Gonadorelin

Gonadorelin itself (the drug ingredient) IS FDA-approved, but only in specific prescription drug formulations — for example:

  • Factrel® (gonadorelin hydrochloride)
  • Lutrepulse® (no longer sold in the U.S.)


Overview: Gonadorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH). It binds to GnRH receptors (GnRHR) in pituitary gonadotroph cells and is used in research settings to study pulsatile vs continuous GnRH signaling, pituitary physiology, and hypothalamic-pituitary-gonadal (HPG) axis regulation.

  • Pulsatile Exposure: Intermittent administration of GnRH stimulates pituitary gonadotropes, leading to cyclic release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This pattern is frequently modeled in laboratory studies examining reproductive endocrinology.
  • Continuous Exposure: Sustained GnRH exposure can lead to receptor desensitization and downregulation of gonadotropin secretion. This is commonly used in research exploring pituitary suppression, receptor dynamics, and desensitization pathways.
  • HPG Axis Modeling: Gonadorelin is widely used in academic research to investigate hormonal signaling, pituitary responsiveness, feedback mechanisms, and gonadal steroidogenesis under various experimental conditions.
  1. Liu Y, Gong B, Xie W, et al. The pulsatile gonadorelin pump induces earlier spermatogenesis than cyclical gonadotropin therapy in congenital hypogonadotropic hypogonadism men. Am J Mens Health. 2019;13(5):1557988319871375. DOI
  2. Al-Inany HG, Youssef MA, Ayeleke RO, et al. Gonadotrophin-releasing hormone antagonists for assisted reproductive technology. Cochrane Database Syst Rev. 2016;4(4):CD001750. DOI
  3. Bhasin S, Steiner BS, Handelsman DJ, et al. Hormonal effects of GnRH agonist in men. J Clin Endocrinol Metab. 1987;64(3):548–555. DOI
  4. Rashidi B, Haghollahi F, Shariat M, Zayerii F. Effect of GnRH agonist vs hCG on final oocytes for ovulation triggering in IUI. Int J Reprod BioMed. 2017;15(7):433–438. DOI
  5. Pitteloud N, Boepple PA, DeCruz S, et al. The fertile eunuch variant of idiopathic hypogonadotropic hypogonadism. J Clin Endocrinol Metab. 2002;87(9):4460–4465. DOI

*Summaries below reflect preclinical, physiological, or mechanistic insights only—not clinical outcomes.

  • Pituitary Response Studies:
Used to evaluate LH/FSH release patterns following pulsatile versus continuous stimulation.
  • Receptor Regulation:
Supports investigation of GnRHR desensitization, internalization, and receptor-mediated signaling.
  • Endocrine Axis Mapping:
Helps characterize hypothalamic-pituitary interactions in in-vitro and in-vivo research models.
  • Steroidogenesis Pathways:
Employed in studies examining hormonal cascade activation and downstream androgen/estrogen biosynthesis.
  • Developmental Endocrinology Models:
Provides a tool to explore neuroendocrine regulation, feedback mechanisms, and reproductive hormone physiology.

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