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    Wyświetlanie 1-18 z 18
    Tytuł:
    Экстремальный аргумент в неосуществленном споре (А. Чехов „Дуэль”)
    An extreme reason in unwinnable dispute (Anton Chekhov’s “The duel”)
    Autorzy:
    Шелогурова, Галина
    Powiązania:
    https://bibliotekanauki.pl/articles/968526.pdf
    Data publikacji:
    2015
    Wydawca:
    Uniwersytet Łódzki. Wydawnictwo Uniwersytetu Łódzkiego
    Tematy:
    duel
    conflict
    dialogue
    antagonist
    controversy
    дуэль
    конфликт
    антагонист
    спор
    Opis:
    Феномен дуэли в одноименной повести Чехова рассматривется в контексте осмысления писателем одной из базовых моделей русской культуры на фоне сложившейся в течение XIX века литературной традиции. Кардинальное переосмысление последней в данном произведении анализируется с опорой на специфику диалога в творчестве писателя, что позволяет интерпретировать дуэль как показательный элемент «бесконтактного» спора, не имеющего перспективы разрешения.
    The paper presents an attempt to interpret the duel in Chekhov’s novella as an argument of the implicit controversy. From this point of view the reason declared by Von Koren (a clash of ideas) is corresponding with plot and seems to be false. The author tries to prove that personal categories (envy, hate) are more significant in the particular type of conflict described by Chekhov.
    Źródło:
    Acta Universitatis Lodziensis. Folia Litteraria Rossica; 2015, 08; 79-86
    1427-9681
    2353-4834
    Pojawia się w:
    Acta Universitatis Lodziensis. Folia Litteraria Rossica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Functionalized cellulose as a matrix for the synthesis of library of molecular receptors useful for screening of compounds with anti-histamine activity
    Autorzy:
    Walczak, M. E.
    Frączyk, J.
    Kamiński, Z. J.
    Kolesińska, B.
    Powiązania:
    https://bibliotekanauki.pl/articles/285956.pdf
    Data publikacji:
    2017
    Wydawca:
    Akademia Górniczo-Hutnicza im. Stanisława Staszica w Krakowie. Polskie Towarzystwo Biominerałów
    Tematy:
    molecular receptors
    immobilized peptides
    binding pocket
    agonist/antagonist
    histamine receptors
    Opis:
    The library of molecular receptors was formed by self-organization of N-heptanoylated dipeptides anchored in the regular fashion via aminophenylamino- 1,3,5-triazine linker to the surface of cellulose membrane. SPOT method was used for the synthesis of peptide library. As C-terminal amino acids of peptide fragments were attached: Ala, Pro and Phe, while as a N-terminal amino acids were applied all natural amino acids. DMT/NMM/TosO- was selected as a coupling reagent for synthesis of library of N-heptanoylated dipeptides. These constructs were used as a tool for distinguishing pharmaceutically active compounds acting on histamine receptors. In the studies as active compounds were tested: Doxylamine and Difenhydramine with histamine agonist activity, Ranitidine and Cimetidine with antagonist activity as well as Histamine – natural ligand. The binding of colourless ligands was monitored by staining with Brilliant Black used as reporter dye and quantitative colour measurement was performed in 256 grade gray scale by using Image-Quant software. Substantial differences in the ability of interactions of agonists and antagonists with bounding pockets were observed with selected molecular receptors. From 60 elements library of molecular receptors were selected 12, which were able to distinguish between agonists or antagonists. It has been found that even small changes (Leu residue vs Val residue) in the structure of molecular receptor influenced specificity of agonist or antagonist binding.
    Źródło:
    Engineering of Biomaterials; 2017, 20, 142; 2-6
    1429-7248
    Pojawia się w:
    Engineering of Biomaterials
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Balancing Bilinearly Interfering Elements
    Autorzy:
    Carfì, D.
    Gambarelli, G.
