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Altrenogest
Altrenogest, sold under the brand names Swinemate and Altren manufactured by Aurora Pharmaceutical and Regumate manufactured by Merck, is a progestin of the 19-nortestosterone group which is widely used in veterinary medicine to suppress or synchronize estrus in horses and pigs. It is available for veterinary use in both Europe (as Regumate) and the United States (as Matrix). Uses Veterinary Altrenogest is used in veterinary medicine. Pharmacology Pharmacodynamics An ''in vitro'' yeast structure–activity relationships bioassay study found that altrenogest was the most potent agonist of both the progesterone receptor (PR) and the androgen receptor (AR) of a large selection of other progestogens as well as anabolic–androgenic steroids (AAS). The observed potency of altrenogest even exceeded that of metribolone (methyltrienolone, R-1881), which was the second most potent compound. In the study, it showed an EC50 of 0.64 nM for the AR and 688% of the relative activational p ...
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Norethisterone
Norethisterone, also known as norethindrone and sold under the brand name Norlutin among others, is a progestin medication used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders. The medication is available in both low-dose and high-dose formulations and both alone and in combination with an estrogen (medication), estrogen. It is used oral administration, by mouth or, as norethisterone enanthate, by intramuscular injection, injection into muscle. Side effects of norethisterone include menstrual irregularities, headaches, nausea, breast tenderness, mood (psychology), mood changes, acne, hirsutism, increased hair growth. Norethisterone is a progestin, or a synthetic compound, synthetic progestogen (medication), progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak androgenic and estrogen (medication), estrogenic activity, mostly at high dosages, an ...
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Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ...
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Androgen Receptor
The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone, in the cytoplasm and then translocating into the Cell nucleus, nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding protein, DNA-binding transcription factor that Gene expression regulation, regulates gene expression; however, the androgen receptor has other functions as well. Androgen-regulated genes are critical for the development and maintenance of the male sexual phenotype. Function Effect on development In some cell types, testosterone interacts directly with androgen receptors, whereas, in others, testosterone is converted by 5-alpha reductase, 5-alpha-reductase to dihydrot ...
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Anabolic
Anabolism () is the set of metabolic pathways that construct macromolecules like DNA or RNA from smaller units. These reactions require energy, known also as an endergonic process. Anabolism is the building-up aspect of metabolism, whereas catabolism is the breaking-down aspect. Anabolism is usually synonymous with biosynthesis. Pathway Polymerization, an anabolic pathway used to build macromolecules such as nucleic acids, proteins, and polysaccharides, uses condensation reactions to join monomers. Macromolecules are created from smaller molecules using enzymes and cofactors. Energy source Anabolism is powered by catabolism, where large molecules are broken down into smaller parts and then used up in cellular respiration. Many anabolic processes are powered by the cleavage of adenosine triphosphate (ATP). Anabolism usually involves reduction and decreases entropy, making it unfavorable without energy input. The starting materials, called the precursor molecules, are joi ...
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Roussel Uclaf
Roussel Uclaf S.A. was a French pharmaceutical company and one of several predecessor companies of today's Sanofi. It was the second largest French pharmaceutical company before it was acquired by Hoechst AG of Frankfurt, Germany in 1997, with pharmaceutical operations combined into the Hoechst Marion Roussel (HMR) division in the United States. Roussel Uclaf's agrochemical operations had been transferred to Hoechst Schering AgrEvo GmbH in 1994. HMR subsequently merged in 1999 with Rhône-Poulenc to form Aventis, which then merged in 2004 with Sanofi-Synthélabo to form Sanofi-Aventis, which was since renamed Sanofi. Hoechst Schering AgrEvo merged in 1999 with Rhône-Poulenc's agrochemical division to form Aventis CropScience, which was acquired by Bayer AG in 2002 and combined with Bayer's agrochemical division to form Bayer CropScience. RU-486 In April 1980, as part of a formal research project at Roussel-Uclaf for the development of glucocorticoid receptor antagonists ...
