Description
Deslorelin is an injectable gonadotropin releasing hormone super-agonist also known as an LHRH agonist. It stops the production of sex hormones with potential antineoplastic activity. Deslorelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Continuous, prolonged administration of goserelin in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.
Chemical Properties
White powder, tens of times more biologically active than natural LH-RH, is synthesized by solid-phase or liquid-phase synthesis method using the corresponding protected amino acid monomers as raw materials.
Uses
Induction of ovulation in estrous mares
Reproduction control in dogs
Definition
ChEBI: Deslorelin is an oligopeptide.
brand name
Somagard [as acetate] (Roberts Pharmaceutical).
General Description
Deslorelin (brand names: SucroMate, Suprelorin F, Suprelorin 12, Suprelorin-6) is a synthetic hormone used to induce ovulation and manage artificial insemination programs in horses, modulate reproduction in dogs, or manage adrenal disease in ferrets. In the U.S., deslorelin is only FDA approved for use in mares and ferrets, and 'off label' or 'extra-label' use is prohibited at this time.
Side effects
The most common side effects include swelling, sensitivity, and redness or warmth at the injection site. Rarely reported side effects in dogs include prolonged estrus and uterine infections.
Veterinary Drugs and Treatments
Deslorelin is approved for inducing ovulation in estrual mares.
There is also interest in developing dosages and dosage forms as a
long-term, reversible contraceptive in a variety of animal species, as
a treatment for prostatic disease in male dogs, and incontinence in
ovariectomized dogs. At the time of writing, deslorelin in not available
in the USA, but is marketed in Canada.
In humans, deslorelin has been investigated for treating children
with precocious puberty, and in adults for prostate carcinoma, dysmenorrhea,
fibroids, and endometriosis.
Description
Deslorelin is a potent LHRH/GnRH agonist has a molecular formula of C
64H
83N
17O
12, pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHC
2H
5 having an Mw of 1284.4 Dalton.
Background
Deslorelin is being studied in the treatment of cancer as a way to block sex hormones made by the ovaries or testicles. It belongs to the family of drugs called gonadotropin-releasing hormone analogs. It is used for the induction of ovulation in mares. Deslorelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Continuous, prolonged administration of goserelin in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.
References
[1] CLAIRE GROSSET. Contraceptive effect and potential side-effects of deslorelin acetate implants in rats (Rattus norvegicus): preliminary observations.[J]. Canadian journal of veterinary research = Revue canadienne de recherche veterinaire, 2012, 76 3: 209-214.
[2] STEFANO ROMAGNOLI. Chronic Use of Deslorelin in Dogs: Six Cases (2005-2022).[J]. Animals, 2023, 13 2. DOI:
10.3390/ani13020265.
[3] K E OERTER. Adult height in precocious puberty after long-term treatment with deslorelin.[J]. Journal of Clinical Endocrinology & Metabolism, 1991, 73 6: 1235-1240. DOI:
10.1210/jcem-73-6-1235.
