Alarelin Acetate

Uses

Alarelin acetate is a synthetic GnRH agonist, it can stimulate the release of FSH and LH from the pituitary gland.

Biological Activity

alarelin (gonadotrophin-releasing hormone) is a synthetic gnrh agonist. alarelin is found in higher amounts than that of lh-rh in rat hypophyseal stimulation of gonadotropin secretion in vivo and in vitro and in ovulation inductions. alarelin is known for its induction of ovulation and is used to treat endmometriosis. alarelin acetate is the acetate form of a hypothalamic peptide that stimulates the release of fsh and lh from the pituitary gland.

Cytotoxicity

Cell Assay
The cells are trypsinized in a solution of 2.5 g/L trypsin and seeded in a 96-well plate. After the cells are grown for 24 h to approximately 800 g/L subconfluent state, 0.1 mL medium containing 2.5% calf serum and various concentrations (0.001, 0.1, 10 μM) of alarelin is added to each well, respectively, and incubated for 24 h in a CO2 incubator. Each concentration is tested in at least 12 wells. Briefly, 15 μL of MTT solution is added to each well and incubated for 4 h. Then, the medium and MTT are removed and 150 μL of DMSO is added to each well and shaken for 10 min to dissolve the crystal. The OD is determined at 490 nm using an ELISA reader.
Animal Administration
Rats: Male Sprague-Dawley rats are divided into two groups. In Group I: Gastric acid secretion is measured in a chambered stomach. Briefly, the abdomen is incised, and both the stomach and duodemun are exposed and tied respectively; then 1.5 mL 0.9% sodium chloride (containing Alarelin, 2 μg/kg) is infused into the each chambered stomach. After 15, 30, 45, 60 min, the gastric juice is drew out of the chambered stomach and the pH is measured in the ABL-500 respectively. The control is infused saline instead of Alarelin. In Group II: After anaesthetized, 2 mL Alarelin (2 μg/kg) is administered into the tail vein. The control is injected the saline instead of Alarelin. Then, the stomach and duodenum are tied and infused 1.5 mL saline immediately. After 15, 30, 45, 60 min, the gastric juice is also drew out of the chambered stomach and the pH is measured in the ABL-500 respectively.

in vivo

Description

Alarelin acetate peptide is a single, non-glycosylated polypeptide chain containing 9 amino acids, having a molecular mass of 1167.3 Dalton and a Molecular formula of C₅₆H₇₈N₁₆O₁₂ x C₂H₄O₂. The CAS No. is 79561-22-1.

Background

Alarelin (Gonadotrophin-releasing hormone) is a synthetic LH-RH agonist that is found in higher amounts than that of LH-RH in rat hypophyseal stimulation of gonadotropin secretion in vivo and in vitro and in ovulation inductions. Alarelin is known for its induction of ovulation. Alarelin acetate is the acetate form of a hypothalamic peptide that stimulates the release of FSH and LH from the pituitary gland.

References

[1] Chen L, et al. Expression of gonadotropin-releasing hormone receptor and effect of gonadotropin-releasing hormone analogue on proliferation of cultured gastric smooth muscle cells of rats. World J Gastroenterol. 2004 Jun 15;10(12):1780-4. DOI:10.3748/wjg.v10.i12.1780
[2] Chen L, et al. Distribution, cloning and sequencing of GnRH, its receptor, and effects of gastric acid secretion of GnRH analogue in gastric parietal cells of rats. Life Sci. 2005 Feb 4;76(12):1351-65. DOI:10.1016/j.lfs.2004.10.005