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Pharmaceutical Company
The pharmaceutical industry is a Medicine, medical industry that discovers, develops, produces, and markets pharmaceutical goods such as medications and medical devices. Medications are then administered to (or Self-medicate, self-administered by) patients for curing or preventing disease or for alleviating symptoms of illness or injury. List of pharmaceutical companies, Pharmaceutical companies may deal in Generic drug, generic drugs, branded drugs, or both, in different contexts. Generic materials are without the involvement of intellectual property, whereas branded materials are protected by Chemical patent, chemical patents. The industry's various subdivisions include distinct areas, such as manufacturing Biopharmaceutical, biologics and total synthesis. The industry is subject to a Legal drug trade, variety of laws and regulations that govern the patenting, efficacy testing, Drug safety, safety evaluation, and marketing of these drugs. The global pharmaceutical market produ ...
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Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is virtual screening, screened for structural analogs of a ...
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Norgestrel
Norgestrel, sold under the brand name Opill among others, is a progestin which is used in birth control pills. It is often combined with the estrogen ethinylestradiol, marketed as Ovral. It is also used in menopausal hormone therapy. It is taken by mouth. Side effects of norgestrel include menstrual irregularities, headaches, nausea, and breast tenderness. The most common side effects of the norgestrel include irregular bleeding, headaches, dizziness, nausea, increased appetite, abdominal pain, cramps, or bloating. Norgestrel is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak androgenic activity and no other important hormonal activity. Norgestrel was patented in 1961 and came into medical use, specifically in birth control pills, in 1966. It was subsequently introduced for use in menopausal hormone therapy as well. Norgestrel is sometimes referred to as a " ...
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Noretynodrel
Noretynodrel, or norethynodrel, sold under the brand name Enovid among others, is a progestin medication which was previously used in birth control pills and in the treatment of gynecological disorders but is now no longer marketed. It was available both alone and in combination with an estrogen. The medication is taken by mouth. Noretynodrel is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It is a relatively weak progestogen. The medication has weak estrogenic activity, no or only very weak androgenic activity, and no other important hormonal activity. It is a prodrug of various active metabolites in the body, such as norethisterone among others. Noretynodrel was introduced for medical use in 1957. It was specifically approved at this time in combination with mestranol for the treatment of gynecological and menstrual disorders. Subsequently, in 1960, this formulation was ...
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Progesterone (medication)
Progesterone (P4), sold under the brand name Prometrium among others, is a medication and naturally occurring steroid hormone. It is a progestogen (medication), progestogen and is used in combination with estrogen (medication), estrogens mainly in hormone replacement therapy, hormone therapy for menopause, menopausal symptoms and hypogonadism, low sex hormone levels in women. It is also used in women to support pregnancy and fertility and to treat gynecological disorders. Progesterone can be taken oral administration, by mouth, intravaginal administration, vaginally, and by injection (medicine), injection into muscle or fat, among other route of administration, routes. A progesterone vaginal ring and progesterone intrauterine device used for hormonal contraception, birth control also exist in some areas of the world. Progesterone is tolerability, well tolerated and often produces few or no side effects. However, a number of side effects are possible, for instance mood (psych ...
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Testosterone (medication)
Testosterone is a medication and naturally occurring testosterone, steroid hormone. It is used to treat male hypogonadism, gender dysphoria, and certain types of breast cancer. It may also be used to increase athletic ability in the form of doping in sport, doping. It is unclear if the use of testosterone for andropause, low levels due to aging is beneficial or harmful. Testosterone can be administered through several different routes, including Topical medication, topical gels or transdermal patch, patches, nasal sprays, subdermal implants, or Buccal administration, tablets dissolved inside the mouth. Testosterone therapy has been associated with improvements in Depression (mood), depressive symptoms (especially in Hypogonadism, hypogonadal men), increased exercise capacity and muscle strength in men with Heart failure, chronic heart failure, and Male contraceptive, male contraception effectiveness. Common side effects of testosterone include acne, swelling (medical), swel ...
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EC50
] Half maximal effective concentration (EC50) is a measure of the concentration of a drug, antibody or toxicant which induces a stimulus–response model, biological response halfway between the baseline and maximum after a specified exposure time. More simply, EC50 can be defined as the ''concentration required to obtain a 50% ..effect'' and may be also written as sub>50. It is commonly used as a measure of a drug's potency, although the use of EC50 is preferred over that of 'potency', which has been criticised for its vagueness. EC50 is a measure of concentration, expressed in molar units (M), where 1 M is equivalent to 1  mol/ L. The EC50 of a ''graded'' dose response curve therefore represents the concentration of a compound where 50% of its maximal effect is observed. The EC50 of a ''quantal'' dose response curve represents the concentration of a compound where 50% of the population exhibit a response, after a specified exposure duration. For clarification, ...
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