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Androstenedione

Sex Hormones & TRT
Andro4-Androstenedione

Overview

Androstenedione, also known as Andro or 4-Androstenedione, is an endogenous steroid hormone and a precursor in the biosynthesis of testosterone and estrogens. It is primarily produced in the adrenal glands and gonads. Chemically, it belongs to the class of androgens, which are steroid hormones that regulate the development and maintenance of male characteristics in vertebrates. Androstenedione is a key intermediate in the conversion of cholesterol to active sex hormones. Researchers have found that androstenedione plays a crucial role in the regulation of sexual differentiation and reproductive function. It serves as a precursor to both testosterone and estrone, a type of estrogen, making it a significant focus in studies related to sex hormone synthesis and metabolism. Its physiological roles extend to influencing muscle mass, bone density, and mood regulation. The mechanism of action of androstenedione involves its conversion to testosterone and estrone, which then bind to androgen and estrogen receptors, respectively. This binding initiates a cascade of biological processes that influence gene expression and cellular function. The pathways involved include the hypothalamic-pituitary-gonadal axis, which regulates the production and release of sex hormones. Pharmacokinetically, androstenedione has a circulating half-life of approximately 70 minutes. It is metabolized primarily in the liver and exhibits poor oral bioavailability due to first-pass metabolism. Researchers have observed that the bioavailability and half-life can vary depending on the route of administration. Clinically, androstenedione has been used in hormone replacement therapy and as a dietary supplement, although its use is controversial and regulated in many countries. In the United States, it is classified as a controlled substance due to its potential for abuse and side effects. Regulatory agencies have restricted its use, and it is not approved by the FDA for therapeutic use.

Mechanism of Action

Androstenedione acts primarily through its conversion to testosterone and estrone, which then bind to androgen and estrogen receptors. This binding triggers a series of biological events that regulate gene expression and influence cellular processes related to sexual development and reproduction.

Molecular Data

FormulaC19H26O2
Molecular Weight286.4 g/mol
CAS Number63-05-8
PubChem CID6128

Half-Life & Pharmacokinetics

EndogenousCirculating half-life ~70 minutes
OralPoor bioavailability due to first-pass

Bioavailability and half-life can vary significantly depending on the route of administration.

Storage

Temperature

Store at room temperature (15-30°C)

Light

Protect from light

Form

Stable in solid form for extended periods

Notes

Avoid exposure to moisture and extreme temperatures.

Solubility

Androstenedione is poorly soluble in water but more soluble in organic solvents like ethanol.

Legal Status

🇩🇪DE

Verschreibungspflichtig (prescription only); not listed under BtMG.

🇺🇸US

Classified as a controlled substance; not approved by the FDA for therapeutic use.

🇦🇺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.

10 Research Publications

Andrographolide suppresses chondrosarcoma cell migration and invasion by inhibiting the PI3K/Akt/mTOR signaling pathway and activating autophagy.

Unknown

Frontiers in oncology · 2025

Researchers found that andrographolide, a compound derived from a plant, can reduce the movement and spread of chondrosarcoma cells, a type of bone cancer. They observed that this effect is linked to the inhibition of certain cellular pathways and the activation of autophagy, a process that helps cells recycle and remove damaged components.

  • Andrographolide suppresses chondrosarcoma cell migration and invasion.
  • The compound targets key signaling pathways, including PI3K/Akt/mTOR.
  • Andrographolide promotes autophagy, enhancing cellular health.
PubMed

Unknown

ACS infectious diseases · 2024

Researchers found that cholesterol serves as an important source of carbon for certain biological processes. This discovery could help in understanding how cholesterol impacts health and metabolism. Further research may reveal more about its role in various diseases.

  • Cholesterol is a key carbon source.
  • Understanding its role could impact health insights.
  • Further research is needed to explore its effects on diseases.
PubMed

Andrographolide exhibits antinociceptive effects in neuropathic rats via inhibiting class Ⅱ MHC associated response and regulating synaptic plasticity.

Animal

Phytomedicine : international journal of phytotherapy and phytopharmacology · 2024

Researchers found that Andrographolide, a compound from the Andrographis paniculata plant, can reduce neuropathic pain in rats by influencing inflammation and improving nerve function. They observed that Andrographolide was more effective than the traditional pain medication Gabapentin in alleviating pain symptoms.

  • Andrographolide significantly reduced neuropathic pain in rat models.
  • It was found to be more effective than Gabapentin for pain relief.
  • The compound works by modulating inflammation and enhancing nerve function.
PubMed

Phase 3 Trial of Crinecerfont in Pediatric Congenital Adrenal Hyperplasia.