    Powiązania:
    https://bibliotekanauki.pl/articles/375967.pdf
    Data publikacji:
    2015
    Wydawca:
    Akademia Górniczo-Hutnicza im. Stanisława Staszica w Krakowie. Wydawnictwo AGH
    Tematy:
    bargaining problems
    game theory
    antagonist elements
    interfering elements
    optimal dosage
    synergies
    Opis:
    Many decisions in various fields of application have to take into account the joint effects of two elements that can interfere with each other. This happens, for example, in Medicine (synergic or antagonistic drugs), Agriculture (anti-cryptogamics), Public Economics (interfering economic policies), Industrial Economics (where the demand of an asset can be influenced by the supply of another asset), Zootechnics, and so on. When it is necessary to decide about the dosage of such elements, there is sometimes a primary interest for one effect rather than another; more precisely, it may be of interest that the effects of an element are in a certain proportion with respect to the effects of the other. It may also be necessary to take into account minimum quantities that must be assigned. In Carfì, Gambarelli and Uristani (2013), a mathematical model was proposed to solve the above problem in its exact form. In this paper, we present a solution in closed form for the case in which the function of the effects is bilinear.
    Źródło:
    Decision Making in Manufacturing and Services; 2015, 9, 1; 27-49
    1896-8325
    2300-7087
    Pojawia się w:
    Decision Making in Manufacturing and Services
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Thioperamide, antagonist of histamine H3 receptors, increases brain production of kynurenic acid
    Autorzy:
    Jaroslawska-Zych, A.
    Kowalczyk, M.S.
    Kloc, R.
    Urbanska, E.M.
    Powiązania:
    https://bibliotekanauki.pl/articles/3367.pdf
    Data publikacji:
    2010
    Wydawca:
    Instytut Medycyny Wsi
    Tematy:
    thioperamide
    antagonist
    histamine
    H3 receptor
    brain
    production
    kynurenic acid
    in vitro
    Źródło:
    Journal of Pre-Clinical and Clinical Research; 2010, 04, 1
    1898-2395
    Pojawia się w:
    Journal of Pre-Clinical and Clinical Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Hereditary angioedema: treatment options and availability. Balance between patients’ needs and stakeholders’ plans
    Opcje terapeutyczne i ich dostępność we wrodzonym obrzęku naczynioruchowym: pomiędzy potrzebami pacjentów a planami decydentów
    Autorzy:
    Valerieva, Anna
    Perego, Francesca
    Porebski, Grzegorz
    Staevska, Maria
    Cicardi, Marco
    Powiązania:
    https://bibliotekanauki.pl/articles/1034427.pdf
    Data publikacji:
    2018
    Wydawca:
    Oficyna Wydawnicza Mediton
    Tematy:
    C1 inhibitor
    bradykinin receptor antagonist
    hereditary angioedema
    kallikrein inhibitors
    prophylaxis
    treatment
    Opis:
    Hereditary angioedema is a rare and disabling disease characterized by severe, acute, self- limiting edema of the subcutaneous and mucosal tissue. The disease carries significant mortality when the upper airways are involved. It is determined by a transient dysregulation in vascular permeability with a sudden increase in fluid extravasation. The most common genetic defects recognized on the SERPING1 gene leads to complement C1-inhibitor deficiency (C1-INH-HAE). In the last few years mutation on the factor XII gene, the angiopoietin, and the plasminogen genes were recognized to cause angioedema with normal C1-INH levels (nC1-INH-HAE). However, it is not uncommon to have family history of angioedema and unknown genetic defect. The burden of the disease on the individual patients is unpredictable since the number, location and severity of the attacks spans from silent disease to an extremely high number of attacks during lifetime. Nowadays effective and safe treatment for the C1-INH-HAE forms are available and new drugs are under investigation both for the on demand therapy and for the prophylaxis of the attacks. Acute treatments has been proved to reduce severity and duration of attack, prophylaxis reduces the number of attacks thus positively affecting the quality of life and reducing the indirect costs of the disease. Unfortunately, the costs of the medications are high limiting the accessibility and availability of treatment in different countries. This paper reviews the treatment options and the differences in the availability of the medications in three European countries, with practical suggestions for the management of the disease.
