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Spirorenone Synthesis
Spirorenone (INN; developmental code ZK-35973) is a steroidal antimineralocorticoid of the spirolactone group that was never marketed. Spirorenone possesses 5–8 times the antimineralocorticoid activity of spironolactone in animal studies. The initial discovery of spirorenone was deemed a great success, as no compound with greater antimineralocorticoid activity had been developed since spironolactone in 1957. Moreover, spirorenone itself has virtually no affinity for the androgen receptor while its progestogenic activity shows species differences, being somewhat greater than that of spironolactone in rabbits but absent in mice and rats. As such, it was characterized as a highly potent antimineralocorticoid with far fewer hormonal side effects relative to spironolactone. In clinical trials, spirorenone was found to be 4- to 10-fold as potent as spironolactone as an antimineralocorticoid, and is said to be the most active antimineralocorticoid identified to date. However, it was se ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spiro Compounds
In organic chemistry, spiro compounds are compounds that have at least two molecular rings sharing one common atom. Simple spiro compounds are bicyclic (having just two rings). The presence of only one common atom connecting the two rings distinguishes spiro compounds from other bicyclics.For all four categories, see The specific chapters can be found aan respectively, same access date. For the description featuring adjacent atoms for all but the isolated category, see Clayden, op. cit. Spiro compounds may be fully carbocyclic (all carbon) or heterocyclic (having one or more non-carbon atom). One common type of spiro compound encountered in educational settings is a heterocyclic one— the acetal formed by reaction of a diol with a cyclic ketone. The common atom that connects the two (or sometimes three) rings is called the ''spiro atom''. In carbocyclic spiro compounds like spiro .5ndecane, the spiro-atom is a quaternary carbon, and as the ''-ane'' ending implies, these ar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progestogens
Progestogens, also sometimes written progestins, progestagens or gestagens, are a class of natural or synthetic steroid hormones that bind to and activate the progesterone receptors (PR). Progesterone is the major and most important progestogen in the body. The progestogens are named for their function in maintaining pregnancy (i.e., ''progestational''), although they are also present at other phases of the estrous and menstrual cycles. The progestogens are one of three types of sex hormones, the others being estrogens like estradiol and androgens/anabolic steroids like testosterone. In addition, they are one of the five major classes of steroid hormones, the others being the androgens, estrogens, glucocorticoids, and mineralocorticoids, as well as the neurosteroids. All endogenous progestogens are characterized by their basic 21-carbon skeleton, called a pregnane skeleton (C21). In similar manner, the estrogens possess an estrane skeleton (C18), and androgens, an androstane sk ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pregnanes
Pregnane, also known as 17β-ethylandrostane or as 10β,13β-dimethyl-17β-ethylgonane, is a C21 steroid and, indirectly, a parent of progesterone. It is a parent hydrocarbon for two series of steroids stemming from 5α-pregnane (originally allopregnane) and 5β-pregnane (17β-ethyl etiocholane). It has a gonane core. 5β-Pregnane is the parent of pregnanediones, pregnanolones, and pregnanediols, and is found largely in urine as a metabolic product of 5β-pregnane compounds. Pregnanes Pregnanes are steroid derivatives with carbons present at positions 1 through 21. Most biologically significant pregnane derivatives fall into one of two groups: pregnenes and pregnadienes. Another class is pregnatrienes. Pregnenes Pregnenes have a double bond. Examples include: * Cortisone * Hydrocortisone * Progesterone Pregnadienes Pregnadienes have two double bonds. Examples include: * Cyproterone acetate * Danazol Danazol, sold as Danocrine and other brand names, is a me ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclopropanes
Cyclopropanes are a family of organic compounds containing the cyclopropyl group. The parent is cyclopropane (). Synthesis and reactions Most cyclopropanes are not prepared from the parent cyclopropane, which is somewhat inert. Instead, yclopropyl groups are often prepared by cyclization of 1,3-difunctional alkanes. An example of the former, cyclopropyl cyanide is prepared by the reaction of 4- chlorobutyronitrile with a strong base. Phenylcyclopropane is produced analogously from the 1,3-dibromide. A second major route to cyclopropanes entails addition of methylene (or its substituted derivatives) to an alkene, a process called cyclopropanation. Substituted cyclopropanes undergo the reactions associated with the cyclopropyl ring or the substituents. Vinylcyclopropanes are a special case as they undergo vinylcyclopropane rearrangement. Simple substituted cyclopropanes * Chlorocyclopropane * Cyclopropane carboxylic acid * Cyclopropyl amine * Cyclopropyl cyanide * Cycloprop ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mespirenone
