Barusiban, renowned for its selective and potent qualities, possesses the intriguing ability to act as an oxytocin receptor antagonist, rendering it a remarkable candidate within the biomedical realm. This exceptional substance finds its purpose in combating preterm labor and uterine hyperactivity, where it diligently undertakes the role of inhibiting uterine contractions. By skillfully delaying or even evading the occurrence of premature birth, Barusiban exhibits its profound impact on reproductive health.
CAT No: R2074
CAS No:285571-64-4
Chemical Name:(4S,7S,10S,13S,16R)-N-[(2S)-5-amino-1-hydroxypentan-2-yl]-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-10-[(2R)-butan-2-yl]-16-(1H-indol-3-ylmethyl)-N-methyl-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
Barusiban is a synthetic peptide compound characterized as a potent and selective oxytocin receptor antagonist. Structurally engineered to mimic and modulate peptide-receptor interactions, Barusiban is widely recognized for its role in dissecting oxytocin-mediated signaling pathways. The compound's high affinity and specificity for the human oxytocin receptor make it a valuable molecular tool for researchers investigating the physiological and biochemical processes governed by oxytocin. Its unique properties have positioned Barusiban as an essential reagent in receptor pharmacology, functional peptide studies, and the development of new assay systems within the broader field of neuroendocrine and reproductive biology.
Receptor Pharmacology Research: As a selective oxytocin receptor antagonist, Barusiban is extensively utilized in studies aiming to elucidate the molecular mechanisms of oxytocin receptor activation and inhibition. By competitively binding to the receptor, it enables precise dissection of oxytocin's role in various physiological contexts, including uterine contractility, social behavior modulation, and central nervous system signaling. Researchers employ Barusiban to differentiate between oxytocin-specific effects and those mediated by related neuropeptides, thereby advancing the understanding of receptor-ligand dynamics and downstream signaling cascades.
Peptide Functional Studies: The compound serves as a critical control in peptide functional assays, allowing scientists to investigate the specificity and efficacy of endogenous or synthetic oxytocin analogs. Its use in competitive binding experiments and functional readouts, such as calcium mobilization or cAMP response assays, helps clarify the contribution of oxytocin signaling to cellular and tissue-level responses. Barusiban's well-characterized antagonist profile supports the development of robust experimental protocols for mapping peptide-driven physiological pathways.
Cell-Based Assay Development: In the context of assay development, Barusiban is employed as a reference antagonist for validating high-throughput screening platforms targeting the oxytocin receptor. Its reproducible inhibitory activity is instrumental in optimizing assay sensitivity, selectivity, and reproducibility. By serving as a benchmark compound, it facilitates the identification and characterization of novel oxytocin receptor modulators, supporting both academic research and pharmaceutical discovery efforts focused on neuropeptide signaling.
Signal Transduction Analysis: Researchers leverage Barusiban to dissect the downstream effects of oxytocin receptor blockade on intracellular signaling networks. Its application in studies of G protein-coupled receptor (GPCR) pathways enables detailed mapping of signal transduction events, including the modulation of second messengers, kinase activation, and gene expression profiles. Such analyses provide valuable insights into the broader physiological consequences of oxytocin receptor inhibition and inform the design of targeted interventions in basic research settings.
Comparative Ligand Profiling: The availability of Barusiban as a selective antagonist supports comparative studies of receptor subtype selectivity and cross-reactivity among related peptide hormones, such as vasopressin. By enabling side-by-side evaluation of ligand binding and functional responses, it aids in the characterization of receptor pharmacology across different species or tissue types. This approach is particularly valuable in translational research, where understanding the nuances of peptide-receptor interactions can inform the development of next-generation receptor modulators and enhance the predictive value of preclinical models.
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