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Search results for: ANTAGONISM
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Antagonist adhesion effects due to variable substrate surface
PublicationThe effects of variability of intrinsic adhesion within a joint have been studied using a single cantilever beam (SCB) test. Fracture energy was found not to be a simple function of relative areas of 2 surface pre-treatments: a 'weak' zone decreased strength more than expected from simple, additive considerations. By severing the adhesive along the strong-weak transition, fracture energy increased.The prior antagonist effect appears...
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Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
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Towards β-selectivity in functional estrogen receptor antagonists
PublicationBased on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...
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Cannabinoid CB1 antagonists and dopamine antagonists produce different effects on a task involving response allocation and effort-related choice in food-seeking behavior
PublicationW przeprowadzonych badaniach iniekcja antagonistów dopaminy (DA) szczurom powoduje znaczny spadek użycia siły przez zwierzęta w poszukiwaniu żywności i jednoczesny wzrost spożycia jedzenia laboratoryjnego. Przeciwnie, iniekcja antagonisty AM4113 lub odwrotnego agonisty AM251 receptora CB1 powoduje zmniejszenie ilości jedzenia granulek, ale nie wpływa na zwiększenie konsumpcji jedzenia laboratoryjnego. Efekty wywierane na zwierzęta...
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Enhanced Toxicity of Bisphenols Together with UV Filters in Water: Identification of Synergy and Antagonism in Three-Component Mixtures
PublicationContaminants of emerging concern (CEC) localize in the biome in variable combinations of complex mixtures that are often environmentally persistent, bioaccumulate and biomagnify, prompting a need for extensive monitoring. Many cosmetics include UV filters that are listed as CECs, such as benzophenone derivatives (oxybenzone, OXYB), cinnamates (2-ethylhexyl 4-methoxycinnamate, EMC) and camphor derivatives (4-methylbenzylidene-camphor,...
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QSPR analysis of some agonists and antagonists of α-adrenergic receptors
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The neuroprotective activity of new phenylalanine-based AMPA receptor antagonists
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Non-vitamin K antagonist oral anticoagulants (NOACs) in cancer patients with atrial fibrillation
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Phenylalanine-Based AMPA Receptor Antagonist as the Anticonvulsant Agent with Neuroprotective Activity—In Vitro and In Vivo Studies
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Synergisms and antagonisms between MoS2 nanotubes and representative oil additives under various contact conditions
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Intrinsic effects of AM4113, a putative neutral CB1 receptor selective antagonist, on open-field behaviors in rats
PublicationW pracy przedstawiono wyniki testów otartego pola na zachowanie szczurów po iniekcji zwierzętom WIN55,21-2 (WIN; 3 mg/kg) agonisty receptora kanabinoidowego CB1R, bądź AM4113 (0.3−5.6 mg/kg) przypuszczalnie neutralnego antagonisty receptora kanabinoidowego CB1R oraz mieszaniny obu związków. W badaniach pod uwagę brano następujące zachowania zwierząt; ilość kwadratów, którą szczury przechodziły na czterech nogach, częstotliwość...
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Antagonist activation exercises elicit similar post-activation performance enhancement as agonist activities on throwing performance
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In Vivo, In Vitro and In Silico Studies of the Hybrid Compound AA3266, an Opioid Agonist/NK1R Antagonist with Selective Cytotoxicity
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Structural and Pharmacological Characterization of Phenylalanine-Based AMPA Receptor Antagonists at Kainate Receptors
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Solution conformations of bradykinin antagonists modified with CαCα cyclized nonaromatic residues
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Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors
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Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors
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Conformational Studies of Two Bradykinin Antagonists by Using Two-dimensional NMR Techniques and Molecular Dynamics Simulations
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A New Phenylalanine Derivative Acts as an Antagonist at the AMPA Receptor GluA2 and Introduces Partial Domain Closure: Synthesis, Resolution, Pharmacology, and Crystal Structure
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Highly Potent Antidiuretic Antagonists: Conformational Studies of Vasopressin Analogues Modified with 1-Naphthylalanine Enantiomers at Position 2
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Wnt pathway antagonists, SFRP1, SFRP2, SOX17, and PPP2R2B, are methylated in gliomas and SFRP1 methylation predicts shorter survival
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The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses ood intake and food-reinforced behavior but does not induce signs of nausea in rats
PublicationPrzeprowadzone badania biochemiczne wykazują, że związek AM4113 wiąże się z receptorem kanabinoidowym CB1, ale nie wykazuje właściwości odwrotnego agonisty (między innymi nie wpływa na powstawanie cyklicznego AMP). W testach na swobodne przemieszczanie się szczurów i znieczulenie związek AM4113 osłabia wpływ agonisty AM411 na receptor CB1. AM4113 wpływa na zachowanie szczurów związane z karmieniem oraz powoduje spadek łaknienia...
