Cargando…

High-affinity fluorescent ligands for the 5-HT(3) receptor

The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT(3) receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT(3)AR.

Detalles Bibliográficos
Autores principales:	Simonin, Jonathan, Vernekar, Sanjeev Kumar V., Thompson, Andrew J., Hothersall, J. Daniel, Connolly, Christopher N., Lummis, Sarah C.R., Lochner, Martin
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Elsevier Science Ltd 2012
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3277886/ https://www.ncbi.nlm.nih.gov/pubmed/22189135 http://dx.doi.org/10.1016/j.bmcl.2011.11.097

Ejemplares similares

Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives
por: Vernekar, Sanjeev Kumar V., et al.
Publicado: (2010)

Agonists and antagonists induce different palonosetron dissociation rates in 5-HT(3)A and 5-HT(3)AB receptors()
por: Lummis, Sarah C.R., et al.
Publicado: (2013)

Loop B Is a Major Structural Component of the 5-HT(3) Receptor
por: Thompson, A. J., et al.
Publicado: (2008)

Varenicline Interactions at the 5-HT(3) Receptor Ligand Binding Site are Revealed by 5-HTBP
por: Price, Kerry L., et al.
Publicado: (2015)

Prolonged inhibition of 5-HT(3) receptors by palonosetron results from surface receptor inhibition rather than inducing receptor internalization
por: Hothersall, J Daniel, et al.
Publicado: (2013)

Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
por: Thompson, AJ, et al.
Publicado: (2013)

5-HT(3) Receptors
por: Lummis, Sarah C. R.
Publicado: (2012)

Structure–Activity Relationships of Quinoxaline-Based 5-HT(3)A and 5-HT(3)AB Receptor-Selective Ligands
por: Thompson, Andrew J, et al.
Publicado: (2013)

5-Hydroxytryptamine (5-HT) Cellular Sequestration during Chronic Exposure Delays 5-HT(3) Receptor Resensitization due to Its Subsequent Release
por: Hothersall, J. Daniel, et al.
Publicado: (2014)

Detection of human and rodent 5-HT(3B )receptor subunits by anti-peptide polyclonal antibodies
por: Reeves, David C, et al.
Publicado: (2006)

Structural basis of ligand recognition in 5-HT(3) receptors
por: Kesters, Divya, et al.
Publicado: (2013)

The binding characteristics and orientation of a novel radioligand with distinct properties at 5-HT(3)A and 5-HT(3)AB receptors
por: Thompson, Andrew J., et al.
Publicado: (2014)

A single channel mutation alters agonist efficacy at 5-HT(3)A and 5-HT(3)AB receptors
por: Thompson, A J, et al.
Publicado: (2013)

Cysteine modification reveals which subunits form the ligand binding site in human heteromeric 5-HT(3)AB receptors
por: Thompson, A J, et al.
Publicado: (2011)

Design, Synthesis, and Structure–Activity Relationships of Highly Potent 5-HT(3) Receptor Ligands
por: Verheij, Mark H. P., et al.
Publicado: (2012)

Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor()
por: Del Cadia, Marta, et al.
Publicado: (2013)

Ginkgolide B and bilobalide block the pore of the 5-HT(3) receptor at a location that overlaps the picrotoxin binding site
por: Thompson, Andrew J., et al.
Publicado: (2011)

The muscarinic antagonists scopolamine and atropine are competitive antagonists at 5-HT(3) receptors
por: Lochner, Martin, et al.
Publicado: (2016)

Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT(3) receptor via a common vestibule site
por: Brams, Marijke, et al.
Publicado: (2020)

5-HT(3) Receptor MX Helix Contributes to Receptor Function
por: Mocatta, James, et al.
Publicado: (2022)

5-Fluorotryptamine is a partial agonist at 5-HT(3) receptors, and reveals that size and electronegativity at the 5 position of tryptamine are critical for efficient receptor function
por: Bower, Kiowa S., et al.
Publicado: (2008)

Novel N-Arylsulfonylindoles Targeted as Ligands of the 5-HT(6) Receptor. Insights on the Influence of C-5 Substitution on Ligand Affinity
por: Arrieta-Rodríguez, Loreto, et al.
Publicado: (2021)

5-HT(3) Receptor Brain-Type B-Subunits are Differentially Expressed in Heterologous Systems
por: Corradi, Jeremias, et al.
Publicado: (2015)

A Hydrogen Bond in Loop A Is Critical for the Binding and Function of the 5-HT(3) Receptor
por: Price, Kerry L., et al.
Publicado: (2008)

Identification of novel α7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric α7 receptor ligand binding domain
por: Akdemir, Atilla, et al.
Publicado: (2012)

Classification of 5-HT(1A) Receptor Ligands on the Basis of Their Binding Affinities by Using PSO-Adaboost-SVM
por: Cheng, Zhengjun, et al.
Publicado: (2009)

Trans−cis Switching Mechanisms in Proline Analogues and Their Relevance for the Gating of the 5-HT(3) Receptor
por: Melis, Claudio, et al.
Publicado: (2009)

Diolistics: incorporating fluorescent dyes into biological samples using a gene gun
por: O’Brien, John A., et al.
Publicado: (2007)

The pharmacological profile of ELIC, a prokaryotic GABA-gated receptor
por: Thompson, Andrew J., et al.
Publicado: (2012)

Therapeutic Potential of 5-HT(2C) Receptor Ligands
por: Jensen, Nanna H., et al.
Publicado: (2010)

Overcoming Depression with 5-HT(2A) Receptor Ligands
por: Zięba, Agata, et al.
Publicado: (2021)

Pharmacophore Directed Screening of Agonistic Natural Molecules Showing Affinity to 5HT(2C) Receptor
por: Veeramachaneni, Ganesh Kumar, et al.
Publicado: (2019)

New Triazine Derivatives as Serotonin 5-HT(6) Receptor Ligands
por: Łażewska, Dorota, et al.
Publicado: (2023)

Phenylalanine in the Pore of the Erwinia Ligand-Gated Ion Channel Modulates Picrotoxinin Potency but Not Receptor Function
por: Thompson, Andrew J., et al.
Publicado: (2014)

High-Affinity Functional Fluorescent Ligands for Human β-Adrenoceptors
por: Mitronova, Gyuzel Y., et al.
Publicado: (2017)

Measuring ligand-cell surface receptor affinities with axial line-scanning fluorescence correlation spectroscopy
por: Eckert, Antonia Franziska, et al.
Publicado: (2020)

An Algorithm to Identify Target-Selective Ligands – A Case Study of 5-HT7/5-HT1A Receptor Selectivity
por: Kurczab, Rafał, et al.
Publicado: (2016)

An atypical residue in the pore of Varroa destructor GABA-activated RDL receptors affects picrotoxin block and thymol modulation
por: Price, Kerry L., et al.
Publicado: (2014)

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H(4) and the ion channel serotonin 5-HT(3A)
por: Verheij, Mark H.P., et al.
Publicado: (2011)

Low Basicity as a Characteristic for Atypical Ligands of Serotonin Receptor 5-HT2
por: Podlewska, Sabina, et al.
Publicado: (2021)

Cannot write session to /tmp/vufind_sessions/sess_3f9ootdqtqaoo2culamev63nr9