Moxestrol: Difference between revisions

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'''Moxestrol''' is a synthetic, steroidal [[estrogen]] that was developed for medical use but is no longer marketed. It is an [[estrogen receptor]] agonist, and hence, an estrogen itself. Moxestrol is a derivative of [[estradiol]], the major endogenous estrogen in humans. It is specifically a derivative of [[ethinylestradiol]], which is estradiol with an ethynyl group at the C17α position.
== Moxestrol ==


==Chemistry==
[[File:Moxestrol_structure.svg|Structure of Moxestrol|thumb|right]]
Moxestrol, also known as 11β-methoxy-17α-ethynylestradiol, is a synthetic estrane steroid and a derivative of [[estradiol]]. It is more specifically a derivative of [[ethinylestradiol]] and is a member of the family of ethinylestradiol derivatives, which also includes [[mestranol]], [[quinestrol]], and [[chlorotrianisene]].


==Pharmacology==
'''Moxestrol''' is a synthetic [[estrogen]] that has been used in scientific research and has potential applications in [[hormone replacement therapy]]. It is a potent estrogenic compound and is a derivative of [[estradiol]], the primary female sex hormone. Moxestrol is known for its high affinity for estrogen receptors and its ability to mimic the effects of natural estrogens in the body.
As an [[estrogen]], moxestrol has similar effects in the body as other estrogens. It has strong estrogenic effects and weak antiestrogenic effects. Moxestrol binds to the [[estrogen receptor]] and activates it, resulting in estrogenic effects in the body. It has been found to have high affinity for the estrogen receptor and to be a full agonist of the receptor.


==History==
== Chemical Properties ==
Moxestrol was developed in the 1960s and was introduced for medical use by 1968. However, it is no longer marketed and hence is no longer available for use.


==Society and culture==
Moxestrol is a [[steroid]]al estrogen and is chemically related to estradiol. It is characterized by the presence of a 17α-ethynyl group, which enhances its oral bioavailability and potency. The chemical structure of moxestrol allows it to bind effectively to estrogen receptors, leading to its strong estrogenic activity.
Moxestrol was marketed under the brand name [[Ovestin]] among others. It was available as an oral tablet and was used in the treatment of menopausal symptoms, gynecological disorders, and certain hormone-sensitive cancers.


==See also==
== Mechanism of Action ==
* [[List of estrogens]]
 
* [[List of estrogen esters]]
Moxestrol exerts its effects by binding to [[estrogen receptors]] in target tissues. These receptors are part of the nuclear receptor family and, upon activation by moxestrol, they modulate the expression of specific genes involved in the regulation of reproductive and other physiological processes. The binding of moxestrol to estrogen receptors can lead to the activation or repression of gene transcription, depending on the tissue and the presence of co-regulatory proteins.
 
== Pharmacokinetics ==
 
Moxestrol is known for its high oral bioavailability, which is attributed to its chemical modifications. Once administered, it is rapidly absorbed and distributed throughout the body. Moxestrol is metabolized primarily in the liver and is excreted in the urine. Its half-life and duration of action are influenced by its strong binding affinity to estrogen receptors.
 
== Clinical Applications ==
 
While moxestrol has been primarily used in research settings, it has potential applications in [[hormone replacement therapy]] for postmenopausal women. Its potent estrogenic effects can help alleviate symptoms associated with estrogen deficiency, such as [[hot flashes]], [[osteoporosis]], and [[vaginal atrophy]]. However, its use in clinical practice is limited due to the availability of other estrogenic compounds with more established safety profiles.
 
== Side Effects ==
 
As with other estrogens, moxestrol can cause a range of side effects, particularly when used in high doses or for extended periods. Common side effects include [[nausea]], [[breast tenderness]], and [[headaches]]. Long-term use of potent estrogens like moxestrol may increase the risk of [[endometrial hyperplasia]] and [[breast cancer]].
 
== Research Uses ==
 
Moxestrol is frequently used in scientific research to study the effects of estrogens on various biological systems. It serves as a tool to investigate the role of estrogen receptors in different tissues and to explore the molecular mechanisms underlying estrogenic signaling pathways.
 
[[File:Moxestrol_molecule_ball.png|Ball-and-stick model of Moxestrol|thumb|left]]
 
== Related Pages ==
 
* [[Estrogen]]
* [[Estradiol]]
* [[Hormone replacement therapy]]
* [[Estrogen receptor]]


{{Pharmaceuticals}}
{{Estrogens}}
[[Category:Estrogens]]
[[Category:Estrogens]]
[[Category:Abandoned drugs]]
[[Category:Synthetic hormones]]
[[Category:Synthetic estrogens]]
[[Category:Steroidal estrogens]]
[[Category:Estrane steroids]]
[[Category:Phenols]]
[[Category:Alcohols]]
[[Category:Ketones]]
[[Category:Human drug metabolites]]
{{medicine-stub}}
<gallery>
File:Moxestrol structure.svg|Moxestrol structure
File:Moxestrol molecule ball.png|Moxestrol molecule ball
</gallery>
<gallery>
File:Moxestrol structure.svg|Moxestrol structure
File:Moxestrol molecule ball.png|Moxestrol molecule ball
</gallery>

Latest revision as of 10:46, 23 March 2025

Moxestrol[edit]

Structure of Moxestrol

Moxestrol is a synthetic estrogen that has been used in scientific research and has potential applications in hormone replacement therapy. It is a potent estrogenic compound and is a derivative of estradiol, the primary female sex hormone. Moxestrol is known for its high affinity for estrogen receptors and its ability to mimic the effects of natural estrogens in the body.

Chemical Properties[edit]

Moxestrol is a steroidal estrogen and is chemically related to estradiol. It is characterized by the presence of a 17α-ethynyl group, which enhances its oral bioavailability and potency. The chemical structure of moxestrol allows it to bind effectively to estrogen receptors, leading to its strong estrogenic activity.

Mechanism of Action[edit]

Moxestrol exerts its effects by binding to estrogen receptors in target tissues. These receptors are part of the nuclear receptor family and, upon activation by moxestrol, they modulate the expression of specific genes involved in the regulation of reproductive and other physiological processes. The binding of moxestrol to estrogen receptors can lead to the activation or repression of gene transcription, depending on the tissue and the presence of co-regulatory proteins.

Pharmacokinetics[edit]

Moxestrol is known for its high oral bioavailability, which is attributed to its chemical modifications. Once administered, it is rapidly absorbed and distributed throughout the body. Moxestrol is metabolized primarily in the liver and is excreted in the urine. Its half-life and duration of action are influenced by its strong binding affinity to estrogen receptors.

Clinical Applications[edit]

While moxestrol has been primarily used in research settings, it has potential applications in hormone replacement therapy for postmenopausal women. Its potent estrogenic effects can help alleviate symptoms associated with estrogen deficiency, such as hot flashes, osteoporosis, and vaginal atrophy. However, its use in clinical practice is limited due to the availability of other estrogenic compounds with more established safety profiles.

Side Effects[edit]

As with other estrogens, moxestrol can cause a range of side effects, particularly when used in high doses or for extended periods. Common side effects include nausea, breast tenderness, and headaches. Long-term use of potent estrogens like moxestrol may increase the risk of endometrial hyperplasia and breast cancer.

Research Uses[edit]

Moxestrol is frequently used in scientific research to study the effects of estrogens on various biological systems. It serves as a tool to investigate the role of estrogen receptors in different tissues and to explore the molecular mechanisms underlying estrogenic signaling pathways.

Ball-and-stick model of Moxestrol

Related Pages[edit]