TY - JOUR
T1 - The rate of n-demethylation of n,n-dimethylanilines and n-methylanilines by rat-liver microsomes is related to their first ionization potential, their lipophilicity and to a steric bulk factor
AU - Galliani, G.
AU - Nali, M.
AU - Rindone, B.
AU - Tollari, S.
AU - Rocchetti, M.
AU - Salmona, M.
PY - 1986
Y1 - 1986
N2 - 1. The N-demethylation of a series of 12 p-substituted N,N-dimethylanilines, nine m-substituted N,N-dimethylanilines, one o-substituted N,N-dimethylaniline and four p-substituted N-methylanilines by rat-liver microsomes was studied. 2. For each compound, the apparent Vmax and Km values were determined and these parameters were correlated with their electronic, lipophilicity and steric bulk parameters reported in the literature. 3. Multi-parameter linear regression analysis showed a good correlation between log Vmax and these parameters for the p-substituted N,N-dimethylanilines. A lower degree of correlation was observed with the meta-substituted N,N-dimethylanilines.
AB - 1. The N-demethylation of a series of 12 p-substituted N,N-dimethylanilines, nine m-substituted N,N-dimethylanilines, one o-substituted N,N-dimethylaniline and four p-substituted N-methylanilines by rat-liver microsomes was studied. 2. For each compound, the apparent Vmax and Km values were determined and these parameters were correlated with their electronic, lipophilicity and steric bulk parameters reported in the literature. 3. Multi-parameter linear regression analysis showed a good correlation between log Vmax and these parameters for the p-substituted N,N-dimethylanilines. A lower degree of correlation was observed with the meta-substituted N,N-dimethylanilines.
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U2 - 10.3109/00498258609043539
DO - 10.3109/00498258609043539
M3 - Article
C2 - 3751107
AN - SCOPUS:0022615027
VL - 16
SP - 511
EP - 517
JO - Xenobiotica
JF - Xenobiotica
SN - 0049-8254
IS - 6
ER -