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Safety and efficacy of P2X3 receptor antagonist for the treatment of refractory or unexplained chronic cough: A systematic review and meta-analysis of 11 randomized controlled trials
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Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus
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Compatible Mixture of Bacterial Antagonists Developed to Protect Potato Tubers from Soft Rot Caused by Pectobacterium spp. and Dickeya spp.
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The PARAGON Heart Failure trial – ongoing investigation of the angiotensin receptor antagonist/neprilysin inhibitor sacubitril/valsartan in heart failure patients with hypertension and preserved ejection fraction
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The exposure to UV filters: Prevalence, effects, possible molecular mechanisms of action and interactions within mixtures
PublicationSubstances that can absorb sunlight and harmful UV radiation such as organic UV filters are widely used in cosmetics and other personal care products. Since humans use a wide variety of chemicals for multiple purposes it is common for UV filters to co-occur with other substances either in human originating specimens or in the environment. There is increasing interest in understanding such co-occurrence in form of potential synergy, antagonist,...
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Study of New Oxytocin Antagonist Barusiban (Fe200 440) Affinity Toward Human Oxytocin Receptor Versus Vasopressin V1a and V2 Receptors - Molecular Dynamics Simulation in POPC Bilayer
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Antioxidant Interactions between Major Phenolic Compounds Found in 'Ataulfo' Mango Pulp: Chlorogenic, Gallic, Protocatechuic and Vanillic Acids
PublicationPhenolic compounds are known to have antioxidant capacity; however, there is little information about molecular interactions between particular phenolics found in fruits at different developmental stages. Therefore, the total antioxidant capacity of the phenolic compounds of a fruit may not correspond to the sum of individual antioxidant capacity given by antioxidants from that tissue. In this study, individual antioxidant capacity...
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P4018Reduced fibrin clot permeability is associated with an increased risk of both ischemic stroke and major bleeding in atrial fibrillation patients treated with vitamin K antagonists
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Impact of inorganic ions and pH variations on toxicity and endocrine potential of selected environmentally relevant pharmaceuticals
PublicationAssessment of the impact of pharmaceutical residues on living organisms is a very complex subject. Apart from taking into account the toxicity of individual compounds, environmental factors should also be taken into account. In this paper, attempts were made to assess the impact of coexisting inorganic ions and changes in pH on the toxicity of ten selected pharmaceuticals. Two bioassays were used to measure the estrogenic and androgenic...
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Application of bioassays in studies on the impact of pharmaceuticals on the environment
PublicationDrug interactions are often desirable particularly in medicine, when treatment of a patient requires using a mixture of drugs in specific doses to produce the adequate therapeutic effect. Unfortunately, interactions between drugs in the environment are not as desirable, despite the fact that drugs are present in the environment at low concentration levels [1]. Pharmaceuticals are present in the environment in a mixture of compounds,...
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Study of the effect of residues of pharmaceuticals on the environment on the example of bioassay Microtox®
PublicationResidues of pharmaceuticals present in the aqueous environment can be found in a mixture of different substances wherein drugs not remain inert with respect to each other. In such mixtures a phenomenon of synergism or antagonism may occur, which can contribute to increase or decrease the overall toxicity of the mixture of drugs. Pharmaceuticals namely: diclofenac (sodium salt), oxyteracycline hydrochloride, fluoxetine hydrochloride,...
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Detection of some volatile degradation products released during photoexposition of ranitidine in a solid state
PublicationRanitidine (RAN) is on top of the list of prescribed drugs, due to its popularity as a selective H2-receptor antagonist, which efficiently decreases the amount of acid produced in the stomach. RAN is not stable both in a solid state and in a solution, which creates manufacturing problems, requires appropriate storage conditions, and results in a short drug shelf-life. The aim of this work was to study the emission of volatile...
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Application of vibrational spectroscopy, thermal analyses and X-Ray diffraction in the rapid evaluation of the stability in solid-state of ranitidine, famotidine and cimetidine
PublicationThis paper reports the study on applicability of Fourier transform infrared (FTIR), near-infrared (NIR) and Raman spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) for the estimation of the chemical stability and photostability of histamine H2-receptor antagonist substances. Ranitidine hydrochloride (RAN), famotidine (FAM) and cimetidine (CIM) were tested and differences in sensitivity were measured...
