Search Results - "COASSOLO, P"

Evaluation of the effect of culture configuration on morphology, survival time, antioxidant status and metabolic capacities of cultured rat hepatocytes by Richert, L, Binda, D, Hamilton, G, Viollon-Abadie, C, Alexandre, E, Bigot-Lasserre, D, Bars, R, Coassolo, P, LeCluyse, E

“…We evaluated the antioxidant status, namely cellular lipid peroxidation, by measuring thiobarbituric acid reactive substances (TBARS), cellular reduced…”
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Qualitative and quantitative assessment of drug-drug interaction potential in man, based on Ki, IC50 and inhibitor concentration by Blanchard, N, Richert, L, Coassolo, P, Lavé, T

“…Strategies used to screen new drug entities as potential inhibitors of CYP450 enzymes are now widely used to select candidates in the drug discovery process…”
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Comparison of clearance predictions using primary cultures and suspensions of human hepatocytes by Blanchard, N, Alexandre, E, Abadie, C., Lavé, T, Heyd, B, Mantion, G, Jaeck, D., Richert, L, Coassolo, P

“…Various incubation conditions of human hepatocytes were compared for their accuracy in predicting the in vivo hepatic clearance (CLH) of model compounds. The…”
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Cryopreservation of adult human hepatocytes obtained from resected liver biopsies by Alexandre, E, Viollon-Abadie, C, David, P, Gandillet, A, Coassolo, P, Heyd, B, Mantion, G, Wolf, P, Bachellier, P, Jaeck, D, Richert, L

“…Isolated human hepatocytes have been shown to represent a valuable in vitro model to investigate the metabolism and cytotoxicity of xenobiotics. In addition,…”
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Impact of serum on clearance predictions obtained from suspensions and primary cultures of rat hepatocytes by Blanchard, Nadège, Richert, Lysiane, Notter, Brigitte, Delobel, Frederic, David, Pascale, Coassolo, Philippe, Lavé, Thierry

“…The objective of the present study was to compare two configurations of the hepatocyte model namely suspensions (SH) and conventional primary cultures (CPC)…”
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Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists by RÖVER, S, ADAMS, D. R, HEBEISEN, P, KENNETT, G. A, KNIGHT, A. R, MALCOLM, C. S, MATTEI, P, MISRA, A, MIZRAHI, J, MULLER, M, PORTER, R. H. P, RICHTER, H, BENARDEAU, A, TAYLOR, S, VICKERS, S. P, BENTLEY, J. M, BICKERDIKE, M. J, BOURSON, A, CLIFFE, I. A, COASSOLO, P, DAVIDSON, J. E. P, DOURISH, C. T

“…Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT(2C) receptor agonists are described…”
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The use of human hepatocytes to select compounds based on their expected hepatic extraction ratios in humans by LAVE, T, DUPIN, S, SCHMITT, C, VALLES, B, UBEAUD, G, CHOU, R. C, JAECK, D, COASSOLO, P

“…The present investigation retrospectively evaluates the use of human hepatocytes to classify compounds into low, intermediate or high hepatic extraction ratio…”
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Strain difference (WKY, SPRD) in the hepatic antioxidant status in rat and effect of hypertension (SHR, DOCA). Ex vivo and in vitro data by Binda, D, Nicod, L, Viollon-Abadie, C, Rodriguez, S, Berthelot, A, Coassolo, P, Richert, L

“…We assessed the hepatic antioxidant status of spontaneously (SHR) and desoxicorticosterone acetate (DOCA)-induced hypertensive rats and that of respective…”
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Interspecies scaling of bosentan, a new endothelin receptor antagonist and integration of in vitro data into allometric scaling by Lave, T, Coassolo, P, Ubeaud, G, Brandt, R, Schmitt, C, Dupin, S, Jaeck, D, Chou, R C

“…The goal of this study was to find a rational and reliable method of using animal data to predict the clearance of metabolised drugs in humans. One such…”
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Metabolism of mofarotene in hepatocytes and liver microsomes from different species. Comparison with in vivo data and evaluation of the cytochrome P450 isoenzymes involved in human biotransformation by Valles, B, Schiller, C D, Coassolo, P, De Sousa, G, Wyss, R, Jaeck, D, Viger-Chougnet, A, Rahmani, R

