Nafarelin acetate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
CAT No: 10-101-24
CAS No:76932-56-4 (net)
Synonyms/Alias:Synarela;NAFARELIN ACETATE;76932-60-0;Nafarelin acetate anhydrous;TH2HMT9YBQ;UNII-TH2HMT9YBQ;(6-D-(2-Naphthyl)alanine)LHRH acetate;nafarelin acetate (anhydrous);UNII-8ENZ0QJW4H;CHEBI:167202;DTXSID50227720;Nasanyl;NAFARELIN ACETATE (MART.);RS-94991;Synrelina;6-[3-(2-Naphthalenyl)-D-alanine]-luteinizing Hormone-releasing Factor (pig) Acetate Salt; Nafareline Acetate; [6-D-(2-naphthyl)-alanine]LH-RH Acetate;;Nafarelin (acetate);5-OXO-PRO-HIS-TRP-SER-TYR-3-(2-NAPHTHYL)-D-ALA-LEU-ARG-PRO-GLYCINAMIDE ACETATE;Nafarelin Acetate, Hydrate;SCHEMBL166006;(D-2-Nal6)-LHRH Acetate;DTXCID00150211;NAFARELIN ACETATE [WHO-DD];MFCD01716231;AKOS040744807;NAFARELIN ACETATE ANHYDROUS [MI];Nafarelin acetate(76932-56-4 free base);RS-94991298;Q27289963;
Nafarelin Acetate is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), designed to act as a potent regulator of the pituitary-gonadal axis. Characterized by its high affinity for GnRH receptors, this compound is widely recognized for its ability to modulate the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) through receptor agonism followed by downregulation. Its peptide structure, enhanced by specific amino acid substitutions and acetylation, confers increased metabolic stability and bioactivity, making it a valuable tool in diverse biochemical and physiological studies. Researchers appreciate Nafarelin Acetate for its predictable pharmacodynamic profile, which enables precise experimental control over reproductive hormone cascades in various in vitro and in vivo models.
Reproductive Endocrinology Research: Nafarelin Acetate is extensively employed in reproductive endocrinology to investigate the mechanisms underlying gonadotropin regulation and feedback. By mimicking endogenous GnRH while providing longer-lasting effects, it facilitates the study of pituitary desensitization and the suppression of gonadal steroidogenesis in animal models. Scientists utilize this peptide to dissect the temporal dynamics of LH and FSH secretion, analyze downstream gene expression changes, and elucidate the roles of sex steroids in reproductive physiology. Its application in these studies advances the understanding of fertility, reproductive aging, and the pathophysiology of hormone-dependent disorders.
Cancer Biology Studies: In the field of oncology, Nafarelin Acetate serves as a research tool for exploring hormone-responsive tumor growth, particularly in cancers where gonadal steroids play a critical role in cell proliferation. By inducing a reversible hypogonadal state in experimental systems, researchers can assess the impact of sex hormone deprivation on tumor progression, gene expression, and cellular signaling pathways. This approach aids in the identification of molecular targets and therapeutic strategies for hormone-dependent malignancies, including certain subtypes of breast and prostate cancer.
Animal Model Development: The compound is instrumental in the development and validation of animal models that mimic human reproductive disorders. By precisely controlling the hormonal milieu, investigators can induce states such as hypogonadism, delayed puberty, or altered estrous cycling, which are essential for studying disease mechanisms and testing novel interventions. Nafarelin Acetate's predictable action enables reproducible and reversible modulation of endocrine function, facilitating longitudinal studies and cross-species comparisons in translational research.
Neuroendocrine Axis Investigation: Nafarelin Acetate is also utilized to probe the intricate interactions between the central nervous system and the endocrine system. Its ability to modulate GnRH signaling provides a means to examine neuroendocrine feedback loops, neuronal plasticity, and the influence of gonadal hormones on brain development and behavior. Researchers leverage these properties to uncover the neural substrates of reproductive behaviors, stress responses, and neuropsychiatric conditions with hormonal components.
Peptide Drug Development: The role of Nafarelin Acetate extends to the evaluation and optimization of peptide-based therapeutics targeting GnRH receptors. Its well-characterized structure and activity profile make it an ideal reference compound for screening new analogs, assessing receptor binding affinities, and benchmarking in vitro and in vivo efficacy. This work supports the rational design of next-generation peptide drugs with improved pharmacokinetics, selectivity, and safety profiles, contributing to the advancement of peptide therapeutics in endocrinology and related fields.
Nafarelin acetate (less than Glu-His-Trp-Ser-Tyr-3-(2-naphthyl)-D-Ala-Leu-Arg-Pro-Gly-NH2) is a potent agonistic analogue of luteinizing hormone-releasing hormone. After a single iv administration of nafarelin acetate (with 14C label at C-3 of 3-(2-naphthyl)-D-Ala) to female rhesus monkeys, about 80% of the radioactivity was eliminated in urine. Five major radioactive urinary metabolites were isolated and purified by reversed phase HPLC. Four of these metabolites, identified by amino acid analysis, were short peptides: the 5-10-hexapeptide amide, the 6-10-pentapeptide amide, the 5-7-tripeptide, and the 6-7-dipeptide. The fifth metabolite, which accounted for about 15% of the radioactivity administered, was shown by NMR and mass spectrometry to be 2-naphthylacetic acid. A possible pathway of its formation is by oxidative deamination of 3-(2-napthyl)-D-Ala to give the corresponding alpha-keto acid, followed by oxidative decarboxylation of the alpha-keto acid. These five metabolites together accounted for about 70% of the radioactivity recovered in the urine of rhesus monkeys, or more than half of the radioactivity in the administered dose. A minor metabolite, which was not isolated, coeluted with 3-(2-naphthyl)-D-Ala in two solvent systems on HPLC. Nafarelin acetate was also present in small amounts. Several of these metabolites were also present in plasma of the rhesus monkey.
Chan, R. L., & Chaplin, M. D. (1985). Identification of major urinary metabolites of nafarelin acetate, a potent agonist of luteinizing hormone-releasing hormone, in the rhesus monkey. Drug metabolism and disposition, 13(5), 566-571.
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