Gonadorelin

Chemical Properties

Off-white freeze-dried powder. Soluble in water and saline.

Uses

Gonad-stimulating principle.

Uses

Gonadorein is a Gonadotropin-releasing hormone. Gonadorelin agonist treatment for men with locoregional prostate cancer may be associated with an increased risk of incident diabetes and ardiovascular disease.

Definition

ChEBI: Gonadorelin is a ten-membered synthetic oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, glycyl, leucyl, arginyl, prolyl and glycinamide residues joined in sequence. It has a role as a gonadotropin releasing hormone agonist. It is an oligopeptide and a peptide hormone.

brand name

Lutrepulse (Ferring Pharmaceuticals).

Biological Activity

luteinizing hormone releasing hormone human acetate salt (lhrh) is a selective acitivator of mmp-2 and mmp-9 [1, 2].luteinizing hormone-releasing hormone (lhrh), also known as gonadotropin-releasing hormone (gnrh) is a trophic peptide hormone which secreted by gnrh neurons and plays an important role in the release of follicle-stimulating hormone (fsh) and luteinizing hormone (lh) from the anterior pituitary [3].mmp-2 (matrix metalloproteinase-2) and mmp-9 (matrix metalloproteinase-9) belong to the mmp family that play an important role in the breakdown of extracellular matrix (ecm) in normal physiological processes, for example, embryonic development, reproduction, and tissue remodeling, as well as in disease processes, such as arthritis and metastasis [2].when tested with ishikawa and ecc-1 cell lines, lhrh resulted in the increase of mmp-9 expression which induced cell invasion and it was also showed that gpr101 mediated the lhrh activity and cooperated to function in the metastatic potential of endometrial cancer cells [1]. in human decidual endometrial stromal cells, lhrh with its receptor induced the activation of mmp-2 and mmp-9 [2].

Side effects

If you experience a rare allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives) to gonadorelin, seek emergency medical attention.
Other less serious side effects may also occur. Notify your doctor if you experience: headache; flushing; nausea or abdominal discomfort; dizziness or lightheadedness; pain, swelling, or itching at the injection site; or skin rash.

Veterinary Drugs and Treatments

Gonadorelin is indicated (approved) for the treatment of ovarian follicular cysts in dairy cattle. Additionally, gonadorelin has been used in cattle to reduce the time interval from calving to first ovulation and to increase the number of ovulations within the first 3 months after calving. This may be particularly important in increasing fertility in cows with retained placenta.
In dogs, gonadorelin has been used experimentally to help diagnose reproductive disorders or to identify intact animals versus castrated ones by maximally stimulating FSH and LH production. It has also been used experimentally in dogs to induce estrus through pulsatile dosing. While apparently effective, specialized administration equipment is required for this method.
Gonadorelin has been used in cats as an alternate therapy to FSH or hCG to induce estrus in cats with prolonged anestrus.
In Europe, a synthetic analogue buserelin has been used in horses to stimulate cyclic estrus. Its efficacy rates poorly when compared to an artificial light program, however.
In human medicine, gonadorelin has been used for the diagnosis of hypothalamic-pituitary dysfunction, cryptorchidism, and depression secondary to prolonged severe stress.

Description

Lutenizing Hormone Releasing Hormone Human Synthetic is a single, non-glycosylated, polypeptide chain containing 10 amino acids and having a molecular mass of 1182.2 Dalton. The molecular formula is C₅₅H₇₅N₁₇O₁₃.C₂H₄O₂. The CAS Number is 71447-49-9.

Background

Gonadotropin-releasing hormone 1 (GNRH1), also known as Luteinising-hormone releasing hormone (LHRH), is a peptide hormone responsible for the release of FSH and LH from the anterior pituitary. GNRH1 is synthesized and released by the hypothalamus.
At the pituitary, GNRH1 stimulates the synthesis and secretion of the gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH). These processes are controlled by the size and frequency of GNRH1 pulses, as well as by feedback from androgens and estrogens. Low requency GNRH1 pulses lead to FSH release, whereas high frequency GNRH1 pulses stimulate LH release.
There are differences in GNRH1 secretion between males and females. In males, GNRH1 is secreted in pulses at a constant frequency, but in females the frequency of the pulses varies during the menstrual cycle and there is a large surge of GNRH1 just before ovulation.
GNRH1 secretion is pulsatile in all vertebrates, and is necessary for correct reproductive function. Thus, a single hormone, GNRH1, controls a complex process of follicular growth, ovulation, and corpus luteum maintenance in the female, and spermatogenesis in the male.

References

[1]. cho-clark, m., et al., gnrh-(1-5) activates matrix metallopeptidase-9 to release epidermal growth factor and promote cellular invasion. mol cell endocrinol, 2015.
[2]. wu, h.m., et al., gonadotropin-releasing hormone type ii (gnrh-ii) agonist regulates the motility of human decidual endometrial stromal cells: possible effect on embryo implantation and pregnancy. biol reprod, 2015. 92(4): p. 98.
[3]. garnick, m.b. and m. campion, abarelix depot, a gnrh antagonist, v lhrh superagonists in prostate cancer: differential effects on follicle-stimulating hormone. abarelix depot study group. mol urol, 2000. 4(3): p. 275-7.