Elagolix, sold under the brand name Orilissa, is a gonadotropin-releasing hormone antagonist (GnRH antagonist) medication which is used in the treatment of pain associated with endometriosis in women. (wikipedia.org)
Elagolix is a short-acting GnRH antagonist, and can be used to achieve either partial or more substantial suppression of sex hormone levels. (wikipedia.org)
Unlike GnRH agonists and older GnRH antagonists, which are peptides and first-generation GnRH modulators, elagolix is not a GnRH analogue as it is not structurally related to GnRH. (wikipedia.org)
The introduction of elagolix in the United States and Canada was followed by that of relugolix (brand name Relumina), the next second-generation GnRH antagonist, in Japan in January 2019. (wikipedia.org)
Other approved and off-label uses of GnRH antagonists in general are the same as those of GnRHR desensitization therapy with GnRH agonists such as leuprorelin, and include uterine fibroids and breast cancer in premenopausal women, prostate cancer in men, precocious puberty in children, and hormone therapy in transgender adolescents and adults, among others. (wikipedia.org)
It is characterized by the low endogenous GnRH-induced gonadotropin secretion, thus triggering the ovarian blockade and a hypoestrogenic condition. (researchgate.net)
The purpose of this study was, therefore, to evaluate the effects of a long term treatment with orntide, a GnRH antagonist, on testosterone levels and fertility in male rats. (biomedcentral.com)
These results suggest that lack of fertility due to testosterone suppression is reversible after cessation of treatment with this GnRH antagonist. (biomedcentral.com)
They act by hyper-stimulation of GnRH receptors on the gonadotroph cells of the pituitary, resulting in an initial phase of elevated levels of testosterone and androgens, followed by down-regulation of the receptors. (biomedcentral.com)
These are GnRH antagonists, which immediately block the GnRH receptors to access by native GnRH peptides. (biomedcentral.com)
This report is an evaluation of the effect of a long term treatment with a GnRH antagonist, orntide acetate, on the fertility of male rats. (biomedcentral.com)
Cetrorelix (GnRH antagonist) inhibited the preovulatory LH surge induced by OIF in llamas suggesting that LH secretion is modulated by a direct or indirect effect of OIF on GnRH neurons in the hypothalamus. (biomedcentral.com)
In mammals, ovulation implies pulsatile secretion of gonadotropin-releasing hormone (GnRH) from the medio-basal nuclei of the hypothalamus into the hypophyseal portal system, followed by the release of LH from the anterior pituitary into systemic circulation [ 1 ]. (biomedcentral.com)
Agonists2
While the net result of the treatments by agonists and antagonists appears to be the same, two characteristic of the antagonists make it essential to determine whether return to fertility may be a problem and of regulatory interest. (biomedcentral.com)
Synergistic effects of Obatoclax with androgen receptor inactivation can be observed. (oncotarget.com)
Altogether, our results suggest that MCL1 is a key molecule deciding over the fate of PCa cells upon inactivation of androgen receptor signaling. (oncotarget.com)
Hormone3
Moreover, orexins have been reported to greatly influence gonadotropin-releasing hormone neurons and their secretions to regulate reproductive functions via modulation of the hypothalamic-pituitary-gonadal axis. (researchgate.net)
The aim of the present study was to evaluate the expression of receptors for luteinizing hormone-releasing hormone (LHRH) in human specimens of triple-negative breast cancers (TNBC). (uni-luebeck.de)
In addition, we used in vitro and in vivo models of TNBC to investigate if these receptors are suitable targets for the treatment with the LHRH antagonist Cetrorelix. (uni-luebeck.de)
Tumors of mice treated with Cetrorelix expressed less mRNA for EGFR and HER3 receptors than untreated tumors. (uni-luebeck.de)
Given the low toxicity and clinical availability of Cetrorelix, this peptide antagonist should be considered for phase II studies in patients with advanced TNBC. (uni-luebeck.de)
Synergistic1
Synergistic activation of estrogen receptor with combinations of environmental chemicals. (cdc.gov)
Treatment1
The concern is heightened by the likelihood that antagonists will be used for treatment of benign prostatic hypertrophy, a condition in men who might wish at some future time to sire offspring. (biomedcentral.com)
Cells1
Recent research also has thrown lights upon a significant role of orexins, especially orexin A, in regulation of male reproductive functions owing to their receptor expressions in vital testicular cells, such as Leydig cells, Sertoli cells as well as spermatozoa at different developmental stages, even in the epididymis and penis. (researchgate.net)
