Cargando…

Fentanyl Family at the Mu-Opioid Receptor: Uniform Assessment of Binding and Computational Analysis

Interactions of 21 fentanyl derivatives with μ-opioid receptor (μOR) were studied using experimental and theoretical methods. Their binding to μOR was assessed with radioligand competitive binding assay. A uniform set of binding affinity data contains values for two novel and one previously uncharac...

Descripción completa

Detalles Bibliográficos
Autores principales:	Lipiński, Piotr F. J., Kosson, Piotr, Matalińska, Joanna, Roszkowski, Piotr, Czarnocki, Zbigniew, Jarończyk, Małgorzata, Misicka, Aleksandra, Dobrowolski, Jan Cz., Sadlej, Joanna
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	MDPI 2019
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6412969/ https://www.ncbi.nlm.nih.gov/pubmed/30791394 http://dx.doi.org/10.3390/molecules24040740

Ejemplares similares

Structural Insights into σ(1) Receptor Interactions with Opioid Ligands by Molecular Dynamics Simulations
por: Kurciński, Mateusz, et al.
Publicado: (2018)

Gα(i)-derived peptide binds the µ-opioid receptor
por: Kossoń, Piotr, et al.
Publicado: (2023)

In Vivo, In Vitro and In Silico Studies of the Hybrid Compound AA3266, an Opioid Agonist/NK1R Antagonist with Selective Cytotoxicity
por: Matalińska, Joanna, et al.
Publicado: (2020)

Antinociceptive and Cytotoxic Activity of Opioid Peptides with Hydrazone and Hydrazide Moieties at the C-Terminus
por: Dyniewicz, Jolanta, et al.
Publicado: (2020)

Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics
por: Lipiński, Piotr F. J., et al.
Publicado: (2022)

β(2)-Homo-Amino Acid Scan of µ-Selective Opioid Tetrapeptide TAPP
por: Tymecka, Dagmara, et al.
Publicado: (2020)

Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors
por: Halik, Paweł K., et al.
Publicado: (2020)

In Vitro Biological Evaluation of Aprepitant Based (177)Lu-Radioconjugates
por: Halik, Paweł K., et al.
Publicado: (2022)

Phenylisoserine in the gas-phase and water: Ab initio studies on neutral and zwitterion conformers
por: Rode, Joanna E., et al.
Publicado: (2010)

Novel NK1R-Targeted (68)Ga-/(177)Lu-Radioconjugates with Potential Application against Glioblastoma Multiforme: Preliminary Exploration of Structure–Activity Relationships
por: Matalińska, Joanna, et al.
Publicado: (2022)

On Integral INICS Aromaticity of Pyridodiazepine Constitutional Isomers and Tautomers
por: Jarończyk, Małgorzata, et al.
Publicado: (2023)

Bifunctional Opioid/Melanocortin Peptidomimetics for Use in Neuropathic Pain: Variation in the Type and Length of the Linker Connecting the Two Pharmacophores
por: Witkowska, Ewa, et al.
Publicado: (2022)

The enantioselective synthesis of (S)-(+)-mianserin and (S)-(+)-epinastine
por: Roszkowski, Piotr, et al.
Publicado: (2015)

Can Keratin Scaffolds be used for Creating Three-dimensional Cell Cultures?
por: Bochynska-Czyz, Marta, et al.
Publicado: (2020)

Some mechanistic aspects regarding the Suzuki–Miyaura reaction between selected ortho-substituted phenylboronic acids and 3,4,5-tribromo-2,6-dimethylpyridine
por: Pomarański, Piotr, et al.
Publicado: (2018)

Metabolism of N-Acylated-Dopamine
por: Zajac, Dominika, et al.
Publicado: (2014)

On Raman optical activity sign-switching between the ground and excited states leading to an unusual resonance ROA induced chirality
por: Machalska, Ewa, et al.
Publicado: (2020)

Structure-Based Approach for the Prediction of Mu-opioid Binding Affinity of Unclassified Designer Fentanyl-Like Molecules
por: Floresta, Giuseppe, et al.
Publicado: (2019)

