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Progesterone Synthesis Inhibitor
A progesterone synthesis inhibitor, or progestogen synthesis inhibitor, is a type of drug which inhibits the enzymatic synthesis of progesterone. They include: * Cholesterol side-chain cleavage enzyme inhibitors (P450SCC/CYP11A1 inhibitors): inhibit the synthesis of pregnenolone from cholesterol, thereby inhibiting the synthesis of most steroid hormones (which are derived from pregnenolone) including progesterone * 3β-Hydroxysteroid dehydrogenase inhibitors (3β-HSD inhibitors): inhibit the conversion of pregnenolone into progesterone Inhibitors of cholesterol synthesis can also reduce progesterone production by inhibiting cholesterol production. Progesterone synthesis inhibitors have been researched for medical applications including use as contraceptives, abortifacients, and oxytocics, though ultimately they have never been marketed for such indications. Examples of such agents include the 3β-HSD inhibitors azastene (WIN-17625) and epostane (WIN-32729). Since progesterone ...
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Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. Reve ...
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Oxytocic
A uterotonic, also known as ecbolic, are pharmacological agents used to induce contraction or greater tonicity of the uterus. Uterotonics are used both to induce labor and to reduce postpartum hemorrhage. Labor induction in the third trimester of pregnancy may be required due to medical necessity, or may be desired for social reasons. Generally, labor induction is indicated when the risk of carrying the pregnancy outweighs the risk of delivering. These reason include, but are not limited to, pregnancies that are prolonged, prelabor rupture of the fetal membranes, and concerns about the health and safety of the mother and/or child. There are multiple techniques available to stimulate uterine contractions including mechanical, pharmacological, and alternative medicine methods to initiate contractions prior to spontaneous onset of labor. Postpartum hemorrhage, also known as PPH, is defined as a loss of 500 mL or greater of blood within 24 hours after giving birth. It is one of the lea ...
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Androgen Synthesis Inhibitor
An androgen synthesis inhibitor is a type of drug which inhibits the enzymatic synthesis of androgens, such as testosterone and dihydrotestosterone (DHT). They include: * CYP17A1 inhibitors (17α-hydroxylase/17,20-lyase inhibitors): inhibit the synthesis of androgens from pregnanes * 3β-Hydroxysteroid dehydrogenase inhibitors (3β-HSD inhibitors): inhibit the conversion of weaker androgens such as dehydroepiandrosterone (DHEA) and androstenediol into more potent androgens like and testosterone * Cholesterol side-chain cleavage enzyme inhibitors (P450SCC/CYP11A1 inhibitors): inhibit the synthesis of pregnenolone from cholesterol, thereby inhibiting the synthesis of most steroid hormones (which are derived from pregnenolone) including androgens * 17β-Hydroxysteroid dehydrogenase inhibitors (17β-HSD inhibitors): inhibit the interconversion of androgens, including the synthesis of testosterone from the less-potent androstenedione * 5α-Reductase inhibitors (5α-RIs; SRD5A inhibitor ...
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Neurosteroid
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. The term ''neurosteroid'' was coined by the French physiologist Étienne-Émile Baulieu and refers to steroids synthesized in the brain. The term, ''neuroactive steroid'' refers to steroids that can be synthesized in the brain, or are synthesized by an endocrine gland, that then reach the brain through the bloodstream and have effects on brain function. The term neuroactive steroids was first coined in 1992 by Steven Paul and Robert Purdy. In addition to their actions on neuronal membrane receptors, some of these steroids may also exert effects on gene expression via nuclear steroid hormone receptors. Neurosteroids have a wide range of potential clinical applications from sedation to treatment of epilepsy and traumatic brain injury. Ganaxolone, a synthetic analog of the end ...
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Mineralocorticoid
Mineralocorticoids are a class of corticosteroids, which in turn are a class of steroid hormones. Mineralocorticoids are produced in the adrenal cortex and influence salt and water balances (electrolyte balance and fluid balance). The primary mineralocorticoid is aldosterone. Physiology The name mineralocorticoid derives from early observations that these hormones were involved in the retention of sodium, a mineral. The primary endogenous mineralocorticoid is aldosterone, although a number of other endogenous hormones (including progesterone and deoxycorticosterone) have mineralocorticoid function. Aldosterone acts on the kidneys to provide active reabsorption of sodium and an associated passive reabsorption of water, as well as the active secretion of potassium in the principal cells of the cortical collecting tubule and active secretion of protons via proton ATPases in the lumenal membrane of the intercalated cells of the collecting tubule. This in turn results in an increase ...
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Glucocorticoid
Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The name "glucocorticoid" is a portmanteau (glucose + cortex + steroid) and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure below). Glucocorticoids are part of the feedback mechanism in the immune system, which reduces certain aspects of immune function, such as inflammation. They are therefore used in medicine to treat diseases caused by an overactive immune system, such as allergies, asthma, autoimmune diseases, and sepsis. Glucocorticoids have many diverse (pleiotropic) effects, including potentially harmful side effects. They also interfere with some of the abnormal mechanisms in cancer cells, so they are used in high doses to ...
