Atosiban, also known as ORF 22164, RWJ 22164, is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Although initial studies suggested it could be used as a nasal spray and hence would not require hospital admission, it is not used in that form.
CAT No: R1968
CAS No:914453-95-5
Synonyms/Alias:Atosiban acetate;914453-95-5;UNII-0P5DNO7CEF;0P5DNO7CEF;ATOSIBAN ACETATE [WHO-DD];ATOSIBAN ACETATE [EMA EPAR];acetic acid;(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide;GLYCINAMIDE, O-ETHYL-N-(3-MERCAPTO-1-OXOPROPYL)-D-TYROSYL-L-ISOLEUCYL-L-THREONYL-L-ASPARAGINYL-L-CYSTEINYL-L-PROLYL-L-ORNITHYL-, CYCLIC (1->5)-DISULFIDE, ACETATE (1:1);GLYCINAMIDE, O-ETHYL-N-(3-MERCAPTO-1-OXOPROPYL)-D-TYROSYL-L-ISOLEUCYL-L-THREONYL-L-ASPARAGINYL-L-CYSTEINYL-L-PROLYL-L-ORNITHYL-, CYCLIC (1->5)-DISULFIDE, MONOACETATE (SALT);GLYCINAMIDE, O-ETHYL-N-(3-MERCAPTO-1-OXOPROPYL)-D-TYROSYL-L-ISOLEUCYL-L-THREONYL-L-ASPARAGINYL-L-CYSTEINYL-L-PROLYL-L-ORNITHYL-, CYCLIC (1->5)-DISULPHIDE, ACETATE (1:1);GLYCINAMIDE, O-ETHYL-N-(3-MERCAPTO-1-OXOPROPYL)-D-TYROSYL-L-ISOLEUCYL-L-THREONYL-L-ASPARAGINYL-L-CYSTEINYL-L-PROLYL-L-ORNITHYL-, CYCLIC (1->5)-DISULPHIDE, MONOACETATE (SALT);OXYTOCIN, 1-(3-MERCAPTOPROPANOIC ACID)-2-(O-ETHYL-D-TYROSINE)-4-L-THREONINE-8-L-ORNITHINE-, ACETATE;DTXSID60238569;Atosiban (as acetate);SCHEMBL4410202;CHEMBL5315050;DTXCID60161060;EX-A7437;C45H71N11O14S2;MFCD08692014;AKOS030485985;FA40914;DA-50781;G13510;Q27237053;(Deamino-Cys1,D-Tyr(Et)2,Thr4,Orn8)-Oxytocin Acetate;
Chemical Name:acetic acid;(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
Atosiban Acetate is a synthetic peptide compound that functions as an oxytocin and vasopressin receptor antagonist, widely recognized for its significance in receptor signaling research and peptide pharmacology. Structurally designed to mimic endogenous peptide ligands, it selectively inhibits the binding of oxytocin and vasopressin to their respective receptors, offering a valuable tool for dissecting the molecular basis of peptide-receptor interactions. Its high specificity and well-characterized mechanism of action make it particularly useful for studies involving uterine contractility, intracellular signaling pathways, and the broader field of peptide-based modulation of physiological responses. As a research-use-only product, it serves as an essential reagent in academic, industrial, and pharmaceutical laboratories investigating peptide hormone function and receptor dynamics.
Receptor Pharmacology: Atosiban Acetate is extensively utilized in receptor binding assays and functional studies aimed at elucidating the pharmacological profiles of oxytocin and vasopressin receptors. By selectively antagonizing these G protein-coupled receptors, it enables researchers to characterize receptor subtypes, map ligand-receptor interactions, and investigate the downstream signaling events triggered by peptide hormones. Its application is pivotal in advancing the understanding of receptor specificity and the molecular determinants of peptide ligand recognition.
Signal Transduction Research: The compound serves as a critical tool for probing intracellular signaling cascades initiated by oxytocin and vasopressin. By inhibiting receptor activation, Atosiban Acetate allows for the precise delineation of second messenger systems and effector proteins involved in cellular responses to peptide hormones. This facilitates detailed studies of calcium mobilization, phosphoinositide turnover, and MAP kinase pathway activation, providing insights into the regulatory networks that govern smooth muscle contractility and other physiological processes.
Peptide Antagonist Profiling: Researchers employ Atosiban Acetate to validate and benchmark novel peptide antagonists targeting oxytocin and vasopressin receptors. Its well-defined antagonistic properties make it an ideal reference compound in comparative studies assessing the potency, selectivity, and efficacy of new drug candidates or experimental peptides. Such profiling is integral to the rational design and optimization of next-generation modulators of peptide hormone signaling.
Functional Assays in Uterine Tissue: The peptide is widely used in ex vivo and in vitro contractility assays involving uterine smooth muscle preparations. By blocking oxytocin-induced contractions, it enables the investigation of the physiological roles of endogenous peptides in myometrial activity. These assays are fundamental for elucidating the mechanisms underlying uterine motility, receptor desensitization, and the interplay of multiple signaling pathways in reproductive biology research.
Peptide Structure-Activity Relationship (SAR) Studies: Atosiban Acetate provides a robust model for exploring structure-activity relationships among peptide antagonists. Its defined sequence and receptor selectivity offer a reference point for systematic modifications, aiding in the identification of key structural features that influence receptor binding and antagonistic potency. SAR analyses leveraging this compound contribute to the broader understanding of peptide engineering, receptor targeting, and the development of novel bioactive peptides for research applications.
3. SERS spectrum of the peptide thymosin‐β4 obtained with Ag nanorod substrate
4. Immune responses to homocitrulline-and citrulline-containing peptides in rheumatoid arthritis
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