M, McDonald J, Morari M, Lambert DG, Salvadori S, and Regoli D

Subjects
Animals, CHO Cells, Cricetinae, Dose-Response Relationship, Drug, Guinea Pigs, In Vitro Techniques, Male, Mice, Motor Activity drug effects, Motor Activity physiology, Opioid Peptides chemistry, Pain Measurement drug effects, Peptide Fragments chemistry, Peptide Fragments metabolism, Rabbits, Rats, Rats, Sprague-Dawley, Nociceptin Receptor, Narcotic Antagonists, Opioid Peptides metabolism, Opioid Peptides pharmacology, Peptide Fragments pharmacology, Receptors, Opioid metabolism
Abstract

1. Nociceptin/orphanin FQ (N/OFQ) modulates several biological functions by activating a specific G-protein coupled receptor (NOP). Few molecules are available that selectively activate or block the NOP receptor. Here we describe the in vitro and in vivo pharmacological profile of a novel NOP receptor ligand, [Nphe(1),Arg(14),Lys(15)]N/OFQ-NH(2) (UFP-101). 2. UFP-101 binds to the human recombinant NOP receptor expressed in Chinese hamster ovary (CHO) cells with high affinity (pK(i) 10.2) and shows more than 3000 fold selectivity over classical opioid receptors. UFP-101 competitively antagonizes the effects of N/OFQ on GTPgamma(35)S binding in CHO(hNOP) cell membranes (pA(2) 9.1) and on cyclic AMP accumulation in CHO(hNOP) cells (pA(2) 7.1), being per se inactive at concentrations up to 10 microM. 3. In isolated peripheral tissues of mice, rats and guinea-pigs, and in rat cerebral cortex synaptosomes preloaded with [(3)H]-5-HT, UFP-101 competitively antagonized the effects of N/OFQ with pA(2) values in the range of 7.3 - 7.7. In the same preparations, the peptide was inactive alone and did not modify the effects of classical opioid receptor agonists. 4. UFP-101 is also active in vivo where it prevented the depressant action on locomotor activity and the pronociceptive effect induced by 1 nmol N/OFQ i.c.v. in the mouse. In the tail withdrawal assay, UFP-101 at 10 nmol produces per se a robust and long lasting antinociceptive effect. 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.

Published
2002
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results