Gonadotropin-releasing hormone (GnRH): features, drugs and analogues

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2018-03-19 12:00:16

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Gonadotropin-releasing hormone (GnRH) is known as a hormone that releases luteinizing hormone (LHRH) and luliberin, which is a trophic peptide hormone responsible for the release of FSH (follicle stimulating hormone) and (LH) luteinizing hormone from the anterior pituitary. GnRH-a hormone synthesized and released in the hypothalamus of GnRH neurons. Is a peptide belonging to the family of gonadotropin-releasing hormone representing sincely stage pituitary-hypothalamo-adrenal system. This article will also include antagonists of gonadotropin-releasing hormone.

antagonists of gonadotropin releasing hormone

Structure

Nobel laureate Andrew V. schally and Roger Hymen said in 1977, characteristics of GnRH ID: piroglu-GIS-TRP-Ser-Tyr-Gli-LEU-Arg-Pro-Gli-NH2. As is customary in the presentation of peptides, the sequence is given from N-to C-Terminus for presentation of the peptide, as usual, and is also standard to omit designation of the chirality, suggesting that amino acids in their L-form are. The above abbreviations refer to the standard proteinogenic amino acids. The exception is piroglu – Pyroglutamate acid, a derivative of the acid glutaminol. C-end NH2 indicates that the chain ends with carboxydomonas instead of a free carboxylate.

Synthesis

The Precursor of gonadotropin-releasing hormone GNRH1 gene is located in chromosome 8 8. Normal mammalian Decapeptide synthesized 92 amino acid pre-prohormone in the front preoptičeskoj division of the hypothalamus. It is a target different mechanisms regulating system of the pituitary-hypothalamo-adrenal axis, ingibiruya by increasing the body's level of estrogen.

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Functionality

gonadotropin releasing hormone price

Gonadotropin-releasing hormone is secreted into the bloodstream of the portal vein pituitary region of the elevation median. GnRH is transported to the pituitary by the blood flow of the portal vein containing gonadotropic cells, where GnRH activates receptors, hormone receptors gonadotropin-releasing, 7 transmembrane receptors, which are associated with G-protein and stimulating the beta-isoform of phosphoinositide phospholipase C, resulting to mobilization of protein kinase C and calcium. This causes the activation of proteins involved in the secretion and synthesis of the gonadotropins FSH and LH. During proteolysis GnRH is cleaved in a few minutes. As a child, her activity is very low, increasing in adolescence or puberty. The success of reproductive function depends on pulsatile activity, which is critical, driven by a feedback loop. But the activity of GnRH during pregnancy is required. Disease or dysfunction, as well as organic damage, type of injuries and tumors of the pituitary gland and hypothalamus can cause disruption pulsational activity. Increased level of prolactin decreases the activity of GnRH and hyperinsulinemia it increases and causes a disturbance in the activity of FSH and LH, as, for example, in the polycystic ovaries. Kallman syndrome is characterized by lack of synthesis of GnRH.

Neurohormones

GnRH can be attributed to the neurohormones. Produces gonadotropin-releasing hormone in preoptičeskoj area of the hypothalamus that contains most of the GnRH-secreting neurons. These neurons occur in the tissues of the nose and migrate into the brain, where the medial wall dissipated and then connect the hypothalamus with the help of long dendrites, more than 1 mm long. In synchronization of GnRH release helps them connecting to the beams to produce a single synaptic input. Using several different transmitters, e.g., GABA, glutamate and norepinephrine are regulated by GnRH-secreting neurons. For example, after the introduction of women's estrogen-progesterone dopamine stimulates the release of LH; after oophorectomy in women dopamine can inhibit the release of LH. The most important regulator of GnRH release kiss-peptid may also be regulated by estrogen. However, it was noted the existence of neurons secreting kiss-Patin and also expressing estrogen receptor alpha.

gonadotropin releasing hormone preparations

It is Important to know what are the agonists of gonadotropin-releasing hormone. This article will information about this.