Human

The New England journal of medicine · 2024

Researchers found that crinecerfont, a new oral medication, effectively reduced elevated androstenedione levels in children with congenital adrenal hyperplasia (CAH) compared to a placebo. Additionally, participants taking crinecerfont were able to lower their glucocorticoid doses while maintaining hormone control, suggesting a safer treatment option for managing CAH.

  • Crinecerfont significantly decreased androstenedione levels in children with CAH.
  • Participants on crinecerfont reduced their glucocorticoid doses by 18% while maintaining hormone control.
  • Common side effects included headache, fever, and vomiting.
PubMed

Phase 3 Trial of Crinecerfont in Adult Congenital Adrenal Hyperplasia.

Human

The New England journal of medicine · 2024

Researchers observed that crinecerfont, a new oral medication, significantly reduced the need for glucocorticoid treatment in adults with congenital adrenal hyperplasia (CAH) while effectively controlling hormone levels. Compared to a placebo, patients taking crinecerfont experienced a greater decrease in glucocorticoid dosage and improved hormone balance.

  • Crinecerfont led to a 27.3% reduction in glucocorticoid dose compared to 10.3% in the placebo group.
  • 63% of patients on crinecerfont achieved a physiologic glucocorticoid dose, compared to 18% on placebo.
  • Androstenedione levels decreased significantly in patients taking crinecerfont.
PubMed

Anti-Müllerian hormone a surrogate of follicular fluid oxidative stress in polycystic ovary syndrome?

Unknown

Frontiers in cell and developmental biology · 2024

Researchers found that Anti-Müllerian hormone (AMH) may not only indicate ovarian reserve but could also reflect oxidative stress levels in women with polycystic ovary syndrome (PCOS). This connection suggests that AMH might be useful in understanding the reproductive challenges associated with PCOS.

  • AMH is a marker for ovarian reserve and morphology in PCOS.
  • Oxidative stress negatively impacts reproductive health, including in PCOS.
  • The study explores the link between AMH levels and oxidative stress in follicular fluid.
PubMed

Neuroprotection of Andrographolide against Neurotoxin MPP

Unknown

International journal of molecular sciences · 2023

Researchers observed that andrographolide, a compound with various health benefits, may protect brain cells from damage caused by a neurotoxin linked to Parkinson's disease. This protection could help counteract the harmful effects of oxidative stress and improve cell function.

  • Andrographolide shows potential neuroprotective effects against neurotoxin MPP.
  • It may help reduce oxidative stress and improve mitochondrial function.
  • Andrographolide has been studied for its anti-inflammatory and other health benefits.
PubMed

The andro-accelerator hypothesis.

Human

JPMA. The Journal of the Pakistan Medical Association · 2020

Researchers observed that while testosterone levels typically decrease with age, certain external factors can actually boost testosterone production in middle-aged men. This phenomenon, explained by the andro-accelerator hypothesis, suggests that social and environmental influences can reset hormonal levels, leading to inappropriate behaviors. The study emphasizes the importance of addressing testosterone imbalances rather than simply viewing age-related changes as a medical condition.

  • Testosterone levels decline with age but can be influenced by external stimuli.
  • Social and environmental factors may increase testosterone production in middle-aged men.
  • The study advocates for addressing hormonal imbalances rather than treating age-related changes as a disease.
PubMed

Oral andro-related prohormone supplementation: do the potential risks outweigh the benefits?

Review

Canadian journal of applied physiology = Revue canadienne de physiologie appliquee · 2003

Researchers found that the claims made by manufacturers about the benefits of Andro prohormones, such as increased testosterone and muscle mass, are largely unsupported by evidence. Instead, they observed that these supplements may raise estrogen levels and increase the risk of certain cancers and cardiovascular issues, raising concerns about their long-term use.

  • Andro prohormones do not significantly improve testosterone levels or muscle strength as claimed.
  • Use of Andro can lead to elevated estrogen levels, potentially increasing cancer risk.
  • Long-term use may raise the risk of cardiovascular disease due to negative effects on blood lipids.
PubMed

[Endocrine maturation].

Unknown

Anales espanoles de pediatria · 1983

Researchers observed that the onset of puberty is linked to changes in hormone sensitivity and may involve the adrenal glands and pineal gland. They found that genetic factors regulate pubertal development, and bone age is a better indicator of growth than chronological age.

  • The start of puberty is triggered by decreased sensitivity to sexual hormones.
  • The adrenal glands and pineal gland may play significant roles in this process.
  • Bone age is a more accurate measure of development than chronological age.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.