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Bisphenols (A, S, and F) affect the basic hormonal activity determined for pharmaceuticals – Study of Saccharomyces cerevisiae
PublicationPharmaceuticals and analogs of bisphenol A (BPA) are increasingly threatening environmental pollutants. In this study, mixtures of selected pharmaceuticals (diclofenac sodium salt, chloramphenicol, oxytetracycline hydrochloride, fluoxetine hydrochloride, estrone, ketoprofen, progesterone, gemfibrozil and androstenedione) were prepared with BPA and its two analogs (namely, bisphenols F and S) at such ratios to reflect environmentally...
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Importance of Conjugation of the Bile Salt on the Mechanism of Lipolysis
PublicationWe aim to advance the discussion on the significance of the conjugation of bile salts (BS) in our organism. We hypothesize that conjugation influences the rate of lipolysis. Since the rate of lipolysis is a compound parameter, we compare the effect of conjugation on four surface parameters, which contribute to the rate. Since deconjugation is due to gut microbiota, we hypothesize that microbiota may affect the rate of lipolysis....
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Identification and antimicrobial susceptibility of fecal coliforms isolated from surface water
Publicationof 274 fecal coliforms isolated from two watercourses influencing the costal water quality of the gdańsk and the puck bay, 265 were identified as escherichia coli. the remained strains belonged to: acinetobacter spp. (n=1), enterobacter spp. (n=3), klebsiella spp. (n=4) and shigella spp. (n=1). the susceptibility of 222 e. coli was tested against 19 antimicrobial agents: aminoglycosides, carbapenems, cephalosporines, folate antagonists,...
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Genotoxicity of selected pharmaceuticals, their binary mixtures, and varying environmental conditions – study with human adenocarcinoma cancer HT29 cell line
PublicationPharmaceutical residues are present in the environment in mixtures and their adverse effects may also result from interactions that occur between compounds. Studies presented in this work focus on genotoxicity of pharmaceuticals from different therapeutic groups in mixtures and in individual solutions impacted with different environmental conditions assessed using comet assay (alkaline approach). Binary mixtures of pharmaceuticals...
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Inhibition of T-type calcium channel disrupts Akt signaling and promotes apoptosis in glioblastoma cells.
PublicationGlioblastoma multiforme (GBM) are brain tumors that are exceptionally resitant to both radio- and chemotherapy regimens and novel approaches to treatment are needed. T-type calcium channels are one type of low voltage-gated channel (LVCC) involved in embryonic cell proliferation and differentiation; however they are often over-expressed in tumors, including GBM. In this study, we found that inhibition of T-type Ca channels in GBM...
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Phylogenetic relationship and antimicrobial resistance in Escherichia coli isolated from the Reda River and the Oliwski Stream, Northern Poland = Lekooporność i przynależność filogenetyczna szczepów Escherichia Coli izolowanych z rzeki Redy i Potoku Oliwskiego
PublicationThe high abundance of fecal bacteria in surface water is usually related to poor agricultural practice, pollution caused by domesticated and wild animals as well as with septic tank failures. Identification of fecal contamination sources seems to be crucial in order to effectively estimate the inherent risk. In this study, the phylogenetic relationship of 30 isolates of E. coli, originated from surface water, was estimated by employing...
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Tetracycline and ampicillin resistance of Escherichia coli strains of surface water origin: the potential for horizontal transfer of resistance genes = Oporność na tetracyklinę i ampicylinę szczepów Escherichia Coli wyizolowanych z wody powierzchniowej : możliwość horyzontalnego przenoszenia genów oporności
PublicationThe aim of this preliminary study was to assess the occurrence and molecular diversity of tetracycline and ampicillin resistance genes carried by Escherichia coli present in surface water. Bacterial strains were isolated from two watercourses (the Reda River and the Oliwski Stream) that influence the quality of coastal waters in the Gdańsk Bay (Northern Poland) by direct discharge. The bacterial drug susceptibility, tested against...
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Warzywa jako narzędzie wykorzystywane w biomonitoringu metali ciężkich
PublicationW ostatnich dekadach miały miejsce istotne zmiany w gospodarce i to zarówno w skali globalnej jak i regionalnej oraz lokalnej. W sposób istotny wzrosło zapotrzebowanie na energię, transport ludzi i towarów. Tym zmianom w coraz większym stopniu towarzyszy wzrost dbałości o stan środowiska. Dlatego też coraz więcej uwagi zwraca się na coraz dokładniejszy monitoring i kontrolę poziomu zanieczyszczenia poszczególnych elementów środowiska...