    Wrodzony obrzęk naczynioruchowy jest rzadką, upośledzającą funkcjonowanie chorobą chrakteryzującą się ciężkimi, ostrymi, samoograniczającymi się obrzękami tkanki podskórnej i podśluzówkowej. W przypadku zajęcia górnych dróg oddechowych, schorzenie obarczona jest znaczącą śmiertelnością. Choroba jest determinowana przejściową dysregulacją przepuszczalności naczyniowej ze nagłym wzrostem ilości wynaczynionego płynu. Najczęściej spotykane defekty genetyczne występujące w genie SERPING1 prowadzą do niedoboru inhibitora składowej C1 układu dopełniacza (C1-INH-HAE). W ostatnich kilku latach poznano mutację genów czynnika XII, angiopoetyny i plazminogenu powodujące obrzęk naczynioruchowy z prawidłowym poziomem C1-INH (HAEnC1-INH). Jednakże, nie jest sytuacją niezwykłą występowanie rodzinnego wywiadu w kierunku obrzęku przy nieznanym defekcie genetycznym. Obciążenia związane z chorobą u poszczególnych pacjentów są trudne do przewidzenia, ponieważ liczba, lokalizacja i ciężkość napadów w ciągu życia zmienia się: od okresów remisji, do okresów ze skrajnie częstymi objawami. Obecnie dostępne są skuteczne i bezpieczne formy leczenia C1-INH-HAE, a w trakcie badań są nowe leki, zarówno do doraźnej, jaki i profilaktycznej terapii napadów obrzęku. Leki stosowane w stanach ostrych mają potwierdzone dzia- łanie zmniejszające ciężkość i czas trwania napadów, a leki stosowane w profilaktyce zmniejszają częstość napadów wpływając pozytywnie na jakość życia i redukując pośrednie koszty choroby. Niestety koszty leczenia są wysokie i ograniczają jego dostępność w wielu krajach. W niniejszej pracy dokonano przeglądu możliwych opcji terapeutycznych i ich dostępności w trzech krajach europejskich, poszerzonego o praktyczne sugestie dotyczące leczenia choroby.
    Źródło:
    Alergia Astma Immunologia - przegląd kliniczny; 2018, 23, 4; 175-185
    1427-3101
    Pojawia się w:
    Alergia Astma Immunologia - przegląd kliniczny
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Management of soil-borne diseases of organic vegetables
    Autorzy:
    Shafique, H.A.
    Sultana, V.
    Ehteshamul-Haque, S.
    Athar, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/66619.pdf
    Data publikacji:
    2016
    Wydawca:
    Polska Akademia Nauk. Czytelnia Czasopism PAN
    Tematy:
    management
    soil-borne disease
    vegetable
    organic agriculture
    control
    biological antagonist
    organic manure
    seaweed
    Opis:
    With the rising awareness of the adverse effects of chemical pesticides, people are looking for organically grown vegetables. Consumers are increasingly choosing organic foods due to the perception that they are healthier than those conventionally grown. Vegetable crops are vulnerable to a range of pathogenic organisms that reduce yield by killing the plant or damaging the product, thus making it unmarketable. Soil-borne diseases are among the major factors contributing to low yields of organic produce. Apart from chemical pesticides there are several methods that can be used to protect crops from soil-borne pathogens. These include the introduction of biocontrol agents against soil-borne plant pathogens, plants with therapeutic effects and organic soil amendments that stimulate antagonistic activities of microorganisms to soil-borne diseases. The decomposition of organic matter in soil also results in the accumulation of specific compounds that may be antifungal or nematicidal. With the growing interest in organic vegetables, it is necessary to find non chemical means of plant disease control. This review describes the impact of soil-borne diseases on organic vegetables and methods used for their control.
    Źródło:
    Journal of Plant Protection Research; 2016, 56, 3
    1427-4345
    Pojawia się w:
    Journal of Plant Protection Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Expression of soluble recombinant TGF-β type II receptor fused with the Fc portion of human IgG1 (sTβRII-Fc) in NS0 cells
    Autorzy:
    Kwiatkowska, Eliza
    Kazimierczak, Urszula
    Mackiewicz, Andrzej
    Kowalczyk, Dariusz
    Powiązania:
    https://bibliotekanauki.pl/articles/1041250.pdf
    Data publikacji:
    2006
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    GS-NS0 expression system
    chimeric receptor
    TGF-β
    TGF-βreceptor
    TGF antagonist
    Opis:
    We have constructed and expressed recombinant chimeric soluble TGF-β type II receptor fused with the Fc portion of human IgG1 (sTβRII-Fc) in NS0 mouse myeloma cells and isolated cell lines constitutively secreting very high levels of biologically active protein. The GS-NS0 expression system takes advantage of the strong human cytomegalovirus immediate early promoter expression vector and glutamine synthetase as a selectable marker. The recombinant chimeric receptor could be produced in high amounts and efficiently purified by one step chromatography on a protein A column. Biochemical studies revealed that recombinant sTβRII-Fc binds native TGF-β1 and TGF-β3 isoforms and neutralizes their activity in vitro.
