Indications

Gonadorelin is a synthetic decapeptide with a structure identical with the natural Gonadotrophin Releasing Hormone (Gn-RH) in mammalian species.Gonadorelin is recommended for the treatment of reproductive disorders associated with ovarian cysts and for improvement of fertility in cows and for the induction of ovulation in rabbits. The mechanism of action underlying the therapeutic use is the stimulation of the release from and also the synthesis of LH and FSH in the anterior pituitary gland.

Biological Activity

Gonadorelin is a tropic hormone and agonist of the gonadotropin-releasing hormone receptor (GNRHR; Ki = 13 nM in CHO cells expressing the human receptor). It stimulates luteinizing hormone (LH) and follicle- stimulating hormone (FSH) release from rat anterior pituitary cultures when administered at a dose of 0.1 μg. It also stimulates LH release from bovine anterior pituitary cultures at a concentration of 1 μM. In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (Item No. 23555; ED50 = 610.3 ng/kg). Formulations containing gonadorelin have been used as diagnostic agents to assess pituitary gland function.

Safety Profile

A poison by intravenous route. Moderately toxic by ingestion and subcutaneous routes. Experimental reproductive effects. When heated to decomposition it emits acrid smoke and irritating vapors.

Preparation and handling

Gonadorelin (acetate) is supplied as a crystalline solid. A stock solution may be made by dissolving the gonadorelin (acetate) in the solvent of choice. Gonadorelin (acetate) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of gonadorelin (acetate) in ethanol is approximately 0.25 mg/ml and approximately 30 mg/ml in DMSO and DMF. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of gonadorelin (acetate) can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of gonadorelin (acetate) in PBS, pH 7.2, is approximately 10 mg/ml. We do not recommend storing the aqueous solution for more than one day.

Application

Ovarian follicular cysts (veterinary medicine)Use in reproduction medicineDiagnosis of the hypothalamic-pituitary-gonadal axis functionCryptorchismSynchronization of ovulation (veterinary medicine)