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Tytuł:
Anticonvulsant and reproductive toxicological studies of the imidazole-based histamine H3R antagonist 2-18 in mice
Autorzy:
Kieć-Kononowicz, Katarzyna
Shafiullah, Mohamed
Abdulrazzaq, Yousef M.
Bastaki, Salim M.
Sadek, Bassem
Więcek, Małgorzata
Opis:
The imidazole-based H3R antagonist 2-18 with high in vitro H3R antagonist affinity, excellent in vitro selectivity profile, and high in vivo H3R antagonist potency was tested for its anticonvulsant effect in maximal electroshock (MES)-induced convulsions in mice having valproic acid (VPA) as a reference antiepileptic drug (AED). Additionally, H3R antagonist 2-18 was evaluated for its reproductive toxicity in the same animal species. The results show that acute systemic administration (intraperitoneal; i.p.) of H3R antagonist 2-18 (7.5, 15, 30, and 60 mg/kg, i.p.) significantly and dose dependently protected male as well as female mice against MES-induced convulsion. The protective action observed for H3R antagonist 2-18 in both mice sexes was comparable to that of VPA and was reversed when mice were pretreated with the selective H3R agonist (R)-alpha-methylhistamine (RAMH, 10 mg/kg, i.p.). Moreover, the results show that acute systemic administration of single (7.5, 15, 30, or 60 mg/kg, i.p.) or multiple doses (15×3 mg/kg, i.p.) of H3R antagonist 2-18 on gestation day (GD) 8 or 13 did not affect the maternal body weight of mice when compared with the control group. Furthermore, no significant differences were observed in the average number of implantations and resorptions between the control and H3R antagonist 2-18-treated group at the early stages of gestation and the organogenesis period. However, oral treatment with H3R antagonist 2-18 (15 mg/kg) on GD 8 induced a reduced number of live embryos when compared with the i.p.-treated mice. In addition, no significant changes in the fetal body and placental weights were observed after injection of H3R antagonist 2-18 with all selected doses. However, three dose groups of i.p. and oral 15 mg/kg on GD 13 significantly affected the placental weight when compared with control group. Notably, the treatment of pregnant female with the H3R antagonist 2-18 did not produce significant malformation in the fetus in both groups. In conclusion, the novel H3R antagonist 2-18 proves to be a very safe compound and displays a low incidence of malformations, demonstrating that H3R antagonist 2-18 may have a potential future therapeutic value in epilepsy.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
C-11, a New Antiepileptic Drug Candidate : Evaluation of the Physicochemical Properties and Impact on the Protective Action of Selected Antiepileptic Drugs in the Mouse Maximal Electroshock-Induced Seizure Model
Autorzy:
Raszewski, Grzegorz
Andres-Mach, Marta
Chrościńska-Krawczyk, Magdalena
Szewczyk, Aleksandra
Szala-Rycaj, Joanna
Kamiński, Krzysztof
Zagaja, Mirosław
Abram, Michał
Opis:
C-11 is a hybrid compound derived from 2-(2,5-dioxopyrrolidin-1-yl) propanamide, with a wide spectrum of anticonvulsant activity and low neurotoxicity. The aim of this study was to determine the effects of C-11 on the protective action of various antiepileptic drugs (i.e., carbamazepine CBZ, lacosamide LCM, lamotrigine LTG, and valproate VPA) against maximal electroshock-induced seizures (MES) in mice, as well as its neuroprotective and physicochemical/pharmacokinetic properties. Results indicate that C-11 (30 mg/kg, i.p.) significantly enhanced the anticonvulsant action of LCM (p < 0.001) and VPA (p < 0.05) but not that of CBZ and LTG in the MES test. Neither C-11 (30 mg/kg) alone nor its combination with other anticonvulsant drugs (at their ED50 values from the MES test) affected motor coordination; skeletal muscular strength and long-term memory, as determined in the chimney; grip strength and passive avoidance tests, respectively. Pharmacokinetic characterization revealed that C-11 had no impact on total brain concentrations of LCM or VPA in mice. Qualitative analysis of neuroprotective properties of C-11, after a single administration of pilocarpine, revealed no protective effect of this substance in the tested animals. Determination of physicochemical descriptors showed that C-11 meets the drug-likeness requirements resulting from Lipinski and Veber’s rules and prediction of gastrointestinal absorption and brain penetration, which is extremely important for the CNS-active compounds.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
No effect of3-(N-p-isopropoxyphenylsuccinimidomethylamino)-cinnamic acid on anticonvulsant action of different classical antiepileptic drugs in mouse maximal electroshock-induced seizure model
Autorzy:
Luszczycki, J. J.