    Źródło:
    Acta Biochimica Polonica; 2006, 53, 2; 361-369
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    On the peptide-antipeptide interactions in interleukin-1 receptor system.
    Autorzy:
    Kluczyk, Alicja
    Cebrat, Marek
    Zbozień-Pacamaj, Renata
    Lisowski, Marek
    Stefanowicz, Piotr
    Wieczorek, Zbigniew
    Siemion, Ignacy
    Powiązania:
    https://bibliotekanauki.pl/articles/1043318.pdf
    Data publikacji:
    2004
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    vaccinia virus C10L protein
    immunomodulation
    interleukin-1 receptor antagonist
    complementary peptides
    interleukin-1
    Opis:
    Interleukin-1 receptor antagonist (IL-1Ra) and vaccinia virus protein C10L share a VTXFYF motif, with X being Lys or Arg residue, respectively. Peptides of such sequence compete successfully with IL-1 for the cellular receptor. A pair of complementary peptides, based on the Siemion's hypothesis on the periodicity of the genetic code (QWLNIN and QWANIN), and another pair, in which, following the Root- Bernstein theory, Lys was used as complementary amino acid to Phe (QWLKIK and QWAKIK), were investigated for the peptide-antipeptide interactions using mass spectrometry (ESI-MS) and circular dichroism (CD) methods. The CD measurements indicated some conformational changes, more pronounced in the Siemion's pairs, however, no heterodimer formation was found by MS. In the region of IL-1 receptor situated close to the position of IL-1Ra in the IL-1Ra-receptor complex, a KQKL motif is present, suggesting a possibility of complementary recognition of the Root-Bernstein type in the IL-1 receptor. The biological activity of the complementary peptides is similar to that of the original ones. They efficiently compete with IL-1 and show moderate immunosuppressory activity in humoral and cellular immune response. The inhibition of the IL-1-IL-1 receptor interaction may result from the complementary peptides acting as mini-receptors with affinity for IL-1.
    Źródło:
    Acta Biochimica Polonica; 2004, 51, 1; 57-66
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Fungal pathogens and antagonists in root-soil zone in organic and integrated systems of potato production
    Autorzy:
    Lenc, L.
    Kwasna, H.
    Jeske, M.
    Jonczyk, K.
    Sadowski, C.
    Powiązania:
    https://bibliotekanauki.pl/articles/66844.pdf
    Data publikacji:
    2016
    Wydawca:
    Polska Akademia Nauk. Czytelnia Czasopism PAN
    Tematy:
    fungal pathogen
    antagonist
    root
    soil
    organic system
    integrated system
    potato
    biological control
    cropping system
    fungi
    Oomycota
    Opis:
    Occurrence of culturable Fungi and Oomycota in root-soil habitat of potato cv. Owacja in organic and integrated production systems at Osiny (northern Poland) was compared in 2008–2010. The densities of both pathogens were significantly greater in the organic system. The eudominant fungal taxa (with frequency > 10% in at least one habitat) included species of Fusarium + Gibberella + Haematonectria, Penicillium, Phoma and Trichoderma. The dominant taxa (with frequency 5–10%) included species from 13 genera. In the rhizoplane, rhizosphere and non-rhizosphere soil, the total density of potential pathogens was greater in the integrated system, and of potential antagonists in the organic system. Among eudominant and dominant pathogens, Fusarium oxysporum and Gibellulopsis nigrescens occurred at greater density in the integrated system and Haematonectria haematococca and Phoma spp. in the organic system. Among eudominant antagonists, Trichoderma species occurred at greater density in the organic system. The organic system provided more disease suppressive habitat than the integrated system. The occurrence of brown leaf spot and potato blight was however similar in both systems. The mean yield of organic potatoes (24.9 t · ha–1) was higher than the mean organic potato yield in Poland (21.0 t · ha–1) and similar to the mean in other European countries (Germany 25.1 t · ha–1, Great Britain 25.0 t · ha–1). The organic system, based on a 5-year rotation, with narrow-leafed lupin, white mustard and buckwheat as a cover crop, inorganic fertilization based on ground rock phosphate + potassium sulphate, and biological and chemical control of insects and diseases (Bacillus thuringiensis ssp. tenebrionis + copper hydroxide + copper oxychloride), may be recommended for use in central Europe.
