Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

Zapytanie: ANTKIEWICZ-MICHALUK
Liczba odnalezionych rekordów: 5



Przejście do opcji zmiany formatu | Wyświetlenie wyników w wersji do druku

1/5

Tytuł oryginału: Role of noradrenergic system in the mechanism of action of endogenous neurotoxin 1,2,3,4-tetrahydroisoquinoline: biochemical and functional studies.
Autorzy: Michaluk Jerzy, Krygowska-Wajs Anna, Karolewicz Beata, Antkiewicz-Michaluk Lucyna
Źródło: Pol. J. Pharmacol. 2002: 54 (1) s.19-25, il., tab., bibliogr. 43 poz.
Sygnatura GBL: 313,156

Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • szczury

    Streszczenie angielskie: It is well recognized that 1,2,3,4-tetrahydroisoquinoline (TIQ) is a substance capable of inducing in animals a syndrome, regarded as an animal model of Parkinson's disease. This study was designed to evaluate the effect of the endogenous neruotoxin TIQ on the brain noradrenaline (NA) metabolism in mice and on an arterial blood pressure in rats. It was shown for the first time that TIQ significantly increased NA metabolism, induced NA release and raised the level of its final metabolite, 3-methoxy-4-hydroxyphenylglycol (MHPG), in mouse brain. The comparative biochemical studies using specific agonist (clonidine) and antagonist (yohimbine) of ŕ2-adrenergic receptors ligands have shown that observed biochemical effects were similar to those produced by ŕ2-adrenergic antagonist, yohimbine. In functional studies, the systolic and diastolic blood pressure was measured using a non-invasive blood pressure transducer. Both acute and multiple treatment with TIQ produced a strong hypotensive effect, haveing decreased both systolic and diastoic blood pressure in rats. Development of tolerance to the hypotensive effect was observed after multiple treatment with TIQ. The data coming from these experimental studies apparently suggest an important role of the noradrenergic system in the mechanism of action of endogenous compounds from TIQ group. The results may also support the hypothesis assuming a causal relationship between noradrenergic dennervation, activity of the nigrostriatal dopamine system, and some clinical manifestation of Parkinson's disease.


    2/5

    Tytuł oryginału: Synthesis, antiarrhythmic, and antihypertensive effect of novel 1-substituted pyrrolidin-2-one and pyrrolidine derivatives with adrenolytic activity.
    Autorzy: Malawska Barbara, Kulig Katarzyna, Filipek Barbara, Sapa Jacek, Maciąg Dorota, Zygmunt Małgorzata, Antkiewicz-Michaluk Lucyna
    Źródło: Eur. J. Med. Chem. 2002: 37 (3) s.183-195, il., tab., bibliogr. 23 poz.
    Sygnatura GBL: 312,629

    Hasła klasyfikacyjne GBL:
  • farmacja

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

    Wskaźnik treści:
  • zwierzęta
  • szczury

    Streszczenie angielskie: A series of 1-substituted pyrrolidin-2-one and pyrrolidine derivatives were syntheised and tested for electrocardiographic, antiarrhythmic, and antihypertensive activity as well as for ŕ1- and ŕ2-adrenoceptors binding affinities. Among the newly synthesised derivatives several compounds with 3-(4-arylpiperazin-1-yl)propyl moiety displayed strong antiarrhythmic (7a-12a) and antihypertensive (7a-11a) activities. Compound 11a, 1-[2-acetoxy-3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one, was the most potent in this series. The pharmacological results and binding studies that their antiarrhythmic and hypotensive effects may be related to their ŕ-adrenolytic properties, and that those properties depend on the presence of the 1-phenylpiperazine moiety with a methoxy- or chloro- substituent in the ortho position in the phenyl ring.


    3/5

    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.


    4/5

    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...


    5/5

    Tytuł oryginału: Endogenous risk factors in Parkinson's disease: dopamine and tetrahydroisoquinolines.
    Autorzy: Antkiewicz-Michaluk Lucyna
    Źródło: Pol. J. Pharmacol. 2002: 54 (6) s.567-572, bibliogr. 20 poz.
    Sygnatura GBL: 313,156

    Hasła klasyfikacyjne GBL:
  • neurologia

    Typ dokumentu:
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • ludzie
  • zwierzęta
  • in vitro

    Streszczenie angielskie: The cause of chronic nigral cell death in Parkinson's disease (PD) and the underlying mechanisms remain elusive. The selective action of exogenous and endogenous neurotoxic substances can provide partial explanation of these processes. 1-Methyl-4phenyl-1,2,3,6-tetrahydropyridine (MPTP) is an exogenous neurotoxin producing parkinsonism in humans, monkeys and various animals as the result of MAO B-catalyzed conversion of it to the 1-methyl-4-phenyl-pyridinum ion (MPP+), which selectively kills the nigrostriatal dopaminergic neurons. On the other hand, various isoquinoline derivatives were found in the brain, and they considered to be the endogenous neurotoxins with neurochemical properties similar to those of MPTP, which cause PD. Among them, 1,2,3,4-tetrahydroisoquinoline (TIQ), 1-benzyl-TIQ, and 1-methyl-5,6-dihydroxy-TIQ (salsolinol) have the most potent neurotoxic action. Since PD is a slowly progressing neurodegenerative disease, it has been suggested that is could be connected with excitotoxicity and apoptosis. Therapeutic strategies should focused on the search for the drugs exhibiting antiapoptotic potential such as: antioxidants, MAO B inhibitors, dopaminergic drugs and free radical scavengers.

    stosując format: