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Lilopristone
Lilopristone (INN; development codes ZK-98734 and 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 Onapristone () (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a sile ... * Telapristone * Toripristone 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] |
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. These drugs competitively inhibit progestin at progesterone receptors, acting by blocking the progesterone receptor (PR) and/or inhibiting or suppressing progestogen production. Antiprogestogens are one of three types of sex hormone antagonists, alongside antiestrogens and antiandrogens. Clinical applications Antiprogestogens are used as abortifacients, emergency contraceptives, and in the treatment of uterine fibroids. They are also being studied in the treatment of breast cancer. Examples include the progesterone receptor weak partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full ago ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiprogestogens
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. These drugs competitively inhibit progestin at progesterone receptors, acting by receptor antagonist, blocking the progesterone receptor (PR) and/or steroidogenesis inhibitor, inhibiting or antigonadotropin, suppressing progestogen biosynthesis, production. Antiprogestogens are one of three types of sex-hormonal agent, sex hormone antagonists, alongside antiestrogens and antiandrogens. Clinical applications Antiprogestogens are used as abortifacients, emergency contraception, emergency contraceptives, and in the treatment of uterine fibroids. They are also being studied in the treatment of breast cancer. Examples include the progesterone receptor weak partial agonist mifepristone, the selective progesterone receptor modulator (SPRM) ulipristal acetate, and the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Onapristone
Onapristone () (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. 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). 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. Onapristone has been found to be effective in the treatment of breast cancer. As of 2016, onapristone has re-emerg ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estranes
Estrane is a C18 steroid derivative, with a gonane core. ''Estrenes'' are estrane derivatives that contain a double bond, with an example being nandrolone. ''Estratrienes'' (estrins) are estrane derivatives that contain three double bonds, for instance estrin (compound), estrin (estra-1,3,5(10)-triene). A class of female sex hormones, estrogens, such as estradiol, estrone, and estriol are estratrienes. See also * Androstane * Pregnane References Estranes {{Steroid-stub ... [...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 hydrogen. Dimethylamine is a base (chemistry), 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 Ammonia is an inorganic chemical compound of nitrogen and hydrogen with the chemical formula, formula . A Binary compounds of hydrogen, stable binary hydride and the simplest pnictogen hydride, ammoni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkene Derivatives
In organic chemistry, an alkene, or olefin, is a hydrocarbon containing a carbon–carbon double bond. The double bond may be internal or at the terminal position. Terminal alkenes are also known as α-olefins. The International Union of Pure and Applied Chemistry (IUPAC) recommends using the name "alkene" only for acyclic hydrocarbons with just one double bond; alkadiene, alkatriene, etc., or polyene for acyclic hydrocarbons with two or more double bonds; cycloalkene, cycloalkadiene, etc. for cyclic ones; and "olefin" for the general class – cyclic or acyclic, with one or more double bonds. Acyclic alkenes, with only one double bond and no other functional groups (also known as mono-enes) form a homologous series of hydrocarbons with the general formula with ''n'' being a >1 natural number (which is two hydrogens less than the corresponding alkane). When ''n'' is four or more, isomers are possible, distinguished by the position and conformation of the double bond. A ... [...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. 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 Onapristone () (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a sile ... * Telapristone Referen ... [...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 activity. See also * List of investigational sex-hormonal agents § Progestogenics * Aglepristone * Lilopristone * Onapristone * Toripristone Toripristone (INN; developmental code name RU-40555) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed. It is reported as a potent and highly selective antagonist of the glucocorticoid receptor (GR) ... References External lin ... [...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 Onapristone () (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a sile ... * Telapristone * Toripristone References Abortifacients Alkene derivatives Dimethylamino compounds Antiglucocorticoids Antiprogestogens Estranes Enones Theriogenology Veterinary drugs {{steroid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