Marczewski, T.
Marzeda, E.
Durmowicz, D.
Podgorska, D.
Kocharov, S. L.
Florek-Luszczki, M.
Tematy:
antiepileptic drugs
maximal electroshock-induced seizures
pharmacokinetic/pharmacodynamic interaction
p-isopropoxyphenylsuccinimide derivative
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Wydawca:
Instytut Medycyny Wsi
Powiązania:
https://bibliotekanauki.pl/articles/972739.pdf  Link otwiera się w nowym oknie
Opis:
Introduction and objective: The aim of the study was to determine the effects of 3-(N-p-isopropoxyphenylsuccinimidomethylamino)-cinnamic acid (IPPSMA-CA – a new succinimide derivative) on the protective action of 4 classical antiepileptic drugs (AEDs): carbamazepine [CBZ], phenobarbital [PB], phenytoin [PHT] and valproate [VPA]), against maximal electroshock (MES)-induced tonic seizures in mice. Materials and methods: Tonic hind limb extension (seizure activity) was evoked in adult male albino Swiss mice by a current (sine-wave, 25 mA, 500 V, 50 Hz, 0.2 s stimulus duration) delivered via auricular electrodes. Acute adverse-effectprofiles of the combination of IPPSMA-CA and 4 classical AEDs (CBZ, PB, PHT and VPA) with respect to motor performance, long-term memory and skeletal muscular strength were measured in the chimney, passive avoidance and grip-strength tests, respectively. Results: IPPSMA-CA administered at 150 mg/kg (i.p.) significantly elevated the threshold for electroconvulsions in mice (p<0.01). IPPSMA-CA at doses of 50 and 100 mg/kg, however, had no significant impact on the threshold for electroconvulsions in mice. Nor did IPPSMA-CA (100 mg/kg) significantly affect the anticonvulsant activity of CBZ, PB, PHT and VPA in the MES test in mice. None of the examined combinations of IPPSMA-CA (100 mg/kg, i.p.) with CBZ, PB, PHT and VPA (at their ED50 values from the MES-induced seizure test) affected motor coordination in the chimney test, long-term memory in the passive avoidance task, and muscular strength in the grip-strength test in mice. This indicates no possible acute adverse effects in animals. Conclusions: IPPSMA-CA elevated the threshold for electroconvulsions in mice in a dose-dependent manner. However, IPPSMA-CA at a sub-protective dose of 100 mg/kg did not affect the anticonvulsant action of various classical AEDs in the mouse MES model. Thus, the combinations of IPPSMA-CA with CBZ, PB, PHT and VPA are neutral from a preclinical viewpoint.
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
TC-G 1008 facilitates epileptogenesis by acting selectively at the GPR39 receptor but non-selectively activates CREB in the hippocampus of pentylenetetrazole-kindled mice
Autorzy:
Wyska, Elżbieta
Doboszewska, Urszula
Pieróg, Mateusz
Szewczyk, Bernadeta
Maćkowiak, Marzena
Sowa, Ireneusz
Sawicki, Jan
Nieoczym, Dorota
Rafało-Ulińska, Anna
Sajnóg, Adam
Esguerra, Camila V.
