|
Onapristone
Onapristone () (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering in and described in 1984 but was never marketed. in in It is a silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone (which is a weak partial agonist of the receptor). in Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findings that liver function abnormalities developed in a majority patients. in Onapristone has been found to be effective in the treatment of breast cancer. As of 2016, onapristone h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiprogestogen
Antiprogestogens, or antiprogestins, also known as progesterone antagonists or progesterone blockers, are a class of drugs which prevent progestogens like progesterone from mediating their biological effects in the body. They act by blocking the progesterone receptor (PR) and/or inhibiting or suppressing progestogen production. Antiprogestogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiandrogens. Antiprogestogens are used as abortifacients and emergency contraceptives and in the treatment of uterine fibroids. They are also being studied in the treatment of breast cancer. Examples of antiprogestogens include the progesterone receptor weak partial agonist mifepristone, the selective progesterone receptor modulator (SPRM) ulipristal acetate, and the silent antagonist aglepristone. For medical abortion, mifepristone is combined with a prostaglandin (e.g., gemeprost). Several hundred antiprogestogens have been developed, but only ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiprogestogen
Antiprogestogens, or antiprogestins, also known as progesterone antagonists or progesterone blockers, are a class of drugs which prevent progestogens like progesterone from mediating their biological effects in the body. They act by blocking the progesterone receptor (PR) and/or inhibiting or suppressing progestogen production. Antiprogestogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiandrogens. Antiprogestogens are used as abortifacients and emergency contraceptives and in the treatment of uterine fibroids. They are also being studied in the treatment of breast cancer. Examples of antiprogestogens include the progesterone receptor weak partial agonist mifepristone, the selective progesterone receptor modulator (SPRM) ulipristal acetate, and the silent antagonist aglepristone. For medical abortion, mifepristone is combined with a prostaglandin (e.g., gemeprost). Several hundred antiprogestogens have been developed, but only ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progesterone Receptor
The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found inside cells. It is activated by the steroid hormone progesterone. In humans, PR is encoded by a single ''PGR'' gene residing on chromosome 11q22, it has two isoforms, PR-A and PR-B, that differ in their molecular weight. The PR-B is the positive regulator of the effects of progesterone, while PR-A serve to antagonize the effects of PR-B. Mechanism Progesterone is necessary to induce the progesterone receptors. When no binding hormone is present the carboxyl terminal inhibits transcription. Binding to a hormone induces a structural change that removes the inhibitory action. Progesterone antagonists prevent the structural reconfiguration. After progesterone binds to the receptor, restructuring with dimerization follows and the complex enters the nucleus and binds to DNA. There transcription takes place, resulting in formation of messenger RNA that is t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Liver
The liver is a major organ only found in vertebrates which performs many essential biological functions such as detoxification of the organism, and the synthesis of proteins and biochemicals necessary for digestion and growth. In humans, it is located in the right upper quadrant of the abdomen, below the diaphragm. Its other roles in metabolism include the regulation of glycogen storage, decomposition of red blood cells, and the production of hormones. The liver is an accessory digestive organ that produces bile, an alkaline fluid containing cholesterol and bile acids, which helps the breakdown of fat. The gallbladder, a small pouch that sits just under the liver, stores bile produced by the liver which is later moved to the small intestine to complete digestion. The liver's highly specialized tissue, consisting mostly of hepatocytes, regulates a wide variety of high-volume biochemical reactions, including the synthesis and breakdown of small and complex molecule ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimethylamino Compounds
Dimethylamine is an organic compound with the formula (CH3)2NH. This secondary amine is a colorless, flammable gas with an ammonia-like odor. Dimethylamine is commonly encountered commercially as a solution in water at concentrations up to around 40%. An estimated 270,000 tons were produced in 2005. Structure and synthesis The molecule consists of a nitrogen atom with two methyl substituents and one proton. Dimethylamine is a weak base and the pKa of the ammonium CH3--CH3 is 10.73, a value above methylamine (10.64) and trimethylamine (9.79). Dimethylamine reacts with acids to form salts, such as dimethylamine hydrochloride, an odorless white solid with a melting point of 171.5 °C. Dimethylamine is produced by catalytic reaction of methanol and ammonia at elevated temperatures and high pressure: :2 CH3OH + NH3 → (CH3)2NH + 2 H2O Natural occurrence Dimethylamine is found quite widely distributed in animals and plants, and is present in many foods at the level of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abortifacients
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 abortifa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Toripristone
Toripristone ( INN) (developmental code name RU-40555) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed.https://mednet-communities.net/inn/db/media/docs/p-innlist61.pdf It is reported as a potent and highly selective antagonist of the glucocorticoid receptor (GR) (Ki = 2.4 nM), though it also acts as an antagonist of the progesterone receptor (PR). The pharmacological profile of toripristone is said to be very similar to that of mifepristone, except that toripristone does not bind to orosomucoid (α1-acid glycoprotein). The drug has been used to study the hypothalamic-pituitary-adrenal axis and has been used as a radiotracer for the GR. Its INN was given in 1990. See also * Aglepristone * Lilopristone * Onapristone * Telapristone Telapristone (), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Telapristone
Telapristone (), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids. It was originally developed by the National Institutes of Health (NIH), and, as of 2017, is in phase II clinical trials for the aforementioned indications. In addition to its activity as an SPRM, the drug also has some antiglucocorticoid An antiglucocorticoid is a drug which reduces glucocorticoid activity in the body. They include direct glucocorticoid receptor antagonists such as mifepristone and synthesis inhibitors such as metyrapone, ketoconazole, and aminoglutethimide. They ... activity. See also * List of investigational sex-hormonal agents § Progestogenics * Aglepristone * Lilopristone * Onapristone * Toripristone References External ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lilopristone
Lilopristone ( INN) (developmental code names ZK-98734, ZK-734) is a synthetic, steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and was patented in 1985. It is described as an abortifacient and endometrial contraceptive. The drug differs from mifepristone only in the structure of its C17α side chain, and is said to have much reduced antiglucocorticoid activity in comparison. See also * Aglepristone * Onapristone * Telapristone * Toripristone Toripristone ( INN) (developmental code name RU-40555) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed.https://mednet-communities.net/inn/db/media/docs/p-innlist61.pdf It is reported as a potent an ... References Further reading * * Abortifacients Alkene derivatives Dimethylamino compounds Antiglucocorticoids Antiprogestogens Estranes Enones Conjugated dienes {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aglepristone
Aglepristone () (brand name Alizin; former developmental code names RU-46534, RU-534) is a synthetic, steroidal antiprogestogen related to mifepristone which is marketed by Virbac in several European countries for use in veterinary medicine. It is specifically used as an abortifacient in pregnant animals. Aglepristone, similarly to mifepristone, also possesses some antiglucocorticoid activity. See also * Lilopristone * Onapristone * Telapristone * Toripristone Toripristone ( INN) (developmental code name RU-40555) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed.https://mednet-communities.net/inn/db/media/docs/p-innlist61.pdf It is reported as a potent an ... References Abortifacients Alkene derivatives Dimethylamino compounds Antiglucocorticoids Antiprogestogens Estranes Enones Theriogenology Veterinary drugs {{steroid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Sex-hormonal Agents
This is a list of investigational sex-hormonal agents, or sex-hormonal agents that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' Androgenics Androgen receptor agonists * EC586 – oral prodrug of testosterone (androgen/anabolic steroid) with improved pharmacokinetics Androgen receptor antagonists * Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer ref name="pmid33160761"> [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