The effects on other organs

The Role of GnRH in the processes of life in addition to the pituitary and hypothalamus are poorly understood. There is a possibility that it affects the sex glands and placental well as GnRH receptor and GnRH itself have been detected in cancer cells of ovarian, endometrial, prostate and breast cancer.

Influence on behavior

The behavior of the hormone GnRH is also affected. Family taledovich fish showing social dominance, experiences reinforced the regulation of GnRH secretion, when cichlids are socially dependent reduction of regulation of secretion of GnRH. The size of neurons secreting GnRH-dependent behavior and the social environment. More individualistic males are larger GnRH-secreting neurons, Sanchez males are less isolated. Also breeding females have a smaller size of neurons than females in the control group. It speaks about the social regulation of hormone GnRH.

Agonists gonadotropin-releasing hormone will be discussed below.

Medical use

agonists gonadotropin releasing hormone preparations

For the treatment of sick people previously, were prescribed natural GnRH as hydrochloride gonadorelin (Factrel) and diacetoacetate gonadorelin, (Cystorelin). Modification of the structure of GnRH Decapeptide led to the creation of analogues of stimulating or inhibiting the gonadotropins for a longer half-life. And these synthetic analogs were replaced by the natural hormone. Analogue leuprorelin used to treat endometriosis, carcioma breast carcioma prostate, and after some research from the 1980s, including those performed by Dr. Florence by Comicom from the University of Yale, for the treatment of precocious puberty in a continuous infusion.

Gonadotropin-releasing hormone: the price

The Average cost per bottle - from 300 rubles.

analogues of gonadotropin releasing hormone

Sexual behavior in animals

Differences of sexual behavior also is due to the activity of GnRH. For example, the demonstration increased the sexual behavior of females results in an increase in GnRH. From the bald zonotrichia increases the requirement of copulation after administration of GnRH, and in mammals is enhanced by a demonstration of sexual behavior in females, as can be seen in the long-tailed white-toothed shrew and her reduced latent period while demonstrating the rear of the male, and the movement in the direction of the tail. The activity of testosterone of males increases GnRH is increased by excess activity of normal testosterone levels. The deterioration of GnRH causes the aversive effect of reproductive physiology and maternal behavior. If you compare female mice, normal GnRH system, females care more about posterity than with a lower number of neurons is 30%. Most probably, the mouse will leave the pups separately, which will lead to more long searches.

Usage in veterinary medicine

Where applicable gonadotropin-releasing hormone? Drugs are used in veterinary medicine as a remedy for the treatment of cystic ovarian disease in cattle. And its synthetic analogue, deslorelin used for veterinary control of reproductive functions with the help of the implant and a sustained release of the drug.

Consider the analogues of gonadotropin-releasing hormone.

agonists gonadotropin releasing hormone

Agonists and antagonists of gonadotropin-releasing hormone

Separately, a group of drugs which mechanism of action can rightly be called an agonist of gonadotropin-releasing hormone. This means that the impact of this group of drugs on the pituitary gland causes an effect identical to the effect of its own hormone. Representatives of this group include: “Synarel”, “Lucrin Depo Gonapeptyl”. That agonists of gonadotropin-releasing hormone. Drugs are used before and after treatment of fibroids, treatment of endometriosis surgically and prior to removal of the uterus (a hysterectomy) for the treatment of infertility. Active substances under the influence of gastric juice and disintegrate because all drugs administered under the skin, internetline or into a muscle.

gonadotropin releasing hormone

Gonadotropin-releasing hormone antagonists are ‘Cetrotide” (“Cetrorelix”), “Ganirelix” etc.

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Alin Trodden - author of the article, editor
"Hi, I'm Alin Trodden. I write texts, read books, and look for impressions. And I'm not bad at telling you about it. I am always happy to participate in interesting projects."

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