A5032275285- Neuropeptides and Animal Physiology
- Receptor Mechanisms and Signaling
- Pain Mechanisms and Treatments
- Pharmacological Receptor Mechanisms and Effects
- Antimicrobial Peptides and Activities
- Neurotransmitter Receptor Influence on Behavior
- Chemical Synthesis and Analysis
- Cannabis and Cannabinoid Research
- Cancer, Stress, Anesthesia, and Immune Response
- Alcohol Consumption and Health Effects
- Tryptophan and brain disorders
- Pharmacological Effects and Assays
- Protein Hydrolysis and Bioactive Peptides
- Peptidase Inhibition and Analysis
- Cancer Treatment and Pharmacology
- Neuroscience of respiration and sleep
- Computational Drug Discovery Methods
- Pharmacological Effects and Toxicity Studies
- Alcoholism and Thiamine Deficiency
- Infant Nutrition and Health
- Asthma and respiratory diseases
- Caveolin-1 and cellular processes
- GABA and Rice Research
- Proteins in Food Systems
- Pain Management and Treatment
Uczelnia Warszawska im. Marii Skłodowskiej-Curie
2024
Institute of Psychology
2024
Wojskowy Instytut Higieny i Epidemiologii
2020-2023
Medical University of Warsaw
2014-2021
Mossakowski Medical Research Institute, Polish Academy of Sciences
2010-2017
Polish Academy of Sciences
2005-2017
The design and development of hybrid compounds as a new class drug candidates remains an excellent opportunity to improve the pharmacological properties drugs (including enzymatic stability, efficacy pharmacokinetic pharmacodynamic profiles). In addition, considering various complex diseases and/or disorders, conjugate chemistry approach is highly acceptable justified. Opioids have long been recognized most potent analgesics serve basic pharmacophore for that may be useful in pain...
Background: The clinical treatment of various types pain relies upon the use opioid analgesics. However most them produce, in addition to analgesic effect, several side effects such as development dependence and addiction well sedation, dysphoria, constipation. One solution these problems are chimeric compounds which pharmacophore is hybridized with another type compound incease antinociceptive effects. Neurotensin-induced antinociception not mediated through system. Therefore, hybridizing...
Abstract Background An important limiting factor in the development of centrally acting pharmaceuticals is blood-brain barrier (BBB). Transport therapeutic peptides through this highly protective physiological remains a challenge for peptide drug delivery into central nervous system (CNS). Because most common strategy to treat moderate severe pain consists activation opioid receptors brain, active analogues as potential analgesics requires compounds with high resistance enzymatic degradation...
This work presents the successful synthesis of a library novel peptidomimetics via Ugi multicomponent reaction. Most these contain differently substituted aminocoumarin; 7-amino-4-methylcoumarin and 7-amino-4-(trifluoromethyl) coumarin. Inspired by biological properties coumarin derivatives peptidomimetics, we proposed incorporated peptidomimetics. We studied potential synthesized compounds as antimicrobial drugs on model E. coli bacterial strains (k12 R2-R4). To highlight importance in...
Finding the ideal antimicrobial drug with improved efficacy and a safety profile that eliminates antibiotic resistance caused by pathogens remains difficult task. Indeed, there is an urgent need for innovation in design development of microbial inhibitor. Given many promising peptides excellent broad-spectrum antibacterial properties are secreted some frog species (e.g., bombesins, opioids, temporins, etc.), our goal was to identify amphibian-derived dermorphin ranatensin peptides, which...
Polymeric hydrogels play an increasingly important role in medicine, pharmacy and cosmetology. They appear to be one of the most promising groups biomaterials due their favorable physicochemical properties biocompatibility. The objective presented study was synthesize new poly(chitosan-ester-ether-urethane) kinetic release genistein (GEN) from these biomaterials. In view above, six non-toxic were synthesized via Ring-Opening Polymerization (ROP) polyaddition processes. poly(ester-ether)...
Several neurotransmitter and neuromodulatory systems can control physiological glutamatergic activity. For example, opioid receptor ligands were shown to partially inhibit N-methyl-D-aspartic acid (NMDA) receptor-dependent excitotoxicity. Also, the endogenous tridecapeptide neurotensin (NT) was found modulate excessive glutamate release activity in neurons. Alternatively one target-one drug approach, it has been well documented that hybrid compounds encompassing two pharmacophores molecular...
Over 20 years ago, the Sadowski group separated two mouse lines, one with high (HA) and other low (LA) sensitivity to swim stress-induced analgesia (SSIA). Recently, we proposed that increased leakage of blood-brain barrier (BBB) in HA line created difference response SSIA. To search for further evidence this hypothesis, differences levels BBB proteins occludin claudin-5 were analysed. In addition, sought evaluate practical permeability by examining antinociceptive LA lines after IV...
Diverse chemical and pharmacological strategies are currently being explored to minimize the unwanted side effects of used opioid analgesics while achieving effective pain relief. The use multitarget ligands with activity at more than one receptor represents a promising therapeutic approach. We recently reported bifunctional peptide-based hybrid LENART01 combining dermorphin ranatensin pharmacophores, which displays mu-opioid (MOR) dopamine D2 (D2R) in rat brains spinal cords. In this study,...