A5071644961- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Vanadium and Halogenation Chemistry
- Receptor Mechanisms and Signaling
- Metal-Catalyzed Oxygenation Mechanisms
- Neurotransmitter Receptor Influence on Behavior
- Pharmacological Receptor Mechanisms and Effects
- Metal complexes synthesis and properties
- Synthesis and Biological Evaluation
- Chemical synthesis and alkaloids
- Neuropeptides and Animal Physiology
- Neuroscience and Neuropharmacology Research
- Diet and metabolism studies
- Phosphodiesterase function and regulation
- Ion Channels and Receptors
- Computational Drug Discovery Methods
- Tryptophan and brain disorders
- Eicosanoids and Hypertension Pharmacology
- Phenothiazines and Benzothiazines Synthesis and Activities
- Bipolar Disorder and Treatment
- Natural Compound Pharmacology Studies
- Alkaloids: synthesis and pharmacology
- Neurobiology and Insect Physiology Research
- Birth, Development, and Health
- Heme Oxygenase-1 and Carbon Monoxide
Jagiellonian University
2015-2024
National Center for Drug Screening
2020
In order to target behavioral and psychological symptoms of dementia (BPSD), we used molecular modeling-assisted design obtain novel multifunctional arylsulfonamide derivatives that potently antagonize 5-HT(6/7/2A) D2 receptors, without interacting with M1 receptors hERG channels. vitro studies confirmed their antagonism 5-HT(7/2A) weak interactions key antitargets (M1R hERG) associated side effects. Marked 5-HT6 receptor affinities were also observed, notably for...
Alzheimer's disease (AD) is a major public health problem, which due to its increasing prevalence and lack of effective therapy or diagnostics. The complexity the AD pathomechanism requires complex treatment, e.g. multifunctional ligands targeting both causes symptoms disease. Here, we present new multitarget-directed combining pharmacophore fragments that provide blockade serotonin 5-HT6 receptors, acetyl/butyrylcholinesterase inhibition, amyloid β antiaggregation activity. Compound 12 has...
Aim Schizophrenia involves complex interactions between biological and environmental factors, including childhood trauma, cognitive impairments, premorbid adjustment. Predicting its severity progression remains challenging. Biomarkers like glial cell line-derived neurotrophic factor (GDNF) miRNA-29a may bridge aspects. The goal was to explore the connections miRNAs neural proteins functioning, adjustment in first episode of psychosis (FEP). Method This study included 19 FEP patients who...
The aim of this study was to further characterize pharmacological properties two phenylpiperazine derivatives: 1-{2-[2-(2,6-dimethlphenoxy)ethoxy]ethyl}-4-(2-methoxyphenyl)piperazynine hydrochloride (HBK-14) and 2-[2-(2-chloro-6-methylphenoxy)ethoxy]ethyl-4-(2- methoxyphenyl)piperazynine dihydrochloride (HBK-15) in radioligand binding functional vitro assays as well vivo models. Antidepressant-like were investigated the forced swim test (FST) mice rats. Anxiolytic-like activity evaluated...
The search for drugs with anorectic activity, acting within the adrenergic system has attracted interest of researchers. Partial α2-adrenoceptor agonists might offer potential effective and safe treatment obesity. We compared effectiveness safety ligands in reducing body mass. also analyzed if antagonist partial α2-adrenoceptor––yohimbine guanfacine––act similarly, determined which course action is connected activity. tested intrinsic activity effect on lipolysis these compounds cell...
Abstract Benzophenone-3 (BP-3), the most widely used UV chemical filter, is absorbed well through skin and gastrointestinal tract can affect some body functions, including survival of nerve cells. Previously, we showed that BP-3 evoked a neurotoxic effect in male rats, but since effects this compound are known to depend on gender, aim present study was show concentration potential action female rat brain. administered dermally rats during pregnancy, then 7th 8th weeks age their offspring....
Janusz Szklarzewicz*a, Anna Jurowskaa, Maciej Hodorowicza, Ryszard Grybośa, Krzysztof Kruczałaa, Monika Głuch-Lutwinb & Grzegorz Kazekba aFaculty of Chemistry, Jagiellonian University, Kraków, Poland; b bFaculty Pharmacy, University Medical College, Poland
Abstract Twenty-four oxidovanadium(IV,V) complexes with tridentate Schiff base ligands based on 5-nitrosalicylaldehyde, 5-methoxysalicylaldehyde, or 5-sulfosalicylaldehyde and respective hydrazide were isolated, characterized using physicochemical spectroscopic methods. Three of them structurally by single-crystal X-ray structure determination. The biological activity studies included inhibition human tyrosine phosphatases, myocyte C2C12, adipocyte 3T3-L1, hepatocyte HepG2 cell lines,...
A series of 2-fluoro and 3-trifluoromethylphenylpiperazinylalkyl derivatives 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione (4-21) were synthesized evaluated for their serotonin (5-HT1A/5-HT7) receptor affinity phosphodiesterase (PDE4B PDE10A) inhibitor activity. The study enabled the identification potent 5-HT1A, 5-HT7 mixed 5-HT1A/5-HT7 ligands with weak inhibitory potencies PDE4B PDE10A. tests have been completed determination lipophilicity metabolic stability using micellar electrokinetic...
Abstract Background: A homocysteine (Hcy) metabolite, thioester Hcy-thiolactone, whose reaction with protein lysine residues affords N-homocysteinylated proteins, has been implicated in cardiovascular disease. Proteolytic turnover of proteins generates the isopeptide Nɛ-homocysteinyl-lysine (N-Hcy-Lys). Methods: We determined N-Hcy-Lys serum and a NO syntase inhibitor asymmetric dimethylarginine (ADMA), as well symmetric (SDMA) glutathione plasma by high performance liquid chromatography 52...