A5018841545- Retinoids in leukemia and cellular processes
- Retinal Development and Disorders
- Carcinogens and Genotoxicity Assessment
- Pharmacogenetics and Drug Metabolism
- Chronic Obstructive Pulmonary Disease (COPD) Research
- Synthesis and Biological Evaluation
- Chemical Reactions and Isotopes
- Cardiac electrophysiology and arrhythmias
- Sulfur Compounds in Biology
- Amino Acid Enzymes and Metabolism
- Synthetic Organic Chemistry Methods
- Advanced Chemical Sensor Technologies
- Estrogen and related hormone effects
- Neuroscience of respiration and sleep
- Birth, Development, and Health
- Ion channel regulation and function
- Reproductive Health and Contraception
- Diet and metabolism studies
- Vanadium and Halogenation Chemistry
- Ovarian function and disorders
- Hormonal and reproductive studies
- Signaling Pathways in Disease
- Advanced biosensing and bioanalysis techniques
- Pregnancy and preeclampsia studies
- Pharmacological Effects and Assays
Integrative Research Laboratories
2021
AstraZeneca (Sweden)
2012-2016
Freie Universität Berlin
1988-1990
Uppsala University
1981-1988
Swedish University of Agricultural Sciences
1986
Abstract A fully automated reversed-phase high-performance liquid chromatography (HPLC) procedure with precolumn switching is presented which allows quantitative assay of 13-cis-retinoic acid and all-trans-retinoic acid, their 4-oxo-metabolites retinol in plasma, amniotic fluid tissue homogenates. binary gradient system allowed baseline separation the retinoids within 15 minutes. Sample preparation was kept simple order to minimize degradation isomerization unstable substances required only...
Abstract: Low‐temperature whole‐body autoradiography in Syrian golden hamsters, 11 and 15 days pregnant, given N‐ 14 C‐nitrosodiethylamine, indicated an ability of the non‐metabolized substance to freely pass cellular membranes maternal, placental foetal tissues. Experiments vitro with tissues adult hamsters showed a capacity nasal olfactory respiratory mucosa, trachea, lung, lateral gland, liver kidney degrade N‐nitrosodiethylamine. Autoradiography localization non‐volatile...
1. By the use of whole-body autoradiography, localization N-nitroso[14C]pyrrolidine and its metabolites was demonstrated in tissues C57B1-mice Sprague—Dawley rats.2. On basis autoradiorgraphic data, were selected tested for their ability to metabolize 14CO2 tissue-bound metabolites.3. The results indicated that only a few had marked degrade N-nitrosopyrrolidine. These liver nasal mucosa both species, tracheo-bronchial mice, lower extent kidneys species.
The in vitro metabolic stability assays are indispensable for screening the liability of new chemical entities (NCEs) drug discovery. Intrinsic clearance (CLint) values from liver microsomes and/or hepatocytes frequently used to assess as well quantitatively predict vivo hepatic plasma (CLH). An often approximation is so called wellstirred model which has gained widespread use. applications well-stirred typically dependent on several measured parameters and hence with potential...
Etretinate (Tegison^®, Tigason^®), a retinoid used for the treatment of skin disorders such as psoriasis, was shown to be teratogenic in human. Because long terminal half-life this drug ( 100 days), considerable plasma levels etretinate and its main metabolite, etretin (acitretin), were observed up 2 years following discontinuation therapy. We have therefore investigated, newly developed animal model, potential risk persisting these aromatic retinoids.Etretinate administered by intragastric...
NMRI mice were treated on day 11 (day 0 = plug day) of gestation with a single oral dose 100 mg/kg either all-trans-etretin (acitretin) or 13-cis-etretin. For teratology studies sacrificed 18 gestation, and the fetuses examined for malformations. pharmacokinetic studies, groups 5 after 5, 10, 30 min 1, 2, 4, 8 h. The concentrations retinoids in maternal plasma embryos determined by newly developed HPLC gradient method. All-trans-etretin induced malformations 94% fetuses, mainly fore hind...
In the Western world, over 350,000 deaths and $30 billion in medical costs are attributed annually to stroke. Head spinal cord trauma cause an estimated 250,000 result of $15 billion. Although stroke head/spinal leading causes disability death humans, no adequate neuroprotective treatment is available. Glutamate antagonists derived from quinoxa-linedione scaffold as drug candidates for neuroprotection trauma. Quinoxalinedione derivatives such 2,3-dihydroxy-6-...
Abstract: Rats were given 14 C‐halothane intravenously and whole‐body autoradiography with freeze‐dried sections, or sections extracted in trichloroacetic acid, water, organic solvents, was carried out to trace tissues accumulating halothane metabolites. In vitro incubations of tissue homogenates performed examine the capacity by various organs form tissue‐bound C from C‐halothane. Autoradiography isolated after incubation study localization metabolites formed under conditions. A observed...
Abstract The management of Parkinson's disease (PD) is frequently compromised by complications induced dopaminergic treatment such as involuntary movements (dyskinesias) and psychosis. Mesdopetam (IRL790) a novel dopamine D3 receptor antagonist developed for the therapy in PD. This study evaluated safety, tolerability, pharmacokinetics escalating single multiple doses mesdopetam. We conducted prospective, single‐center, randomized, double‐blind, placebo‐controlled phase I, first‐in‐human...
The objectives were to estimate and compare, in silico vivo, the effects of a strong moderate CYP3A4 inhibitor on AZD1305 pharmacokinetics. In silico, simulations performed with computer software Simcyp, predicted outcome was compared results observed healthy male subjects. geometric mean plasma exposure + ketoconazole showed 7.1-fold higher AUC 4.4-fold Cmax alone. Coadministration verapamil gave 1.9-fold 1.7-fold 7.7-fold 4.8 -fold 2.2-fold 2.0-fold maximum QTcF increase from baseline 407,...