Development and therapeutic effect of deserelin acetate

Background

Deslorelin acetate is a kind of injectable gonadotropin releasing hormone (GnRH) agonist.

One way of doing business with deserelin acetate is to market peptech with the brand name ovuplant. Another method is available abroad, sucromate equine, which was approved by FDA in November 2010 for mounting. It was manufactured by thornebo science LLC and then entered the U.S. market. Ovuplant withdrew. Deslorelin is currently licensed for veterinary medicine and ovulation promotion in mares as part of the whole process of artificial insemination. It is also used to stabilize high-risk pregnancies, mainly livestock. Unlike other GnRH agonists, the key to inhibiting luteinizing hormone and follicle stimulating hormone can be based on the final decline of the above pituitary gland, dilorelin is mainly used in the above pituitary original light spot effect, as well as the associated surge in LH metabolism.

Suprelorin is a slowly released deslorelin prosthesis for chemical castration of dogs and ferrets. It is sold in the virbac market. Deslorelin was also used to treat benign prostatic hyperplasia in dogs. Deslorelin has been developed and designed for the treatment of endometriosis, polycystic ovary syndrome, precocious puberty, prostate cancer and uterine tumor, and has achieved the phase III clinical study of prostate cancer, but the development of all the indications has been terminated by 2001.

Gonadotropin releasing hormone (GnRH) is a kind of releasing hormone, which undertakes to release follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is a kind of subtropical peptide hormone, which is produced and released by GnRH neurons in hypothalamus. The peptide belongs to the GnRH family. It forms the initial process of the hypothalamus pituitary gonadal axis.

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Deslorelin acetate is metabolized in the blood of pituitary portal vein. The portal vein blood nocturnal zone carries GnRH to the pituitary gland, where it contains gonadotropic gland cells, where GnRH activates its own receptor, gonadotropin releasing hormone receptor (GnRHR), an isophosphoinositide phospholipase C that stimulates the beta seven transmembrane G-protein-coupled receptor, which moves forward to encourage calcium and protein kinase C. This leads to the activity of proteins involved in the production and metabolism of gonadotropins LH and FSH.

When GnRH was de graded, the protein hydrolysis reaction would take place within more than ten minutes. GnRH activity was very low in childhood and activated in adolescence or adolescence. Pulse activity is particularly important for successful reproduction during the reproductive age, which is controlled by feedback loops. However, once the pregnancy is defined, GnRH activity is not required. Hypothalamic pituitary disorders, dysfunction (i.e., hypothalamic suppression) or organic lesions (trauma, tumor) can destroy pulsatile activity. Elevated prolactin levels reduced GnRH activity. Hyperinsulinemia, in turn, increases pulse activity, leading to confusion in LH and FSH activity, as shown by polycystic ovary syndrome. （PCOS）。 In Kallmann syndrome, GnRH production is absent in the first place.

Application

The previous requirement for natural GnRH was the use of factrel and cystorelin in the treatment of human diseases. Modification of the decapeptide structure of GnRH to increase the half-life leads to gnrh1 analogue drug stimulation (gnrh1 agonist) or inhibition (GnRH antagonist) of gonadotropins. The analogues have replaced natural hormones in clinical medicine. In the 1920's, it was used by Dr. Yale University to treat endometrial cancer of the prostate, which is similar to that used in the treatment of endometrial cancer by Dr. Yale University of Italy.

At the end:

Deserelin acetate is used as an organic and pharmaceutical intermediate. Gutuo Biotechnology Co., Ltd. is a professional manufacturer of peptide synthesis and peptide customization. It also supplies the raw materials of deserelin acetate. Companies who need to buy API are welcome to purchase.

For any requests of Peptide for research purpose, welcome to contact us. www.gtpeptide.com , sales1@gotopbio.com.