Informacja

Drogi użytkowniku, aplikacja do prawidłowego działania wymaga obsługi JavaScript. Proszę włącz obsługę JavaScript w Twojej przeglądarce.

English (EN)·Polski (PL)·Yкраїнський (UK)
Przejdź do strony domowej biblioteki Centralna Biblioteka Wojskowa Link otwiera się w nowym oknie Logo biblioteki Prolib Integro - strona głównaCentralna Biblioteka Wojskowa

Wyszukujesz frazę "antagonist" wg kryterium: Temat

  Lista filtrów
Wyrównaj
Wyświetlanie 1-15 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
Wyświetlanie 1-15 z 18

Ta witryna wykorzystuje pliki cookies do przechowywania informacji na Twoim komputerze. Pliki cookies stosujemy w celu świadczenia usług na najwyższym poziomie, w tym w sposób dostosowany do indywidualnych potrzeb. Korzystanie z witryny bez zmiany ustawień dotyczących cookies oznacza, że będą one zamieszczane w Twoim komputerze. W każdym momencie możesz dokonać zmiany ustawień dotyczących cookies