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Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).
- M. Gillard, C. Van der Perren, N. Moguilevsky, R. Massingham, P. Chatelain
- Biology, ChemistryMolecular pharmacology
- 1 February 2002
Binding results indicated that the interaction between cetirizine, its enantiomers, and histamine is compatible with a competitive behavior, in contrast with the noncompetitive profile of cetIRizine and levocetirIZine observed in isolated organs.
Comparative Study of Membrane Potential-Sensitive Fluorescent Probes and their Use in Ion Channel Screening Assays
The authors concluded that the FRET dyes from PanVera and the FMP dye are unable to measure the gramicidin-induced cell membrane hyperpolarizations.
Profiling of Olfactory Receptor Gene Expression in Whole Human Olfactory Mucosa
- Christophe Verbeurgt, F. Wilkin, M. Tarabichi, F. Grégoire, J. Dumont, P. Chatelain
- BiologyPloS one
- 6 May 2014
A TaqMan Low Density Array (Applied Biosystems), containing probes for 356 predicted human olfactory receptor loci is designed to investigate their expression in whole human Olfactory mucosa tissues and provide an opportunity to select the frequently expressed and potentially functional olfFactory receptors in view of a systematic deorphanization.
Pharmacological Differences between Human and Guinea Pig Histamine H1 Receptors: Asn84 (2.61) as Key Residue within an Additional Binding Pocket in the H1 Receptor
The data provide the first evidence that for some H1R ligands, the binding pocket is not only limited to TMs 3, 4, 5, and 6 but also comprises an additional pocket formed by TMs 2 and 7.
Binding characteristics of levetiracetam to synaptic vesicle protein 2A (SV2A) in human brain and in CHO cells expressing the human recombinant protein.
SR 33589, a New Amiodarone‐like Antiarrhythmic Agent: Electrophysiological Effects in Anesthetized Dogs
- A. Manning, Vincent Thisse, D. Hodeige, J. Richard, J. Heyndrickx, P. Chatelain
- Medicine, BiologyJournal of cardiovascular pharmacology
- 1 February 1995
It is suggested that acute administration of SR 33589 results in electro-physiological actions similar to those produced by amiodarone, and prolonged VERP more at longer CL than at shorter CL, but the degree of reduction at short CL was less with SR 335 89 than with amioarone.
Amiodarone partitioning with phospholipid bilayers and erythrocyte membranes.
Partition coefficient measurements on erythrocyte ghosts suggested that amiodarone partitioned to a similar extent in the protein and lipid content of the membrane.
BRAIN DISTRIBUTION OF CETIRIZINE ENANTIOMERS: COMPARISON OF THREE DIFFERENT TISSUE-TO-PLASMA PARTITION COEFFICIENTS: Kp, Kp,u, AND Kp,uu
- Anubha Gupta, P. Chatelain, R. Massingham, E. Jonsson, M. Hammarlund-Udenaes
- Biology, ChemistryDrug Metabolism and Disposition
- 1 February 2006
It is shown that the enantiomers are effluxed to a large extent across the BBB, and when determining stereoselectivity in brain distribution, it is important to study all factors governing this distribution, binding in blood and brain, and theBBB equilibrium.
Interaction of the antiarrhythmic agents SR 33589 and amiodarone with the β‐adrenoceptor and adenylate cyclase in rat heart
- P. Chatelain, L. Meysmans, J. Matteazzi, P. Beaufort, M. Clinet
- Biology, MedicineBritish journal of pharmacology
- 1 October 1995
It is proposed that SR 33589 and amiodarone interact with the β‐adrenoceptor at a site close to the intracellular loops which are involved in the coupling with Gs and contain the phosphorylable sites.