Cargando…

The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (K(d) or K(i) value) or target modulation (IC(50)). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and...

Descripción completa

Detalles Bibliográficos
Autores principales:	Bosma, Reggie, Witt, Gesa, Vaas, Lea A. I., Josimovic, Ivana, Gribbon, Philip, Vischer, Henry F., Gul, Sheraz, Leurs, Rob
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Frontiers Media S.A. 2017
Materias:	Pharmacology
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5627017/ https://www.ncbi.nlm.nih.gov/pubmed/29033838 http://dx.doi.org/10.3389/fphar.2017.00667

Ejemplares similares

Route to Prolonged Residence Time at the Histamine H(1) Receptor: Growing from Desloratadine to Rupatadine
por: Bosma, Reggie, et al.
Publicado: (2019)

Exploring the Effect of Cyclization of Histamine H(1) Receptor Antagonists on Ligand Binding Kinetics
por: Wang, Zhiyong, et al.
Publicado: (2021)

Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H(3) Receptor
por: Mocking, Tamara A. M., et al.
Publicado: (2019)

Modulation of cellular signaling by herpesvirus-encoded G protein-coupled receptors
por: de Munnik, Sabrina M., et al.
Publicado: (2015)

BRET-Based Biosensors to Measure Agonist Efficacies in Histamine H(1) Receptor-Mediated G Protein Activation, Signaling and Interactions with GRKs and β-Arrestins
por: Verweij, Eléonore W. E., et al.
Publicado: (2022)

Pharmacotherapy of Itch—Antihistamines and Histamine Receptors as G Protein-Coupled Receptors
por: Fukasawa, Takemichi, et al.
Publicado: (2022)

Development of novel fluorescent histamine H(1)-receptor antagonists to study ligand-binding kinetics in living cells
por: Stoddart, Leigh A., et al.
Publicado: (2018)

Analysis of Missense Variants in the Human Histamine Receptor Family Reveals Increased Constitutive Activity of E410(6.30×30)K Variant in the Histamine H(1) Receptor
por: Ma, Xiaoyuan, et al.
Publicado: (2021)

Identification of TSPAN4 as Novel Histamine H(4) Receptor Interactor
por: Ma, Xiaoyuan, et al.
Publicado: (2021)

Antihistaminic effect of Bauhinia racemosa leaves
por: Nirmal, SA, et al.
Publicado: (2011)

Structural basis for recognition of antihistamine drug by human histamine receptor
por: Peng, Xueqian, et al.
Publicado: (2022)

A Photoswitchable Agonist for the Histamine H(3) Receptor, a Prototypic Family A G‐Protein‐Coupled Receptor
por: Hauwert, Niels J., et al.
Publicado: (2019)

The Role of Histamine in the Pathophysiology of Asthma and the Clinical Efficacy of Antihistamines in Asthma Therapy
por: Yamauchi, Kohei, et al.
Publicado: (2019)

Parkinsonism Attenuation by Antihistamines via Downregulating the Oxidative Stress, Histamine, and Inflammation
por: Ayaz, Maira, et al.
Publicado: (2022)

Development of a Conformational Histamine H(3) Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists
por: Schihada, Hannes, et al.
Publicado: (2020)

Covalent Inhibition of the Histamine H(3) Receptor
por: Wágner, Gábor, et al.
Publicado: (2019)

Histamine release theory and roles of antihistamine in the treatment of cytokines storm of COVID-19
por: Eldanasory, Omar Abdelhay, et al.
Publicado: (2020)

Molecular Determinants of the Kinetic Binding Properties of Antihistamines at the Histamine H(1) Receptors
por: Akimoto, Hayato, et al.
Publicado: (2021)

Effects of histamine and antihistamine on the hard tick Haemaphysalis longicornis during blood sucking
por: Islam, Mohammad Saiful, et al.
Publicado: (2023)

Differential Role of Serines and Threonines in Intracellular Loop 3 and C-Terminal Tail of the Histamine H(4) Receptor in β-Arrestin and G Protein-Coupled Receptor Kinase Interaction, Internalization, and Signaling
por: Verweij, Eléonore W. E., et al.
Publicado: (2020)

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor
por: Bosma, Reggie, et al.
Publicado: (2019)

Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H(1) Receptor
por: Kok, Zhi Yuan, et al.
Publicado: (2022)

Suppression of wheal and flare in histamine test by the main H1 antihistamines commercialized in Brazil
por: Maciel-Guerra, Helena, et al.
Publicado: (2018)

Primary Non-Adherence to Antihistamines—Conclusions From E-Prescription Pilot Data in Poland
por: Kardas, Grzegorz, et al.
Publicado: (2020)

Histamine and Delirium: Current Opinion
por: Chazot, Paul L., et al.
Publicado: (2019)

Effect of histamine strength and devices on skin prick test (SPT) response following antihistamine inhibition
por: Plunkett, Greg, et al.
Publicado: (2012)

Histamine receptor antagonism and anti-tumour activity.
por: Collins, M., et al.
Publicado: (1982)

Genetic Variation in the Histamine Production, Response, and Degradation Pathway Is Associated with Histamine Pharmacodynamic Response in Children with Asthma
por: Jones, Bridgette L., et al.
Publicado: (2017)

Knowledge and Attitude of Medical Resident Doctors Toward Antihistamines
por: Chainani, Esha, et al.
Publicado: (2015)

Covid‐19 Histamine theory: Why antihistamines should be incorporated as the basic component in Covid‐19 management?
por: Mashauri, Harold L.
Publicado: (2023)

The histamine H(4) receptor: from orphan to the clinic
por: Thurmond, Robin L.
Publicado: (2015)

COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms
por: Malone, Robert W., et al.
Publicado: (2021)

Histamine can be Formed and Degraded in the Human and Mouse Heart
por: Neumann, Joachim, et al.
Publicado: (2021)

Histamine 2 Receptor Agonism and Histamine 4 Receptor Antagonism Ameliorate Inflammation in a Model of Psoriasis
por: ROSSBACH, Kristine, et al.
Publicado: (2020)

High affinity histamine-binding and antihistaminic activity of the salivary nitric oxide-carrying heme protein (nitrophorin) of Rhodnius prolixus
Publicado: (1994)

Physiological implications of biased signaling at histamine H2 receptors
por: Alonso, Natalia, et al.
Publicado: (2015)

FCERI and Histamine Metabolism Gene Variability in Selective Responders to NSAIDS
por: Amo, Gemma, et al.
Publicado: (2016)

Multiple Targeting Approaches on Histamine H(3) Receptor Antagonists
por: Khanfar, Mohammad A., et al.
Publicado: (2016)

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)

Ambivalent antihistamines.
Publicado: (1994)

Cannot write session to /tmp/vufind_sessions/sess_ol1ns0nq4gqc08v7049t0kl5d2