These drugs intimate dopamine receptors in the brain and prevent the release of prolactin from the pituitary glands. (healthresource4u.com)
Primary1
The primary function of the orexin system, i.e. the orexins, their receptors and associated neuronal circuitries, perhaps is to increase spontaneous physical activity and food intake, thereby promoting an increase in energy expenditure. (researchgate.net)
Expression1
1994. Ah receptor in embryonic mouse palate and effects of TCDD on receptor expression. (cdc.gov)
Release1
Clinically the antagonists differ from the superagonists in that the initial hyper-stimulation and release of LH and FSH do not occur [ 6 ]. (biomedcentral.com)
Pituitary8
The combination of desogestrel and ethinyl estradiol reduces the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary by decreasing the amount of gonadotropin-releasing hormones (GnRHs). (medscape.com)
Gonadotropin-releasing hormone (GnRH) analogues produce a hypogonadotrophic-hypogonadic state by downregulation of the pituitary gland. (medscape.com)
Since GH stimulation by DA via pituitary D1 receptor is well-documented in fish models, the receptor specificity for follistatin regulation by DA was also investigated. (frontiersin.org)
Using a pharmacological approach, the inhibitory effect of DA on follistatin gene expression was confirmed to be mediated by pituitary D1 but not D2 receptor. (frontiersin.org)
Furthermore, activation of D1 receptor by the D1-specific agonist SKF77434 was also effective in blocking follistatin mRNA expression induced by activin and GH treatment both in carp pituitary cells as well as in carp somatotrophs enriched by density gradient centrifugation. (frontiersin.org)
In mammals (e.g., rodents), the activin/follistatin system is a key component for reproductive function both in the pituitary (for gonadotropin regulation) and at the gonadal level (for oocyte/sperm maturation and steroid production) ( 5 ). (frontiersin.org)
In the rat pituitary, activin is expressed mainly in gonadotrophs ( 22 ) and stimulates FSH secretion and gene expression with parallel rise in GnRH receptor expression ( 23 ). (frontiersin.org)
The effects of the dopamine type-2 receptor (D-2) antagonist domperidone on pituitary and brain amine concentrations and serum gonadotropin levels in the goldfish were investigated. (shengsci.com)
Selective Antagonists1
The five most potent 3,5-Ps behaved as selective antagonists of f-Met-Leu-Phe-induced superoxide anion release by neutrophils. (shengsci.com)
GNRH Antagonist1
The introduction of elagolix in the United States and Canada was followed by that of relugolix (brand name Relumina), the next second-generation GnRH antagonist, in Japan in January 2019. (wikipedia.org)
Elagolix1
These studies enabled a comprehensive understanding of elagolix mechanism of action and the downstream pharmacodynamic (PD) effects on gonadotropin and ovarian hormones, as well as full characterization of the PK/PD (PKPD) relationships of elagolix at various dosages, including the approved 150 mg once daily and 200 mg twice daily dosing regimens for the management of moderate to severe pain associated with endometriosis. (nih.gov)
Potent1
The most potent f-Met-Leu-Phe antagonist identified, 1,2-diphenyl-4-(3-(1-naphthyl)-propyl)-3,5-pyrazolidinedione (DPN), may also possess an improved pharmacodynamic specificity compared with phenylbutazone and sulfinpyrazone, as it was less potent than phenylbutazone in the inhibition of prostaglandin synthesis and it was not cytotoxic. (shengsci.com)
Vivo1
In addition, we used in vitro and in vivo models of TNBC to investigate if these receptors are suitable targets for the treatment with the LHRH antagonist Cetrorelix. (uni-luebeck.de)
Patients with advanced1
Given the low toxicity and clinical availability of Cetrorelix, this peptide antagonist should be considered for phase II studies in patients with advanced TNBC. (uni-luebeck.de)
Activity1
To explore the structure-activity relationship of this family of drugs for f-Met-Leu-Phe receptor binding, 36 drugs with the 3,5-P structure, a structure related to antipyrine, or an unrelated structure were tested as competitors for the binding of f-Met-Leu-Phe-Lys-fluorescein isothiocyanate on human neutrophils by flow cytometric analysis. (shengsci.com)
Effective1
Nolvadex - tamoxifen is a popular and very effective selective estrogen receptor modulator (SERM) that is often called an anti-estrogen. (stealthhealth.co)
Similar1
After all, not only are they structurally similar, but they are both classified as estrogen receptor antagonists. (stealthhealth.co)