Cargando…

In Vivo Phenotypic Screening for Treating Chronic Neuropathic Pain: Modification of C2-Arylethynyl Group of Conformationally Constrained A(3) Adenosine Receptor Agonists

[Image: see text] (N)-Methanocarba adenosine 5′-methyluronamides containing 2-arylethynyl groups were synthesized as A(3) adenosine receptor (AR) agonists and screened in vivo (po) for reduction of neuropathic pain. A small N(6)-methyl group maintained binding affinity, with human > mouse A(3)AR...

Descripción completa

Detalles Bibliográficos
Autores principales:	Tosh, Dilip K., Finley, Amanda, Paoletta, Silvia, Moss, Steven M., Gao, Zhan-Guo, Gizewski, Elizabeth T., Auchampach, John A., Salvemini, Daniela, Jacobson, Kenneth A.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2014
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4266358/ https://www.ncbi.nlm.nih.gov/pubmed/25422861 http://dx.doi.org/10.1021/jm501021n

Ejemplares similares

Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A(3) Adenosine Receptor Agonists
por: Tosh, Dilip K., et al.
Publicado: (2016)

Structural Probing of Off-Target G Protein-Coupled Receptor Activities within a Series of Adenosine/Adenine Congeners
por: Paoletta, Silvia, et al.
Publicado: (2014)

Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists
por: Tosh, Dilip K., et al.
Publicado: (2018)

Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A(3 )adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts
por: Wan, Tina C, et al.
Publicado: (2011)

Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development
por: Jacobson, Kenneth A., et al.
Publicado: (2019)

Adenosine A(3) Receptor (A(3)AR) Agonist for the Treatment of Bleomycin-Induced Lung Fibrosis in Mice
por: Sgambellone, Silvia, et al.
Publicado: (2022)

John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors()
por: Jacobson, Kenneth A., et al.
Publicado: (2014)

Species dependence of A(3) adenosine receptor pharmacology and function
por: Gao, Zhan-Guo, et al.
Publicado: (2022)

Targeting the A(3) adenosine receptor to prevent and reverse chemotherapy-induced neurotoxicities in mice
por: Singh, Anand Kumar, et al.
Publicado: (2022)

Bitopic fluorescent antagonists of the A(2A) adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners
por: Duroux, Romain, et al.
Publicado: (2017)

Thermostabilization and purification of the human dopamine transporter (hDAT) in an inhibitor and allosteric ligand bound conformation
por: Navratna, Vikas, et al.
Publicado: (2018)

Adenosine Metabotropic Receptors in Chronic Pain Management
por: Luongo, Livio, et al.
Publicado: (2021)

2,4-Bis(arylethynyl)-9-chloro-5,6,7,8-tetrahydroacridines: synthesis and photophysical properties
por: Tka, Najeh, et al.
Publicado: (2021)

Thermostabilisation of an Agonist-Bound Conformation of the Human Adenosine A(2A) Receptor
por: Lebon, Guillaume, et al.
Publicado: (2011)

4,5-Bis(arylethynyl)-1,2,3-triazoles—A New Class of Fluorescent Labels: Synthesis and Applications
por: Govdi, Anastasia I., et al.
Publicado: (2022)

Arylethynyl- or Alkynyl-Linked Pyrimidine and 7-Deazapurine 2′-Deoxyribonucleoside 3′-Phosphoramidites for Chemical Synthesis of Hypermodified Hydrophobic Oligonucleotides
por: Jestřábová, Ivana, et al.
Publicado: (2023)

Synthesis of Conformationally Constrained d-Glu-meso-DAP Analogs as Innate Immune Agonists
por: Guzelj, Samo, et al.
Publicado: (2020)

Lack of efficacy of a partial adenosine A1 receptor agonist in neuropathic pain models in mice
por: Metzner, Katharina, et al.
Publicado: (2021)

Synthesis and Anti-Renal Fibrosis Activity of Conformationally Locked Truncated 2-Hexynyl-N(6)-Substituted-(N)-Methanocarba-nucleosides as A(3) Adenosine Receptor Antagonists and Partial Agonists
por: Nayak, Akshata, et al.
Publicado: (2014)

Design and Synthesis of New 5-aryl-4-Arylethynyl-1H-1,2,3-triazoles with Valuable Photophysical and Biological Properties
por: Efremova, Mariia M., et al.
Publicado: (2021)

Flexible modulation of agonist efficacy at the human A(3 )adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000
por: Gao, Zhan-Guo, et al.
Publicado: (2008)

Convergent synthesis of 2-thioether-substituted (N)-methanocarba-adenosines as purine receptor agonists
por: Suresh, R. Rama, et al.
Publicado: (2021)

Targeting neuroinflammation in neuropathic pain and opioid use
por: Salvemini, Daniela, et al.
Publicado: (2022)

Conformally invariant constrained fermion models
por: Cabra, D C, et al.
Publicado: (1990)

Constraining ribosomal RNA conformational space
por: Favaretto, Paola, et al.
Publicado: (2005)

Structural Probing and Molecular Modeling of the A(3) Adenosine Receptor: A Focus on Agonist Binding
por: Ciancetta, Antonella, et al.
Publicado: (2017)

Downregulation of adenosine and adenosine A1 receptor contributes to neuropathic pain in resiniferatoxin neuropathy
por: Kan, Hung-Wei, et al.
Publicado: (2018)

Magnesium-mediated sp(3) C–H activation in cascade cyclization of 1-arylethynyl-2-alkyl-o-carboranes: efficient synthesis of carborane-fused cyclopentanes
por: Zhang, Jie, et al.
Publicado: (2020)

Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A(2A )adenosine receptor agonists
por: Das, Arijit, et al.
Publicado: (2010)

Different analgesic effects of adenosine between postoperative and neuropathic pain
por: Yamaoka, Gotaro, et al.
Publicado: (2012)

New Insight into the Role of Adenosine in Demyelination, Stroke and Neuropathic Pain
por: Coppi, Elisabetta, et al.
Publicado: (2021)

Electroacupuncture improves neuropathic pain: Adenosine, adenosine 5’-triphosphate disodium and their receptors perhaps change simultaneously☆
por: Ren, Wen, et al.
Publicado: (2012)

A(2B) Adenosine Receptor and Cancer
por: Gao, Zhan-Guo, et al.
Publicado: (2019)

The Role of Adenosine Receptor Agonists in Regulation of Hematopoiesis
por: Hofer, Michal, et al.
Publicado: (2011)

Non-Nucleoside Agonists of the Adenosine Receptors: An Overview
por: Dal Ben, Diego, et al.
Publicado: (2019)

Epigenetic modifications in neuropathic pain
por: Luo, Danzhi, et al.
Publicado: (2021)

Photomodulation of G Protein-Coupled Adenosine Receptors by a Novel Light-Switchable Ligand
por: Bahamonde, María Isabel, et al.
Publicado: (2014)

The Histamine H(4) Receptor Participates in the Anti-Neuropathic Effect of the Adenosine A(3) Receptor Agonist IB-MECA: Role of CD4(+) T Cells
por: Micheli, Laura, et al.
Publicado: (2021)

Uncovering the Mechanisms of Adenosine Receptor-Mediated Pain Control: Focus on the A(3) Receptor Subtype
por: Coppi, Elisabetta, et al.
Publicado: (2021)

Adenosine-Related Mechanisms in Non-Adenosine Receptor Drugs
por: Jacobson, Kenneth A., et al.
Publicado: (2020)

Cannot write session to /tmp/vufind_sessions/sess_gpb7l72uccodj5a7lmku3fn4h8