Histrelin acetate 

Histrelin acetate, a GnRH analogue, is a GnRH Receptor agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis^[1][2][5].

Histrelin (10-100 nM) acetate stimulates the release of vasopressin (VP) from from isolated rat hypothalamo-neurohypophysial explants^[4].
Histrelin (100 nM) acetate stimulates oxytocin (OT) release from the rat hypothalamo-neurohypophysial system^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Histrelin (0.1 mg/kg, subcutaneous injection) acetate rescues the circulating LH concentrations in Csfm^op/Csfm^op mice^[2].
Histrelin (10,30, or 100 μg /day, subcutaneous injection) acetate reduces the number of endometrial glands and atrophied the stroma in rabbits^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1323.50 (free base)

C₆₆H₈₆N₁₈O₁₂.xC₂H₄O₂

220810-26-4

Solid

White to off-white

{Pyr}-His-Trp-Ser-Tyr-{d-His(Bzl)}-Leu-Arg-Pro-{NHEt}

{Pyr}-HWSY-{d-His(Bzl)}-LRP-{NHEt}

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Emma D Deeks, et al. Histrelin: in advanced prostate cancer. Drugs. 2010 Mar 26;70(5):623-30.  [Content Brief]

  [2]. Marlena Juszczak, et al. Hypothalamic gonadotropin-releasing hormone receptor activation stimulates oxytocin release from the rat hypothalamo-neurohypophysial system while melatonin inhibits this process. Brain Res Bull. 2010 Jan 15;81(1):185-90.  [Content Brief]

  [3]. P E Cohen, et al. Colony-stimulating factor-1 plays a major role in the development of reproductive function in male mice. Mol Endocrinol. 1997 Oct;11(11):1636-50.  [Content Brief]

  [4]. D W Hahn, et al. Development of an animal model for quantitatively evaluating effects of drugs on endometriosis. Fertil Steril. 1985 Sep;44(3):410-5.  [Content Brief]

  [5]. E Boczek-Leszczyk, et al. Vasopressin release from the rat hypothalamo-neurohypophysial system: effects of gonadotrophin-releasing hormone (GnRH), its analogues and melatonin. J Physiol Pharmacol. 2010 Aug;61(4):459-66.  [Content Brief]