Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

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Tytuł oryginału: Role of nitric oxide in benzodiazepines-induced antinociception in mice.
Autorzy: Talarek Sylwia, Fidecka Sylwia
Źródło: Pol. J. Pharmacol. 2002: 54 (1) s.27-34, il., bibliogr. 39 poz., sum.
Sygnatura GBL: 313,156

Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • tytuł obcojęzyczny

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  • zwierzęta
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    Streszczenie angielskie: The influence of nitric oxide (NO) on antinociceptive acivity of diazepam (DZ), chlordiazepoxide (CDP) and clonazepam (CZ) was examined using the writhing test in mice. The effect of DZ was also studied in mice using hot plate and tail flick tests. DZ (1.25, 2.5 and 5 mg/kg), CDP (1.25, 2.5, 5, 10 and 20 mg/kg) and CZ (0.075, 0.3125, 0.625, 1.25 and 2.5 mg/kg) produced significant, dose-dependent (DZ CDP) antinociception in mice. The benzodiazepines (BZs)-induced antinociception was antagonized by flumazenil (5 mg/kg) and was not changed by naloxone (2.5, 5 and 10 mg/kg), except that of CZ, which was reversed by 5 mg/kg of naloxone. N**G-nitro-L-arginine methyl ester hydrochloride (L-NAME) as well as 7-nitroinadzole (7-NI) intensified antinociceptive activity of BZs. The antinociceptive effect resulting from co-administration of L-NAME with CZ and 7-NI with CDP was reversed by L-arginine. Methylene blue (MB) increased, whereas L-arginine (but not D-arginine) decreased antinociceptive effects of the studied BZs. These results suggest that the NO-cGMP pathway is involved in the mechanism of BZs-induced antinociception in the writhing test in mice.

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    Tytuł oryginału: Lack of interaction between the behavioral effects of ketamine and benzodiazepines in mice.
    Autorzy: Fidecka Sylwia, Pirogowicz Ewa
    Źródło: Pol. J. Pharmacol. 2002: 54 (2) s.111-117, il., tab., bibliogr. 38 poz.
    Sygnatura GBL: 313,156

    Hasła klasyfikacyjne GBL:
  • farmacja
  • neurologia

    Typ dokumentu:
  • praca doświadczalna
  • tytuł obcojęzyczny

    Wskaźnik treści:
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    Streszczenie angielskie: The effect of co-administration of ketamine at the sub-effective dose with diazepam, chlordiazepoxide and clonazepam on their antinociceptive and protective efficacy against pentetrazole-induced seizures were studied in mice. Ketamine alone produces dose-dependent antinociception manifested as reduction in the number of writhing episodes evoked by acetic acid. In the writhing test, the antinociceptive effects of the threshold doses of diazepam, chlordiazepoxide or clonazepam were not changed by ketamine, whereas that of morphine was intensified by ketamine. In the hot plate test, slight antinonciceptive effects of the threshold dose of diazepam, but not that of chlordizepoxide (except the results at 120 min of observation), were significantly intensified by ketamine vs ketamine alone. Ketamine alone was able to protect mice, in the dose-related manner, against penetrazole-induced seizures. The anticonvulsant effects of the threshold doses of diazepam, chlordizepoxide and clonazepam were not changed by ketamine. These findings indicate that co-administration of ketamine (at the sub-effective dose) with diazepam, chlordiazepoxide and clonazepam (at non-effective) resulted in an intensification of neither antinociceptive nor protective effect against pentetrazole-induced seizures in mice. These data seem to indicate the lack of interaction between ketamine and benzodiazepines with respect to their antinociceptive and anticonvulsant efficacy.

