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Acetothiolutamide
Acetothiolutamide is a selective androgen receptor modulator (SARM) derived from the nonsteroidal antiandrogen bicalutamide that was described in 2002 and was one of the first SARMs to be discovered and developed. It is a high-affinity, selective ligand of the androgen receptor (AR) (Ki = 2.1–4.9 nM), where it acts as a full agonist ''in vitro'', and has ''in vitro'' potency comparable to that of testosterone. However, ''in vivo'', acetothiolutamide displayed overall negligible androgenic effects, though significant (albeit very low) anabolic effects were observed at high doses. In addition, notable antiandrogen effects were observed in castrated male rats treated with testosterone propionate. The discrepancy between the ''in vitro'' and ''in vivo'' actions of acetothiolutamide was determined to be related to rapid plasma clearance and extensive hepatic metabolism into a variety of metabolites with differing pharmacological activity, including AR partial agonism and antagonism ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bicalutamide
Bicalutamide, sold under the brand name Casodex among others, is an antiandrogen medication that is primarily used to treat prostate cancer. It is typically used together with a gonadotropin-releasing hormone (GnRH) analogue or surgical removal of the testicles to treat advanced prostate cancer. To a lesser extent, it is used for early prostate cancer at a higher dosage as a monotherapy without castration. Bicalutamide is also used to treat excessive hair growth and scalp hair loss in women, as a component of feminizing hormone therapy for transgender women, to treat early puberty in boys, and to prevent overly long-lasting erections in men. It is taken by mouth. Common side effects in men include breast enlargement, breast tenderness, and hot flashes. Other side effects in men include feminization and sexual dysfunction. Some side effects like breast changes and feminization are minimal when combined with castration. While the medication appears to produce few side effe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective Androgen Receptor Modulator
Selective Androgen Receptor Modulators or SARMs are a class of androgen receptor ligands that maintain some of the desirable effects of androgens, such as preventing osteoporosis and muscle loss while reducing risks of developing prostate cancer. In the late 1990s, the first nonsteroidal SARM, an analog of bicalutamide, was discovered. They are intended to have the same kind of effects as androgenic drugs, such as anabolic-androgenic steroids, but be more selective in their action. At present, there are no SARMs which have been approved for therapeutic use by the U.S. Food and Drug Administration. Comparison to testosterone As previously mentioned, the purpose of research in relation to SARMs is to replace testosterone supplementation in disease treatment with selective androgen receptor molecules. This is due to the fact that testosterone supplementation can have adverse effects on patients, which are detailed on the testosterone page. Thinking of testosterone as a model mole ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LG-121071
LG121071 (or LGD-121071) is a selective androgen receptor modulator (SARM) developed by Ligand Pharmaceuticals that was first described in 1999 and was the first orally active nonsteroidal androgen to be discovered. It is a tricyclic quinolone derivative, structurally distinct from other nonsteroidal AR agonists like andarine and enobosarm (ostarine). The drug acts as a high-affinity full agonist of the androgen receptor (AR) (Ki = 17 nM), with a potency and efficacy that is said to be equivalent to that of dihydrotestosterone (DHT). Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by 5α-reductase in androgenic tissues (nor aromatized into estrogenic metabolites), and for this reason, show tissue-selective androgenic effects. In accordance, they are said to possess full anabolic activity with reduced androgenic activity, similarly to anabolic-androgenic steroids. The ''in vitro'' metabolism Metabolism (, from ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Andarine
Andarine (developmental code names GTx-007, S-4) is an investigational selective androgen receptor modulator (SARM) developed by GTX, Inc for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy, using the nonsteroidal antiandrogen bicalutamide as a lead compound. Andarine is an orally active partial agonist of the androgen receptor (AR). In intact male rats, 0.5 mg andarine daily was shown to reduce prostate weight to 79.4%, and non-significantly increased levator ani muscle weight. In castrated male rats, this dose restored only 32.5% prostate weight, but 101% levator ani muscle weight This suggests that andarine is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist actions at the androgen receptor prevent the side effects associated with the antiandrogens traditionally used for treatment of BPH. See also * Acetothiolutamide * Enobosarm Enobosarm, als ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc. Some antibiotics use primary metabolites as precursors, such as actinomycin, which is created from the primary metabolite tryptophan. Some sugars are metabolites, such as fructose or glucose, which are both p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enobosarm
