A comparative study of antiestrogen action: temporal patterns of antagonism of estrogen stimulated uterine growth and effects on estrogen receptor levels

E R Ferguson, B S Katzenellenbogen


Studies were undertaken to ascertain the effects of structural modification of two well-known antiestrogens (CI-628 and U-11,100A) on their estrogenic and antiestrogenic potencies and temporal patterns of effectiveness in the immature rat uterus. Changes in the chemical structures of these anti-estrogens produce compounds with markedly different affinities for the uterine estrogen receptor as measured in an in vitro cell-free cytosol system; binding affinities relative to estradiol (100%) are: CI-628, 4%; CI-680, 34%; 94X1127 (94X),222%; U-11,100A (UA), 6%; and U-23,469 (U-23), 0.1%. Although all five antiestrogens (daily injections of 50 microng over three days) appear equally effective in stimulating 72 h uterine weight when given alone, or in blocking the estradiol-stimulated weight increase when given with estradiol, marked differences in their potencies are noted when the effects of the compounds are monitored beyond 24 h following a single injection. The compounds CI-628, CI-680 and UA (50 microng sc in saline), which have a methylated hydroxyl group (at the site analogous to the steroid position 3), show a prolonged maintenance of elevated levels of nuclear receptor (beyond 48 h) and elevated uterine weight (until 72 h);...Continue Reading


Feb 1, 1995·Biulleten' eksperimental'noĭ biologii i meditsiny·P V SergeevSh N Abusalimov
Jan 1, 1979·Journal of Steroid Biochemistry·M Bichon, F Bayard
Oct 1, 1980·Journal of Steroid Biochemistry·M R WaltersJ H Clark
Jan 1, 1980·Journal of Steroid Biochemistry·J H Clark, S A McCormack
Dec 1, 1981·Journal of Steroid Biochemistry·B S KatzenellenbogenR L Eckert
Dec 1, 1981·Journal of Steroid Biochemistry·A E WakelingL R Hughes
Oct 1, 1988·Journal of Steroid Biochemistry·J F Miquel, J Gilbert
Oct 1, 1988·Journal of Steroid Biochemistry·T C SpelsbergR Singh
Oct 1, 1988·Journal of Steroid Biochemistry·J R PasqualiniN Giambiagi
Oct 1, 1988·Journal of Steroid Biochemistry·B W Ennis, W E Stumpf
Dec 1, 1977·Molecular and Cellular Endocrinology·P S RennieN Bruchovsky
Jul 1, 1978·Molecular and Cellular Endocrinology·F Capony, H Rochefort
Apr 1, 1981·Molecular and Cellular Endocrinology·L J BlackR L Goode
Jan 1, 1982·Molecular and Cellular Endocrinology·R L Sutherland, L C Murphy
Jan 1, 1992·Reproductive Toxicology·Y C ChouH A Bern
Mar 1, 1978·Journal of Toxicology and Environmental Health·V C JordanL Rowsby
Mar 1, 1983·Journal of Toxicology and Environmental Health·B W GabrielW A Anderson
Jun 1, 1995·Environmental Health Perspectives·B M MarkaverichR R Gregory
May 28, 1979·Biochemical and Biophysical Research Communications·H RochefortJ L Borgna
Nov 14, 1979·Biochemical and Biophysical Research Communications·R L Sutherland, M S Foo
Oct 1, 1979·Experimental Cell Research·E J PavlikB S Katzenellenbogen
May 1, 1986·European Journal of Cancer & Clinical Oncology·C L LimT K Das Gupta
Aug 1, 1981·European Journal of Cancer & Clinical Oncology·D P RoseV C Jordan
Oct 1, 1987·Journal of Bone and Mineral Research : the Official Journal of the American Society for Bone and Mineral Research·R T TurnerN H Bell
Jan 1, 1986·Annals of the New York Academy of Sciences·I T Landau
Dec 19, 1979·Biochimica Et Biophysica Acta·G Leclercq, J C Heuson

❮ Previous
Next ❯

Related Concepts

Trending Feeds


Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.


Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.


Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.