    Źródło:
    Journal of Plant Protection Research; 2016, 56, 2
    1427-4345
    Pojawia się w:
    Journal of Plant Protection Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Diltiazem enhances the protective activity of oxcarbazepine against maximal electroshock-induced seizures in mice
    Autorzy:
    Zadrozniak, A.
    Trojnar, M.K.
    Trojnar, M.P.
    Kimber-Trojnar, Z.
    Dudra-Jastrzebska, M.
    Andres-Mach, M.M.
    Luszczki, J.J.
    Powiązania:
    https://bibliotekanauki.pl/articles/3526.pdf
    Data publikacji:
    2008
    Wydawca:
    Instytut Medycyny Wsi
    Tematy:
    calcium channel antagonist
    diltiazem
    protective activity
    oxcarbazepine
    maximal electroshock-induced seizure
    mice
    mouse
    drug interaction
    pharmacodynamic interaction
    Źródło:
    Journal of Pre-Clinical and Clinical Research; 2008, 02, 2
    1898-2395
    Pojawia się w:
    Journal of Pre-Clinical and Clinical Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Anti-schizophrenic activities of histamine H3 receptor antagonists in rats treated with MK-801
    Autorzy:
    Mahmood, D.
    Akhtar, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/972708.pdf
    Data publikacji:
    2015
    Wydawca:
    Instytut Medycyny Wsi
    Tematy:
    animal model
    antischizophrenic activity
    histamine H3 receptor
    antagonist
    rat
    treatment
    MK-801
    dizocilpine zob.MK-801
    Opis:
    Animal models based on N-methyl-d-aspartate (NMDA) receptor blockade have been widely reported. Ketamine and MK-801, the two noncompetitive antagonists of NMDA receptors, produce behaviors related to schizophrenia and exacerbated symptoms in patients with schizophrenia. The study presented here investigated the effect of subchronic dosing (once-daily, 7 day) of histamine H3 receptor (H3R) antagonists, ciproxifan (CPX) (3 mg/kg, i.p.) and clobenpropit (CBP) (15 mg/kg, i.p) including clozapine (CLZ) (3.0 mg/kg, i.p.) and chlorpromazine (CPZ) (3.0 mg/kg, i.p.), the atypical and typical antipsychotic, respectively, on MK-801(0.2 mg/kg, i.p.)-induced locomotor activity, and dopamine and histamine levels in rats. Atypical and typical antipsychotic was used to serve as clinically relevant reference agents to compare the effects of the H3R antagonists. MK-801 significantly increased horizontal activity which was reduced with CPX and CBP. The attenuation of MK-801-induced locomotor hyperactivity produced CPX and CBP were comparable to CLZ and CPZ. Dopamine and histamine levels were measured in striatum and hypothalamus, respectively, of rat brain. The MK-801 induced increase of the striatal dopamine level was reduced in rats pretreated with CPX and CBP including CLZ. CPZ also significantly lowered striatal dopamine levels, though the decrease was less robust compared to CLZ, CPX and CBP. MK-801 increased histamine content although to a lesser degree. Subchronic treatment with CPX and CBP exhibited further increased histamine levels in the hypothalamus compared to MK-801 treatment alone. Histamine H3 receptor agonist, R-α methylhistamine (10 mg/kg, i.p.) counteracted the effect of CPX and CBP. The findings of the present study support our previous work showing positive effects of CPX and CBP on MK-801-induced schizophrenia like behaviors in rodents. However, clinical studies have reported no antipsychotic effects with histamine H3 receptor antagonists.
    Źródło:
    Journal of Pre-Clinical and Clinical Research; 2015, 09, 1; 11-17
    1898-2395
    Pojawia się w:
    Journal of Pre-Clinical and Clinical Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Prostaglandins and arterial wall lipid metabolism - in vitro, ex-vivo and in vivo radioisotopic studies
    Autorzy:
    Sinzinger, H
    Rogatti, W.
