Cargando…

Structure–Activity Relationships of Quinoxaline-Based 5-HT(3)A and 5-HT(3)AB Receptor-Selective Ligands

Until recently, discriminating between homomeric 5-HT(3)A and heteromeric 5-HT(3)AB receptors was only possible with ligands that bind in the receptor pore. This study describes the first series of ligands that can discriminate between these receptor types at the level of the orthosteric binding sit...

Descripción completa

Detalles Bibliográficos
Autores principales:	Thompson, Andrew J, Verheij, Mark H P, van Muijlwijk-Koezen, Jacqueline E, Lummis, Sarah C R, Leurs, Rob, de Esch, Iwan J P
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	WILEY-VCH Verlag 2013
Materias:	Full Papers
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4063337/ https://www.ncbi.nlm.nih.gov/pubmed/23640722 http://dx.doi.org/10.1002/cmdc.201300032

Ejemplares similares

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

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)

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

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)

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)

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)

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

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)

High-affinity fluorescent ligands for the 5-HT(3) receptor
por: Simonin, Jonathan, et al.
Publicado: (2012)

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

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

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

Anxiolytic-like effects observed in rats exposed to the elevated zero-maze following treatment with 5-HT(2)/5-HT(3)/5-HT(4) ligands
por: Bell, Rob, et al.
Publicado: (2014)

Azologization of serotonin 5-HT(3) receptor antagonists
por: Rustler, Karin, et al.
Publicado: (2019)

Distribution of 5-HT(3), 5-HT(4), and 5-HT(7) Receptors Along the Human Colon
por: Yaakob, Nor S, et al.
Publicado: (2015)

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

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

Review: 5-HT(1), 5-HT(2), 5-HT(3) and 5-HT(7) Receptors and their Role in the Modulation of Pain Response in the Central Nervous System
por: Cortes-Altamirano, Jose Luis, et al.
Publicado: (2018)

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)

5-HT3 and 5-HT4 antagonists inhibit peristaltic contractions in guinea-pig distal colon by mechanisms independent of endogenous 5-HT
por: Sia, Tiong C., et al.
Publicado: (2013)

5-HT1A agonists, 5-HT3 antagonists and benzodiazepines : their comparative behavioural pharmacology /
Publicado: (1991)

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

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)

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)

5-HT(2A), 5-HT(1B/D), 5HT(3) and 5-HT(7) receptors as mediators of serotonin-induced direct contractile response of bovine airway smooth muscle
por: Da Costa Guevara, Darwin, et al.
Publicado: (2021)

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)

Expression Patterns of Serotonin Receptors 5-HT1A, 5-HT2A, and 5-HT3A during Human Fetal Lung Development
por: Nikolić, Jelena, et al.
Publicado: (2023)

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)

Central and peripheral 5-HT3 receptors
Publicado: (1992)

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

Exploring the Activity Profile of TbrPDEB1 and hPDE4 Inhibitors Using Free Energy Perturbation
por: Zara, Lorena, et al.
Publicado: (2022)

Cardiac Roles of Serotonin (5-HT) and 5-HT-Receptors in Health and Disease
por: Neumann, Joachim, et al.
Publicado: (2023)

Constitutively Active 5-HT Receptors: An Explanation of How 5-HT Antagonists Inhibit Gut Motility in Species Where 5-HT is Not an Enteric Neurotransmitter?
por: Spencer, Nick J.
Publicado: (2015)

Conservation of 5-HT(1A) receptor-mediated autoinhibition of serotonin (5-HT) neurons in mice with altered 5-HT homeostasis
por: Araragi, Naozumi, et al.
Publicado: (2013)

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)

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

Model structure–activity relationship studies of potential tropane 5HT(1A), 5HT(2A), and D(2) receptor ligands
por: Słowiński, Tomasz, et al.
Publicado: (2012)

Human 5–HT(4) and 5–HT(7) Receptor Splice Variants: Are they Important?
por: Coupar, Ian M, et al.
Publicado: (2007)

Cannot write session to /tmp/vufind_sessions/sess_khrsuol3m0kmdao5elo7bc815r