Trimethyltrienolone
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Trimethyltrienolone
Trimethyltrienolone (TMT), also known by its developmental code name R-2956 or RU-2956, is an antiandrogen medication which was never introduced for medical use but has been used in scientific research. Side effects Due to its close relation to metribolone (methyltrienolone), it is thought that TMT may produce hepatotoxicity. Pharmacology Pharmacodynamics TMT is a selective and highly potent competitive antagonist of the androgen receptor (AR) with very low intrinsic/partial androgenic activity and no estrogenic, antiestrogenic, progestogenic, or antimineralocorticoid activity. The drug is a derivative of the extremely potent androgen/anabolic steroid metribolone (R-1881; 17α-methyltrenbolone), and has been reported to possess only about 4-fold lower affinity for the AR in comparison. In accordance, it has relatively high affinity for the AR among steroidal antiandrogens, and almost completely inhibits dihydrotestosterone (DHT) binding to the AR ''in vitro'' at a mere 10-fold ...
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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, seborrhea, ...
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Metribolone
Metribolone (developmental code R1881, also known as methyltrienolone) is a synthetic compound, synthetic and oral administration, orally active anabolic–androgenic steroid (AAS) and a 17α-alkylated anabolic steroid, 17α-alkylated nandrolone (19-nortestosterone) chemical derivative, derivative which was never marketed for medical use but has been widely used in scientific research as a hot ligand in androgen receptor (AR) ligand binding assays (LBAs) and as a photoaffinity labeling, photoaffinity label for the AR. More precisely, metribolone is the 17α-methylated derivative of trenbolone. It was investigated briefly for the treatment of advanced breast cancer in women in the late 1960s and early 1970s, but was found to produce signs of severe hepatotoxicity at very low dosages, and its development was subsequently discontinued. Medical uses Metribolone was never approved for medical use, a situation unlikely to change given its liver toxicity even at low doses. It was studied ...
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Metribolone
Metribolone (developmental code R1881, also known as methyltrienolone) is a synthetic compound, synthetic and oral administration, orally active anabolic–androgenic steroid (AAS) and a 17α-alkylated anabolic steroid, 17α-alkylated nandrolone (19-nortestosterone) chemical derivative, derivative which was never marketed for medical use but has been widely used in scientific research as a hot ligand in androgen receptor (AR) ligand binding assays (LBAs) and as a photoaffinity labeling, photoaffinity label for the AR. More precisely, metribolone is the 17α-methylated derivative of trenbolone. It was investigated briefly for the treatment of advanced breast cancer in women in the late 1960s and early 1970s, but was found to produce signs of severe hepatotoxicity at very low dosages, and its development was subsequently discontinued. Medical uses Metribolone was never approved for medical use, a situation unlikely to change given its liver toxicity even at low doses. It was studied ...
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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 women, 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, depression (mood), ...
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Steroidal Antiandrogen
A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) and by suppressing gonadal androgen production. SAAs lower concentrations of testosterone through simulation of the negative feedback inhibition of the hypothalamus. SAAs are used in the treatment of androgen-dependent conditions in men and women, and are also used in veterinary medicine for the same purpose. They are the converse of nonsteroidal antiandrogens (NSAAs), which are antiandrogens that are not steroids and are structurally unrelated to testosterone. Medical uses SAAs are used in clinical medicine for the following indications: * Prostate cancer in men * Benign prostatic hyperplasia in men * Androgen-dependent skin and hair conditions like acne, hirsutism, seborrhea, and pattern hair loss (androgenic alopecia) in women * Hy ...
