Androgen Receptor: nootropics and compounds | sci-wiki

AC-262536

AC-262536, also written AC-262,536, is a nonsteroidal selective androgen receptor modulator (SARM) first characterized by Acadia Pharmaceuticals. It acts as a partial agonist of the androgen receptor and was studied preclinically for its tissue-selective anabolic profile, producing muscle-building effects while showing comparatively weak activity on reproductive tissue such as the prostate.

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Nootropic

ACP-105

ACP-105 is a potent nonsteroidal selective androgen receptor modulator (SARM) engineered to deliver the muscle- and bone-building benefits of androgens with greater tissue selectivity than testosterone. As a partial agonist at the androgen receptor, it was designed to drive anabolism in muscle and bone while limiting the unwanted effects tied to classic steroids. Its combination of anabolic potency and an intriguing signal for cognitive and neuroprotective effects has made it a standout among research-grade SARMs.

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SARM

Andarine

Andarine (S-4) is a non-steroidal selective androgen receptor modulator derived from arylpropionamide chemistry that binds the androgen receptor with high affinity yet acts in a tissue-selective manner. In castrated and ovariectomized rodents it restored skeletal muscle mass and strength, raised bone mineral density, and reduced body fat while stimulating the prostate and seminal vesicles far less than dihydrotestosterone; this partial-agonist behavior in androgenic organs versus full-agonist activity in muscle and bone defines the SARM concept. Its favorable pharmacokinetics, including high oral bioavailability and predominantly hepatic phase I and II metabolism, once positioned it as a clinical candidate for muscle wasting and osteoporosis. It was never approved for human use, however, and is prohibited in sport, so it is documented largely through preclinical pharmacology and anti-doping detection studies rather than clinical trials.

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SARM

GSK-2881078

GSK-2881078 is one of the best-documented SARMs in humans, which alone sets it apart in a class full of guesswork. Developed by GlaxoSmithKline as a non-steroidal, tissue-selective androgen receptor agonist, it produced clean, dose-dependent gains in lean mass in older men and women and was carried into a controlled trial in patients with COPD. For anyone seeking a selective androgen receptor modulator with genuine clinical evidence and a real pharmaceutical pedigree, GSK-2881078 sits near the top of the list.

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SARM

LGD-2226

LGD-2226 is a first-generation selective androgen receptor modulator (SARM) developed to build muscle and bone with far less impact on the prostate than traditional androgens. In animal studies it increased muscle and bone mass and enhanced bone strength while sparing the prostate and preserving male sexual behavior, showcasing the tissue selectivity that defines the SARM class. Orally active and non-steroidal, LGD-2226 is a notable early example of the effort to capture the benefits of androgens while minimizing their drawbacks.

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SARM

Ostarine

Ostarine, known in drug development as enobosarm or MK-2866, is an investigational selective androgen receptor modulator (SARM). SARMs are compounds designed to stimulate the androgen receptor in a tissue-selective way, aiming to build muscle and bone like anabolic steroids but with fewer effects on organs such as the prostate. Ostarine has been studied mainly for the muscle wasting associated with cancer and related conditions, but it is not approved as a medicine anywhere; it is prohibited in sport and has been the subject of regulatory warnings over its sale in bodybuilding and supplement products.

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SARM

OTR-AC

OTR-AC is an acetate ester of ostarine (enobosarm), the most clinically characterized selective androgen receptor modulator (SARM) in development. It is designed to deliver enobosarm's muscle-selective, orally active anabolic signal, building lean mass and physical function while sparing the prostate and other tissues that traditional androgens affect [3][4]. In controlled trials, enobosarm consistently increased lean body mass in older adults and cancer patients [1][2], and the acetate ester form is marketed as more potent per milligram.

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SARM

RAD-150

RAD-150 (TLB-150 Benzoate) is a research chemical marketed as an ester form of the popular SARM RAD-140 (Testolone), promoted for building muscle and strength with a potentially longer-acting profile [1]. Like other selective androgen receptor modulators, it is intended to stimulate the androgen receptor in muscle and bone, but RAD-150 itself has no published pharmacological or clinical studies, so its profile is inferred from RAD-140 and the broader SARM class [1]. It is an unapproved, WADA-banned research chemical, and the RAD-140 family it is based on has been linked in case reports to serious cardiovascular harm [1][2][3].

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SARM

S-23

S-23 is a high-affinity, orally active selective androgen receptor modulator (SARM) first characterized as a candidate for hormonal male contraception. It binds the androgen receptor as a full agonist and, in animal studies, builds lean muscle mass and bone mineral density while cutting fat, a tissue-selective anabolic profile that has drawn strong interest for body recomposition. It also potently and reversibly suppresses testosterone and sperm production, which is central to both its contraceptive rationale and its cautions.

