Triptorelin is a gonadotropin releasing hormone (GnRH) agonist that is a potent inhibitor of the synthesis of testosterone (in men) and estrogen (in women) and is used to treat advanced prostate cancer.
CAT No: R1945
CAS No:57773-63-4
Synonyms/Alias:TRIPTORELIN;57773-63-4;Triptoreline;Triptorelina;Arvekap;Triptorelinum;Triptodur;(D-Trp6)-GnRH;Triptorelin pamoate;Decapeptyl;tryptorelin;Diferelin;Trelstar;D-Tryptophan-LH-RH;Diphereline;pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2;UNII-9081Y98W2V;CHEBI:63633;CL 118532;CL-118532;CL 118,532;BIM 21003;Wy 42422;[D-Trp6]-LH-RH;Triptoreline [INN-French];Triptorelinum [INN-Latin];Triptorelina [INN-Spanish];AY-25650;DTXSID2048375;Pamorelin;Salvacyl;Trelstar depot;9081Y98W2V;5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolylglycinamide;Trelstar LA;(D-Trp6)-LH-RH;Triptoreline (INN-French);Triptorelinum (INN-Latin);Triptorelina (INN-Spanish);6-D-tryptophan-LH-RH;D-Trp-6-LH-RH;LHRH, Tryptophyl(6)-;Wy 42462;GnRH, Trp(6)-;LHRH, Trp(6)-;Detryptoreline;AY 25650;Trellasar;Moapar;Triptorelin [USAN:INN:BAN];Decapeptyl SR;Pamorelin LA;Triptorelin (swine);Wy-42462;D-Trp6-LHRH;Debio-8206;Triptorelin (USAN/INN);TRIPTORELIN (MART.);GTPL1177;SCHEMBL5079698;CHEMBL1201334;DTXCID8028349;SCHEMBL22289009;L02AE04;VXKHXGOKWPXYNA-PGBVPBMZSA-N;HMS2090C17;EX-A3857;BIM-21003;AKOS030213249;CS-5745;DB06825;NCGC00167301-01;NCGC00167301-02;AS-71149;BN-52014;DA-48936;HY-12551;CL-118,532;C75704;D06247;[D-Trp6]-LH-RH, >=97% (HPLC), powder;AB01275488-01;6-D-Tryptophanluteinizing Hormone-releasing Factor;A936467;EN300-18527985;pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-GlyNH2;Q1992452;BRD-K62685538-001-01-7;(S)-1-((3S,6S,9S,12S,15R,18S,21S)-3-((1H-imidazol-5-yl)methyl)-6,15-bis((1H-indol-3-yl)methyl)-21-(3-guanidinopropyl)-12-(4-hydroxybenzyl)-9-(hydroxymethyl)-18-isobutyl-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;Glycinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolyl-;
Chemical Name:(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-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
Triptorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), widely utilized in biochemical and endocrinological research. As a potent GnRH agonist, it exhibits high affinity for the GnRH receptor, enabling precise modulation of the hypothalamic-pituitary-gonadal (HPG) axis in experimental systems. Its structural modifications confer enhanced metabolic stability and prolonged receptor activation compared to native GnRH, making it a valuable tool for probing neuroendocrine pathways and hormonal regulation mechanisms. Triptorelin's well-characterized action profile and reproducible biological effects have established it as a standard reagent in studies involving reproductive endocrinology, peptide-receptor interactions, and hormone signaling.
Endocrine research: Triptorelin is extensively applied in the investigation of pituitary gonadotropin secretion and feedback regulation within the HPG axis. By stimulating GnRH receptors in pituitary cells, it induces the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), facilitating the study of downstream hormonal cascades. Researchers employ this peptide to dissect the temporal dynamics of gonadotropin release, evaluate receptor sensitivity, and elucidate the molecular basis of hormonal feedback mechanisms in both in vitro and in vivo models.
Receptor binding studies: The high receptor affinity and specificity of triptorelin make it an ideal ligand for characterizing GnRH receptor function and pharmacology. It is frequently used in radioligand binding assays, receptor occupancy experiments, and signaling pathway analyses to assess agonist potency, receptor desensitization, and internalization processes. These applications provide critical insights into receptor-ligand interactions, aiding the development of novel modulators and mapping of receptor distribution in target tissues.
Peptide synthesis validation: Triptorelin serves as a reference standard in peptide synthesis laboratories, where its well-defined sequence and bioactivity offer a benchmark for quality control and process optimization. Analytical chemists utilize it to calibrate chromatographic systems, verify synthetic protocols, and assess peptide purity and stability. Its inclusion in peptide synthesis workflows supports the development of robust methodologies for the production and analysis of complex peptide analogs.
Neuroendocrine signaling research: The compound is instrumental in elucidating the mechanisms of neuroendocrine signal transduction, particularly in the context of hypothalamic control over pituitary function. By acting as a surrogate for endogenous GnRH, triptorelin enables the controlled activation of GnRH pathways, allowing researchers to parse the contributions of specific signaling intermediates and transcriptional regulators. These studies advance the understanding of neuropeptide-mediated communication and its broader physiological implications.
Animal model studies: In preclinical research, triptorelin is utilized to manipulate reproductive hormone levels in animal models, enabling the study of gonadal function, reproductive behavior, and endocrine feedback loops. Its predictable pharmacodynamic properties permit the creation of experimental paradigms that mimic physiological or pathological states, supporting investigations into reproductive biology, developmental endocrinology, and the effects of hormonal modulation on various organ systems. By providing a reliable means to control GnRH signaling, triptorelin underpins a wide range of experimental designs in basic and translational science.
A total of 22 months' worth of data were analyzed (or 1 041 638 total items, monthly average 47 347 items). Goserelin; leuprorelin, and triptorelin are the medicines most used by total quantity in the study period. Simple descriptive statistics show that mean values have declined during the pandemic. The Interrupted Time Series (ARIMA Modeling) shows declining trends.
Ravina Barrett, Robert Barrett, Kalyan Dhar, Gonadorelins adherence in prostate cancer: A time-series analysis of England’s national prescriptions during the COVID-19 pandemic (from Jan 2019 to Oct 2020)
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3. The spatiotemporal control of signalling and trafficking of the GLP-1R
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