    Powiązania:
    https://bibliotekanauki.pl/articles/69328.pdf
    Data publikacji:
    1994
    Wydawca:
    Polskie Towarzystwo Fizjologiczne
    Tematy:
    metabolism
    prostaglandin
    lipid
    calcium antagonist
    in vivo
    lipid metabolism
    radioisotopic study
    in vitro
    hypercholesterolemia
    low density lipoprotein
    atherosclerosis
    Źródło:
    Journal of Physiology and Pharmacology; 1994, 45, 1
    0867-5910
    Pojawia się w:
    Journal of Physiology and Pharmacology
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Assessment of combined treatment with vigabatrin and antihypertensive drugs against electroconvulsions in mice
    Autorzy:
    Lukawski, K.
    Raszewski, G.
    Czuczwar, S.J.
    Powiązania:
    https://bibliotekanauki.pl/articles/3559.pdf
    Data publikacji:
    2015
    Wydawca:
    Instytut Medycyny Wsi
    Tematy:
    combined treatment
    treatment
    vigabatrin
    antihypertensive drug
    electroconvulsion
    mice
    mouse
    receptor antagonist
    diuretic drug
    cardiovascular drug
    human disease
    anticonvulsant effect
    Opis:
    Introduction and objective: It is likely that cardiovascular drugs will be used in epileptic patients because heart failure and hypertension are common comorbid conditions with epilepsy. Experimental studies show that some cardiovascular drugs can affect the protective activity of antiepileptics. The aim of this study was to examine the effects in mice of angiotensin-converting enzyme (ACE) inhibitors (captopril and perindopril), angiotensin AT1 receptor antagonists (losartan and candesartan) and diuretics (hydrochlorothiazide and ethacrynic acid) on the anticonvulsant activity of vigabatrin (VGB), a second generation antiepileptic drug. Material and Methods: Adult Swiss mice were used in the study. The anticonvulsant action of VGB was assessed in the maximal electroshock seizure threshold test. Combined treatment with VGB and antihypertensive drugs was also tested for adverse effects in the passive avoidance task and chimney test. All drugs were administered intraperitoneally. Results: Captopril (50 mg/kg), perindopril (10 mg/kg), losartan (50 mg/kg), candesartan (8 mg/kg), hydrochlorothiazide (100 mg/kg) and ethacrynic acid (100 mg/kg) did not influence the protective action of VGB. The combined treatment with VGB (700 mg/kg) and antihypertensive drugs showed a strong tendency towards impaired retention in the passive avoidance task, and in the case of the combination of VGB with ethacrynic acid it reached statistical significance (P < 0.05). Mice were not disturbed in the chimney test following applied treatment. Conclusions: From the preclinical point of view, the use of the tested antihypertensive drugs in patients treated with VGB seems neutral regarding its anticonvulsant activity.
    Źródło:
    Journal of Pre-Clinical and Clinical Research; 2015, 09, 1
    1898-2395
    Pojawia się w:
    Journal of Pre-Clinical and Clinical Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Determination of in vitro metabolism of new non-imidazole histamine H3 receptor antagonist 1-[3-(4-tert-butylphenoxy)propyl]piperidine
    Autorzy:
    Kryczyk-Poprawa, Agata
    Szafarz, Małgorzata
    Palak, Aneta Palak
    Łażewska, Dorota
    Kuś, Kamil
    Opoka, Włodzimierz
    Szymura-Oleksiak, Joanna
    Powiązania:
    https://bibliotekanauki.pl/articles/895240.pdf
    Data publikacji:
    2019-10-30
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    1-[3-(4-tert-butylphenoxy)propyl]piperidin
    well-stirred model
    parallel tube model
    non-imidazole histamine H3 receptor antagonist
    Opis:
    Early understanding of the pharmacokinetics of drug candidates is essential during the evaluation of drug development process. DL76 1-[3-(4-tert-butylphenoxy)propyl]piperidine is a novel promising non-imidazole H3 receptor antagonist. Presented study was undertaken to compare with each other the predicted hepatic clearance values of DL76 calculated, using two most common mathematical models “well-stirred” and “parallel tube”, based on the data obtained in in vitro experiments. The metabolic intrinsic clearance of DL76 equaled to 0.4848 mL/min/mg protein was scaled up and the values of hepatic clearance estimated from "well-stirred" and "parallel tube" models were 55.47 mL/min/kg and 58.80 mL/min/kg, respectively. They were further compared with pharmacokinetic parameters calculated based on the concentration-time profile obtained following intravenous administration of DL76 to rats at the dose of 6 mg/kg. The estimated systemic serum clearance value of 144.5 mL/h/kg and blood clearance value of 81.17 mL/min/kg indicate the potential extrahepatic metabolism of the investigated compound. This study demonstrates the utility of rat liver microsomes for the prediction of DL76 hepatic clearance.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 5; 877-884
