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Your search keyword '"Opiod receptors"' showing total 4 results
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4 results on '"Opiod receptors"'

1. Novel Mixed NOP/Opioid Receptor Peptide Agonists

Author

Erika Marzola, Chiara Ruzza, Davide Illuminati, Salvatore Pacifico, Delia Preti, Claudio Trapella, Davide Malfacini, Ettore Lo Cascio, Valentina Albanese, Martina Marangoni, Remo Guerrini, Alessandro Arcovito, Martina Fabbri, Davide Fattori, Victor A D Holanda, Romina Nassini, Chiara Sturaro, Girolamo Calò, Federica Ferrari, and Stefano Della Longa

Subjects
Male, Opiod receptors, NOP, MOP, Nociceptin, NOP, Receptors, Opioid, mu, Peptide, Pharmacology, 01 natural sciences, Nociceptin Receptor, Opioid receptor, Drug Discovery, Receptors, Receptor, chemistry.chemical_classification, Animals, Binding Sites, Cough, Disease Models, Animal, Guinea Pigs, Humans, Hydrophobic and Hydrophilic Interactions, Molecular Dynamics Simulation, Peptides, Receptors, Opioid, Recombinant Proteins, Structure-Activity Relationship, 0303 health sciences, Chemistry, Nociceptin, Nociceptin receptor, Molecular Medicine, μ-opioid receptor, medicine.drug, Agonist, medicine.drug_class, Opioid, Article, NO, 03 medical and health sciences, medicine, Settore BIO/10 - BIOCHIMICA, 030304 developmental biology, MOP, Animal, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, mu, Disease Models
Abstract

The nociceptin/orphanin FQ (N/OFQ)/N/OFQ receptor (NOP) system controls different biological functions including pain and cough reflex. Mixed NOP/opioid receptor agonists elicit similar effects to strong opioids but with reduced side effects. In this work, 31 peptides with the general sequence [Tyr/Dmt1,Xaa5]N/OFQ(1-13)-NH2 were synthesized and pharmacologically characterized for their action at human recombinant NOP/opioid receptors. The best results in terms of NOP versus mu opioid receptor potency were obtained by substituting both Tyr1 and Thr5 at the N-terminal portion of N/OFQ(1-13)-NH2 with the noncanonical amino acid Dmt. [Dmt1,5]N/OFQ(1-13)-NH2 has been identified as the most potent dual NOP/mu receptor peptide agonist so far described. Experimental data have been complemented by in silico studies to shed light on the molecular mechanisms by which the peptide binds the active form of the mu receptor. Finally, the compound exerted antitussive effects in an in vivo model of cough.

Published
2021

2. Synthesis, biological evaluation and docking studies of a novel class of sulfur-bridged diazabicyclo[3.3.1]nonanes

Author

Stefania Gessi, Gérard Aimé Pinna, Veronika Temml, Girolamo Calo, Sonja Herdlinger, Enrica Battistello, Paola Corona, Nicoletta Galeotti, Daniela Schuster, Battistina Asproni, Stefania Merighi, Gabriele Murineddu, and Chiara Sturaro

Subjects
9-diazabicyclo[3.3.1]nonanes, Binding affinities, Opiod receptors, μ receptor, Stereochemistry, chemistry.chemical_element, 01 natural sciences, Biochemistry, NO, 3-thia-7,9-diazabicyclo[3.3.1]nonanes, Opiod receptors, Binding affinities, Antinociceptive activity, Molecular docking, Structure-Activity Relationship, chemistry.chemical_compound, Alkanes, Drug Discovery, Humans, Receptor, Molecular Biology, Biological evaluation, Molecular Structure, 010405 organic chemistry, Antinociceptive activity, Organic Chemistry, Sulfur, 3-thia-7, Molecular docking, 0104 chemical sciences, Molecular Docking Simulation, 010404 medicinal & biomolecular chemistry, chemistry, Docking (molecular), Thermal pain, Nonane, Selectivity
Abstract

A small library of 3-thia-7,9-diazabicyclo[3.3.1]nonanes was synthesized and their opioid receptors affinity and selectivity evaluated. Among these novel sulfur-bridged compounds, the (E) 9-[3′-(3-chlorophenyl)-but-2′-en-1′-yl]-7-propionyl-3-thia-7,9-diazabicyclo[3.3.1]nonane 2i emerged as the derivative with the highest μ receptor affinity (Ki = 85 nM) and selectivity (Ki μ/δ = 58.8, Ki μ/κ > 117.6). The antinociceptive activity of 2i was also evaluated in acute thermal pain. Docking studies disclosed the specific pattern of interactions of these derivatives.

Published
2020

3. Cardioplegic arrest is associated with overexpression of opioid receptors delta and kappa in diabetic and non-diabetic patients undergoing on-pump cardiac surgery

Author

Giuseppe Faggian, Louis D. Saravolatz, Mahmoud Ismail, Giovanni Battista Luciani, Mebratu Alebachew Gebrie, Alessio Rungatscher, Tiziano M. Scarabelli, Riccardo Raddino, and Carol Chen-Scarabelli

Subjects
medicine.medical_specialty, diabetes, business.industry, cardioplegia, cardiac surgery, opiod receptors, diabetes, medicine.disease, Cardiac surgery, Opioid, Anesthesia, Diabetes mellitus, medicine, cardioplegia, Cardiology and Cardiovascular Medicine, Receptor, business, opiod receptors, Kappa, cardiac surgery, medicine.drug, Non diabetic
Published
2017

4. Synthesis, biological evaluation and docking studies of a novel class of sulfur-bridged diazabicyclo[3.3.1]nonanes.

Author

Murineddu G, Asproni B, Corona P, Gessi S, Merighi S, Battistello E, Sturaro C, Calò G, Galeotti N, Temml V, Herdlinger S, Schuster D, and Pinna GA

Subjects
Humans, Molecular Structure, Structure-Activity Relationship, Alkanes chemical synthesis, Molecular Docking Simulation methods, Sulfur chemistry
Abstract

A small library of 3-thia-7,9-diazabicyclo[3.3.1]nonanes was synthesized and their opioid receptors affinity and selectivity evaluated. Among these novel sulfur-bridged compounds, the (E) 9-[3'-(3-chlorophenyl)-but-2'-en-1'-yl]-7-propionyl-3-thia-7,9-diazabicyclo[3.3.1]nonane 2i emerged as the derivative with the highest μ receptor affinity (K i  = 85 nM) and selectivity (K i μ/δ = 58.8, K i μ/κ > 117.6). The antinociceptive activity of 2i was also evaluated in acute thermal pain. Docking studies disclosed the specific pattern of interactions of these derivatives., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Inc. All rights reserved.)

Published
2020
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