Brain masculinization requires androgen receptor function.
Researchers observed that androgen receptor function is crucial for perinatal brain masculinization and the expression of male-typical behaviors in mice.
DHT · 5α-Dihydrotestosterone · Androstanolone · Stanolone
Dihydrotestosterone (DHT) is a potent androgen hormone derived from testosterone through the action of the enzyme 5α-reductase, primarily produced in the prostate, testes, and hair follicles. Researchers primarily study DHT for its critical role in male sexual development, prostate function, and its implications in conditions such as prostate cancer. Key findings indicate that DHT binds to androgen receptors in target tissues, regulating gene expression essential for prostate homeostasis and influencing muscle strength through novel membrane receptors. Additionally, studies suggest that DHT's interaction with androgen receptors is complex, involving various ancillary proteins that modulate its effects across different tissues. Current research continues to explore DHT's multifaceted roles in health and disease, highlighting its clinical relevance in understanding androgen-related disorders.
Dihydrotestosterone (DHT), also known as 5α-Dihydrotestosterone or Androstanolone, is an endogenous androgen sex hormone produced primarily in the gonads and adrenal glands. It belongs to the class of steroid hormones derived from testosterone via the action of the enzyme 5α-reductase. DHT is a potent androgen, more so than its precursor testosterone, and plays a crucial role in the development of male characteristics. Researchers have found that DHT is involved in various physiological processes, including the development of male secondary sexual characteristics, regulation of prostate growth, and maintenance of muscle strength. It is also a subject of interest in research areas such as prostate cancer, androgen receptor signaling, and muscle physiology. DHT exerts its effects primarily by binding to androgen receptors (ARs) in target tissues. Upon binding, the DHT-AR complex translocates to the nucleus, where it interacts with specific DNA sequences to regulate the transcription of androgen-responsive genes. Recent studies have also identified a membrane receptor, GPR133, that DHT activates, suggesting additional pathways for its action. Pharmacokinetically, DHT has a relatively short circulating half-life, and its metabolism involves conversion from testosterone by 5α-reductase. Its bioavailability varies depending on the route of administration, with oral administration being limited due to first-pass metabolism. Clinically, DHT is used in hormone replacement therapies, although its use is regulated due to potential side effects. It is not approved for use in all countries and is often subject to prescription and control regulations.
| Formel | C19H30O2 |
| Molekulargewicht | 290.4g/mol |
| CAS-Nummer | 521-18-6 |
| PubChem CID | 10635 |
Dihydrotestosterone acts primarily on nuclear androgen receptors, forming a DHT-AR complex that translocates to the nucleus to regulate gene transcription. Researchers have also identified its action on the membrane receptor GPR133, which increases intracellular cAMP levels and enhances muscle strength.
Dihydrotestosterone (DHT) primarily exerts its effects through binding to the androgen receptor (AR), leading to the formation of a DHT-AR complex that translocates to the nucleus and regulates the transcription of androgen-responsive genes via androgen receptor signaling. Additionally, DHT has been shown to activate the membrane receptor GPR133, which increases intracellular cyclic AMP (cAMP) levels, enhancing muscle strength through the cAMP/PKA pathway. While the nuclear mechanism is well characterized, the full extent of DHT's actions, particularly through GPR133 and other potential membrane receptors, remains to be fully elucidated.
Circulating half-life ~70 minutes
Poor bioavailability due to first-pass metabolism
DHT is primarily metabolized from testosterone and has limited oral bioavailability.
Temperature
Store at room temperature (15-30C)
Light
Protect from light
Form
Oil solution stable for 2+ years
Notes
Ensure storage conditions are maintained to preserve stability.
Dihydrotestosterone is poorly soluble in water but soluble in ethanol and oils, relevant for formulation in oil-based solutions.
🇩🇪DE
Verschreibungspflichtig; not listed under BtMG.
🇺🇸US
Not FDA-approved for any indication; not scheduled by DEA but requires a prescription.
🇦🇺AU
Schedule 4 (S4) prescription-only medicine.
🇬🇧UK
Prescription-only medicine (POM); regulated by MHRA.
Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.
Current evidence is limited regarding the specific mechanisms by which 5α-dihydrotestosterone (DHT) interacts with newly identified membrane receptors, such as GPR133, and how these interactions may differ across various tissues and cell types. Further research is needed to elucidate the role of endocrine disruptors in modulating DHT signaling pathways in the prostate, particularly in relation to prostate cancer risk and progression. Additionally, larger randomized controlled trials are necessary to explore the long-term effects of frequent ejaculation on prostate health and its potential protective mechanisms against prostate cancer, especially in diverse populations with varying risk factors.
3,584
Total Citations
24
Human/RCT
2.5
Avg. Influence
2025
Latest
Researchers observed that androgen receptor function is crucial for perinatal brain masculinization and the expression of male-typical behaviors in mice.
Researchers observed that skeletal muscle can synthesize dihydrotestosterone from testosterone and/or DHEA, activating glucose metabolism-related signaling pathways.
The study demonstrated that testosterone accounts for at least 70% of plasma dihydrotestosterone in males, while androstenedione is a significant precursor in females, highlighting differences in androgen sources between sexes.
The study demonstrated that serum dihydrotestosterone levels increased in adult rats but remained unchanged in older rats, highlighting age-related variations in androgen levels.
Researchers observed that 5α-dihydrotestosterone does not affect serotonin transporter expression in male rat brain, suggesting that testosterone's effects on SERT are likely mediated through its conversion to estradiol.
Researchers observed that androgens, including dihydrotestosterone (DHT), have multiple genomic and non-genomic effects on cardiovascular function, influencing various physiological processes in male reproductive tissues.
The study demonstrated that dihydrotestosterone increases glucose consumption in human Sertoli cells while decreasing lactate secretion, indicating its role in metabolic regulation.
Researchers observed that treatment with 5α-dihydrotestosterone increases ovulation rates in postpubertal gilts, correlating with elevated FSH receptor mRNA levels.
Researchers observed that intratumoral metabolism of androgens, including dihydrotestosterone, plays a crucial role in the pathogenesis of hormone-dependent breast carcinoma, although its exact mechanisms remain unclear.
The study demonstrated that exercise upregulates sex steroid hormone synthesis, including DHT, in skeletal muscle, positively impacting muscle mass and glycemic control in obese and diabetic rats and older men.
3
Total Trials
166
Total Enrolled
ASCEND Therapeutics
128
2004
Change in Body Composition
University of Washington
31
2007
Prostate Tissue DHT and Testosterone Levels After 28 Days of Treatment With Dihydrotestosterone [DHT] Gel Versus Placebo Gel.
Wake Forest University Health Sciences
7
2012
To map diffusion and clearance rates of this marker in normal and cancerous tissue.
Log cycles, set reminders and visualize serum levels.
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