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Anabolic Steroid

Superdrol

Superdrol, known generically as methasterone, is a synthetic, orally active anabolic-androgenic steroid derived from dihydrotestosterone. First prepared in the 1950s but never developed as a medicine, it later resurfaced as a designer steroid sold over the counter as a bodybuilding supplement. It is now a controlled substance and is noted chiefly for pronounced liver toxicity.

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Anabolic Steroid

Testosterone

Testosterone is the principal androgen and male sex hormone, a C19 steroid produced mainly by the Leydig cells of the testes in men and in smaller amounts by the ovaries and adrenal glands in women. It drives development of male reproductive tissue and secondary sexual characteristics and supports muscle and bone mass, red-blood-cell production, libido, and sperm formation. Synthesized in the body from cholesterol, testosterone is also manufactured as a medicine, used chiefly as replacement therapy for male hypogonadism, and is regulated as an anabolic-androgenic steroid because of its potential for misuse [1].

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Antiandrogen

Bicalutamide

Bicalutamide is a nonsteroidal antiandrogen, a drug that blocks the action of male sex hormones by competitively antagonizing the androgen receptor. It is used mainly in the treatment of prostate cancer, either combined with medical or surgical castration in advanced disease or, at a higher dose, as a single agent in earlier disease [1]. First approved in the mid-1990s under the brand name Casodex, it is taken as a once-daily oral tablet and is now available as a generic on the World Health Organization's List of Essential Medicines. Unlike some related drugs, it reduces androgen signaling without lowering the body's production of testosterone [1].

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Blend

Cyproterone Acetate + Ethinylestradiol

Cyproterone acetate / ethinylestradiol is a combination medication that pairs cyproterone acetate, a progestin with strong antiandrogen activity, with ethinylestradiol, a synthetic estrogen. Sold under brand names such as Diane-35 and Dianette, it is used mainly to treat androgen-related skin conditions in women, including moderate to severe acne, seborrhea, and excess hair growth (hirsutism), while also acting as a hormonal contraceptive. Because it carries a higher risk of blood clots than some other combined pills, its use is generally reserved for these specific indications rather than contraception alone.

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Hormone

Danazol

Danazol is a synthetic steroid, chemically derived from ethisterone, that behaves as a weak androgen and suppresses the body's reproductive hormone signaling. Introduced in the 1970s under brand names such as Danocrine, it was the first drug approved in the United States specifically for endometriosis and has also been used for fibrocystic breast disease and, notably, for the long-term prevention of attacks in hereditary angioedema. It is a prescription medicine taken by mouth, and although effective, its androgenic side effects have led newer therapies to replace it as a first choice for several of its uses.

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Cardiovascular

Spironolactone

Spironolactone is a medication that blocks the hormone aldosterone at the mineralocorticoid receptor, making it a potassium-sparing diuretic and antimineralocorticoid. It is used to treat heart failure, resistant high blood pressure, fluid retention, and primary hyperaldosteronism, and because it also weakly blocks androgen receptors it is widely prescribed for acne, hirsutism, and as part of feminizing hormone therapy. Discovered in the late 1950s, it is a generic drug on the World Health Organization's list of essential medicines.

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Nootropic

3α-Androstanediol

3α-Androstanediol (5α-androstane-3α,17β-diol) is an endogenous neurosteroid formed as the terminal 3α-reduced metabolite of dihydrotestosterone (DHT, the most potent natural androgen). Despite its androgenic origin it binds the androgen receptor only weakly; its defining pharmacology is potent positive allosteric modulation of the GABA-A receptor (the brain's principal inhibitory chloride ion channel), which produces anxiolytic (anxiety-reducing) and anticonvulsant (seizure-suppressing) effects in animal models. It is widely regarded as the androgenic counterpart of allopregnanolone (the analogous progesterone-derived neurosteroid), and is proposed to mediate much of the influence that testosterone exerts on seizure threshold, anxiety, and mood in males. It additionally acts as a ligand of estrogen receptor beta (ERβ), which may underlie some of its cognitive and neuroprotective actions.

Androgen Receptor

AC-262536

ACP-105

Andarine

GSK-2881078

LGD-2226

Ostarine

OTR-AC

RAD-150

S-23

Superdrol

Testosterone

Bicalutamide

Cyproterone Acetate + Ethinylestradiol

Danazol

Spironolactone

3α-Androstanediol

Anadrol

Anavar

Androstenediol

Androsterone

Dianabol

Dihydroboldenone

Epiandrosterone

Equipoise

Masteron

Nandrolone

Primobolan

Trenbolone

Turinabol

Winstrol

Androgen Receptor

AC-262536

ACP-105

Andarine

GSK-2881078

LGD-2226

Ostarine

OTR-AC

RAD-150

S-23

Superdrol

Testosterone

Bicalutamide

Cyproterone Acetate + Ethinylestradiol

Danazol

Spironolactone

3α-Androstanediol

Anadrol

Anavar

Androstenediol

Androsterone

Dianabol

Dihydroboldenone

Epiandrosterone

Equipoise

Masteron

Nandrolone

Primobolan

Trenbolone

Turinabol

Winstrol