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    Tytuł oryginału: Synthesis and pharmacological activity of new carbonyl derivatives of 1-aryl-2-iminoimidazolidine. P. 3: Synthesis and pharmacological activity of 1-aryl-5,6(1H)dioxo-2,3-dihydroimidazol[1,2-a]imidazoles.
    Autorzy: Matosiuk Dariusz, Fidecka Sylwia, Antkiewicz-Michaluk Lucyna, Dybala Izabela, Kozioł Anna E.
    Źródło: Eur. J. Med. Chem. 2002: 37 (10) s.845-853, il., tab., bibliogr. 20 poz.
    Sygnatura GBL: 312,629

    Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • praca opublikowana za granicą
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • myszy

    Streszczenie angielskie: Synthesis and pharmacological activity of 1-aryl-5,6(1 H)dioxo-2,3-dihydroimidazo[1,2-a]imidazoles (D) are presented. The title compounds were obtained from 1-aryl-2-iminoimidazolidines (1) by cyclization reaction with oxalic acid derivatives-ethyl ester (2) or chloride (3). They were tested for pharmacological activity in animal and binding assay tests. With moderate acute toxicity (LD50 ~ 200 mg kg**-1, i.p.), they exhibited significant and serotonergic activities as results of the `writhing' and the `hot plate' tests indicated, and reduced number of `head twitch' episodes after 5-HTP (5-hydroxytryptophan) administration. Reversion of the antinociception produced in the `writhing' test by small dose of naloxon (5 mg kg**-1) can suggest an opioid-like mechanism of their analgesic activity. The probable receptor inhibition mechanism of their analgesic and serotonergic activity was confirmed in the binding assay tests (by radioligand displacement) toward the opioid ć and serotonin 5-HT2 receptors. Additionally, they exhibited affinity toward the benzodiazepine (BZD) receptor as well, although in behavioral tests compounds did not produce any clear depressive effect on the central nervous system (CNS) of mice. Simple chemical structure of the title compounds, in comparison to other carbonyl derivatives of 1-aryl-2-iminoimidazolidine presented in this series of papers, underline very important role both of a hydrophobic moiety (aromatic ring) and polar groups (hydrogen-bond acceptors) in the serotonin receptor interaction. The coexistence of opioid-like, serotonergic and BZD receptor inhibition activity can be very interesting and can lead to creation of the novel group of antidepressants.

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    Tytuł oryginału: Synthesis and pharmacological activity of new carbonyl derivatives of 1-aryl-2-iminoimidazolidine. P. 2: Synthesis and pharmacological activity of 1,6-diaryl-5,7(1H)dioxo-2,3-dihydroimidazo[1,2-ŕ][1,3,5]triazines.
    Autorzy: Matosiuk Dariusz, Fidecka Sylwia, Antkiewicz-Michaluk Lucyna, Lipkowski Janusz, Dybala Izabela, Koziol Anna E.
    Źródło: Eur. J. Med. Chem. 2002: 37 (9) s.761-772, il., tab., bibliogr. 12 poz.
    Sygnatura GBL: 312,629

    Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • praca opublikowana za granicą
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • myszy

    Streszczenie angielskie: Synthesis and pharmacological activity of 1,6-diaryl-5,7 (1H)dioxo-2,3-dihydroimidazo-[1,2-ŕ][1,3,5]triazines (C) are presented. The title compounds were obtained from 1-aryloimidazolinurea derivatives in cyclization reaction with difunctional carbonyl reagents - phosgene (method I) or carbonyldiimidazole (CDI) (method II). Their molecular structures were confirmed by the X-ray analysis of 1-phenyl-6-(4-chlorophenyl)-5,7(1H)-dioxo-2,3-dihydroimidazo[1,2-ŕ][1,3,5]triazine C2) crystals. Compounds C exhibited significant depressive action on the central nervous system (CNS) of the laboratory animals, correlated with very low acute toxicity (LD50 2000 mg kg**-1 i.p.), and showed antinociceptive activity in behavioural models. Reversion of this effect by small dose of naloxone (5 mg kg**-1) can suggest opioid-like mechanism of antinociception produced by these and other carbonyl derivatives of 1-aryl-2-iminoimidazolidine. Additionally, an effect on the serotonin neurotransmission pathway was also observed. The receptor mechanism of activity for investigated compounds was confirmed only for the opioid ć receptor in binding affinity assay test. Same tests performed for the serotonin 5-HT2 and benzodiazepine BZD receptors showed no affinity for tested compounds. The opioid-like and serotonergic activities are similar to these described earlier for chain carbonyl 1-aryl-2-iminoimidazolidine derivatives containing urea moiety, mainly due to similar chemical structure, although compounds C are not able to adopt any of the higher energy confirmations of urea derivatives...

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