Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

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1/5

Tytuł oryginału: Journal of Pharmacy and Pharmacology
Tytuł polski: Pharmacological properties and SAR of new 1,4-disubstituted piperazine derivatives with hypnotic-sedative activity.
Autorzy: Chilmonczyk Zdzisław, Mazgajska Maria, Iskra-Jopa Joanna, Chojnacka-Wójcik Ewa, Tatarczyńska Ewa, Kłodzińska Aleksandra, Nowak Jerzy Z.
Źródło: J. Pharm. Pharmacol. 2002: 54 (5) s.689-698, il., tab., bibliogr. s. 696-698
Sygnatura GBL: 300,961

Hasła klasyfikacyjne GBL:
  • farmacja

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

    Wskaźnik treści:
  • zwierzęta
  • myszy

    Streszczenie angielskie: Preparation, pharmacological properties and structure-activity relationships of new pyrimidylpiperazine derivatives, exhibiting sedative and hypnotic activity in mice, are reported. The hypnotic activity of the compounds was comparable with that of zopiclone (the known hypnotic-sedative agent), their interaction with ethanol, however, being much lower. The obtained results suggested that zopiclone and pyrimidylpiperazines 2, 4 and 5 exerted their pharmacological activity through a different mechanism - zopiclone through the interaction with benzodiazepine receptors and compounds 2, 4 and 5 through an unidentified molecular target. The pharmacological properties of compound 3 could be the result of a mixed mechanism of action, combining the properties of zopiclone and those of compounds 2, 4 and 5. A common feature of zopiclone and compounds 2 and 3 was that, after their systemic administration, independently of mechanism of action, together with the hypnotic effect a reduction of the 5-HT turnover in the mouse brain was observed. Minimum structural requirements for the hypnotic activity were formulated. Structural considerations have shown that removing the ŕ-carbonyl group did not influence the drug's ability to inhibit the locomotor activity. However, it did influence its ability to disturb motor coordination or abolish the righting reflex within non-lethal doses.

    2/5

    Tytuł oryginału: Group II mGlu receptor agonists inhibit behavioural and electrophysiological effects of DOI in mice.
    Autorzy: Kłodzińska Aleksandra, Bijak Maria, Tokarski Krzysztof, Pilc Andrzej
    Źródło: Pharmacol. Biochem. Behav. 2002: 73 (2) s.327-332, il., bibliogr. s. 331-332
    Sygnatura GBL: 312,498

    Hasła klasyfikacyjne GBL:
  • farmacja

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

    Wskaźnik treści:
  • zwierzęta
  • myszy

    Streszczenie angielskie: It has been suggested that metabotropic glutamate (mGlu) receptor agonists selective for Group II mGlu receptors may have antipsychotic action. Therefore, we studied whether the effects, which could be related to psychotomimetic action of hallucinogenic drugs, are inhibited by Group II mGlu receptor agonists. The selective mGlu2/3 agonist LY354740 and LY379268 inhibited (ń)1-(2,5-dimethoxy-4-iodophenyl)-2-aminoproprane (DOI)-induced head twitches in mice in a dose-dependent manner. Furthermore, LY379268 suppressed an increase in the frequency of sponataneous excitatory synaptic potentials induced by bath-applied DOI in layer V pyramidal cells recorded in the murine medial frontal cortex. The data indicate that Group II mGlu receptor agonist may counteract the effects of hallucinogenic drugs.

    3/5

    Tytuł oryginału: Multiple MPEP administrations evoke anxiolytic- and antidepressant-like effects in rats.
    Autorzy: Pilc A., Kłodzińska A., Brański P., Nowak G., Pałucha A., Szewczyk B., Tatarczyńska E., Chojnacka-Wójcik E., Wierońska J. M.
    Źródło: Neuropharmacology 2002: 43 (2) s.181-187, il., tab., bibliogr. s. 186-187
    Sygnatura GBL: 305,141

    Hasła klasyfikacyjne GBL:
  • psychiatria i psychologia
  • farmacja
  • neurologia

