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: 10-101-211
CAS No:76932-56-4, 76932-60-0, 86220-42-0
Synonyms/Alias:NAFARELIN;76932-56-4;Nafareline;NAFARELIN ACETATE;Nafarelina;Nafarelinum;Nafarelinum [Latin];UNII-1X0094V6JV;LHRH, Ala(2-naphthyl)(6)-;1X0094V6JV;Nafarelinum (Latin);Nafareline [French];Nafarelina [Spanish];Nafarelin [INN:BAN];(S)-1-(((R)-2-((S)-2-((S)-2-((S)-2-((S)-3-(1H-imidazol-4-yl)-2-((S)-5-oxopyrrolidine-2-carboxamido)propanamido)-3-(1H-indol-3-yl)propanamido)-3-hydroxypropanamido)-3-(4-hydroxyphenyl)propanamido)-3-(naphthalen-2-yl)propanoyl)-L-leucyl-L-arginyl)-N-(2-amino-2-oxoethyl)pyrrolidine-2-carboxamide;NAFARELIN [INN];CHEBI:7445;Nafarelin?;HS-2018;NAFARELIN [MI];NAFARELIN [VANDF];NAFARELIN [WHO-DD];SCHEMBL22518;BIDD:GT0760;GTPL3902;6-D-(2-naphthyl)alanyl-GnRH;BDBM84707;H01CA02;DTXSID001031284;(6-D-(2-naphthyl)alanine)-GnRH;AKOS015895038;CCG-270673;DB00666;FN65097;NS00078790;C76463;EN300-7480908;Q3869873;5-OXOPRO-HIS-TRP-SER-TYR-D-NAL(2)-LEU-ARG-PRO-GLY-NH2;(2S)-N-(2-amino-2-oxoethyl)-1-((2S,5S,8R,11S,14S,17S,20S)-2-(3-carbamimidamidopropyl)-11-(4-hydroxybenzyl)-14-(hydroxymethyl)-20-(1H-imidazol-4-ylmethyl)-17-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-8-(naphthalen-2-ylmethyl)-4,7,10,13,16,19,22-heptaoxo-22-((2S)-5-oxopyrrolidin-2-yl)-3,6,9,12,15,18,21-heptaazadocosan-1-oyl)pyrrolidine-2-carboxamide;(S)-1-((3S,6S,9S,12S,15R,18S,21S)-3-((1H-imidazol-5-yl)methyl)-6-((1H-indol-3-yl)methyl)-21-(3-guanidinopropyl)-12-(4-hydroxybenzyl)-9-(hydroxymethyl)-18-isobutyl-15-(naphthalen-2-ylmethyl)-1,4,7,10,13,16,19-heptaoxo-1-((S)-5-oxopyrrolidin-2-yl)-2,5,8,11,14,17,20-heptaazadocosan-22-oyl)-N-(2-amino-2-oxoethyl)pyrrolidine-2-carboxamide;5-oxo-L-prolyl L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-3-(2-naphthyl)-D-alanyl-L-leucyl-L-arginyl-L-prolylglycinamide;L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-3-(2-naphthyl)-D-alanyl-L-leucyl-L-arginyl-L-prolyl-glycinamide;
Nafarelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), structurally optimized to enhance receptor affinity and metabolic stability for research applications. As a potent GnRH agonist, it mimics endogenous GnRH while providing extended bioactivity, making it a valuable tool in the study of reproductive endocrinology and neuroendocrine regulation. Its well-characterized mechanism of action involves initial stimulation followed by downregulation of pituitary gonadotropin secretion, enabling nuanced exploration of hormone signaling pathways. Nafarelin's robust biochemical profile and receptor selectivity have established it as a preferred reagent for investigating the hypothalamic-pituitary-gonadal (HPG) axis, peptide-receptor interactions, and related cellular responses.
Endocrine signaling research: Nafarelin serves as a critical probe in elucidating the dynamics of GnRH receptor activation and desensitization within pituitary cell models. By precisely modulating luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release, it enables researchers to dissect the temporal and dose-dependent aspects of gonadotropin regulation. Such studies are foundational for understanding reproductive hormone control, feedback mechanisms, and the molecular underpinnings of endocrine disorders.
Reproductive physiology studies: In experimental settings, this decapeptide is frequently employed to investigate the physiological consequences of altered GnRH signaling on gonadal function. Its ability to induce both upregulation and subsequent suppression of gonadotropin release allows for controlled modeling of reproductive axis disruption. This is particularly valuable in studies focused on gametogenesis, steroidogenesis, and the broader impacts of HPG axis modulation in animal and cellular systems.
Peptide receptor characterization: As a highly specific GnRH agonist, nafarelin is instrumental in characterizing the binding kinetics, signal transduction pathways, and receptor internalization processes of GnRH receptors. Researchers utilize it to map receptor-ligand interactions, assess downstream effector activation, and explore receptor subtype selectivity. These insights contribute to the development of new peptide analogs and the refinement of receptor-targeted research tools.
Neuroendocrine pathway analysis: Nafarelin's defined mechanism facilitates investigations into the neuroendocrine integration of reproductive and metabolic cues. By modulating central and peripheral hormone levels in controlled experimental paradigms, it aids in delineating the crosstalk between the central nervous system and endocrine organs. Such applications are essential for advancing the understanding of neuropeptide-driven regulatory networks and their roles in physiological adaptation.
Peptide analog development: The structural features and bioactivity profile of nafarelin make it a valuable reference compound in the design and optimization of novel GnRH analogs. Researchers in peptide chemistry and drug discovery utilize it as a benchmark for evaluating new synthetic peptides, guiding modifications to enhance receptor specificity, metabolic stability, or signaling properties. Its use in comparative studies supports the iterative development of next-generation peptide-based research reagents.
4. The spatiotemporal control of signalling and trafficking of the GLP-1R
5. Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes
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