“…The arotinoid mofarotene is a novel potent anticancer compound. The metabolic profiles obtained from rat, dog, and human plasma showed a good correlation with…”
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A new extrapolation method from animals to man: application to a metabolized compound, mofarotene by Lave, T, Schmitt-Hoffmann, A H, Coassolo, P, Valles, B, Ubeaud, G, Ba, B, Brandt, R, Chou, R C

“…Allometric scaling (a technique which uses data obtained in laboratory animals to predict human pharmacokinetics) works well for drugs that are cleared intact,…”
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An evaluation of the utility of physiologically based models of pharmacokinetics in early drug discovery by Parrott, Neil, Paquereau, Nicolas, Coassolo, Philippe, Lavé, Thierry

“…Generic physiologically-based models of pharmacokinetics were evaluated for early drug discovery. Plasma profiles after intravenous and oral dosing were…”
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Relationships between in vitro and in vivo biotransformation of drugs in humans and animals : pharmaco-toxicological consequences by DE SOUSA, G, FLORENCE, N, VALLES, B, COASSOLO, P, RAHMANI, R

“…Given the crucial role played by hepatocytes in the detoxification/toxification processes of drugs, these cells have been increasingly used during the last…”
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Prediction of hepatic metabolic clearance based on interspecies allometric scaling techniques and in vitro-in vivo correlations by LAVE, T, COASSOLO, P, REIGNER, B

“…This article reviews the methods available for predicting hepatic metabolic clearance in humans, and discusses their application to the processes of drug…”
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Piperidine renin inhibitors: from leads to drug candidates by Märki, H.P., Binggeli, A., Bittner, B., Bohner-Lang, V., Breu, V., Bur, D., Coassolo, Ph, Clozel, J.P., D'Arcy, A., Doebeli, H., Fischli 1, W., Funk, Ch, Foricher, J., Giller, T., Grüninger, F., Guenzi, A., Güller, R., Hartung, T., Hirth, G., Jenny, Ch, Kansy, M., Klinkhammer, U., Lave, T., Lohri, B., Luft, F.C., Mervaala, E.M., Müller, D.N., Müller, M., Montavon, F., Oefner, Ch, Qiu, C., Reichel, A., Sanwald-Ducray, P., Scalone, M., Schleimer, M., Schmid, R., Stadler, H., Treiber 1, A., Valdenaire 2, O., Vieira, E., Waldmeier, P., Wiegand-Chou, R., Wilhelm, M., Wostl, W., Zell, M., Zell, R.

“…Non-peptidomimetic renin inhibitors of the piperidine type represent a novel structural class of compounds potentially free of the drawbacks seen with…”
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Combining in Vitro and in Vivo Pharmacokinetic Data for Prediction of Hepatic Drug Clearance in Humans by Artificial Neural Networks and Multivariate Statistical Techniques by Schneider, Gisbert, Coassolo, Philippe, Lavé, Thierry

“…Several statistical regression models and artificial neural networks were used to predict the hepatic drug clearance in humans from in vitro (hepatocyte) and…”
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Prediction of hepatic metabolic clearance: Comparison and assessment of prediction models by ZUEGGE, Jochen, SCHNEIDER, Gisbert, COASSOLO, Philippe, LAVE, Thierry

“…To perform a comparative quantitative evaluation of the prediction accuracy for human hepatic metabolic clearance of 5 different mathematical models:…”
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Plasma concentrations and pharmacokinetics of midazolam during anaesthesia by Crevat-Pisano, P, Dragna, S, Granthil, C, Coassolo, P, Cano, J P, Francois, G

“…Midazolam and 1-hydroxymidazolam plasma concentrations have been monitored and pharmacokinetic parameters of midazolam estimated during anaesthesia induced and…”
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Pharmacology of tezosentan, new endothelin receptor antagonist designed for parenteral use by Clozel, M, Ramuz, H, Clozel, J P, Breu, V, Hess, P, Löffler, B M, Coassolo, P, Roux, S

“…Tezosentan (Ro 61-0612) [5-isopropyl-pyridine-2-sulfonic acid 6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-1H-tetrazol-5-yl-+ ++pyri…”
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Pharmacokinetics of flunitrazepam following single dose oral administration in liver disease patients compared with healthy volunteers by Drouet-Coassolo, C, Iliadis, A, Coassolo, P, Antoni, M, Cano, J P

“…The pharmacokinetic behaviour of flunitrazepam and its main active metabolite, N-desmethyl flunitrazepam, was investigated in 12 patients with liver disease…”
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