Comparison of luteolytic potencies of aminoglutethimide enantiomers in the rabbit and rat.
The luteolytic potency of D- and L-aminoglutethimide (D- and L-AG) was compared in in vivo assays in the rat and rabbit. By assay of plasma progesterone depletion in the rabbit, the potency of L-AG relative to D-AG was 0.21. By the plasma procedure in the rat, the relative potencies of L-AG and of the racemic mixture to D-AG were 0.04 and 0.37, respectively. By the ovarian progesterone depletion method, the L-form had very little activity and the DL-mixture was half as active as the D-isomer. Thus, in both species, almost all of the activity of the racemic mixture results from the content of D-AG. Interpretation of paradoxical data implies that in the rat, L-AG may inhibit liver degradation of progesterone at levels which do not modify secretion from the corpus luteum.
D000616:Aminoglutethimide / Q000494:pharmacology*; D000818:Animals; D001681:Biological Assay; D003338:Corpus Luteum / Q000187:drug effects*; D005260:Female; D008186:Luteolytic Agents / Q000494:pharmacology*; D010053:Ovary / Q000187:drug effects / Q000378:metabolism; D011374:Progesterone / Q000097:blood; D011817:Rabbits; D051381:Rats; D013237:Stereoisomerism
D008186:Luteolytic Agents; D000616:Aminoglutethimide; D011374:Progesterone