Vree T B, Riemens L, Koopman-Kimenai P M
Department of Clinical Pharmacy, Saint Radboud Hospital, University of Nijmegen, The Netherlands.
J Chromatogr. 1988 Jul 15;428(2):311-9.
The capacity factors of 26 xanthine derivatives were measured by reversed-phase high-performance liquid chromatography. N-Methyl substitution increased the capacity factor and the related lipid solubility. The descending order of the increase in capacity factor by the N-methyl group is: N-1 methyl greater than N-3 methyl greater than N-7 methyl greater than N-9 methyl. C-8 hydroxylation reduces the capacity factor in the xanthines. The reduction factor is 3.34 in xanthines with N-3 methyl substitution, 2.41 in xanthines with N-1 and/or N-7 methyl substitution and 1.68 in xanthines with N-9 methyl substitution.
采用反相高效液相色谱法测定了26种黄嘌呤衍生物的容量因子。N-甲基取代增加了容量因子以及相关的脂溶性。N-甲基基团使容量因子增加的降序排列为:N-1甲基>N-3甲基>N-7甲基>N-9甲基。C-8羟基化降低了黄嘌呤的容量因子。在具有N-3甲基取代的黄嘌呤中,降低因子为3.34;在具有N-1和/或N-7甲基取代的黄嘌呤中,降低因子为2.41;在具有N-9甲基取代的黄嘌呤中,降低因子为1.68。