DescriptionSources: http://www.drugbank.ca/drugs/DB00644Curator's Comment:: Description was created based on several sources, including https://www.drugs.com/cdi/gonadorelin.html
Sources: http://www.drugbank.ca/drugs/DB00644
Curator's Comment:: Description was created based on several sources, including https://www.drugs.com/cdi/gonadorelin.html
Gonadorelin is a synthetic decapeptide prepared using solid phase peptide synthesis. GnRH is responsible for the release of follicle stimulating hormone and leutinizing hormone from the anterior pitutitary. In the pituitary GnRH stimulates synthesis and release of FSH and LH, a process that is controlled by the frequency and amplitude of GnRH pulses, as well as the feedback of androgens and estrogens. The pulsatility of GnRH secretion has been seen in all vertebrates, and it is necessary to ensure a correct reproductive function. Thus a single hormone, GnRH, controls a complex process of follicular growth, ovulation, and corpus luteum maintenance in the female, and spermatogenesis in the male. Its short half life requires infusion pumps for its clinical use. Gonadorelin is used for the treatment of amenorrhea, delayed puberty, and infertility the administration of gonadorelin is used to simulate the physiologic release of GnRH from the hypothalamus in treatment of delayed puberty, treatment of infertility caused by hypogonadotropic hypogonadism, and induction of ovulation in those women with hypothalamic amenorrhea. This results in increased levels of pituitary gonadotropins LH and FSH, which subsequently stimulate the gonads to produce reproductive steroids.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1855 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9784092 |
10.0 nM [IC50] | ||
Target ID: Q96P88 Gene ID: NA Gene Symbol: GNRHR2 Target Organism: Homo sapiens (Human) Sources: http://www.drugbank.ca/drugs/DB00644 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Diagnostic | FACTREL Approved UseHypogonadism (diagnosis)—Gonadorelin as a single dose (gonadorelin test) is indicated for evaluation of the functional capacity and response of gonadotropes in the anterior pituitary in postpubertal patients who are suspected of having gonadotropin deficiency, whether due to hypothalamic function impairment alone or in combination with anterior pituitary function failure. Launch Date4.02105598E11 |
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Primary | FACTREL Approved UseAmenorrhea treatment Launch Date4.02105598E11 |
PubMed
Title | Date | PubMed |
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Effects of intravenous cocaine and cigarette smoking on luteinizing hormone, testosterone, and prolactin in men. | 2003 Oct |
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Cross talk in hormonally regulated gene transcription through induction of estrogen receptor ubiquitylation. | 2005 Aug |
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Kisspeptin immunoreactive cells of the ovine preoptic area and arcuate nucleus co-express estrogen receptor alpha. | 2006 Jul 3 |
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Minireview: kisspeptin neurons as central processors in the regulation of gonadotropin-releasing hormone secretion. | 2006 Mar |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/gonadorelin.html
Curator's Comment:: subcutaneous route is possible
Usual Adult Dose for Gonadotropin Deficiency
0.1 mg injected once subcutaneously or intravenously as a single dose.
Usual Adult Dose for Amenorrhea
5 mcg every 90 minutes (range of 1 to 20 mcg) delivered intravenously by a pump over 1 minute, every ninety minutes for 21 days.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1255667
47 ng/ml Gonadorelin induced luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 5 ng, sc measured at 30 mins post dose by RIA (Rvb = 5.3 +/- 1.5 ng/ml)
Substance Class |
Protein
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Sequence Type | COMPLETE |
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9O7312W37G
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EPA PESTICIDE CODE |
116800
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Gonadotropin-releasing hormone analogue
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CHEMBL1007
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DB00644
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3627
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6384
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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Molecular Formula | CHEMICAL |
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