Search Results - "VAUQUELIN, G"

Sartan-AT1 receptor interactions: in vitro evidence for insurmountable antagonism and inverse agonism by Van Liefde, I, Vauquelin, G

“…Sartans are non-peptide AT(1) receptor antagonists used to treat hypertension and related pathologies. Their effects on the G protein-dependent responses of…”
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Ligands, their receptors and … plasma membranes by Vauquelin, G., Packeu, A.

“…Ligand–receptor interactions are customarily described by equations that apply to solutes. Yet, most receptors are present in cell membranes so that…”
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Molecular mechanisms for the persistent bronchodilatory effect of the β2‐adrenoceptor agonist salmeterol by Szczuka, A, Wennerberg, M, Packeu, A, Vauquelin, G

“…Background:  β2‐adrenoceptor agonists are effective bronchodilators. In vitro studies demonstrated long‐lasting airway smooth muscle relaxation by salmeterol…”
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The influence of drug distribution and drug-target binding on target occupancy: The rate-limiting step approximation by de Witte, W.E.A., Vauquelin, G., van der Graaf, P.H., de Lange, E.C.M.

“…The influence of drug-target binding kinetics on target occupancy can be influenced by drug distribution and diffusion around the target, often referred to as…”
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Estimation of the dissociation rate of unlabelled ligand–receptor complexes by a ‘two‐step’ competition binding approach by Packeu, A, Wennerberg, M, Balendran, A, Vauquelin, G

“…BACKGROUND AND PURPOSE Because the in vivo effectiveness of ligands may also be determined by the rate by which they dissociate from their target receptors,…”
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Molecular characterisation of the interactions between olmesartan and telmisartan and the human angiotensin II AT 1 receptor by Le, M T, Pugsley, M K, Vauquelin, G, Van Liefde, I

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Molecular mechanisms for the persistent bronchodilatory effect of the beta 2-adrenoceptor agonist salmeterol by Szczuka, A, Wennerberg, M, Packeu, A, Vauquelin, G

“…Beta(2)-adrenoceptor agonists are effective bronchodilators. In vitro studies demonstrated long-lasting airway smooth muscle relaxation by salmeterol after…”
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G protein-coupled receptors: a count of 1001 conformations by Vauquelin, G., Van Liefde, I.

“…G protein‐coupled receptors (GPCRs) were initially regarded to adopt an inactive and an active conformation and to activate a single type of G protein. Studies…”
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Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociation by Vauquelin, Georges, Szczuka, Anna

“…The present review addresses the theories which have been advanced to explain experimental observations dealing with insurmountable antagonism and accelerated…”
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Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO‐K1 cells expressing human angiotensin II AT1 receptors by Vanderheyden, P M L, Fierens, F L P, De Backer, J P, Fraeyman, N, Vauquelin, G

“…CHO‐K1 cells that were stably transfected with the gene for the human AT1 receptor (CHO‐AT1 cells) were used for pharmacological studies of non‐peptide AT1…”
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Translocation of the insulin‐regulated aminopeptidase to the cell surface: detection by radioligand binding by Demaegdt, H, Smitz, L, De Backer, J‐P, Le, M T, Bauwens, M, Szemenyei, E, Tóth, G, Michotte, Y, Vanderheyden, P, Vauquelin, G

“…Background and purpose: Insulin‐regulated aminopeptidase (IRAP) and the insulin‐dependent glucose transporter GLUT4 colocalize in specific intracellular…”
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New insights in insurmountable antagonism by Vauquelin, G., Van Liefde, I., Birzbier, B. B., Vanderheyden, P. M. L.

“…Antagonists that produce parallel rightward shifts of agonist dose–response curves with no alteration of the maximal response are traditionally classified as…”
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Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors by Verheijen, Ilse, Fierens, F.L.P., DeBacker, J.P., Vauquelin, G., Vanderheyden, P.M.L.

“…— The interaction between the AT1 receptor‐selective antagonist valsartan, and its human receptor, was investigated by direct radioligand binding as well as by…”
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Autoradiographic distribution of D3-type dopamine receptors in human brain using [3H]7-hydroxy-N,N-di-n-propyl-2-aminotetralin by Herroelen, L, De Backer, J P, Wilczak, N, Flamez, A, Vauquelin, G, De Keyser, J

“…The regional distribution of D3 dopamine receptors was studied in human brain by quantitative autoradiography with…”
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Biological screening of selected medicinal Panamanian plants by radioligand-binding techniques by Caballero-George, C., Vanderheyden, P.M.L., Solis, P.N., Pieters, L., Shahat, A.A., Gupta, M.P., Vauquelin, G., Vlietinck, A.J.

“…Nineteen plants from the Republic of Panama were selected by their traditional uses in the treatment of hypertension, cardiovascular, mental and feeding…”
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Isoquinoline Derivatives Isolated from the Fruit of Annona muricata as 5-HTergic 5-HT1A Receptor Agonists in Rats: Unexploited Antidepressive (Lead) Products by HASRAT, J. A., DE BRUYNE, T., DE BACKER, J.-P., VAUQUELIN, G., VLIETINCK, A. J.

“…The fruit and the leaves of Annona muricata (Annonaceae) are used in traditional medicine for their tranquillizing and sedative properties. Extracts of the…”
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Evaluation of bioactive saponins and triterpenoidal aglycons for their binding properties on human endothelin ETA and angiotensin AT1 receptors by Caballero-George, C., Vanderheyden, P. M. L., Okamoto, Y., Masaki, T., Mbwambo, Z., Apers, S., Gupta, M. P., Pieters, L., Vauquelin, G., Vlietinck, A.

“…Different types of triterpenes including saponins and aglycons were evaluated for their ability to inhibit [3H] BQ‐123 and [3H] angiotensin II binding to the…”
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Slow antagonist dissociation and long-lasting in vivo receptor protection by Vauquelin, Georges, Van Liefde, Isabelle

“…The ability of antagonists to form slowly dissociating complexes with their cognate receptors has repeatedly been proposed to contribute to their long-lasting…”
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Multiple beta adrenergic receptor subclasses mediate the l-isoproterenol-induced lipolytic response in rat adipocytes by Van Liefde, I, Van Witzenburg, A, Vauquelin, G

“…l-Isoproterenol has been proposed to stimulate lipolysis in rat epididymal adipocytes via atypical beta adrenergic receptors, whereas radioligand binding…”
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Differential muscarinic receptor binding of acetylcholinesterase inhibitors in rat brain, human brain and Chinese hamster ovary cells expressing human receptors by Van Den Beukel, I, Dijcks, F A, Vanderheyden, P, Vauquelin, G, Oortgiesen, M

“…Displacement of muscarinic radioligands by the cholinesterase inhibitors parathion, paraoxon, physostigmine and phenyl saligenin cyclic phosphate was examined…”
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