作者:W. T. Stolle、J. A. Easter、E. H. Chew、J. P. McGrath、J. R. Palmer、R. S. P. Hsi
DOI:10.1002/jlcr.2580341208
日期:1994.12
Tirilazad mesylate, 21-[4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl]-16α-methyl-pregna-1,4,9(11)-triene-3,20-dione monomethanesulfonate, is a potent lipid peroxidation inhibitor capable of suppressing progression of tissue damage caused by trauma or ischemia. Several isotopically labeled versions of the compound have been synthesized for conducting in vitro and in vivo metabolic transformations of this experimental drug. These include labeling with carbon-14 at the 16α-methyl group of the steroid portion of the molecule, or at the C-2 position of the pyrimidine ring; also with deuterium at the steroid 16α-methyl group, and/or with carbon-13 at C-2, C-4, and C-6, and with nitrogen-15 at N-1 and N-3 of the pyrimidine ring.
Tirilazad美克酸盐,21-[4-(2,6-二(1-吡咯烷基)-4-嘧啶基)-1-哌嗪基]-16α-甲基-孕-1,4,9(11)-三烯-3,20-二酮单甲烷磺酸盐,是一种有效的脂质过氧化抑制剂,能够抑制由创伤或缺血引起的组织损伤进展。已经合成了几种同位素标记的该化合物用于进行该实验药物的体外和体内代谢转化。这些标记包括在分子类固醇部分的16α-甲基基团处用碳-14标记,或在嘧啶环的C-2位置;也包括在类固醇的16α-甲基基团处用氘标记,以及在C-2、C-4和C-6处用碳-13标记,和在嘧啶环的N-1与N-3处用氮-15标记。