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Aripiprazol: od wyjątkowego mechanizmu działania do szerokich zastosowań
    Aripiprazole: from unique mechanism of action to widespread clinical applications
    Autorzy:
    Sobów, Tomasz
    Powiązania:
    https://bibliotekanauki.pl/articles/941077.pdf
    Data publikacji:
    2016
    Wydawca:
    Medical Communications
    Tematy:
    D2/D3 receptors
    aripiprazole
    bipolar disorder
    partial antagonist
    schizophrenia
    aripiprazol
    choroba afektywna dwubiegunowa
    częściowy antagonista
    receptory d2/d3
    schizofrenia
    Opis:
    Effective treatment of schizophrenia and bipolar disorder, the aim of which is complete symptomatic and functional improvement, still remains a challenge. Comprehensive approach to patient’s problems is thought to be crucial, and the usage of an adequate antipsychotic drug is believed to support this process effectively. Currently common modern antipsychotics exhibit similar efficacy in treating positive symptoms of schizophrenic psychosis and mania. However, they vary considerably in terms of their influence on other symptoms as well as tolerance, treatment acceptance and broadly understood doctor–patient cooperation. Aripiprazole is unique due to its mechanism of action. By contrast with other antipsychotics, it is a partial antagonist of D2/D3 (and certain serotonin receptors). Such a pharmacological profile not only grants it considerable efficacy in psychosis treatment, comparable to other second-generation antipsychotics, but also makes it beneficial in treating affective, cognitive and negative symptoms of schizophrenia. Other benefits granted by the pharmacological profile of this drug include: low risk of parkinsonism, beneficial profile in terms of its influence on metabolism (practically no influence on body weight) and the fact that it does not induce hyperprolactinaemia. Due to these positive pharmacological features, aripiprazole can be used not only in preferred monotherapy, but also in combined treatment, including for improved tolerance of other drugs. More recent studies suggest the extension of its indications to, among others, depression refractory to standard pharmacotherapy and behavioural disorders in patients with dementia.
    Efektywne, nastawione na możliwie kompletną poprawę objawową i funkcjonalną leczenie schizofrenii i choroby afektywnej dwubiegunowej pozostaje w dzisiejszym stanie wiedzy zadaniem trudnym. Uważa się, że kluczowe jest kompleksowe podejście do problemów pacjenta, a zastosowanie odpowiedniego leku przeciwpsychotycznego ma ten proces skutecznie wspomagać. Powszechnie obecnie stosowane nowoczesne leki przeciwpsychotyczne są podobnie skuteczne w zwalczaniu pozytywnych objawów psychozy schizofrenicznej oraz manii, natomiast znacznie różnią się w zakresie wpływu na pozostałe objawy, jak również pod względem tolerancji, akceptacji leczenia i szeroko rozumianej współpracy lekarz – pacjent. Aripiprazol wyróżnia się unikalnym mechanizmem działania – inaczej niż pozostałe leki przeciwpsychotyczne, jest częściowym antagonistą D2/D3 (oraz niektórych receptorów serotoninowych). Taki profil farmakologiczny pozwala na uzyskanie nie tylko znacznej, porównywalnej do innych leków przeciwpsychotycznych II generacji, skuteczności w leczeniu ostrej psychozy, ale także korzystnego wpływu na objawy afektywne, poznawcze i negatywne schizofrenii. Dodatkowymi korzyściami wynikającymi z profilu farmakologicznego leku są niskie ryzyko wywoływania parkinsonizmu, korzystny profil w zakresie wpływu na stan metaboliczny (praktycznie brak wpływu na masę ciała) oraz niewywoływanie hiperprolaktynemii. Te korzystne cechy farmakologiczne powodują, że aripiprazol może być stosowany nie tylko w preferowanej monoterapii, ale także jako leczenie dodane, w tym w celu poprawy tolerancji innych leków. Nowsze badania wskazują na możliwości poszerzenia panelu wskazań, między innymi o depresję oporną na standardową farmakoterapię oraz zaburzenia zachowania u chorych z otępieniem.
