Histrelin is a gonadotropin releasing hormone (GnRH) agonist that is a potent inhibitor of production of testosterone (in men) and estrogen (in women) and is used predominantly to treat advanced prostate cancer. Histrelin is associated with a low rate of transient serum enzyme elevations during therapy, but has not been linked convincingly to cases of clinically apparent acute liver injury.
CAT No: R1965
CAS No:76712-82-8
Synonyms/Alias:histrelin;76712-82-8;Histrelina;Histrelin acetate;Histreline;Histrelinum;Vantaas;ORF 17070;RWJ 17070;Supprelin;Histrelinum [Latin];ORF-17070;UNII-H50H3S3W74;Vantas;BRN 4290557;CHEBI:5739;HSDB 7657;H50H3S3W74;RWJ-17070;ORF 17070RWJ 17070;DTXSID50227543;Histrelinum (Latin);Vantas (TN);HISTRELIN (MART.);HISTRELIN [MART.];5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide;5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-N(tau)-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide;L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-N(im)-benzyl-histidyl-L-leucyl-L-arginyl-L-proline ethylamide;Histreline [French];Histrelina [Spanish];Histrelin [USAN:INN];((ImBl)-D-His(sub 6),Pro(sub 9)-NEt)LHRH;IBHPE-LHRH;HISTRELIN [INN];HISTRELIN [MI];Histrelin (USAN/INN);HISTRELIN [HSDB];HISTRELIN [USAN];5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-Ntau-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide;L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-Nim-benzyl-histidyl-L-leucyl-L-arginyl-L-proline ethylamide;HISTRELIN [VANDF];HISTRELIN [WHO-DD];SCHEMBL17881;5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-N(sup tau)-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide;GTPL3884;CHEMBL1201255;SCHEMBL19409305;SCHEMBL19712198;SCHEMBL22288995;DTXCID00150034;L02AE05;HY-P0056;imbzl-His(6), Pro(9)-NET-GNRH;AKOS030573448;NCGC00181758-01;FH138112;CS-0015085;GnRH, His(imBzl)(6)-N-Et-ProNH2(9)-;LHRH, His(imBzl)(6)-N-Et-ProNH2(9)-;NS00078785;(Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH;D02369;Q5871149;6-His(imBzl)-9-N-Et-ProNH2-10-des-GlyNH2-LHRH;LHRH, histidyl(imBzl)(6)-N-ethylprolinamide(9)-des-glycinamide(10)-;5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-N(sup tau)- benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide;5-OXO-L-PROLYL-L-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TYROSYL-NT-BENZYL-D-HISTIDYL-L-LEUCYL-L-ARGINYL-N-ETHYL-L-PROLINAMIDE;L-Prolinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-(phenylmethyl)-D-histidyl-L-leucyl-L-arginyl-N-ethyl-;Luteinizing hormone-releasing factor (pig), 6-(1-(phenylmethyl)-D- histidine)-9-(N-ethyl-L-prolinamide)-10-deglycinamide-;
Chemical Name:(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-3-(1-benzylimidazol-4-yl)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Histrelin is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH), designed to exhibit enhanced potency and prolonged activity compared to the native hormone. As a peptide compound, it functions as a superagonist at GnRH receptors, leading to profound suppression of gonadotropin secretion upon sustained exposure. Its unique biochemical properties and reliable receptor affinity make it a valuable tool in the study of endocrine signaling, receptor pharmacology, and peptide-based modulation of hormonal pathways. Histrelin's robust activity profile and stability have positioned it as a preferred reagent in various research and development settings focused on neuroendocrinology and peptide therapeutics.
Endocrine signaling research: Histrelin is widely utilized in laboratory investigations focused on the hypothalamic-pituitary-gonadal (HPG) axis. By mimicking and amplifying the actions of endogenous GnRH, it enables precise manipulation of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release in cell-based and animal models. Researchers use it to dissect feedback mechanisms, map receptor-mediated signaling cascades, and elucidate the temporal dynamics of hormone secretion, providing critical insights into reproductive endocrinology and neuroendocrine regulation.
Receptor pharmacology studies: The compound's high affinity and selectivity for GnRH receptors make it an indispensable probe for characterizing receptor-ligand interactions. Histrelin serves as a reference agonist in binding assays, signal transduction experiments, and receptor desensitization studies. Its predictable pharmacodynamics allow for detailed analysis of receptor activation, internalization, and downstream effectors, supporting the development of new peptide analogs and the refinement of GnRH-targeted research tools.
Peptide drug development: As a structurally optimized GnRH analog, histrelin is frequently employed as a model compound in the design and evaluation of novel peptide therapeutics. Its sequence modifications and enhanced metabolic stability provide a benchmark for optimizing pharmacokinetic properties, receptor specificity, and bioactivity of next-generation analogs. Medicinal chemists and peptide engineers utilize it to inform structure-activity relationship (SAR) studies, guide analog synthesis, and validate screening platforms for peptide-based drug discovery.
Neuroendocrine pathway elucidation: Histrelin's ability to modulate central and peripheral hormonal outputs makes it a valuable reagent for mapping neuroendocrine circuits. Experimental protocols employing this peptide facilitate the investigation of neural control over pituitary hormone release, the assessment of feedback inhibition, and the exploration of interactions between the nervous and endocrine systems. Its reproducible effects on hormonal axes are instrumental in advancing the understanding of brain-hormone communication.
Analytical method development: The defined structure and robust bioactivity of histrelin support its use as a standard or control in analytical assays related to peptide quantification and receptor function. It is incorporated into chromatographic, immunoassay, and bioassay platforms to validate detection sensitivity, assess assay specificity, and calibrate analytical instruments. By providing a consistent and well-characterized reference, histrelin enhances the reliability and reproducibility of peptide-focused analytical workflows in research and quality control environments.
2. Immune responses to homocitrulline-and citrulline-containing peptides in rheumatoid arthritis
3. Low bone turnover and low BMD in Down syndrome: effect of intermittent PTH treatment
5. Implications of ligand-receptor binding kinetics on GLP-1R signalling
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