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Estrogen
Estrogen or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal activity: estrone (E1), estradiol (E2), and estriol (E3). Estradiol, an estrane, is the most potent and prevalent. Another estrogen called estetrol (E4) is produced only during pregnancy. Estrogens are synthesized in all vertebrates and some insects. Their presence in both vertebrates and insects suggests that estrogenic sex hormones have an ancient evolutionary history. Quantitatively, estrogens circulate at lower levels than androgens in both men and women. While estrogen levels are significantly lower in males than in females, estrogens nevertheless have important physiological roles in males. Like all steroid hormones, estrogens readily diffuse across the cell membrane. Once inside the cell, they bind to and activate estrogen receptors (E ...
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Androgen
An androgen (from Greek ''andr-'', the stem of the word meaning "man") is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This includes the embryological development of the primary male sex organs, and the development of male secondary sex characteristics at puberty. Androgens are synthesized in the testes, the ovaries, and the adrenal glands. Androgens increase in both males and females during puberty. The major androgen in males is testosterone. Dihydrotestosterone (DHT) and androstenedione are of equal importance in male development. DHT ''in utero'' causes differentiation of the penis, scrotum and prostate. In adulthood, DHT contributes to balding, prostate growth, and sebaceous gland activity. Although androgens are commonly thought of only as male sex hormones, females also have them, but at lower levels: they function in libido and sexual arousal. Also, an ...
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Precursor (biochemistry)
In chemistry, a precursor is a compound that participates in a chemical reaction that produces another compound. In biochemistry, the term "precursor" often refers more specifically to a chemical compound preceding another in a metabolic pathway, such as a protein precursor. Illicit drug precursors In 1988, the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances introduced detailed provisions and requirements relating the control of precursors used to produce drugs of abuse. In Europe the Regulation (EC) No. 273/2004 of the European Parliament and of the Council on drug precursors was adopted on 11 February 2004. (European law on drug precursors) Illicit explosives precursors On January 15, 2013, the Regulation (EU) No. 98/2013 of the European Parliament and of the Council on the marketing and use of explosives precursors was adopted. The Regulation harmonises rules across Europe on the making available, introduction, possession and u ...
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Epostane
Epostane (INN, USAN, BAN) (developmental code name WIN-32729) is an inhibitor of 3β-hydroxysteroid dehydrogenase (3β-HSD) that was developed as a contraceptive, abortifacient, and oxytocic drug but was never marketed. By inhibiting 3β-HSD, epostane blocks the biosynthesis of progesterone from pregnenolone (and also the conversion of dehydroepiandrosterone to androstenedione), thereby functioning as an antiprogestogen and terminating pregnancy. The drug was trialed and in a study was found to be slightly more effective at inducing abortion relative to mifepristone Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol to bring about a medical abortion during pregnancy and manage early miscarriage. This combination is 97% effective during the first 63 days of p .... See also * Nisterime * Trilostane References 3β-Hydroxysteroid dehydrogenase inhibitors Androstanes Antiprogestogens Nitriles Epoxides 1-Methylcyclopen ...
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Azastene
Azastene (INN, USAN) (developmental code name WIN-17625) is a steroidogenesis inhibitor described as a contraceptive, luteolytic, and abortifacient which was never marketed. It acts as a competitive inhibitor of 3β-hydroxysteroid dehydrogenase ( IC50 = 1 μM), and thereby inhibiting the formation of progesterone, corticosteroids, androgens, and estrogens. Due to inhibition of corticosteroid synthesis, azastene is immunosuppressive. Synthesis One synthesis of this compound involves initial alkylation of methyl testosterone by means of strong base and methyl iodide to afford the 4,4-dimethyl derivative. Formylation with alkoxide and methyl formate leads to the 2-hydroxymethyl derivative. Reaction of this last with hydroxylamine Hydroxylamine is an inorganic compound with the formula . The material is a white crystalline, hygroscopic compound.Greenwood and Earnshaw. ''Chemistry of the Elements.'' 2nd Edition. Reed Educational and Professional Publishing Ltd. pp. 431–43 ...
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Abortifacient
An abortifacient ("that which will cause a miscarriage" from Latin: ''abortus'' "miscarriage" and '' faciens'' "making") is a substance that induces abortion. This is a nonspecific term which may refer to any number of substances or medications, ranging from herbs to prescription medications. Common abortifacients used in performing medical abortions include mifepristone, which is typically used in conjunction with misoprostol in a two-step approach. Synthetic oxytocin, which is routinely used safely during term labor, is also commonly used to induce abortion in the second or third trimester. For thousands of years writers in many parts of the world have described and recommended herbal abortifacients to women who seek to terminate a pregnancy, although their use may carry risks to the health of the woman. Medications Because "abortifacient" is a broad term used to describe a substance's effects on pregnancy, there is a wide range of drugs that can be described as abortifac ...
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