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Aldosterone
Aldosterone is the main mineralocorticoid steroid hormone produced by the zona glomerulosa of the adrenal cortex in the adrenal gland. It is essential for sodium conservation in the kidney, salivary glands, sweat glands, and colon. It plays a central role in the homeostatic regulation of blood pressure, plasma sodium (Na+), and potassium (K+) levels. It does so primarily by acting on the mineralocorticoid receptors in the distal tubules and collecting ducts of the nephron. It influences the reabsorption of sodium and excretion of potassium (from and into the tubular fluids, respectively) of the kidney, thereby indirectly influencing water retention or loss, blood pressure, and blood volume.Marieb Human Anatomy & Physiology 9th edition, chapter:16, page:629, question number:14 When dysregulated, aldosterone is pathogenic and contributes to the development and progression of cardiovascular and kidney disease. Aldosterone has exactly the opposite function of the atrial natriure ...
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Estradiol (medication)
Estradiol (E2) is a medication and naturally occurring steroid hormone. It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women. It is also used in hormonal birth control for women, in hormone therapy for transgender women, and in the treatment of hormone-sensitive cancers like prostate cancer in men and breast cancer in women, among other uses. Estradiol can be taken by mouth, held and dissolved under the tongue, as a gel or patch that is applied to the skin, in through the vagina, by injection into muscle or fat, or through the use of an implant that is placed into fat, among other routes. Side effects of estradiol in women include breast tenderness, breast enlargement, headache, fluid retention, and nausea among others. Men and children who are exposed to estradiol may develop symptoms of feminization, such as breast development and a feminine pattern of fat distribution, and men may also experience low t ...
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Testosterone (medication)
Testosterone (T) 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 used as a gel or transdermal patch, patch that is applied to the skin, intramuscular injection, injection into a muscle, tablet that is Buccal administration, placed in the cheek, or tablet that is taken oral administration, by mouth. Common side effects of testosterone include acne, swelling (medical), swelling, and gynecomastia, breast enlargement in men. Serious side effects may include liver toxicity, heart disease, and behavioral changes. Women and children who are exposed may develop virilization, masculinization. It is recommended that individuals with prostate cancer not use the ...
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Progesterone (medication)
Progesterone (P4) is a medication and naturally occurring steroid hormone. It is a progestogen and is used in combination with estrogens mainly in hormone therapy for menopausal symptoms and 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 by mouth, in through the vagina, and by injection into muscle or fat, among other routes. A progesterone vaginal ring and progesterone intrauterine device used for birth control also exist in some areas of the world. Progesterone is well tolerated and often produces few or no side effects. However, a number of side effects are possible, for instance mood changes. If progesterone is taken by mouth or at high doses, certain central side effects including sedation, sleepiness, and cognitive impairment can also occur. The medication is a naturally occurring progestogen and hence is an agonist of the progesterone receptor (PR), t ...
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Ligand (biochemistry)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition of lig ...
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Androstanolone
Androstanolone, or stanolone, also known as dihydrotestosterone (DHT) and sold under the brand name Andractim among others, is an androgen and anabolic steroid (AAS) medication and hormone which is used mainly in the treatment of low testosterone levels in men. It is also used to treat breast development and small penis in males. It is typically given as a gel for application to the skin, but can also be used as an ester by injection into muscle. Side effects of androstanolone include symptoms of masculinization like acne, increased hair growth, voice changes, and increased sexual desire. The medication is a naturally occurring androgen and anabolic steroid and hence is an agonist of the androgen receptor (AR), the biological target of androgens like testosterone and DHT. It has strong androgenic effects and weak muscle-building effects, as well as no estrogenic effects. Androstanolone was discovered in 1935 and was introduced for medical use in 1953. It is used mostly i ...
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Testosterone (medication)
Testosterone (T) 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 used as a gel or transdermal patch, patch that is applied to the skin, intramuscular injection, injection into a muscle, tablet that is Buccal administration, placed in the cheek, or tablet that is taken oral administration, by mouth. Common side effects of testosterone include acne, swelling (medical), swelling, and gynecomastia, breast enlargement in men. Serious side effects may include liver toxicity, heart disease, and behavioral changes. Women and children who are exposed may develop virilization, masculinization. It is recommended that individuals with prostate cancer not use the ...
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