Route to Prolonged Residence Time at the Histamine H1 Receptor: Growing from Desloratadine to Rupatadine (Q91631033)

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23 April 2020

title

Route to Prolonged Residence Time at the Histamine H1 Receptor: Growing from Desloratadine to Rupatadine (English)

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3

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Nick Bushby

4

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23 April 2020

Jelle van den Bor

6

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23 April 2020

Michael J Waring

7

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23 April 2020

Chris de Graaf

8

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23 April 2020

Iwan J P de Esch

9

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23 April 2020

Henry F Vischer

10

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23 April 2020

Maikel Wijtmans

12

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23 April 2020

Rob Leurs

13

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author name string

Reggie Bosma

1

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23 April 2020

Zhiyong Wang

2

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23 April 2020

Sebastiaan Kuhne

5

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Robert J Sheppard

11

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23 April 2020

publication date

5 July 2019

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Journal of Medicinal Chemistry

23 April 2020

published in

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volume

62

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issue

14

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23 April 2020

page(s)

6630-6644

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Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor.

23 April 2020

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Identification of Ligand Binding Hot Spots of the Histamine H1 Receptor following Structure-Based Fragment Optimization

23 February 2021

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BRET-based β-arrestin2 recruitment to the histamine H1 receptor for investigating antihistamine binding kinetics

23 February 2021

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In vivo Target Residence Time and Kinetic Selectivity: The Association Rate Constant as Determinant

23 February 2021

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23 February 2021

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Decoding the Role of Water Dynamics in Ligand-Protein Unbinding: CRF1R as a Test Case.

23 February 2021

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Ligand Residence Time at G-protein-Coupled Receptors-Why We Should Take Our Time To Study It.

23 February 2021

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Development of a highly sensitive LC-MS/MS method for simultaneous determination of rupatadine and its two active metabolites in human plasma: Application to a clinical pharmacokinetic study

23 February 2021

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What can we learn from molecular dynamics simulations for GPCR drug design?

23 February 2021

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Understanding the hysteresis loop conundrum in pharmacokinetic/pharmacodynamic relationships

23 February 2021

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Drug-target residence time--a case for G protein-coupled receptors

23 February 2021

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Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.

23 February 2021

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Pharmacology of antihistamines.

23 February 2021

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A structural chemogenomics analysis of aminergic GPCRs: lessons for histamine receptor ligand design

23 February 2021

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23 February 2021

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The inhibition by levocetirizine and fexofenadine of the histamine-induced wheal and flare response in healthy Caucasian and Japanese volunteers.

23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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Efficacy and tolerability of rupatadine at four times the recommended dose against histamine- and platelet-activating factor-induced flare responses andex vivoplatelet aggregation in healthy males

23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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23 February 2021

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Drug-target residence time and its implications for lead optimization

23 February 2021

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23 February 2021

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23 February 2021

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Changes in pH differently affect the binding properties of histamine H1 receptor antagonists

23 February 2021

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Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines

23 February 2021

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23 February 2021

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Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor

23 February 2021

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Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).

23 February 2021

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[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine

23 February 2021

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[HPLC-determination of loratadine and its active metabolite descarboethoxyloratadine in human plasma]

23 February 2021

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The kinetics of competitive radioligand binding predicted by the law of mass action.

23 February 2021

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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

23 February 2021

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Dual antagonists of platelet-activating factor and histamine. Identification of structural requirements for dual activity of N-acyl-4-(5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidines

23 February 2021

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10.1021/ACS.JMEDCHEM.9B00447

23 February 2021

Identifiers

DOI

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:31274307 AND SRC:MED&resulttype=core&format=json

23 April 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:31274307 AND SRC:MED&resulttype=core&format=json

23 April 2020

PubMed publication ID

31274307

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