Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

  • Chemistry  (1)
  • Cytochrome P-450 3A  (1)
  • Organic Chemistry  (1)
  • enantiomers  (1)
  • propranolol  (1)
  • 1
    ISSN: 1432-0738
    Keywords: Key words FK506 ; Cyclosporin A ; Cytochrome P-450 3A ; Toxicity ; In vitro
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Tacrolimus (FK506) and cyclosporin A (CsA) are two potent immunosuppressants mainly metabolized by hepatic cytochrome P-450 3A (CYP3A) monooxygenase. The aim of this study was to compare the toxic effects of the two drugs on hepatocytes in primary culture as a function of their metabolism and to explore the variations of cytotoxicity when both drugs are associated. The cytotoxicity of FK506 and CsA, as expressed by their IC50 values, was of the same order but with a switch according to whether hepatocytes were induced or uninduced by dexamethasone, CsA being more toxic in its native form and FK506 through its metabolism. Similar results were obtained with the intracellular calcium content. When both drugs were associated at their IC50 values, the expected additive cytotoxic effect was not observed. Moreover, when small quantities of FK506 were added to CsA at its IC50, cell viability improved in the induced cultures. It is hypothesized that the interaction between the two drugs relies on a mechanism involving both competition of FK506 and CsA for CYP3A and of their immunophilin complexes for a common site on the calcineurin-calmodulin complex.
    Type of Medium: Electronic Resource
    Signatur Availability
    BibTip Others were also interested in ...
  • 2
    ISSN: 0899-0042
    Keywords: propranolol ; enantiomers ; immunogen synthesis ; selective antibody ; ELISA ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: A selective antibody to (S)-propranolol enantiomer was produced in rabbits by immunization with a new conjugate of N-aminopropylpropranolol-albumin. A hapten was first prepared by condensing (S)-propranolol or the racemate with 3-bromopropylphthalimide followed by hydrazinolysis, and the resulting compound conjugated to serum albumin by means of a glutaraldehyde- or carbodiimide-mediated reaction. Rabbits were immunized, and titres and specificity of antibodies were determined by ELISA. The antibodies obtained were tested with (S)-, (R)-, (R, S)-propranolol, and other structural analogs. Selective (S)-antibodies recognized (S)-propranolol 20 times more avidly than (R)-isomer while an antiserum against (R, S)-propranolol recognized both (S)- and (R)-isomers to about the same degree. ©1993 Wiley-Liss, Inc.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    Signatur Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...