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In Vitro Pharmacological Characterization of Vilanterol, a Novel Long-Acting β2-Adrenoceptor Agonist with 24-Hour Duration of Action
TLDR
From these investigations, the data for vilanterol are consistent, showing that it is a novel, potent, and selective β2-AR receptor agonist with a long duration of action. Expand
Receptor specificity and trigemino‐vascular inhibitory actions of a novel 5‐HT1B/1D receptor partial agonist, 311C90 (zolmitriptan)
TLDR
The receptor specificity of the drug and its actions on trigeminal‐evoked plasma protein extravasation into the dura mater of the anaesthetized guinea‐pig is described and the inability of 5‐ HT1B/1D agonists to achieve the same maximum as the endogenous agonist 5‐HT is explained by the additional presence of5‐HT2A receptors. Expand
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
TLDR
Compound 13f had high potency, selectivity, fast onset, and long duration of action in vitro and was found to have long duration in vivo, low oral bioavailability in the rat, and to be rapidly metabolized. Expand
Pharmacological Characterization of GSK573719 (Umeclidinium): A Novel, Long-Acting, Inhaled Antagonist of the Muscarinic Cholinergic Receptors for Treatment of Pulmonary Diseases
TLDR
GSK573719 is a potent anticholinergic agent that demonstrates slow functional reversibility at the human M3 mAChR and long duration of action in animal models, which suggested umeclidinium will be a once-daily inhaled treatment of pulmonary diseases. Expand
Characterization of selective Calcium-Release Activated Calcium channel blockers in mast cells and T-cells from human, rat, mouse and guinea-pig preparations.
TLDR
GSK-5498A and GSK-7975A confirm the critical role of CRAC channels in human mast cell and T-cell function, and that inhibition can be achieved in vitro, and the rat displays a similar pharmacology to human, promoting this species for future in vivo research with this series of molecules. Expand
Oxazolidinones as novel human CCR8 antagonists.
TLDR
The synthesis, structure-activity relationships, and optimization of the series of N-substituted-5-aryl-oxazolidinones that led to the identification of SB-649701 (1a) are described. Expand
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
TLDR
Sulfonamide 29b had the best profile of potency, selectivity, onset, andduration of action on both guinea pig trachea and human bronchus and was found to have low oral bioavailability in rat and dog and also to have long duration of action in an in vivo model of bronchodilation. Expand
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