A5049489262- Receptor Mechanisms and Signaling
- Neuroscience and Neuropharmacology Research
- Eicosanoids and Hypertension Pharmacology
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Biological Evaluation
- Nitric Oxide and Endothelin Effects
- Synthesis and biological activity
- Phenothiazines and Benzothiazines Synthesis and Activities
- Neurotransmitter Receptor Influence on Behavior
- Antiplatelet Therapy and Cardiovascular Diseases
- Mast cells and histamine
- Bioactive Compounds and Antitumor Agents
- Synthesis and Characterization of Heterocyclic Compounds
- Vanadium and Halogenation Chemistry
- Pain Mechanisms and Treatments
- X-ray Diffraction in Crystallography
- Computational Drug Discovery Methods
- Neuropeptides and Animal Physiology
- Crystallization and Solubility Studies
- Metal-Catalyzed Oxygenation Mechanisms
- Diet, Metabolism, and Disease
- Liver Disease Diagnosis and Treatment
- Cannabis and Cannabinoid Research
- Inflammatory mediators and NSAID effects
- Chemical synthesis and pharmacological studies
Jagiellonian University
2016-2025
Papieski Wydział Teologiczny we Wrocławiu
2000
University of Warsaw
1995
Vasorelaxant and antiplatelet agents play an important role in preventing combating endothelial dysfunction, atherosclerosis a plethora of associated cardiovascular diseases (CVDs). CVDs are the leading cause death worldwide nowadays occur not only developed but also developing societies. They include, among others, coronary heart disease, cerebrovascular disease peripheral artery disease. Due to their high prevalence, it is seek efficient preventive measures, such as lifestyle changes...
Alzheimer's disease is becoming a growing problem increasing at tremendous rate. Serotonin 5-HT6 receptors appear to be particularly attractive target from therapeutic perspective, due their involvement not only in cognitive processes, but also depression and psychosis. In this work, we present the synthesis broad biological characterization of new series 18 compounds with unique 1,3,5-triazine backbone, as potent receptor ligands. The main aim research compare activity newly synthesized...
The multifactorial origin and neurochemistry of Alzheimer's disease (AD) call for the development multitarget treatment strategies. We report a first-in-class triple acting compound that targets serotonin type 6 3 receptors (5-HT-Rs) monoamine oxidase B (MAO-B) as an approach treating AD. key structural features required MAO-B inhibition 5-HT6R antagonism interaction with 5-HT3R were determined using molecular dynamic simulations cryo-electron microscopy, respectively. Bioavailable PZ-1922...
Histamine H4 receptor (H4R) offers a great potential for new therapeutic strategies the treatment of inflammation-based diseases. The aim this study is to present pharmacological profile two recently synthesized ligands H4R with particular reference their anti-inflammatory and analgesic activity.We used mice rats in vivo tests. We also murine RAW 264.7 cells isolated guinea-pig ileum vitro test.In tests, animals were pre-treated increasing doses investigated compounds (12.5, 25 50 mg/kg)...
Abstract A series of 2‐, 4‐ or 2‐methyl‐6‐substituted xanthone derivatives 8 – 17 containing selected piperazine moieties were synthesized and tested for their electrocardiographic, anti‐arrhythmic, antihypertensive activity, as well the α 1 ‐ β ‐adrenoceptor binding affinities. Of newly derivatives, 2‐(2‐hydroxy‐3‐(4‐(2‐phenoxyethyl)piperazin‐1‐yl)propoxy)‐9 H ‐xanthen‐9‐one dihydrochloride 9 , 4‐(2‐hydroxy‐3‐(4‐(2‐phenoxyethyl)piperazin‐1‐yl)propoxy)‐9 12...
Small drug-like molecules that can block the function of serotonin 5-HT2A receptors have garnered considerable attention due to their ability inhibit platelet aggregation and possible prevention atherosclerotic lesions. Although clinical data provided compelling evidence for efficacy this approach in various cardiovascular conditions, chemical space receptor antagonists is limited ketanserin sarpogrelate. To expand portfolio novel motifs with potential antiplatelet activity, we evaluated...
Many studies involving compounds that enhance histamine release, such as H3 receptor (H3R) antagonists, have shown efficacy in inhibiting weight gain, but none passed clinical trials. As part of the search for ligands additional properties, aim this study is to evaluate activity reduction gain a rat model excessive eating, well impact on selected metabolic parameters, and number size adipocytes two new H3R KSK-60 KSK-74, which also exert significant affinity at sigma-2 receptor. Compounds...
In the present study, a series of original alaninamide derivatives have been designed applying combinatorial chemistry approach, synthesized, and characterized in vivo vitro assays. The obtained molecules showed potent broad-spectrum activity basic seizure models, namely, maximal electroshock (MES) test, 6 Hz (32 mA) model, notably, (44 model pharmacoresistant seizures. Most compounds 26 28 displayed following pharmacological values: ED50 = 64.3 mg/kg (MES), 15.6 (6 Hz, 32 mA), 29.9 44 34.9...
Background: Numerous studies highlight the critical role that neural histamine plays in feeding behavior, which is controlled by central H3 and H1 receptors. This fundamental motivation for increased interest creating receptor antagonists as anti-obesity medications. On other hand, multiple neurotransmitter systems have been identified pharmacotherapeutic targets obesity, including sigma-2 systems. Interestingly, our previous rat excessive eating model, we demonstrated a significant...
Despite the substantial clinical success of aspirin and clopidogrel in secondary prevention ischemic stroke, up to 40% patients remain resistant available antiplatelet treatment. Therefore, there is an urgent need develop novel agents with a mechanism action. Recent studies revealed that potent alpha 2B-adrenergic receptor (alpha 2B-ARs) antagonists could constitute alternative therapy. We have synthesized series N-arylpiperazine derivatives 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as...