Long‐lasting target binding and rebinding as mechanisms to prolong in vivo drug action

G Vauquelin, SJ Charlton - British journal of pharmacology, 2010 - Wiley Online Library
An increasing number of examples in the literature suggest that the in vivo duration of drug
action not only depends on macroscopic pharmacokinetic properties like plasma half‐life and …

Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands

G Vauquelin, SJ Charlton - British journal of pharmacology, 2013 - Wiley Online Library
Bivalent ligands are increasingly important therapeutic agents. Although the naturally occurring
antibodies are predominant, it is becoming more common to combine different antibody …

Isoquinoline Derivatives Isolated from the Fruit of Annona muricata as 5-HTergic 5-HT1A Receptor Agonists in Rats: Unexploited Antidepressive (Lead) Products

…, JP De Backer, G Vauquelin… - Journal of pharmacy …, 1997 - academic.oup.com
The fruit and the leaves of Annona muricata (Annonaceae) are used in traditional medicine
for their tranquillizing and sedative properties. Extracts of the plant have been shown to …

Sartan–AT1 receptor interactions: in vitro evidence for insurmountable antagonism and inverse agonism

I Van Liefde, G Vauquelin - Molecular and cellular endocrinology, 2009 - Elsevier
Sartans are non-peptide AT 1 receptor antagonists used to treat hypertension and related
pathologies. Their effects on the G protein-dependent responses of angiotensin II (Ang II) were …

Effects of target binding kinetics on in vivo drug efficacy: koff, kon and rebinding

G Vauquelin - British journal of pharmacology, 2016 - Wiley Online Library
Background and Purpose Optimal drug therapy often requires continuing high levels of target
occupancy. Besides the traditional pharmacokinetic contribution, target binding kinetics is …

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays

SJ Charlton, G Vauquelin - British journal of pharmacology, 2010 - Wiley Online Library
Calcium is a key intracellular signal that controls manifold cellular processes over a wide
temporal range. The development of calcium‐sensitive fluorescent dyes and proteins …

Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence time

G Vauquelin - Expert opinion on drug discovery, 2010 - Taylor & Francis
Importance of the field: It is well established that the in vivo duration of drug action not only
depends on macroscopic pharmacokinetic properties like its plasma half-life, but also on the …

Involvement of insulin-regulated aminopeptidase in the effects of the renin–angiotensin fragment angiotensin IV: a review

…, D De Bundel, S Sarre, I Smolders, G Vauquelin… - Heart failure …, 2008 - Springer
For decades, angiotensin (Ang) II was considered as the end product and the only bioactive
peptide of the renin–angiotensin system (RAS). However, later studies revealed biological …

Age‐related changes in the human nigrostriatal dopaminergic system

…, G Ebinger, G Vauquelin - Annals of Neurology …, 1990 - Wiley Online Library
A deficiency of dopamine in the striatum may contribute to the decline in motor function
associated with aging. We examined the effect of aging on the densities of the D 1 and D 2 …

Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism

G Vauquelin, S Bostoen, P Vanderheyden… - Naunyn-Schmiedeberg's …, 2012 - Springer
Drug–receptor interactions are traditionally quantified in terms of affinity and efficacy, but
there is increasing awareness that the drug-on-receptor residence time also affects clinical …