ArticleAmerican journal of translational research2025
Sex-dependent endocrine and cellular effects of the GnRH antagonist degarelix in rabbits and cell models.
Article in American journal of translational research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
backgroundDegarelix is a long-acting gonadotropin-releasing hormone (GnRH) antagonist that suppresses gonadotropin and sex steroid secretion via competitive blockade of the GnRH receptor (GnRHR). Although its systemic endocrine effects have been clearly identified, its direct effects on non-pituitary-derived cells, as well as the roles of sex and context-dependent pharmacological properties, remain largely unexplored.
methodsDegarelix was profiled in vitro (HEK293T, CHO-K1 cells) and in vivo (male and female New Zealand rabbits). Cell viability was measured using a cell counting kit-8 (CCK-8) assay. Serum follicle-stimulating hormone (FSH), luteinizing hormone (LH), estradiol (E
resultsIn vitro, degarelix exerted direct, time-dependent, and concentration-dependent effects on the viability of non-pituitary-derived cells (
conclusionThis study systematically demonstrates that degarelix exhibits concentration-dependent, sexually dimorphic, and tissue-specific effects in the regulation of reproductive endocrine functions, as well as direct actions on non-pituitary cells. Furthermore, its direct regulation of non-pituitary cells does not depend on changes in GnRHR protein abundance. These findings provide insight into the mechanisms underlying the antagonistic effects of GnRH and lay a theoretical foundation for the personalized application of degarelix in both experimental and clinical settings.
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