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
… By applying this approach on intact plated recombinant cell lines expressing the human G
protein coupled receptors of interest, we have already detected such rebinding behaviour for …

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
Exploring avidity: understanding the potential gains in functional affinity and target
residence time of bivalent and heterobivalent ligands - Vauquelin - 2013 - British Journal of …

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

I Van Liefde, G Vauquelin - Molecular and cellular endocrinology, 2009 - Elsevier
G protein-dependent effects on blood pressure (via inositol triphosphate production, cytosolic
calcium transients and vascular smooth muscle contraction), there are also long-term G

Imidazoline receptors, non-adrenergic idazoxan binding sites and α2-adrenoceptors in the human central nervous system

…, J De Keyser, JP De Backer, P Bousquet, G Vauquelin - Neuroscience, 1994 - Elsevier
Both [ 3 H]clonidine and [ 3 H]idazoxan bind to α 2 adrenoceptors. The former also labels
imidazoline receptors, and the latter non-adrenergic idazoxan binding sites. In order to …

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 …

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

G Vauquelin - British journal of pharmacology, 2016 - Wiley Online Library
… Interestingly, the occupancy curves remain exactly the same as those shown in Figure 2G
when both k off and k on are changed alike to yield an iso-K D situation in simulations that are …

Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO‐K1 cells expressing human angiotensin II AT1 receptors

…, N Fraeyman, G Vauquelin - British journal of …, 1999 - Wiley Online Library
CHO‐K1 cells that were stably transfected with the gene for the human AT 1 receptor (CHO‐AT
1 cells) were used for pharmacological studies of non‐peptide AT 1 receptor antagonists. …

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 …

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

SJ Charlton, G Vauquelin - British journal of pharmacology, 2010 - Wiley Online Library
… protein-coupled receptors (GPCRs) can trigger an increase in cytosolic calcium concentration,
most commonly by initiating a cascade of events involving G proteins, phospholipase C (…

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 …