Gonadorelin (Decapeptide) GnRH Agonist | High Purity

Product Summary

Gonadorelin, also known as gonadotropin-releasing hormone (GnRH), is a synthetic decapeptide that acts as a potent agonist of the gonadotropin-releasing hormone receptor. It is widely investigated in both preclinical and clinical settings for its role in regulating the hypothalamic-pituitary-gonadal (HPG) axis, its potential applications in various fields of oncology, and its emerging role in neuroprotection. This product is offered as a high-purity research-grade material.

Description

Gonadorelin is chemically identical to the endogenous human GnRH, which is synthesized and released by the hypothalamus. Its primary biological function is to stimulate the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary gland. The therapeutic effects and biological outcomes of Gonadorelin are highly dependent on its mode of administration:

• Pulsatile Administration: Mimics the natural physiological release, leading to stimulation of the pituitary and an increase in LH and FSH secretion, commonly used in fertility treatments.
• Continuous (Non-pulsatile) Administration: Leads to the downregulation and desensitization of the GnRH receptors on the pituitary, resulting in a paradoxical inhibition of gonadotropin release and subsequent suppression of sex hormone production. This mechanism is utilized in treatments for hormone-sensitive cancers and other hormone-dependent conditions.

Properties

The following table summarizes the key properties of the Gonadorelin (Decapeptide) product:

Purity: High Purity (Research Grade)

Form: Crystalline Powder

Solubility: Soluble in water

Peptide Sequence: pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2

Molecular Formula: C55H75N17O13

Molecular Weight:1182.32 g/mol

Target: GnRH Receptor / Pituitary

CAS Number: 51743-69-2

Application and Investigation

Gonadorelin and its synthetic analogs are subject to ongoing research across several medical and biological disciplines.

Endocrine and Reproductive Health

The most established area of research involves its function as a diagnostic agent and therapeutic tool for disorders of the HPG axis.

• Diagnostic Use: Used in the GnRH stimulation test to assess the function of the pituitary gland and diagnose conditions such as delayed puberty or hypogonadotropic hypogonadism.
• Fertility Treatment: Pulsatile administration is studied for the induction of ovulation and spermatogenesis in cases of hypothalamic amenorrhea or infertility caused by GnRH deficiency.

Oncology

Continuous administration of Gonadorelin, or more commonly its long-acting super-agonist analogs, is a cornerstone in the management of hormone-sensitive malignancies.

• Prostate Cancer: Downregulation of the GnRH receptor leads to chemical castration, suppressing testosterone production, which slows cancer progression.
• Breast Cancer: Used in premenopausal women to suppress ovarian function (chemical ovariectomy) to treat estrogen-receptor-positive breast cancer.

Neuroprotection

Emerging research suggests that GnRH receptors are expressed in extra-pituitary tissues, including the central nervous system.

• Cognitive Function: Studies are exploring the potential link between Gonadorelin signaling and neuroprotective effects, particularly in the context of Alzheimer's disease and other neurodegenerative conditions, though this area is highly investigational.

Storage and Handling Protocol

Proper handling and storage are crucial to maintain the integrity and stability of Gonadorelin. Researchers must adhere to the following guidelines:

Important Note: Avoid repeated temperature fluctuations, especially once the powder has been reconstituted. Solutions should be prepared fresh for critical experiments or aliquoted and immediately frozen at -20°C or below.

Safety and Technical Data

This product is for Research Use Only and is not intended for human or animal diagnostic or therapeutic use. Standard laboratory safety protocols should be followed when handling this material.

Preparation of Solution

1. Reconstitution: A suitable sterile solvent, typically sterile water for injection or bacteriostatic water, should be used. The concentration will depend on the experimental protocol.
2. Handling: Wear appropriate personal protective equipment (PPE), including gloves, lab coat, and eye protection. Work in a certified chemical fume hood is recommended, especially during the handling of the dry powder.
3. Disposal: Dispose of all unused material and contaminated waste according to institutional, local, and national regulations.

Chemical Structure

The chemical structure of Gonadorelin is fundamental to its biological activity. The decapeptide sequence dictates its affinity and efficacy at the GnRH receptor.

Mechanism of Action

Gonadorelin exerts its effects by binding to the GnRH receptor (GnRHR), a G protein-coupled receptor primarily located on the gonadotroph cells of the anterior pituitary gland.

• Pulsatile Signaling: When administered in a pulsatile manner (mimicking the physiological release pattern), the binding of Gonadorelin to the GnRHR leads to the activation of the Phospholipase C (PLC) signaling pathway. This ultimately results in a rapid increase in intracellular calcium concentration, which triggers the synthesis and release of LH and FSH into the bloodstream.
• Continuous Signaling (Desensitization): When administered continuously at high doses, the sustained presence of Gonadorelin causes a temporary, reversible downregulation of the GnRHR. This process involves receptor internalization, desensitization, and reduced receptor synthesis, leading to the functional blockade of the HPG axis. The sustained inhibition effectively halts the release of LH and FSH, leading to a profound decrease in peripheral sex hormones (testosterone in males, estradiol in females).

Safety Profile and Considerations

Researchers must be aware of the potent biological activity of Gonadorelin and its impact on the endocrine system. Experiments should be designed with appropriate controls and dosage titration.

• Toxicity: Acute toxicity data are generally low, but chronic administration at pharmacological doses can significantly alter the hormonal balance of research subjects.
• Target Systems: While the primary target is the HPG axis, researchers investigating extra-pituitary GnRH receptors (e.g., in the brain, ovaries, prostate, or immune cells) must consider potential off-target effects related to the peptide's signaling mechanisms.
• Waste Management: All unused research material, solvents, and contaminated materials must be deactivated or disposed of in accordance with established chemical waste protocols.