Leuprolide is a synthetic nonapeptide analogue of gonadotropin-releasing hormone. Leuprolide binds to and activates gonadotropin-releasing hormone (GnRH) receptors. Continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production. This agent reduces testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression.
CAT No: R1949
CAS No:53714-56-0
Synonyms/Alias:Leuprorelin;leuprolide;53714-56-0;Leuproreline;Leuprorelinum;Leuporelin;Leuprorelina;(-)-leuprolide;UNII-EFY6W0M8TG;EFY6W0M8TG;TAP-144 FREE BASE;CCRIS 8462;CHEBI:6427;HSDB 6518;CKD-841;Leuprorelin slow release;ABBOTT-43818 FREE BASE;Leuproreline [INN-French];Leuprorelinum [INN-Latin];NSC 377526;NSC-377526;Leuprorelina [INN-Spanish];DTXSID50872411;(D-Leu(sup 6),des-gly-NH2(sup 10),pro-ethylamide(sup 9))-GNRH;(D-Leu(sup 6),des-gly-NH2(sup 10),pro-ethylamide(sup 9))-LHRH;Leuproreline (INN-French);Leuprorelinum (INN-Latin);Leuprorelina (INN-Spanish);LEUPRORELIN (MART.);LEUPRORELIN [MART.];5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide;pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHC2H5;Leuprorelin acetate (JAN);Leuprolide acetate (USAN);LEUPRORELIN (EP MONOGRAPH);LEUPRORELIN [EP MONOGRAPH];5-OXO-L-PROLYL-L-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TRYOSYL-D-LEUCYL-L-LEUCYL-L-ARGINYL-N-ETHYL-L-PROLINAMIDE;L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-L-proline ethylamide;LEUPRORELIN [INN];MFCD00167544;Leuprolide acetate salt;Leuprorelin [INN:BAN];Leuprorelin?;Leuprolide TFA;LEUPROLIDE [MI];LEUPROLIDE [HSDB];LEUPROLIDE [VANDF];SCHEMBL4585;LEUPRORELIN [WHO-DD];GTPL1175;CHEMBL1201199;DTXCID00820063;L02AE02;GFIJNRVAKGFPGQ-LIJARHBVSA-N;BDBM50369395;AKOS015892744;AKOS030213246;AKOS037515838;CCG-270656;CS-4947;DB00007;HS-2016;NCGC00485984-01;DA-64932;HY-12553;Leuprolide acetate salt, >=98% (HPLC);C75519;pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt;EN300-7481165;Fensolvi (leuprolide acetate injectable suspension);Q907160;BRD-K26323068-001-01-8;Leuprolide acetate, United States Pharmacopeia (USP) Reference Standard;6-D-Leucine-9-(N-ethyl-L-prolinamide)-1-9-luteinizing Hormone-releasing Factor (Pig);(2S)-1-[(2S)-5-carbamimidamido-2-[(2S)-2-[(2R)-2-[(2S)-2-[(2S)-3-hydroxy-2-[(2S)-2-[(2S)-3-(1H-imidazol-4-yl)-2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}propanamido]-3-(1H-indol-3-yl)propanamido]propanamido]-3-(4-hydroxyphenyl)propanamido]-4-methylpentanamido]-4-methylpentanamido]pentanoyl]-N-ethylpyrrolidine-2-carboxamide;6-D-Leucine-9-(N-ethyl-L-prolinamide)-10-deglycinamide Luteinizing Hormone-Releasing Factor (Pig);
Chemical Name:(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-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]-4-methyl-1-oxopentan-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
Leuprolide is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH), widely recognized for its role in modulating the hypothalamic-pituitary-gonadal axis. As a potent GnRH agonist, it exhibits high affinity for GnRH receptors and induces a biphasic response—initially stimulating and subsequently downregulating gonadotropin secretion following prolonged exposure. Its robust biochemical profile and receptor selectivity make it a valuable tool in the study of neuroendocrine regulation, reproductive biology, and peptide-receptor interactions. Leuprolide's stability and well-characterized mechanism of action have positioned it as a reference compound in a range of experimental and industrial applications within peptide research and endocrinology.
Endocrine signaling research: In neuroendocrinology and reproductive biology laboratories, leuprolide is commonly utilized to probe the dynamics of GnRH receptor function and downstream hormonal responses. By simulating GnRH activity, it enables researchers to dissect the feedback mechanisms governing luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. This facilitates detailed investigations into the temporal regulation of the hypothalamic-pituitary-gonadal axis, supporting studies on hormone synthesis, release kinetics, and receptor desensitization in both in vitro and ex vivo systems.
Peptide receptor characterization: Due to its high receptor affinity and defined agonist properties, leuprolide serves as a model ligand for the characterization of GnRH receptor subtypes and their pharmacological profiles. It is frequently employed in radioligand binding assays, receptor internalization studies, and structure-activity relationship (SAR) analyses to elucidate binding kinetics, receptor conformational changes, and signal transduction pathways. Such applications are essential for advancing the understanding of peptide-receptor interactions and for benchmarking new receptor modulators in the discovery pipeline.
Peptide synthesis and formulation studies: Leuprolide's synthetic peptide structure makes it a valuable standard in peptide chemistry, particularly for the development and optimization of solid-phase peptide synthesis protocols. Its use as a reference compound aids in validating synthetic methodologies, assessing peptide purity, and optimizing chromatographic separation techniques. Additionally, it provides a model for investigating peptide stability, aggregation tendencies, and formulation strategies, which are critical parameters in the design of peptide-based research tools and delivery systems.
Cellular signaling pathway analysis: In cellular and molecular biology settings, leuprolide is often applied to cultured pituitary or gonadal cell lines to induce or suppress gonadotropin signaling cascades. Its controlled activation of GnRH receptors allows for the study of intracellular second messenger systems, such as calcium mobilization and protein kinase activation. Researchers leverage these properties to delineate the molecular underpinnings of hormone-regulated gene expression, cell proliferation, and differentiation, generating insights relevant to both basic and applied bioscience.
Endocrine disruptor screening: As a well-characterized GnRH analog, leuprolide provides a benchmark for evaluating the endocrine-disrupting potential of environmental chemicals, pharmaceuticals, or novel synthetic compounds. By comparing the effects of test agents to those elicited by leuprolide in receptor-based bioassays, scientists can assess agonist or antagonist activity, receptor selectivity, and downstream hormonal perturbations. This application supports environmental toxicology, chemical safety assessment, and regulatory science by facilitating the identification of substances that may interfere with endocrine homeostasis.
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