Metyrapone is an established pharmaceutical compound used for its ability to inhibit adrenal corticosteroid synthesis. It acts primarily on 11β-hydroxylase (CYP11B1), an enzyme involved in the final stages of cortisol biosynthesis.
Its well-defined mechanism makes Metyrapone an important compound in endocrinology, adrenal function assessment, steroidogenesis research, and pharmaceutical development.
Metyrapone is available for qualified pharmaceutical research and formulation requirements, subject to applicable regulatory, quality, and commercial requirements.
Metyrapone has an important role in the evaluation of the hypothalamic-pituitary-adrenal (HPA) axis. Cortisol normally provides negative feedback to the hypothalamus and pituitary. When Metyrapone inhibits cortisol production, this feedback is reduced.
As a result, ACTH secretion increases and the adrenal glands produce increased amounts of cortisol precursors, particularly 11-deoxycortisol. Measurement of this response can provide information about the functional capacity of the HPA axis.
This pharmacological response is the basis of the Metyrapone test, an established endocrine diagnostic procedure.
Metyrapone is also useful as a research compound for studying adrenal steroidogenesis and glucocorticoid biosynthesis.
Its selective inhibition of CYP11B1 allows researchers to investigate:
Metyrapone can be used in pharmaceutical formulation development where a controlled inhibition of cortisol synthesis is required.
Pharmaceutical development activities may include analytical method development, formulation studies, stability evaluation, process development, and quality-control testing.
The final formulation and API specifications should be established according to applicable regulatory requirements and the intended pharmaceutical application.
Cortisol is synthesized through a series of enzymatic reactions within the adrenal cortex. 11β-Hydroxylase catalyzes the conversion of 11-deoxycortisol to cortisol.
Metyrapone inhibits this enzymatic step, resulting in reduced cortisol synthesis and accumulation of precursor steroids.
This specific biochemical action makes Metyrapone a useful pharmacological tool for investigating the pathways involved in adrenal glucocorticoid production.
Metyrapone is recognized as an inhibitor of CYP11B1, also known as steroid 11β-hydroxylase.
CYP11B1 is a mitochondrial cytochrome P450 enzyme expressed primarily in the adrenal cortex. It participates in the production of cortisol and corticosterone.
Inhibition of CYP11B1 by Metyrapone reduces the conversion of 11-deoxycortisol into cortisol. This pharmacological property is central to the clinical and research applications of Metyrapone.
Quality is an important consideration when sourcing Metyrapone for pharmaceutical applications. API quality should be assessed using validated analytical procedures and appropriate quality-control systems.
Key quality attributes may include:
Specifications should be established according to the applicable pharmacopoeial, regulatory, customer, and manufacturer requirements.
Swapproop Drugs and Pharmaceuticals supports the sourcing and supply of Metyrapone for qualified pharmaceutical and research requirements.
The product can be considered for pharmaceutical development, analytical research, formulation studies, and other legitimate applications requiring Metyrapone as an active pharmaceutical ingredient.
Customers can request product specifications, technical documentation, quality information, availability, packaging information, and commercial details according to their requirements.
Metyrapone should be stored according to the conditions specified in the approved product specification, safety documentation, and manufacturer stability data.
Appropriate storage should protect the material from unsuitable temperature, moisture, contamination, and other environmental conditions that could affect its quality.
For commercial supply, the exact storage condition and shelf life should be taken from the current approved manufacturer documentation.
Metyrapone packaging should be selected according to the required quantity, pharmaceutical handling requirements, stability considerations, and applicable regulatory standards.
Packaging information may include:
Actual packaging configuration should be confirmed according to the supplied batch and customer requirements.
Analytical testing plays an important role in confirming the identity, purity, and quality of Metyrapone API.
Depending on the applicable specification, analytical evaluation may include:
Validated analytical methods should be used for release and quality-control testing.
Metyrapone is relevant to research involving:
Endocrinology: Study of adrenal hormone production and HPA-axis function.
Steroidogenesis: Investigation of enzymatic pathways involved in steroid hormone biosynthesis.
CYP11B1 Research: Evaluation of 11β-hydroxylase activity and inhibition.
Cortisol Research: Investigation of cortisol synthesis and regulation.
Adrenal Function: Research into adrenal responsiveness and steroid precursor production.
Pharmaceutical Development: Development and evaluation of formulations containing Metyrapone.
Metyrapone offers several characteristics relevant to pharmaceutical research and development:
Product Name: Metyrapone
CAS Number: 54-36-4
Molecular Formula: C14H14N2O
Molecular Weight: 226.28 g/mol
Chemical Class: Pyridine derivative
Pharmacological Class: Adrenal steroidogenesis inhibitor
Primary Target: CYP11B1 / 11β-hydroxylase
Therapeutic Area: Endocrinology
Primary Application: HPA-axis and adrenal function assessment
Route: Oral
Physical Form: Solid
Metyrapone API is the active pharmaceutical ingredient Metyrapone, a CYP11B1 inhibitor used primarily in endocrine diagnostic applications and pharmaceutical research.
The CAS number of Metyrapone is 54-36-4.
The molecular formula of Metyrapone is C14H14N2O.
The molecular weight of Metyrapone is 226.28 g/mol.
Metyrapone primarily inhibits 11β-hydroxylase (CYP11B1).
Metyrapone is primarily used in the assessment of adrenal function and the HPA axis. It is also used in endocrinology and steroidogenesis research.
Metyrapone inhibits CYP11B1, reducing the conversion of 11-deoxycortisol to cortisol and therefore decreasing cortisol production.
The Metyrapone test is an endocrine diagnostic procedure that evaluates the ability of the hypothalamic-pituitary-adrenal axis to respond when cortisol synthesis is inhibited.
The primary pharmacological target of Metyrapone is 11β-hydroxylase (CYP11B1).
Metyrapone is primarily associated with endocrinology and adrenal function.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | Approximately 88–90°C |