Synthesis, biological evaluation, and utility of fluorescent ligands targeting the μ-opioid receptor

QR Code

Synthesis, biological evaluation, and utility of fluorescent ligands targeting the μ-opioid receptor

Fluorescently labeled ligands are useful pharmacological research tools for studying receptor localization, trafficking, and signaling processes via fluorescence imaging. They are also employed in fluorescent binding assays. This study is centered on the design, synthesis, and pharmacological evalua...

Full description

Bibliographic Details
Main Authors:	Schembri, Luke S., Stoddart, Leigh A., Briddon, Stephen J., Kellam, Barrie, Canals, Meritxell, Graham, Bim, Scammells, Peter J.
Format:	Article
Published:	American Chemical Society 2015
Online Access:	https://eprints.nottingham.ac.uk/50604/

Similar Items

Fluorescently labeled morphine derivatives for bioimaging studies
by: Lam, Raymond, et al.
Published: (2018)

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist
by: Stoddart, Leigh A., et al.
Published: (2015)

Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells
by: Stoddart, Leigh A., et al.
Published: (2018)

Effect of a toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization
by: Stoddart, Leigh A., et al.
Published: (2014)

Design, synthesis and pharmacological evaluation of novel fluorescent ligands for the mu-opioid receptor
by: Marshall, William
Published: (2021)

Molecular mechanisms controlling μ-opioid receptor activation
by: Batista Gondin, Arisbel
Published: (2019)

Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers
by: Vernall, Andrea J., et al.
Published: (2013)

Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity
by: Kumar, Vinod, et al.
Published: (2014)

Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925
by: Conroy, Sean, et al.
Published: (2018)

A non-imaging high throughput approach to chemical library screening at the unmodified adenosine-A3 receptor in living cells
by: Arruda, Maria Augusta, et al.
Published: (2017)

Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors
by: Kilpatrick, Laura E., et al.
Published: (2012)

Fragment-based discovery of subtype-selective adenosine receptor ligands from homology models
by: Ranganathan, Anirudh, et al.
Published: (2015)

Fluorescent cannabinoids: Stratagies towards the synthesis of fluorescently labelled CB2 receptor ligands
by: Yates, Andrew Stephen
Published: (2005)

Use of a new proximity assay (NanoBRET) to investigate the ligand binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells
by: Soave, Mark, et al.
Published: (2016)

Design, synthesis and evaluation of fluorescent CB2 cannabinoid receptor ligands
by: Holt, Christopher James
Published: (2009)

Design and evaluation of fluorescent and non-fluorescent bivalent ligands to explore their mode of action at neuropeptide Y receptors
by: Richardson, Rachel
Published: (2019)

Design and synthesis of fluorescent opioids for bioimaging
by: Lam, Raymond
Published: (2018)

Optimisation of Peptide Linker-based Fluorescent Ligands for the Histamine H1 Receptor
by: Kok, Zhi Yuan
Published: (2020)

Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism
by: Corriden, Ross, et al.
Published: (2014)

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors
by: Baker, Jillian G., et al.
Published: (2011)

Synthesis and characterization of high-affinity 4, 4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors
by: Baker, Jillian G., et al.
Published: (2011)

The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs
by: Vernall, Andrea J., et al.
Published: (2014)

Design, Synthesis, and Evaluation of New P2Y2 Receptor Antagonists and Fluorescent Ligands
by: Knight, Rebecca
Published: (2025)

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)

Determination of mitragynine bound opioid receptors
by: Baharuldin, Mohamad Taufik Hidayat, et al.
Published: (2010)

Alkylation of staurosporine to derive a kinase probe for fluorescence applications
by: Disney, Alexander J.M., et al.
Published: (2016)

Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization
by: Hill, Stephen J., et al.
Published: (2014)

Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes
by: Corriden, Ross, et al.
Published: (2013)

The postnatal development of nociceptive and opioid receptor signalling pathways
by: Cooper, Andrew H.
Published: (2017)

NanoBRET to probe ligand-receptor and receptor-receptor interactions in living cells
by: Carvalheira Alcobia, Diana
Published: (2019)

The use of fluorescence correlation spectroscopy to characterize the molecular mobility of fluorescently labelled G protein-coupled receptors
by: Kilpatrick, Laura E., et al.
Published: (2016)

Chemical and in silico exploration of novel 5-hydroxytryptamine 2A receptor (5-HT2AR) ligands
by: Damerum, Luke
Published: (2024)

Studies on the biased signalling of some novel delta opioid receptor agonists
by: Asghar, Muhammad Junaid
Published: (2017)

Targeting TNF-related apoptosis-inducing ligand (TRAIL) receptor by natural products as a potential therapeutic approach for cancer therapy
by: Dai, X., et al.
Published: (2015)

Novel fenofibrate derivatives as cannabinoid receptor ligands
by: Spencer, Sarah Jane
Published: (2011)

Real-time analysis of the binding of fluorescent VEGF₁₆₅a to VEGFR2 in living cells: Effect of receptor tyrosine kinase inhibitors and fate of internalized agonist-receptor complexes
by: Kilpatrick, Laura E., et al.
Published: (2017)

Drug-like antagonists of P2Y receptors — from lead identification to drug development
by: Conroy, Sean, et al.
Published: (2016)

Enhanced antinociceptive effects of mitragynine in combination with morphine via opioid receptors activation
by: Abdul Rahman, Shamima
Published: (2014)

Imaging Cannabinoid Receptors: A Brief Collection of Covalent and Fluorescent Probes for CB1 and CB2 Receptors
by: Hamilton, A.J., et al.
Published: (2021)

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)