Search Results - "Venhorst, J."
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Generation of Bayesian prediction models for OATP-mediated drug–drug interactions based on inhibition screen of OATP1B1, OATP1B1∗15 and OATP1B3
Published in European journal of pharmaceutical sciences (05-04-2015)“…[Display omitted] Human organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 are important hepatic uptake transporters. Early assessment of…”
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Two novel 5-HT6 receptor antagonists ameliorate scopolamine-induced memory deficits in the object recognition and object location tasks in Wistar rats
Published in Neurobiology of learning and memory (01-09-2011)“…► CMP X and CMP Y are two novel and highly selective 5-HT6 receptor antagonists. ► CMP X and CMP Y improved scopolamine-induced deficits in tests for episodic…”
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The selective 5-HT6 receptor antagonist SLV has putative cognitive- and social interaction enhancing properties in rodent models of cognitive impairment
Published in Neurobiology of learning and memory (01-09-2016)“…•SLV is a novel highly selective 5-HT6 antagonist.•SLV was studied in animal models for cognitive impairment and social interaction.•SLV was effective at 20…”
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Hazard assessment of nitrosamine and nitramine by-products of amine-based CCS: Alternative approaches
Published in Regulatory toxicology and pharmacology (01-04-2015)“…•Amine-based post-combustion carbon capture may generate nitrosamines and nitramines.•Predictive models will save animals and allow safety testing to keep up…”
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A novel highly selective 5-HT6 receptor antagonist attenuates ethanol and nicotine seeking but does not affect inhibitory response control in Wistar rats
Published in Behavioural brain research (01-01-2013)“…▸ CMP 42 is a CNS available, selective 5-HT6 antagonist. ▸ CMP 42 was effective in reducing nicotine self-administration in Wistar rats. ▸ CMP 42 reduced…”
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WITHDRAWN: Hazard assessment of nitrosamine and nitramine by-products of amine-based CCS: an alternative approach
Published in Regulatory toxicology and pharmacology (01-10-2014)“…This article has been withdrawn at the request of the author(s) and/or editor. The Publisher apologizes for any inconvenience this may cause. The full Elsevier…”
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Studies on the inhibition of human cytochromes P450 by selenocysteine Se -conjugates
Published in Xenobiotica (2003)“…1. To investigate whether cytochrome P450 (P450) inhibition can contribute to the chemopreventive activity of selenocysteine Se -conjugates (SeCys conjugates),…”
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Development of an intelligence platform for efficient drug Target Safety Assessments
Published in Toxicology letters (16-09-2016)Get full text
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A holistic approach to the safety assessment of exploratory drug targets
Published in Toxicology letters (16-10-2015)Get full text
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Homology Modeling of Rat and Human Cytochrome P450 2D (CYP2D) Isoforms and Computational Rationalization of Experimental Ligand-Binding Specificities
Published in Journal of medicinal chemistry (02-01-2003)“…The ligand-binding characteristics of rat and human CYP2D isoforms, i.e., rat CYP2D1−4 and human CYP2D6, were investigated by measuring IC50 values of 11 known…”
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Identification of Ligand-binding Site III on the Immunoglobulin-like Domain of the Granulocyte Colony-stimulating Factor Receptor
Published in The Journal of biological chemistry (28-09-2001)“…The granulocyte colony-stimulating factor receptor (G-CSF-R) forms a tetrameric complex with G-CSF containing two ligand and two receptor molecules. The…”
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Design, Synthesis, and Characterization of 7-Methoxy-4-(aminomethyl)coumarin as a Novel and Selective Cytochrome P450 2D6 Substrate Suitable for High-Throughput Screening
Published in Chemical research in toxicology (01-07-1999)“…In this study, a selective substrate for cytochrome P450 2D6 was designed using a small molecule model developed by M. J. De Groot et al. [(1997) Chem. Res…”
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Influence of N-Substitution of 7-Methoxy-4-(aminomethyl)-coumarin on Cytochrome P450 Metabolism and Selectivity
Published in Drug metabolism and disposition (01-12-2000)“…A series of six structural analogs of 7-methoxy-4-(aminomethyl)-coumarin (MAMC), a recently developed high-throughput substrate of P450 2D6 (CYP2D6), was…”
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Evaluation of a novel high-throughput assay for cytochrome P450 2D6 using 7-methoxy-4-(aminomethyl)-coumarin
Published in European journal of pharmaceutical sciences (01-12-2000)“…We recently reported on the design, synthesis and characterisation of a novel and selective substrate of human cytochrome P450 2D6 (CYP2D6),…”
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The Histamine H1-Receptor Antagonist Binding Site. A Stereoselective Pharmacophoric Model Based upon (Semi-)Rigid H1-Antagonists and Including a Known Interaction Site on the Receptor
Published in Journal of medicinal chemistry (01-08-1995)“…A new pharmacophoric model for the H1-antagonist binding site is derived which reveals that a simple atom to atom matching of compounds is not sufficient; in…”
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Modeling and molecular dynamics of glutamine transaminase K/cysteine conjugate β-lyase
Published in Journal of molecular graphics & modelling (01-09-2003)“…The homodimeric, pyridoxal 5′-phosphate (PLP)-dependent enzyme glutamine transaminase K/cysteine conjugate β-lyase (GTK/β-lyase) has been implicated in the…”
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The histamine H sub(1)-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H sub(1)-antagonists and including a known interaction site on the receptor
Published in Journal of medicinal chemistry (01-01-1995)“…A new pharmacophoric model for the H sub(1)-antagonist binding site is derived which reveals that a simple atom to atom matching of compounds is not…”
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Simultaneous determination of eight lipid peroxidation degradation products in urine of rats treated with carbon tetrachloride using gas chromatography with electron-capture detection
Published in Journal of chromatography. B, Biomedical sciences and applications (04-07-1997)“…One of the major processes that occur as a result of radical-induced oxidative stress is lipid peroxidation (LPO). Degradation of lipid peroxides results in…”
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