Bibliothek

feed icon rss

Ihre E-Mail wurde erfolgreich gesendet. Bitte prüfen Sie Ihren Maileingang.

Leider ist ein Fehler beim E-Mail-Versand aufgetreten. Bitte versuchen Sie es erneut.

Vorgang fortführen?

Exportieren
Filter
  • 1995-1999  (3)
  • 1
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 354 (1996), S. 320-326 
    ISSN: 1432-1912
    Schlagwort(e): Rat liver ; Transport of organic cations ; OCT1 ; Type I hepatic transport of cationic drugs ; 1-Methyl-4-phenylpyridinium
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The kidneys and the liver are the principal organs for the inactivation of circulating organic cations. Recently, an organic cation transporter (OCT1) has been cloned from rat kidney. In order to answer the question whether OCT1 is involved also in hepatic uptake of organic cations, the pharmacological characteristics of organic cation transport in hepatocytes were compared to the characteristics of transiently expressed OCT1. Primary cultures of rat hepatocytes avidly accumulated the small organic cation 3H-1-methyl-4-phenylpyridinium (3H-MPP+). At equilibrium, the hepatocytes accumulated 3H-MPP+ 56-fold. Initial rates of specific 3H-MPP+ transport in hepatocytes were saturable. The half-saturating concentration was 13 μmol/l. 3H-MPP+ transport was sensitive to quinine (Ki = 0.79 μmol/l) and cyanine863 (Ki = 0.097 µmol/l). Quinine and cyanine863 are known inhibitors of type I hepatic transport of cationic drugs and of renal excretion of organic cations, respectively. To compare the functional characteristics of 3H-MPP+ transport in hepatocytes with those of OCT1, OCT1 has been heterologously expressed and characterized in a mammalian cell line (293 cells). Initial rates of 3H-MPP+ transport were saturable, the Km being 13 μmol/l. The rank order of inhibitory potencies of various inhibitors was almost identical in hepatocytes and 293 cells transiently transfected with OCT1. There was a positive correlation between the Ki's for the inhibition of 3H-MPP+ transport in isolated hepatocytes and transfected 293 cells (r = 0.85; P〈0.01; n = 8). The results indicate that OCT1 is functionally expressed not only in the kidney but also in hepatocytes where it is responsible for the transport of small organic cations which, in the past, have been classified as type I substrates.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 2
    ISSN: 1432-1130
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie
    Notizen: Abstract The National Institute of Standards and Technology (NIST) has developed several Standard Reference Materials (SRMs) based on human serum. NIST SRM 909b, Human Serum, is a lyophilized human serum material with concentrations for seven organic and six inorganic analytes at two levels certified solely by definitive methods (DMs). This material provides the vehicle by which high precision, high accuracy measurements made with DMs at NIST can be transferred through the measurement hierarchy to other laboratories. Isotope dilution gas chromatographic-mass spectrometric (GC-IDMS) methods were applied to measure cholesterol, creatinine, glucose, urea, uric acid, triglycerides, and total glycerides. Thermal ionization isotope dilution mass spectrometry (TI-IDMS) was used for determination of lithium, magnesium, potassium, calcium, and chloride. In addition, chloride was determined by coulometry, providing a comparison between two DMs. Sodium, which lacks a stable isotope that would permit isotope dilution mass spectrometric (IDMS) measurement, was determined by gravimetry. SRM 909b includes certified values for total glycerides and triglycerides, which were not certified in the previous lot of this material (SRM 909a). Improvement in uniformity of vial fill weight in the production of SRM 909b resulted in smaller certified uncertainties over previous freeze-dried serum SRMs. Uncertainties at the 99% level of confidence for relative expanded uncertainty (%) for certification of the organic analytes on a mmol/L/g basis ranged from 0.44% for urea (level II) to 5.04% for glucose (level II). (In-house studies have shown glucose to be a relatively unstable analyte in similar lyophilized serum materials, degrading at about 1% per year.) Relative expanded uncertainties (99% C.I.) for certification of inorganic analytes on a mmol/L/g basis ranged from 0.25% for chloride (level I) to 0.49% for magnesium (level II).
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 3
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 354 (1996), S. 320-326 
    ISSN: 1432-1912
    Schlagwort(e): Key words Rat liver ; Transport of organic cations ; OCT1 ; Type I hepatic transport of cationic drugs ; 1-Methyl-4-phenylpyridinium
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The kidneys and the liver are the principal organs for the inactivation of circulating organic cations. Recently, an organic cation transporter (OCT1) has been cloned from rat kidney. In order to answer the question whether OCT1 is involved also in hepatic uptake of organic cations, the pharmacological characteristics of organic cation transport in hepatocytes were compared to the characteristics of transiently expressed OCT1. Primary cultures of rat hepatocytes avidly accumulated the small organic cation 3H-1-methyl-4-phenylpyridinium (3H-MPP+). At equilibrium, the hepatocytes accumulated 3H-MPP+ 56-fold. Initial rates of specific 3H-MPP+ transport in hepatocytes were saturable. The half-saturating concentration was 13 μmol/l. 3H-MPP+ transport was sensitive to quinine (Ki = 0.79 μmol/l) and cyanine863 (Ki = 0.097 μmol/l). Quinine and cyanine863 are known inhibitors of type I hepatic transport of cationic drugs and of renal excretion of organic cations, respectively. To compare the functional characteristics of 3H-MPP+ transport in hepatocytes with those of OCT1, OCT1 has been heterologously expressed and characterized in a mammalian cell line (293 cells). Initial rates of 3H-MPP+ transport were saturable, the Km being 13 μmol/l. The rank order of inhibitory potencies of various inhibitors was almost identical in hepatocytes and 293 cells transiently transfected with OCT1. There was a positive correlation between the Ki’s for the inhibition of 3H-MPP+ transport in isolated hepatocytes and transfected 293 cells (r = 0.85; P〈0.01; n = 8). The results indicate that OCT1 is functionally expressed not only in the kidney but also in hepatocytes where it is responsible for the transport of small organic cations which, in the past, have been classified as type I substrates.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
Schließen ⊗
Diese Webseite nutzt Cookies und das Analyse-Tool Matomo. Weitere Informationen finden Sie hier...