Enobosarm, also known as ostarine or MK-2866, is an investigational selective androgen receptor modulator (SARM) developed by GTx, Inc. for the treatment of conditions such as muscle wasting and osteoporosis, formerly under development by Merck & Company. Chemistry According to a 2009 paper authored by GTx, "Readers are cautioned to note that the name ostarine is often mistakenly linked to the chemical structure of -4 which is also known as andarine. The chemical structure of ostarine has not been publicly disclosed." A 2009 review stated "Recently, GTx disclosed that compound 5 had advanced into clinical trials. The patent application described detailed data in an initial proof-of-concept Phase IIa clinical trial. It is not explicitly stated that compound 5 is Ostarine (MK-2866). The first quoted sentence is cited tPublished PCT application WO2008127717/ref> As of 2012, the mechanism of action of Enobosarm is still being debated and requires further investigation. History ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Intravenous Injection
Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrients for those who cannot, or will not—due to reduced mental states or otherwise—consume food or water by mouth. It may also be used to administer medications or other medical therapy such as blood products or electrolytes to correct electrolyte imbalances. Attempts at providing intravenous therapy have been recorded as early as the 1400s, but the practice did not become widespread until the 1900s after the development of techniques for safe, effective use. The intravenous route is the fastest way to deliver medications and fluid replacement throughout the body as they are introduced directly into the circulatory system and thus quickly distributed. For this reason, the intravenous route of administration is also used for the consump ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Subcutaneous Injection
Subcutaneous administration is the insertion of medications beneath the skin either by injection or infusion. A subcutaneous injection is administered as a bolus into the subcutis, the layer of skin directly below the dermis and epidermis, collectively referred to as the cutis. The instruments are usually a hypodermic needle and a syringe. Subcutaneous injections are highly effective in administering medications such as insulin, morphine, diacetylmorphine and goserelin. Subcutaneous administration may be abbreviated as SC, SQ, subcu, sub-Q, SubQ, or subcut. Subcut is the preferred abbreviation to reduce the risk of misunderstanding and potential errors. Subcutaneous tissue has few blood vessels and so drugs injected here are for slow, sustained rates of absorption, often with some amount of depot effect. Compared with other routes of administration, it is slower than intramuscular injections but still faster than intradermal injections. Subcutaneous infusion (as opposed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Route Of Administration
A route of administration in pharmacology and toxicology is the way by which a medication, drug, fluid, poison, or other substance is taken into the body. Routes of administration are generally classified by the location at which the substance is applied. Common examples include oral administration, oral and intravenous therapy, intravenous administration. Routes can also be classified based on where the target of action is. Action may be topical medication, topical (local), enteral administration, enteral (system-wide effect, but delivered through the gastrointestinal tract), or #Parenteral, parenteral (systemic action, but delivered by routes other than the GI tract). Route of administration and dosage form are aspects of drug delivery. Classification Routes of administration are usually classified by application location (or exposition). The route or course the active substance takes from application location to the location where it has its target effect is usually rather ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Injection
Drug injection is a method of introducing a drug into the bloodstream via a hollow hypodermic needle, which is pierced through the skin into the body (usually intravenously, but also at an intramuscular or subcutaneous location). Intravenous therapy, a form of drug injection, is universally practiced in modernized medical care. , there were 13.2 million people worldwide who self-administered injection drugs outside of medical supervision, of which 22% are from developed countries. A wide variety of drugs are injected, often opioids: these may include legally prescribed medicines and medication such as morphine, as well as stronger compounds often favored in recreational drug use, which are often illegal. Although there are various methods of taking drugs, injection is favoured by some people as the full effects of the drug are experienced very quickly, typically in five to ten seconds. It also bypasses first-pass metabolism in the liver, resulting in higher bioavailability and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioavailable
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via routes other than intravenous, its bioavailability is generally lower than that of intravenous due to intestinal endothelium absorption and first-pass metabolism. Thereby, mathematically, bioavailability equals the ratio of comparing the area under the plasma drug concentration curve versus time (AUC) for the extravascular formulation to the AUC for the intravascular formulation. AUC is used because AUC is proportional to the dose that has entered the systemic circulation. Bioavailability of a drug is an average value; to take population variability into account, deviation range is shown as ±. To ensure that the drug taker who has poor absorption is dosed appropriately, the bottom value of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as 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 willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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