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Abstract
Anordiol (2α,17α-diethynyl-A-nor-5α-androstane-2β,17β-diol) has been variously characterized
as an estrogen and as an antiestrogen. To more completely understand the pharmacological
properties of this contraceptive steroid, simultaneous responses were studied in uterine,
vaginal, and hepatic tissues. Rats received 4 daily sc injections with either anordiol,
clomiphene citrate (CC), or the vehicle alone (C+) starting on the first day of pseudopregnancy.
Uteri were traumatized on day 4 of pseudopregnancy, and rats were sacrificed 5 days
later. A pseudopregnant group without uterine trauma served as a negative control
(C-). Mean uterine weights per animal and cytosolic estrogen (EcR) and progesterone (PcR) receptor activities per g of DNA were all 5- to 7-fold greater in the C_ group
than in the other groups (all p<0.05). However, anordiol and CC suppressed uterine
weight without suppressing the stromal proliferative response; the DNA content of
the uteri of anordiol- and CC-treated rats was similar to that of C+ rats. Vaginal
tissue exhibited estrogenic responses to anordiol and CC with an increase in epithelial
stratification compared to the C+ and C− groups even though no difference in levels
of ![Math Eq]()
of DNA were expressed 5 days after the last antiestrogen dose. Binding affinities
and serum E2 and progesterone (P) concentrations were not statistically different among the groups.
In conclusion, anordiol produced responses in the uterus and vagina of the pseudopregnant
rat which were indistinguishable from those of CC, and, therefore, we conclude that
anordiol acts on these tissues as an antiestrogen.
of DNA were expressed 5 days after the last antiestrogen dose. Binding affinities
and serum E2 and progesterone (P) concentrations were not statistically different among the groups.
In conclusion, anordiol produced responses in the uterus and vagina of the pseudopregnant
rat which were indistinguishable from those of CC, and, therefore, we conclude that
anordiol acts on these tissues as an antiestrogen.To read this article in full you will need to make a payment
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Article info
Publication history
Accepted:
June 9,
1995
Received in revised form:
May 23,
1995
Received:
February 17,
1995
Identification
Copyright
© 1995 Published by Elsevier Inc.
