ISSN:
1573-904X
Keywords:
partitioning
;
liposomes
;
n-octanol/buffer system
;
imidazolidines
;
correlation analysis
;
quantitative structure–activity relationship (QSAR)
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract The partitioning of 10 imidazolidines in various liposome/buffer systems (log K′ m) has been determined and compared to partitioning in the n-octanol/buffer system (log P′). The log K′ m, which was generally greater than the log P′, increased or decreased upon the addition of dicetylphosphate (DCP) or stearylamine (STA), respectively, to dimyristoylphosphatidylcholine (DMPC) liposomes. Quantitative correlations of α2-adrenergic potencies of imidazolidines have been made by regression analyses with log P′, log K′ m, binding affinity, and intrinsic activity. Both central and peripheral potencies correlated with log K′ m but not with log P′ Multiple regressions yielded improved predictable quantification of these potencies. Thus, the liposomal membrane system shows certain advantages over the n-octanol/buffer system for the prediction of biological activities of the imidazolidines.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1018977731352
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