Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

Zapytanie: MAUREL
Liczba odnalezionych rekordów: 1



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

Tytuł oryginału: Perazine as a potent inhibitor of human CYP1A2 but not CYP3A4.
Autorzy: Wójcikowski Jacek, Pichard-Garcia Lydiane, Maurel Patrick, Daniel Władysława A.
Źródło: Pol. J. Pharmacol. 2002: 54 (4) s.407-410, il., bibliogr. 10 poz.
Sygnatura GBL: 313,156

Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca kazuistyczna
  • komunikat
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • ludzie
  • dorośli = 65 r.ż.
  • płeć żeńska
  • in vitro

    Streszczenie angielskie: The effects of perazine on the activities of CYP1A2 and CYP3A4 in a primary culture of human hepatocytes of one patient were studied in vitro. The CYPs activities were assessed by measuring the rate of acetanilide 4-hydroxylation (CYP1A2) and cyclosporine A oxidation (CYP3A4) after treatment with TCDD (a CYP1A subfamily inducer) or rifampicin (mainly a CYP3A4 inducer). The amounts of the metabolities formed in hepatocytes were assayed in the extracellular medium using the HPLC method. TCDD and rifampicin induced the formation of 4-hydroxyacetanilide and cyclosporine A metabolities (monohydroxycyclosporine A, dihydroxycyclosporine A, N-desmethylcyclosporine A), respectively. The formation of 4-hydroxyacetanilide was strongly inhibited by three different concentrations of perazine (10, 25 and 50 ćM) reaching 8,3 and 2 p.c. of the control value, respectively. In the case of CYP3A4 activity, no such an effect of perazine was observed. Perazine showed only a week inhibition of the activity of cyclosporine A oxidase (to 96-86 p.c. of the control value). The obtained results suggest a strong inhibitory effect of perazine on human CYP1A2 activity with predicted Ki value similar to those of the known for CYP1A2 inhibitors, such as furafylline and fluvoxamine.

    stosując format: