Chemical Properties
Off-white freeze-dried powder. Soluble in water and saline.
Uses
Gonad-stimulating principle.
Definition
ChEBI: A ten-membered synthetic oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, glycyl, leucyl, arginyl, prolyl and glycinamide residues joined in sequence.
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.
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.
