Molecular mechanisms for the persistent bronchodilatory effect of the beta 2-adrenoceptor agonist salmeterol
about
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug actionSalmeterol Efficacy and Bias in the Activation and Kinase-Mediated Desensitization of β2-Adrenergic Receptors.Pharmacogenomics of long-acting β2-agonists.The dopamine D1 receptor is expressed and facilitates relaxation in airway smooth muscle.On the mechanism of the persistent action of salmeterol: what is the current position?Third-generation long-acting β₂-adrenoceptor agonists: medicinal chemistry strategies employed in the identification of once-daily inhaled β₂-adrenoceptor agonists.Design and application of locally delivered agonists of the adenosine A(2A) receptor.Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism.Radioligand dissociation measurements: potential interference of rebinding and allosteric mechanisms and physiological relevance of the biological model systems.Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence time.Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands.On the 'micro'-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action.Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.Cell membranes… and how long drugs may exert beneficial pharmacological activity in vivo'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.Estimation of the dissociation rate of unlabelled ligand-receptor complexes by a 'two-step' competition binding approach.Effects of target binding kinetics on in vivo drug efficacy: koff , kon and rebinding.Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonistsGPCR theme editorial.Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time.Budesonide/salmeterol in fixed-dose combination for the treatment of asthma.Link between a high for drug binding and a fast clinical action: to be or not to be?
P2860
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P2860
Molecular mechanisms for the persistent bronchodilatory effect of the beta 2-adrenoceptor agonist salmeterol
description
2009 nî lūn-bûn
@nan
2009年の論文
@ja
2009年学术文章
@wuu
2009年学术文章
@zh-cn
2009年学术文章
@zh-hans
2009年学术文章
@zh-my
2009年学术文章
@zh-sg
2009年學術文章
@yue
2009年學術文章
@zh
2009年學術文章
@zh-hant
name
Molecular mechanisms for the p ...... drenoceptor agonist salmeterol
@en
Molecular mechanisms for the p ...... renoceptor agonist salmeterol.
@nl
type
label
Molecular mechanisms for the p ...... drenoceptor agonist salmeterol
@en
Molecular mechanisms for the p ...... renoceptor agonist salmeterol.
@nl
prefLabel
Molecular mechanisms for the p ...... drenoceptor agonist salmeterol
@en
Molecular mechanisms for the p ...... renoceptor agonist salmeterol.
@nl
P2093
P2860
P1476
Molecular mechanisms for the p ...... drenoceptor agonist salmeterol
@en
P2093
G Vauquelin
M Wennerberg
P2860
P304
P356
10.1111/J.1476-5381.2009.00296.X
P407
P577
2009-07-07T00:00:00Z