In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist - neurokinin 1 receptor antagonist chimera
por: Guillemyn, Karel, et al.
Publicado: (2012)

Physicochemical properties and in vitro cytotoxicity of iron oxide-based nanoparticles modified with antiangiogenic and antitumor peptide A7R
por: Niescioruk, Anna, et al.
Publicado: (2017)

Tyrosine 7.43 is important for mu-opioid receptor downstream signaling pathways activated by fentanyl
por: Tian, Xiangyun, et al.
Publicado: (2022)

Biphalin—A Potent Opioid Agonist—As a Panacea for Opioid System-Dependent Pathophysiological Diseases? †
por: Redkiewicz, Patrycja, et al.
Publicado: (2021)

The Length of N-Glycans of Recombinant H5N1 Hemagglutinin Influences the Oligomerization and Immunogenicity of Vaccine Antigen
por: Macioła, Agnieszka Katarzyna, et al.
Publicado: (2017)

Resistance of Polymeric Laminates Reinforced with Fabrics against the Growth of Delaminations
por: Czarnocki, Piotr
Publicado: (2021)

The effect of hemostatic dressing prototypes for the uniformed services on selected blood coagulation parameters in pigs
por: Adamiak, Zbigniew, et al.
Publicado: (2017)

Structural studies on radiopharmaceutical DOTA-minigastrin analogue (CP04) complexes and their interaction with CCK2 receptor
por: Lipiński, Piotr F. J., et al.
Publicado: (2018)

Hypertensive Effect of Downregulation of the Opioid System in Mouse Model of Different Activity of the Endogenous Opioid System
por: Skiba, Dominik S., et al.
Publicado: (2021)

In Silico Screening for Novel Leucine Aminopeptidase Inhibitors with 3,4-Dihydroisoquinoline Scaffold
por: Ziemska, Joanna, et al.
Publicado: (2020)

Chiral Lanthanide Complexes with l- and d-Alanine: An X-ray and Vibrational Circular Dichroism Study
por: Lyczko, Krzysztof, et al.
Publicado: (2020)

Opioid Crisis—An Emphasis on Fentanyl Analogs
por: Lutfy, Kabirullah
Publicado: (2020)

A convenient route to symmetrically and unsymmetrically substituted 3,5-diaryl-2,4,6-trimethylpyridines via Suzuki–Miyaura cross-coupling reaction
por: Błachut, Dariusz, et al.
Publicado: (2016)

Diagnostic Interpretation of Non-Uniformly Sampled Electrocardiogram
por: Augustyniak, Piotr
Publicado: (2021)

Higher naloxone dosing in a quantitative systems pharmacology model that predicts naloxone-fentanyl competition at the opioid mu receptor level
por: Moss, Ronald B., et al.
Publicado: (2020)

Synthetic Transition from Thiourea-Based Compounds to Tetrazole Derivatives: Structure and Biological Evaluation of Synthesized New N-(Furan-2-ylmethyl)-1H-tetrazol-5-amine Derivatives
por: Szulczyk, Daniel, et al.
Publicado: (2021)

PK20, a new opioid-neurotensin hybrid peptide that exhibits central and peripheral antinociceptive effects
por: Kleczkowska, Patrycja, et al.
Publicado: (2010)

On the variation of the belt and chiral screw and spring conformations of substituted regioregular HT undecathiophenes
por: Dobrowolski, Jan Cz., et al.
Publicado: (2018)

Correction: Higher naloxone dosing in a quantitative systems pharmacology model that predicts naloxone-fentanyl competition at the opioid mu receptor level
Publicado: (2020)

How μ-Opioid Receptor Recognizes Fentanyl
por: Vo, Quynh N., et al.
Publicado: (2020)

How μ-Opioid Receptor Recognizes Fentanyl
por: Vo, Quynh N., et al.
Publicado: (2020)

How μ-opioid receptor recognizes fentanyl
por: Vo, Quynh N., et al.
Publicado: (2021)

Cannot write session to /tmp/vufind_sessions/sess_pud9or3dfhb3mc4bpeu0rou7q8