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

    Wskaźnik treści:
  • zwierzęta
  • szczury
  • płeć męska

    Streszczenie angielskie: Several lines of evidence suggest a crucial involvement of glutamate in the mechanism of action of anxiolytic and antidepressant drugs. The involvement of group I mGLu receptors in anxiety and depression has also been proposed. In view of the recent discovery of anxiolytic- or antidepressant-like effects of acute injections of 2-methyl-6-(phenylethyl)-pyridine (MPEP), a selective and brain penetrable mGlu5 receptor antagonist, we designed the present study to examine anxiolytic- and/or antidepressant-like effects of multiple administration of this drug. The anxiolytic-like effects of MPEP were evaluated in rats using the conflict drinking test. The antidepressant-like effect was estimated using the rat olfactory bulbectomy model of depression. Seven subsequent injections of MPEP (1 mg/kg) significantly (by 320 p.c.) increased the number of shock accepted during the experimental session in the Vogel test. MPEP given once daily at a dose of 10 mg/kg, restored the learning deficit of bulbectomized rats after 14 days of treatment, remaining without any effect in the sham-operated animals. N-methyl-D-aspartic acid (NMDA)-induced convulsions in mice were not affected by a single injection of MPEP (30 mg/kg) indicating that at this dose MPEP did not block NMDA receptors. The results indicate that the prolonged blockade of mGlu5 receptors exert anxiolytic- and antidepressant-like effects in rats. No tolerance to anxiolytic-like action occurs. The previously mentioned results further indicate that antagonists of group I mGlu receptors may play a role in the therapy of both anxiety and depression.

    4/5

    Tytuł oryginału: Effects of combined administration of 5-HT 1A and/or 5-HT 1B receptor antagonists and paroxetine or fluoxetine in the forced swimming test in rats.
    Autorzy: Tatarczyńska Ewa, Kłodzińska Aleksandra, Chojnacka-Wójcik Ewa
    Źródło: Pol. J. Pharmacol. 2002: 54 (6) s.615-623, tab., bibliogr. 58 poz.
    Sygnatura GBL: 313,156

    Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • szczury
  • płeć męska

    Streszczenie angielskie: Clinical data suggest that coadministration of pindolol, a 5-HT 1A/5-HT 1B/ á-adrenoceptor antagonist, and selective serotonin reuptake inhibitors (SSRIs) may shorten the time of onset a clinical action and may increase beneficial effects of the therapy of drug-resistant depression. Effects of combined administration of SSRIs and 5-HT receptor ligands are currently evaluated in animal models for the detection of an antidepressant-like activity; however, the obtained results turned out to be inconsistent. The aim of the present study was to investigate effects of a 5-HT 1A antagonist (WAY 100635), 5-HT 1B antagonists (SB 216641 and GR 127935) or pindolol, given in combination with parotexine or fluoxetine (SSRIs), in the forced swimming test in rats (Porsolt test). When given alone, paroxetine (10 and 20 mg/kg), fluoxetine (10 and 20 mg/kg), WAY 100635 (0.1 and 1 mg/kg), SB216641 (2 mg/kg), GR 127935 (10 and 20 mg/kg) and pindolol (4 and 8 mg/kg) did not shorten the immobility time of rats in that test. Interstingly, SB 216641 administered alone at a dose of 4 mg/kg produced a significant reduction of the immobility time in that test. A combinationt of paroxetine (20 mg/kg) and WAY 1000635 or pindolol failed to reveal a significant interaction; on the other hand, when paroxetine was given jointly with SB 216641 (2 mg/kg) or GR 127935 (10 and 20 mg/kg), that combination showed a significant antiimmobility action in the forced swimming test in rats. The active behaviors in that test did not reflect increased general activity because combined administration of both the...

    5/5

    Tytuł oryginału: Potencjalne przeciwdepresyjne i przeciwlękowe efekty ligandów glutamatergicznych receptorów metabotropowych
    Autorzy: Kłodzińska Aleksandra; Polska Akademia Nauk Instytut Farmakologii w Krakowie
    Źródło: - Kraków, IF PAN 2002, 16 s. : il., tab., bibliogr. 41 poz., 24 cm.
    Seria: Wykłady Monograficzne 62
    Sygnatura GBL: 660,913

    Hasła klasyfikacyjne GBL:
  • psychiatria i psychologia
  • farmacja
  • neurologia

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