| Autor: |
Yang, Richard, Hey, John A., Aslanian, Robert, Rizzo, Charles A. |
| Předmět: |
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| Zdroj: |
Pharmacology; Nov2002, Vol. 66 Issue 3, p128-135, 8p, 1 Diagram, 1 Chart, 2 Graphs |
| Abstrakt: |
Optical difference spectroscopy was used to identify and quantify human adrenal microsomal and mitochondrial cytochrome P450 enzyme interactions with the histamine H[sub 3] receptor antagonists thioperamide, clobenpropit and ciproxifan. Addition of these structurally diverse imidazole H[sub 3] receptor antagonists to cytochrome-P450-containing human adrenal microsomal and mitochondrial preparations resulted in concentration-dependent type II optical difference spectra. Respective spectral dissociation constants (K[sub S] ) for the drug interactions with human adrenal microsomal and mitochondrial cytochrome P450 were 1.5 and 1.6 μmol/l for thioperamide, 3.1 and 0.28 μmol/l for clobenpropit and 0.10 and 0.11 μmol/l for ciproxifan. The three compounds demonstrated a similar activity profile in cytochrome-P450-containing bovine adrenal microsomal and mitochondrial preparations. Findings indicate direct coordination of these imidazole-containing H[sub 3] receptor antagonists with the heme moiety of human adrenal cytochrome P450 isozymes.Copyright © 2002 S. Karger AG, Basel [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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