Search Results - "Jensen, Klaus Gjervig"
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Discovery of 1-[2-(2,4-Dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): A Novel Multimodal Compound for the Treatment of Major Depressive Disorder
Published in Journal of medicinal chemistry (12-05-2011)“…The synthesis and structure−activity relationship of a novel series of compounds with combined effects on 5-HT3A and 5-HT1A receptors and on the serotonin…”
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Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700
Published in Bioorganic & medicinal chemistry letters (15-09-2022)“…[Display omitted] The N-demethylation of zicronapine (7) and three of its deuterated analogs 8 – 10 has been studied in human in vitro metabolism systems…”
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Test systems in drug discovery for hazard identification and risk assessment of human drug-induced liver injury
Published in Expert opinion on drug metabolism & toxicology (01-07-2017)“…The liver is an important target for drug-induced toxicities. Early detection of hepatotoxic drugs requires use of well-characterized test systems, yet current…”
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Risk assessment of accidental nortriptyline poisoning: The importance of cytochrome P450 for nortriptyline elimination investigated using a population-based pharmacokinetic simulator
Published in European journal of pharmaceutical sciences (09-10-2011)“…It is not possible to make a prospective clinical study that reveals the importance of the nortriptyline metabolising cytochrome P450 (CYP) isoforms (CYP1A2,…”
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5-Hydroxy- l-tryptophan alters gaboxadol pharmacokinetics in rats: Involvement of PAT1 and rOat1 in gaboxadol absorption and elimination
Published in European journal of pharmaceutical sciences (31-01-2010)“…The aim was to investigate the effect of 5-hydroxy- l-tryptophan (5-HTP) on gaboxadol pharmacokinetics in rats. As both 5-HTP and gaboxadol bind to the human…”
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Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential
Published in Bioorganic & medicinal chemistry letters (01-08-2012)“…We describe the discovery of a series of compounds based on…”
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Identification of Cytochrome P450 Isoforms Involved in the Metabolism of Paroxetine and Estimation of Their Importance for Human Paroxetine Metabolism Using a Population-Based Simulator
Published in Drug metabolism and disposition (01-03-2010)“…We identify here for the first time the low-affinity cytochrome P450 (P450) isoforms that metabolize paroxetine, using cDNA-expressed human P450s measuring…”
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N°356 - Muscle velocity recovery cycles as pharmacodynamic biomarker in a first-in-human trial of a first-in-class chloride channel 1 inhibitor: A randomized, double-blind, placebo-controlled, cross-over study in healthy subjects and patients with myasthenia grav
Published in Clinical neurophysiology (01-06-2023)Get full text
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Lack of Exposure in a First-in-Man Study Due to Aldehyde Oxidase Metabolism: Investigated by Use of super(14) C-microdose, Humanized Mice, Monkey Pharmacokinetics, and In Vitro Methods
Published in Drug metabolism and disposition (01-01-2017)“…Inclusion of a microdose of super(14) C-labeled drug in the first-in-man study of new investigational drugs and subsequent analysis by accelerator mass…”
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Metabolites of [14C]-5-(2-Ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine in Mice, Rats, Dogs, and Humans
Published in Drug metabolism and disposition (01-11-1999)“…The M1 muscarine agonist, 5-(2-ethyl-2 H -tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine (Lu 25â109), is extensively metabolized in mice, rats, dogs, and…”
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Effects of organotin compounds on mitosis, spindle structure, toxicity and in vitro microtubule assembly
Published in Mutagenesis (01-09-1991)“…Di- and tri-methyl, -butyl and phenyl tin, all as chlorides were tested for toxicity and spindle disturbances in V79 Chinese hamster cells and for effects on…”
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Lack of Exposure in a First-in-Man Study Due to Aldehyde Oxidase Metabolism: Investigated by Use of 14C-microdose, Humanized Mice, Monkey Pharmacokinetics, and In Vitro Methods
Published in Drug metabolism and disposition (01-01-2017)“…Inclusion of a microdose of C-labeled drug in the first-in-man study of new investigational drugs and subsequent analysis by accelerator mass spectrometry has…”
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Differential effects of γ-secretase and BACE1 inhibition on brain Aβ levels in vitro and in vivo
Published in Journal of neurochemistry (01-09-2009)“…Alzheimer's disease (AD) is hypothesized to result from elevated brain levels of β-amyloid peptide (Aβ) which is the main component of plaques found in AD…”
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Differential effects of [gamma]-secretase and BACE1 inhibition on brain A[beta] levels in vitro and in vivo
Published in Journal of neurochemistry (01-09-2009)“…Alzheimer's disease (AD) is hypothesized to result from elevated brain levels of [beta]-amyloid peptide (A[beta]) which is the main component of plaques found…”
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Organotin compounds induce aneuploidy in human peripheral lymphocytes in vitro
Published in Mutation research (01-01-1991)“…In vitro exposure of PHA-stimulated human lymphocytes to organotin compounds resulted in statistically significant increases in the frequencies of hyperdiploid…”
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Differential effects of gamma-secretase and BACE1 inhibition on brain Abeta levels in vitro and in vivo
Published in Journal of neurochemistry (01-09-2009)“…Alzheimer's disease (AD) is hypothesized to result from elevated brain levels of beta-amyloid peptide (Abeta) which is the main component of plaques found in…”
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New alpha(1)-adrenoceptor antagonists derived from the antipsychotic sertindole - carbon-11 labelling and pet examination of brain uptake in the cynomolgus monkey
Published in Nuclear medicine and biology (01-04-2004)“…Central alpha(1)-adrenergic receptors are potential targets for recently developed antipsychotic drugs. Two new 11C labeled potent and selective…”
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In vitro metabolism of the M1-muscarinic agonist 5-(2-ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine by human hepatic cytochromes P-450 determined at pH 7.4 and 8.5
Published in Drug metabolism and disposition (01-01-1999)“…Biotransformation of the M1-muscarinic agonist Lu 25-109 (5-(2-ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine) , in development for the treatment…”
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