    Źródło:
    Psychiatria i Psychologia Kliniczna; 2016, 16, 3; 160-164
    1644-6313
    2451-0645
    Pojawia się w:
    Psychiatria i Psychologia Kliniczna
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    The effect of selected agonists and antagonists of cholinergic receptors on the motor activity of epithelium of Achatina fulica
    Autorzy:
    Kaczorowski, P.
    Powiązania:
    https://bibliotekanauki.pl/articles/84665.pdf
    Data publikacji:
    2016
    Wydawca:
    Uniwersytet Mikołaja Kopernika. Wydział Biologii i Ochrony Środowiska. Stowarzyszenie Malakologów Polskich
    Tematy:
    agonist
    antagonist
    cholinergic receptor
    motor activity
    epithelium
    Achatina fulica
    land snail
    Achatinidae
    giant African snail
    giant African land snail zob.giant African snail
    snail
    Źródło:
    Folia Malacologica; 2016, 24, 1
    1506-7629
    Pojawia się w:
    Folia Malacologica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Real-life trends of anticoagulant prescribing practices for pulmonary embolism - results of a single-center study based on the experience of a multi-profile clinical hospital
    Autorzy:
    Szymańska, Urszula A.
    Kurzyna, Marcin
    Segiet-Święcicka, Agnieszka
    Kułak, Piotr
    Kosior, Dariusz A.
    Powiązania:
    https://bibliotekanauki.pl/articles/35114663.pdf
    Data publikacji:
    2022
    Wydawca:
    Radomskie Towarzystwo Naukowe
    Tematy:
    anticoagulation
    low molecular weight heparin
    direct oral anticoagulants
    pulmonary embolism
    vitamin K antagonist
    antykoagulacja
    heparyna drobnocząsteczkowa
    bezpośrednie doustne antykoagulanty
    zatorowość płucna
    antagoniści witaminy k
    Opis:
    Acute pulmonary embolism (APE) is one of the main causes of cardiovascular deaths and anticoagulant treatment plays a key role in preventing recurrent episodes, chronic thromboembolic pulmonary hypertension (CTEPH), and deaths. The aim of this study is to assess the real-life trends and to determine factors associated with the choice of anticoagulation therapy in patients with APE. This is a single center prospective open study. We followed 178 consecutive patients admitted to the tertiary clinical center with APE proven with computed tomography (CT) scan within period of 24 months. A total number of 178 patients with APE were enrolled in the study. 48.9% of subjects were hospitalized in cardiology department. As a prolonged anticoagulant therapy 35.7% of study cohort received direct oral anticoagulants (DOACs), 35.1% LMWH, and 29.2% vitamin K antagonists (VKA), respectively. No statistically significant differences were found between the departments regarding frequency of prescribing anticoagulants (p=0.15). The multivariable analysis showed that oral anti-coagulants (OACs) were less likely to be prescribed than LMWH in patients with malignancy, history of major bleeding, serious medical condition and altered mental status. OACs were preferred over LMWH in symptoms of deep vein thrombosis (DVT). VKA were significantly less likely to be chosen than DOACs in patients with history of orthopaedics procedure. After six months anticoagulation therapy was discontinued in 24.3% of patients. Concluding, the form of anticoagulant therapy was associated with the presence of chronic diseases. LMWH was prescribed in high bleeding risk patients more frequently.
    Źródło:
    Scientiae Radices; 2022, 1, 1; 36-45
    2956-4808
    Pojawia się w:
    Scientiae Radices
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Prevention and treatment of ulcers induced by nonsteroidal anti-inflammatory drugs: an update
    Autorzy:
    Dajani, E Z
    Agrawal, N.M.
    Powiązania:
    https://bibliotekanauki.pl/articles/70695.pdf
    Data publikacji:
    1995
    Wydawca:
    Polskie Towarzystwo Fizjologiczne
    Tematy:
    gastric ulcer
    gastrointestinal damage
    sulglycotide
    rheumatic disease
    prostaglandin E
    duodenal ulcer
    disease prevention
    misoprostol
    receptor antagonist
    omeprazole
    antiinflammatory drug
    ulcer
    human physiology
    histamine H2
    sucralfate
    therapy
    Źródło:
    Journal of Physiology and Pharmacology; 1995, 46, 1
    0867-5910
    Pojawia się w:
    Journal of Physiology and Pharmacology
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
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