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Differences in the pregnancy terminating effectiveness of an lhrh analog by sub cutaneous vaginal rectal and nasal routes in rats






Endocrinologia Japonica 29(4): 415-422

Differences in the pregnancy terminating effectiveness of an lhrh analog by sub cutaneous vaginal rectal and nasal routes in rats

A long-acting analog of LHRH, des-Gly10-[D-Leu6]-LHRH-ethylamide (TAP-144), was administered once or twice on day 9 of pregnancy by s.c. vaginal, rectal and nasal routes to rats; the pregnancy-terminating effectiveness of these routes was determined on day 14. When rats were given a single dose of TAP-144, the ED50 value was 1.2 .mu.g/100 g body wt by the vaginal route, the effectiveness being 752 and 1221 times higher than those by the s.c. and rectal routes, respectively. Nasal administration was not effective in terminating pregnancy even at a high dose of 2000 .mu.g/100 g body wt. The addition of a surfactant (BL-9) did not increase the effectiveness by the rectal route. When TAP-144 was administered twice a day, the effectiveness was markedly increased by every route. The ED50 values were 0.32 .mu.g/100 g body wt per time by the s.c. route, which was comparable to that of the vaginal route, 14.2 .mu.g of the rectal route and 84.6 .mu.g of the nasal route. The addition of the surfactant increased the effectiveness 26 times by the nasal route but not by the rectal route. The pregnancy-terminating effect of TAP-144 was reversed by treatment with progesterone.


Accession: 005151486

PMID: 6818022



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