Socała, Katarzyna
Szafarz, Małgorzata
Wlaź, Piotr
Nowak, Gabriel
Barałkiewicz, Danuta
Gawel, Kinga
Młyniec, Katarzyna
Opis:
The pharmacological activation of the GPR39 receptor has been proposed as a novel strategy for treating seizures; however, this hypothesis has not been verified experimentally. TC-G 1008 is a small molecule agonist increasingly used to study GPR39 receptor function but has not been validated using gene knockout. Our aim was to assess whether TC-G 1008 produces anti-seizure/anti-epileptogenic effects in vivo and whether the effects are mediated by GPR39. To obtain this goal we utilized various animal models of seizures/epileptogenesis and GPR39 knockout mice model. Generally, TC-G 1008 exacerbated behavioral seizures. Furthermore, it increased the mean duration of local field potential recordings in response to pentylenetetrazole (PTZ) in zebrafish larvae. It facilitated the development of epileptogenesis in the PTZ-induced kindling model of epilepsy in mice. We demonstrated that TC-G 1008 aggravated PTZ-epileptogenesis by selectively acting at GPR39. However, a concomitant analysis of the downstream effects on the cyclic-AMP-response element binding protein in the hippocampus of GPR39 knockout mice suggested that the molecule also acts via other targets. Our data argue against GPR39 activation being a viable therapeutic strategy for treating epilepsy and suggest investigating whether TC-G 1008 is a selective agonist of the GPR39 receptor.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
SYNTHESIS AND ANTICONVULSANT PROPERTIES OF SOME N-ARYL AND N-ARYLAMINOMETHYL DERIVATIVES OF 3-P-ISOPROPOXYPHENYLPYRROLIDINE-2,5-DIONE
Autorzy:
Kocharov, Sergey L.
Panosyan, Henry
Chmielewski, Jaroslaw
Gworek, Barbara
Łuszczki, Jarogniew J.
Tematy:
maximal electroshock-induced seizures
3-p-Isopropoxyphenylpyrrolidine-2
5-dione
N-aryl derivatives
N-arylaminomethyl derivatives
Pokaż więcej
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Powiązania:
https://bibliotekanauki.pl/articles/895346.pdf  Link otwiera się w nowym oknie
Opis:
Introduction: Anticonvulsant properties of newly synthesized compounds and potential antiepileptic drugs are usually assessed in screen tests in experimental animals. One of the most commonly used screen tests in mice is the maximal electroshock-induced seizure test that reflects tonic-clonic seizures in humans. Materials and Method: A series of 3-p-isopropoxyphenylpyrrolidine-2,5-dione derivatives, including N-aryl and N-arylaminomethyl analogs, were characterized for their anticonvulsant properties in the maximal electroshock-induced seizure test in mice. Electroconvulsions (tonic-clonic seizures) were evoked in adult Albino Swiss mice by a current (sine-wave, 25mA, 50Hz, 500V, 0.2s stimulus duration) delivered via auricular electrodes. Results: N-aryl derivatives did not show any anticonvulsant activity, whereas some representatives of N-arylaminomethyl derivatives, i.e. N-Mannich bases, exhibited a distinct protective action against maximal electroshock-induced (MES) convulsions in mice. Conclusions: Several N-arylaminomethyl derivatives of 3-p-isopropoxyphenylpyrrolidine-2,5-dione may become in future new antiepileptic drugs, or they could serve as valuable supporting materials for obtaining new derivatives with stronger anticonvulsant activities than their maternal compounds.
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Antagonistic interaction of lacosamide with carbamazepine and valproate in the mouse tonic-clonic seizure model
Antagonistyczna interakcja lakozamidu z karbamazepiną i walproainianem w modelu drgawek toniczno-klonicznych u myszy
Autorzy:
Kondrat-Wróbel, M.W.
Załuska, K.
Walczak, A.
Panasiuk-Poterek, A.N.
Gut-Lepiech, A.
Wróblewska-Łuczka, P.
Łuszczki, J.J.