Mespirenone (International Nonproprietary Name, INN; developmental code ZK-94679; also known as Δ1-15β,16β-methylenespironolactone) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. Animal research found that it was 3.3-fold more potent as an antimineralocorticoid relative to spironolactone. In addition to its antimineralocorticoid properties, mespirenone is also a progestogen, antigonadotropin, and antiandrogen. It is 2- to 3-fold as potent as spironolactone as a progestogen and antigonadotropin but its antiandrogenic activity is markedly reduced and weak (though still of significance) in comparison. Mespirenone is also a potency (pharmacology), potent and specific enzyme inhibitor of 18-hydroxylase and thus of mineralocorticoid biosynthesis. The drug was under development by Schering AG, Schering (now Bayer Schering Pharma) and reached Phases of clinical research#Phase II, phase II clinical trials but was discont ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spirorenone Synthesis
Spirorenone (INN; developmental code ZK-35973) is a steroidal antimineralocorticoid of the spirolactone group that was never marketed. Spirorenone possesses 5–8 times the antimineralocorticoid activity of spironolactone in animal studies. The initial discovery of spirorenone was deemed a great success, as no compound with greater antimineralocorticoid activity had been developed since spironolactone in 1957. Moreover, spirorenone itself has virtually no affinity for the androgen receptor while its progestogenic activity shows species differences, being somewhat greater than that of spironolactone in rabbits but absent in mice and rats. As such, it was characterized as a highly potent antimineralocorticoid with far fewer hormonal side effects relative to spironolactone. In clinical trials, spirorenone was found to be 4- to 10-fold as potent as spironolactone as an antimineralocorticoid, and is said to be the most active antimineralocorticoid identified to date. However, it was se ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Contraceptive
Birth control, also known as contraception, anticonception, and fertility control, is the use of methods or devices to prevent pregnancy. Birth control has been used since ancient times, but effective and safe methods of birth control only became available in the 20th century. Planning, making available, and using human birth control is called family planning. Some cultures limit or discourage access to birth control because they consider it to be morally, religiously, or politically undesirable. The World Health Organization and United States Centers for Disease Control and Prevention provide guidance on the safety of birth control methods among women with specific medical conditions. The most effective methods of birth control are sterilization by means of vasectomy in males and tubal ligation in females, intrauterine devices (IUDs), and implantable birth control. This is followed by a number of hormone-based methods including contraceptive pills, patches, vaginal r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyproterone Acetate
Cyproterone acetate (CPA), sold alone under the brand name Androcur or Ethinylestradiol/cyproterone acetate, with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treatment of androgen-dependent conditions such as acne, hirsutism, excessive body hair growth, precocious puberty, early puberty, and prostate cancer, as a component of feminizing hormone therapy for Transgender, transgender individuals, and in oral contraceptive, birth control pills. It is formulated and used both alone and in combination with an estrogen (medication), estrogen. CPA is taken Oral administration, by mouth one to three times per day. Common side effects of high-dose CPA in men include gynecomastia (breast development) and feminization (biology), feminization. In both men and women, possible side effects of CPA include hypogonadism, low sex hormone levels, reversible infertility, sexual dysfunction, fatigue (medical), fatigue ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiandrogen
Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking the androgen receptor (AR) and/or inhibiting or suppressing androgen production. They can be thought of as the functional opposites of AR agonists, for instance androgens and anabolic steroids (AAS) like testosterone, DHT, and nandrolone and selective androgen receptor modulators (SARMs) like enobosarm. Antiandrogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiprogestogens. Antiandrogens are used to treat an assortment of androgen-dependent conditions. In men, antiandrogens are used in the treatment of prostate cancer, enlarged prostate, scalp hair loss, overly high sex drive, unusual and problematic sexual urges, and early puberty. In women, antiandrogens are used to treat acne, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
