Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

Zapytanie: SYREK
Liczba odnalezionych rekordów: 1



Przejście do opcji zmiany formatu | Wyświetlenie wyników w wersji do druku
1/1

Tytuł oryginału: The contribution of cytochrome P-450 isoenzymes to the metabolism of phenothiazine neuroleptics.
Autorzy: Daniel W[ładysława] A., Syrek M., Haduch A.
Źródło: Eur. Neuropsychopharmacol. 2002: 12 (5) s.371-377, il., tab., bibliogr. s. 376-377
Sygnatura GBL: 313,361

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

    Wskaźnik treści:
  • zwierzęta
  • szczury
  • płeć męska
  • in vitro

    Streszczenie angielskie: The aim of the present study was to determine optimum conditions for studying promazine and perazine metabolism in rat liver microsomes and to investigate the influence of specific cytochrome P-450 inhibitors on 5-sulfoxidation and N-denmthylation of these neuroleptics. Based on the developed method, the metabolism of neuroleptics in liver microsomes was studied at linear dependence of product formation on time, and protein and substrate concentrations (incubation time: 10 min; concentration of microsomal proteins; promazine - 0,7 mg ml-1, perazine - 0,5 mg ml-1, substrate concentrations, promazine - 25,40 and 75 nmol ml-1, perazine- 20, 35, 50 mmol ml-1). A Dixon analysis of the metabolism of neuroleptics showed that quinine (a CYP2D1 inhibitor), metyrapone (a CYP2B1/B2 inhibitor) and ŕ-naphthoflavone (a CYP1A2/2 inhibitor) affected, whereas erythromycin (a CYP3A inhibitor) and sulfaphenazole (a CYP2C inhibitor) did not change the neuroleptic biotransformation. N-Demehtylation of promazine was competitively inhibited by quinine (K1=20 ćM) and metyrapone (K1=83 ćM), while of perazine - by quinine (K1=46.5 ćM), metyrapone (K1=46 ćM) and ŕ-napthoflavone (K1=78.8 ćM). 5-Sulfoxidation of promazine was inhibited only by quinine (K1=28.6 ćM), whereas that of perazine - by quinine (K1 = 10 ćM) and metyrapone (K1 = 96 ćM). The results obtained are compared with our previous findings of analogous experiments concerning thioridazine, and with the data on other phenothiazines and species. In summary, it is proposed that N-demethylation of the mentioned phenothiazine neuroleptics...

    stosując format: