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praca opublikowana za granicą

tytuł obcojęzyczny

Wskaźnik treści:

psychiatria i psychologia

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.

2/6

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:

farmacja

neurologia

Typ dokumentu:

praca opublikowana za granicą

tytuł obcojęzyczny

Wskaźnik treści:

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.

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Tytuł oryginału: Pharmacological analysis of the hypothermic effects of NAN-190 and its analogs, postsynaptic 5-HT1A receptor antagonists, in mice.
Autorzy: Wesołowska Anna, Borycz Jolanta, Paluchowska Maria H., Chojnacka-Wójcik Ewa
Źródło: Pol. J. Pharmacol. 2002: 54 (4) s.391-399, il., tab., bibliogr. 40 poz.
Sygnatura GBL: 313,156

Hasła klasyfikacyjne GBL:

farmacja

Typ dokumentu:

tytuł obcojęzyczny

Wskaźnik treści:

myszy

płeć męska

Streszczenie angielskie: In this study, we examined the role of 5-hydroxytryptamine (5-HT)1A and ŕ1-adrenergic receptors in the hypothermia induced by 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]-piperazine (NAN-190) and its analogs, 1-(2-methoxyphenyl)-4-[(4-succinimido)butyl]piperazine (MM77) and trans-1(2-methoxyphenyl)-4-[4-(2-phthalimido)cyclohexyl]piperazine (MP245), which - like NAN-190 - showed a high affinity for 5-HT1A and ŕ1-adrenoceptors. Administration of NAN-190 (a partial agonist of presynaptic and an antagonist of postsynaptic 5-HT1A receptors and ŕ1-adrenoceptors), MM77 and MP245 (antagonists of postsynaptic 5-HT1A receptors), as well as 8-OH-DPAT (a 5-HT1A agonist) and prazosin (an ŕ1-adrenoceptor antagonist) induced a dose-dependent hypothermia in mice. The silent antagonist of 5-HT1A receptors, WAY 100635, which abolished the hypothermic effect of 8-OH-DPAT, inhibited the hypothermia induced by NAN-190 administered at a dose of 1 mg/kg (but not 2 mg/kg) and by MP245 (0.5 and 1 mg/kg), but failed to change the MM77 (1 and 4 mg/kg)-induced decrease in body temperature in mice. The ŕ1-adrenoceptor agonist St587, which reduced the hypothermic effect of prazosin, inhibited the decrease in body temperature evoked by NAN-190 at the higher dose and by MP245at both the doses used, but did not affect the MM77-induced hypothermia in mice. The obtained results suggest that the hypothermia in mice induced by NAN-190 and its constrained analog MP245 is connected with stimulation of 5-HT1A receptors and with blockade of ŕ1-adrenoceptors, participation of these receptors not being equivalent, though. The origin of the hypothermia evoked by MM77 is still unknown.

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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:

tytuł obcojęzyczny

Wskaźnik treści:

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...

5/6

Tytuł oryginału: Novel N-{omega-[4-(2-methoxyphenyl)piperazin-1-yl]-ethyl}pyrid-2(1H)-ones with diversified 5-HT 1A receptor activity.
Autorzy: Paluchowska Maria H., Bugno Ryszard, Charakchieva-Minol Sijka, Wesołowska Anna, Chojnacka-Wójcik Ewa
Źródło: Pol. J. Pharmacol. 2002: 54 (6) s.641-646, il., tab., bibliogr. 22 poz.
Sygnatura GBL: 313,156

Hasła klasyfikacyjne GBL:

farmacja

Typ dokumentu:

tytuł obcojęzyczny

Wskaźnik treści:

psychiatria i psychologia

płeć męska

in vitro

Streszczenie angielskie: Novel omega-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl derivatives 1-6 containing 4-, 5- and/or 6-arylsubstituted pyrid-2(1H)-one moiety were synthesized. All the new compounds were examined in vitro to assess their 5-HT 1A and 5-HT 2A receptor affinities. Compounds 3 and 4 with a 5- or a 6-phenylsubstituted pyridone ring demonstrated high 5-HT 1A receptor affinity (Ki=17 and 38 nM, respectively) and were tested in behavioral functional models. Derivative 3 can be regarded as a weak 5-HT 1A postsynaptic antagoninist, whereas 4 showed features of a weak partial agonist of 5-HT 1A receptors (an agonist of pre- and an antagonist of posstynaptic ones). Binding affinities and in vivo results were discussed in comparison with those for the previously described tetramethylene analogs. The obtained results showed that the shortening of the aliphatic chain to two methylene groups exposed the intrinsic activity of the ligand 4 and 5-HT 1A receptor sites.

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Tytuł oryginału: Anxiolytic- and antidepressant-like effects of group III metabotropic glutamate agonist (1S,3R,4S)-1-aminocyclopentane-1,3,4-tricarboxylic acid (ACPT-I) in rats.
Autorzy: Tatarczyńska Ewa, Pałucha Agnieszka, Szewczyk Bernadeta, Chojnacka-Wójcik Ewa, Wierońska Joanna, Pilc Andrzej
Źródło: Pol. J. Pharmacol. 2002: 54 (6) s.707-710, tab., bibliogr. 14 poz.
Sygnatura GBL: 313,156

Hasła klasyfikacyjne GBL:

farmacja

Typ dokumentu:

komunikat

tytuł obcojęzyczny

Wskaźnik treści: