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Selective progesterone receptor modulators (SPRMs): progesterone receptor action, mode of action on the endometrium and treatment options in gynecological therapies [PDF]
Expert Opinion on Therapeutic Targets, 2016 The progesterone receptor plays an essential role in uterine physiology and reproduction. Selective progesterone receptor modulators (SPRMs) have emerged as a valuable treatment option for hormone dependent conditions like uterine fibroids, which have a major impact on women's quality of life. SPRMs offer potential for longer term medical treatment and
Philippa T K Saunders +1 more
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Selective progesterone receptor modulators 3: use in oncology, endocrinology and psychiatry
Expert Opinion on Pharmacotherapy, 2008A number of synthetic steroids are capable of modulating progesterone receptors with a spectrum of activities ranging from pure antagonism to a mixture of agonism and antagonism. The best known of these are mifepristone (RU 486), asoprisnil (J 867), onapristone (ZK 98299), ulipristal (CDB 2914), Proellex() (CDB 4124), ORG 33628 and ORG 31710.Outside ...
BENAGIANO, Giuseppe +2 more
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Selective progesterone receptor modulators and their use within gynaecology
The Obstetrician & Gynaecologist, 2014Key content Mifepristone, a progesterone receptor antagonist, was initially discovered in the 1980s and has been licensed for use in medical termination since 1991. Subsequently, selective progesterone receptor modulators (SPRM), which have both agonist and antagonist properties, have been developed and have therapeutic advantages over alternative ...
Megan Murdoch, Mark Roberts
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Seminars in Reproductive Medicine, 2004
Asoprisnil is a novel selective progesterone receptor modulator that exhibits partial agonist and antagonist activities in animals and humans. It demonstrates a high degree of progesterone receptor specificity and tissue selectivity. Although asoprisnil at high doses exhibited some antiglucocorticoid activity in animal models, no antiglucocorticoid ...
Kristof, Chwalisz +5 more
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Asoprisnil is a novel selective progesterone receptor modulator that exhibits partial agonist and antagonist activities in animals and humans. It demonstrates a high degree of progesterone receptor specificity and tissue selectivity. Although asoprisnil at high doses exhibited some antiglucocorticoid activity in animal models, no antiglucocorticoid ...
Kristof, Chwalisz +5 more
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2013
2 (July-Dec 2013 ), 8, ไทยไภษัชยนิพนธ์ Thai Bulletin of Pharmaceutical Science (TBPS)
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2 (July-Dec 2013 ), 8, ไทยไภษัชยนิพนธ์ Thai Bulletin of Pharmaceutical Science (TBPS)
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Obstetrical & Gynecological Survey, 2002
Given the importance of progesterone in female reproductive health, it was inevitable that analogues of this molecule would be developed to treat a variety of gynecologic maladies. Such medications, termed progesterone antagonists, act to counteract the effect of progesterone.
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Given the importance of progesterone in female reproductive health, it was inevitable that analogues of this molecule would be developed to treat a variety of gynecologic maladies. Such medications, termed progesterone antagonists, act to counteract the effect of progesterone.
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Preclinical experience with two selective progesterone receptor modulators on breast and endometrium
Steroids, 2000Org 31710 and Org 33628 are two highly selective progesterone receptor modulators (PRMs) with respect to their anti-progestational and anti-glucocorticoid activity. The compounds have been studied both in vitro and in vivo. Org 33628 has approximately four times stronger anti-progestational activity in vitro than does Org 31710, and in rats it is about
H J, Kloosterboer +8 more
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Expert Review of Obstetrics & Gynecology, 2007
Progesterone receptor antagonists (PAs) and selective progesterone receptor modulators (SPRMs) are members of the progesterone receptor ligand family. The PA mifepristone is usually used as a single dose for short-term indications, such as pregnancy termination, cervical dilation, fetal death and emergency contraception.
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Progesterone receptor antagonists (PAs) and selective progesterone receptor modulators (SPRMs) are members of the progesterone receptor ligand family. The PA mifepristone is usually used as a single dose for short-term indications, such as pregnancy termination, cervical dilation, fetal death and emergency contraception.
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Development of the selective progesterone receptor modulator CDB-2914 for clinical indications
Steroids, 2003CDB-2914 (17 alpha-acetoxy-11 beta-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione) is a 19-norprogesterone derivative that acts as an antagonist in progesterone-responsive tissues. It binds to progesterone receptors A and B with high affinity. After oral dosing in humans, CDB-2914 serum levels peak at 60-90 min.
Diana L, Blithe +4 more
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[Selective progesterone receptor modulators and their therapeutical use].
Ceska gynekologie, 2015Currently developed selective progesterone receptor modulators (SPRMs) are steroid derived compounds with a bulky radical substitution at carbon 11. They interact with progesterone receptor and exert antagonistic or/and agonistic effects. Mifepristone was approved for pregnancy termination and ulipristal acetate as emergency contraception and ...
D, Driák, B, Sehnal, I, Svandová
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