[The effect of ovarian steroids on the pharmacokinetics of Terguride in the rat uterus].
The incorporation of 3H-17-beta oestradiol (3H-E2) and 3H-Tergurid (3H-Te) in the uteri of sexually immature rats was monitored for 16 hours following the treatment of the animals with Tergurid, a semisynthetic ergot alkaloid [chemically acid N-(D-6-methyl-8-isoergolin-I-yl)--N',N'-diethylurea maleate; VUFB-6638]. The differences in the incorporation of 3H-Te in relation to the presence of ovarial steroids (E2 and progesterone) were investigated for the same period of time in the adult ovariectomized rats. In all the time intervals under study, the average values of 3H-E2 activities in the uteri of juvenile rats treated with Tergurid were lower than in the controls. This decrease was statistically significant (P less than 0.05) eight hours after treatment. The time course of the incorporation of 3H-Te in the uteri of the experimental and control animals was about the same. The activities of incorporated 3H-Te in the uteri of adult rats treated with E2 were higher in all the intervals, the difference being statistically significant after two hours and 16 hours (P less than 0.05) and after four hours (P less than 0.01). Progesterone did not induce any significant differences in the incorporation of 3H-Te. These results suggest that the increased incorporation of Tergurid in the uteri of adult rats is due to a direct influence of E2. It has been demonstrated by trials on juvenile rats that Tergurid does not combine with oestrogenic receptors. As suggested by the decreased weights of the uteri of juvenile rats treated with Tergurid, the uterine cells are unable to react to exogenous administration of E2.(ABSTRACT TRUNCATED AT 250 WORDS)
D000367:Age Factors; D000818:Animals; D004873:Ergolines / Q000378:metabolism*; D004958:Estradiol / Q000494:pharmacology*; D005260:Female; D007700:Kinetics; D008090:Lisuride / Q000031:analogs & derivatives / Q000378:metabolism* / Q000494:pharmacology; D009929:Organ Size / Q000187:drug effects; D010052:Ovariectomy; D011374:Progesterone / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D014599:Uterus / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism*
D004873:Ergolines; C006208:dironyl; D011374:Progesterone; D004958:Estradiol; D008090:Lisuride
Vliv ovariálních steroidů na farmakokinetiku Terguridu v dĕloze krys.