Tematy:
antiepileptic drugs
isobolography
maximal electroshock
three-drug combination
antagonism
leki przeciwpadaczkowe
izobolografia
elektrowstrząsy
kombinacja trzech leków
antagonizm
Pokaż więcej
Wydawca:
Akademia Bialska Nauk Stosowanych im. Jana Pawła II w Białej Podlaskiej
Powiązania:
https://bibliotekanauki.pl/articles/2053463.pdf  Link otwiera się w nowym oknie
Opis:
Background. It is estimated that approximately 1% of people worldwide suffer from epilepsy. Currently available antiepileptic drugs (AEDs) are able to control epileptic seizures in about 70% of cases. In the remaining patients (30%), the application of two or three AEDs in combination is necessary for effective seizure management. The goal of this work was to characterize the interaction of three AEDs: lacosamide (LCM), carbamazepine (CBZ) and valproate (VPA) at the fixed-ratio of 1:1:1 in the mouse tonic-clonic seizure model. Material and methods. Male albino Swiss mice, after receiving a combination of LCM, CBZ and VPA, were challenged with electric current to evoke tonic hind limb extension (seizure activity). Protection of the mice from tonic-clonic seizures was assessed by isobolographic analysis to determine the type of interaction occurring between these drugs. Results. Type I isobolographic analysis revealed that the combination of LCM, CBZ and VPA produced infra-additive (antagonistic) interaction in the mouse tonic-clonic seizure model. Conclusions. Since the three-drug mixture of LCM, CBZ a nd VPA exerted an antagonistic interaction in the tonic-clonic seizure test in mice, we would caution physicians against treating epilepsy patients with this unfavorable combination.
Wprowadzenie. Szacuje się, że około 1% osób na całym świecie cierpi na padaczkę. Obecnie dostępne leki przeciwpadaczkowe pozwalają na opanowanie napadów padaczkowych w około 70% przypadków. U pozostałych pacjentów z padaczką (30%) konieczne jest zastosowanie dwóch lub trzech leków przeciwpadaczkowych w kombinacji. Celem pracy było scharakteryzowanie interakcji między trzema lekami przeciwpadaczkowymi: lakozamidem (LCM), karbamazepiną (CBZ) i walproinianem (VPA) w stałym stosunku dawek 1:1:1 w modelu drgawek toniczno-klonicznych u myszy. Materiał i metody. Samce myszy albino Swiss, po otrzymaniu kombinacji LCM, CBZ i VPA, poddano działaniu prądu elektrycznego, aby wywołać toniczny wyprost kończyn tylnych (aktywność drgawkową). Ochronę myszy przed napadami toniczno-klonicznymi oszacowano za pomocą analizy izobolograficznej, aby określić typ interakcji zachodzącej między tymi lekami. Wyniki. Analiza izobolograficzna typu I ujawniła, że kombinacja LCM, CBZ i VPA powodowała oddziaływanie infra-addytywne (antagonistyczne) w modelu drgawek toniczno-klonicznych u myszy. Wnioski. Ponieważ trójlekowa mieszanina LCM, CBZ i VPA wywierała antagonistyczną interakcję w teście napadów toniczno-klonicznych u myszy, specjalne ostrzeżenie jest konieczne dla lekarzy, aby nie leczyć pacjentów z padaczką tą niekorzystną kombinacją.
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synthesis and study of substituted amides of some 5-membered isocyclic and heterocyclic acids as potential anticonvulsants
Autorzy:
STRUPIŃSKA, MARZANNA
JAKUBOWICZ, BARTŁOMIEJ
ROSTAFIŃSKA-SUCHAR, GRAŻYNA
PIRIANOWICZ-CHABER, ELŻBIETA
KONAROWSKA, MAGDALENA
MAZUREK, ALEKSANDER P.
Tematy:
Maximal electroshock seizure test
anticonvulsant activity
substituted benzylamides of isocyclic acids
substituted benzylamides of heterocyclic acids
psychomotor seizure test
Pokaż więcej
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Powiązania:
https://bibliotekanauki.pl/articles/895607.pdf  Link otwiera się w nowym oknie
Opis:
A series of substituted amides of isocyclic and heterocyclic acids have been synthesized. All obtained compounds were evaluated qualitatively for their anticonvulsant activity in the maximal electroshock seizure test (MES test) and psychomotor seizure test (6 Hz test) in mice after intraperitoneal administration. The neurological toxicity was determined in the rotorod neurotoxicity test (Tox test). Two of these compounds appeared most promising: 3-oxo-1-cyklopentanecarboxylic acid 2-fluorobenzylamide (5), 1-cyclopentenecarboxylic acid 2-(trifluoromethyl)benzylamide (8) and were tested quantitatively in MES test in mice after oral administration (o.p.) and in 6 Hz test in mice after intraperitoneal administration(i.p.). Compound (5) showed MES ED50 =82.65 mg/kg and compound (8) showed 6 Hz ED50=84.13 mg/kg.
Dostawca treści:
Biblioteka Nauki
Artykuł
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