A5018516942- Antibiotics Pharmacokinetics and Efficacy
- Pharmacological Effects and Toxicity Studies
- Cholinesterase and Neurodegenerative Diseases
- Pharmaceutical studies and practices
- Synthesis and Biological Evaluation
- Epilepsy research and treatment
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Reactivity of Heterocycles
- Pain Mechanisms and Treatments
- Phosphodiesterase function and regulation
- Tryptophan and brain disorders
- Adenosine and Purinergic Signaling
- Chemical Reaction Mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Polyomavirus and related diseases
- Agricultural economics and policies
- Synthesis and Characterization of Heterocyclic Compounds
- Receptor Mechanisms and Signaling
- Bipolar Disorder and Treatment
- Antibiotic Use and Resistance
- Neuroscience and Neuropharmacology Research
- HIV/AIDS drug development and treatment
- Intensive Care Unit Cognitive Disorders
- Nutrition and Health Studies
- Ion channel regulation and function
Jagiellonian University
2014-2025
Akademia Bialska im. Jana Pawła II
2022
Farmak (Czechia)
2015
Alzheimer's disease (AD) has a complex and not-fully-understood etiology. Recently, the serotonin receptor 5-HT6 emerged as promising target for AD treatment; thus, here new series of 5-HT6R ligands with 1,3,5-triazine core selenoether linkers was explored. Among them, 2-naphthyl derivatives exhibited strong affinity selectivity over 5-HT1AR (13–15), 5-HT7R (14 15), 5-HT2AR (13). Compound 15 displayed high other central nervous system receptors low risk cardio-, hepato-, nephrotoxicity no...
Among serotonin receptors, the 5-HT6 subtype is an important protein target and its ligands may play a key role in innovative treatment of cognitive disorders. This study aimed to extend body preclinical research on two naphthyl-derived methylpiperazine-1,3,5-triazine analogues with thioether (WA-22) or Se-ether (PPK-32) linkers, newly described compounds having high affinity selectivity for receptors drug-like parameters vitro. Thus, crystallography-supported deeper insight into their...
Novel 1-(1-benzoylpiperidin-4-yl)methanamine derivatives were designed as "biased agonists" of serotonin 5-HT1A receptors. The compounds tested in signal transduction assays (ERK1/2 phosphorylation, cAMP inhibition, Ca2+ mobilization, and β-arrestin recruitment) which identified ERK1/2 phosphorylation-preferring aryloxyethyl derivatives. novel series showed high receptor affinity, >1000-fold selectivity versus noradrenergic α1, dopamine D2, 5-HT2A, histamine H1, muscarinic M1 receptors,...
The current pharmaceutical market lacks therapeutic agents designed to modulate behavioral disturbances associated with dementia. To address this unmet medical need, we multifunctional ligands characterized by a nanomolar affinity for clinically relevant targets that are the disease pathology, namely, 5-HT2A/6/7 and D2 receptors. Compounds exhibited favorable functional efficacy, water solubility, metabolic stability were selected more detailed study. Pharmacological profiling revealed...
Among the serotonin receptors, one of most recently discovered 5-HT6 subtype is an important protein target and its ligands may play a key role in innovative treatment cognitive disorders. However, none selective have reached pharmaceutical market yet. Recently, new chemical class potent receptor agents, 1,3,5-triazine-piperazine derivatives, has been synthesized. Three members, ortho meta dichloro- (1,2) unsubstituted phenyl (3) proved to be special interest due their high affinities...
A direct fluorometric high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of ibuprofen enantiomers in mouse plasma (100 μl) tissues (brain, liver, kidneys) using liquid-liquid extraction 4-tertbutylphenoxyacetic acid as an internal standard. Separation accomplished a Chiracel OJ-H chiral column based on cellulose tris(4-methylbenzoate) coated 5 μm silica-gel, 250 x 4.6 mm at 22 °C with mobile phase composed n-hexane, 2-propanol, trifluoroacetic...
<title>Abstract</title> <bold>Background </bold>Research on new candidates for antidepressant/anxiolytic drugs from the group of long-chain arylpiperazines (LCAPs) containing a 1,3-dimethylpurine-2,6-dione as terminal amide fragment fits into modern exploration trend. This study aimed to examine, first time in rats, pharmacodynamic (antidepressant- and anxiolytic-like) pharmacokinetic properties...
The aim of this study was to develop quantitative structure-pharmacokinetics relationship (QSPKR) models for a group xanthine derivatives with proven pharmacological activity and investigate its applicability the prediction pharmacokinetics these compounds.
The present study was to develop and validate a rapid analytical method of high-performance liquid chromatography with UV (HPLC/UV) detection for the determination levetiracetam (LEV) concentration in human serum cerebrospinal fluid (CSF) samples. newly developed used measure LEV serum/CSF 29 patients different types epilepsy; 52% (group I, n = 15) were treated monotherapy, 48% II, 14) co-administered other AEDs. Serum CSF levels correlated dosage, concomitant AEDs, therapeutic effect,...
Changes in pharmacokinetic properties of antibacterial drugs critically ill patientsCritically patients are at high risk developing a life-threatening infection leading to severe shock and, as consequence, multi-organ failure and even death.Optimal antimicrobial therapy, especially the first 48 hours, is crucial increasing patients' chances survival.However, effective drug dosing problematic because pathophysiological changes associated with critical state disease affect their properties,...
Comparative analysis of valproic acid concentrations in terms dosing and clinical effect monitoring different age patients with diagnosed epilepsy Subject research.Therapy drug under the control (VPA) is now a well-established tool for treatment epilepsy.The pharmacokinetic variability VPA interindividual differences type/seizure severity depending on patients' determine serum concentration this an individual patient.The application "individual therapeutic concentration" may be useful...
Przedmiot badań. Właściwie prowadzona immunosupresja w terapii potransplantacyjnej jest warunkiem niezbędnym do zminimalizowania ryzyka odrzucenia narządu. Cel Analiza stężeń minimalnych (Cssmin) takrolimusu (TAC) stanie stacjonarnym, pierwszym miesiącu po przeszczepie serca lub nerki. Wyliczono współczynnik zmienności wewnątrzosobniczej (CV), poszukiwano korelacji z parametrami biochemicznymi oraz przedstawiono zalecenia/aktualne wytyczne optymalizacji dawkowania TAC na podstawie baz...
Abstract Background Epilepsy frequently coexists with neuropathic pain. Our approach is based on the search for active compounds multitarget profiles beneficial in terms of potential side effects and implementation screening multidirectional central activity . Methods Compounds were synthesized by means chemical synthesis. After antiseizure neurotoxicity vivo, KM-408 its enantiomers chosen analgesic evaluations. Further safety studies included acute toxicity mice, effect normal...