Gonadorelin
Gonadorelin (GnRH) Acetate
Gonadorelin is a synthetic decapeptide identical in amino acid sequence to native gonadotropin-releasing hormone (GnRH) synthesized in the hypothalamus. In physiological systems, GnRH serves as the master neuroendocrine regulator of reproductive endocrinology, driving the synthesis and pulsatile release of downstream gonadotropins. In experimental models, gonadorelin is extensively utilized to assess the functional capacity and responsiveness of anterior pituitary gonadotrophs. Due to its unmodified native sequence and relatively short biological half-life, it represents an essential reference standard for comparing receptor kinetics against modified GnRH agonists and antagonists. Research applications include mapping signal transduction cascades, evaluating pulsatile versus continuous receptor exposure, and exploring neuroendocrine feedback mechanisms within the hypothalamic-pituitary-gonadal (HPG) axis in cellular and animal models.
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- Purity
- ≥99%
- Form
- Lyophilized powder
- CAS Number
- 33515-09-2
- Molecular Formula
- C55H75N17O13
- Molecular Weight
- 1182.3 g/mol
- Available sizes
- 2mg
Sequence
Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2
Mechanism of Action
Gonadorelin acts by selectively binding to high-affinity G-protein coupled GnRH receptors (GnRHR) on the surface of pituitary gonadotrophs. Receptor activation stimulates the Gq/11 protein pathway, mobilizing phospholipase C to generate inositol 1,4,5-trisphosphate (IP3) and diacylglycerol (DAG), which drives intracellular calcium influx and protein kinase C activation. This downstream signaling cascade promotes the synthesis and exocytosis of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Under sustained or non-pulsatile exposure conditions, gonadorelin causes rapid receptor internalization and desensitization, providing a key mechanism for modeling gonadotropin suppression.
Research Areas
- ●Hypothalamic-pituitary-gonadal (HPG) axis signaling
- ●Pulsatile gonadotropin release kinetics (LH and FSH)
- ●GnRH receptor desensitization and internalization
- ●Comparative receptor binding assays
- ●Endocrine feedback loop modeling
Selected References
- Conn PM et al., Endocrine Reviews, 1986
- Millar RP et al., British Medical Bulletin, 2000
- Kakar SS et al., Mol Cell Endocrinol, 1994
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