Y1 receptor antagonist 1 serves as a functional peptide-derived molecule for analyzing receptor-ligand determinants in neurochemical pathways. Its architecture supports evaluations of steric effects and charge distribution in binding pockets. Researchers employ it to dissect molecular interactions governing receptor modulation. Broad relevance spans biochemical pharmacology models, ligand design, and structural optimization.
CAT No: R2618
CAS No:221697-09-2
Synonyms/Alias:Y1 receptor antagonist 1;221697-09-2;H-409/22;Ar-H040922 freebase;7NCK567YKQ;(2R)-5-(diaminomethylideneamino)-2-[(2,2-diphenylacetyl)amino]-N-[(1R)-1-(4-hydroxyphenyl)ethyl]pentanamide;(2R)-2-((2,2-Diphenylacetyl)amino)-5-guanidino-N-((1R)-1-(4-hydroxyphenyl)ethyl)pentanamide;UNII-7NCK567YKQ;H 409-22;SCHEMBL1593464;AKOS040733811;CS-7270;DA-68753;MS-29063;HY-101704;BENZENEACETAMIDE, N-((1R)-4-((AMINOIMINOMETHYL)AMINO)-1-((((1R)-1-(4-HYDROXYPHENYL)ETHYL)AMINO)CARBONYL)BUTYL)-.ALPHA.-PHENYL-;Benzeneacetamide, N-((1R)-4-((aminoiminomethyl)amino)-1-((((1R)-1-(4-hydroxyphenyl)ethyl)amino)carbonyl)butyl)-alpha-phenyl-;N-((1R)-4-((AMINOIMINOMETHYL)AMINO)-1-((((1R)-1-(4-HYDROXYPHENYL)ETHYL)AMINO)CARBONYL)BUTYL)-.ALPHA.-PHENYLBENZENEACETAMIDE;N-((1R)-4-((Aminoiminomethyl)amino)-1-((((1R)-1-(4-hydroxyphenyl)ethyl)amino)carbonyl)butyl)-alpha-phenylbenzeneacetamide;
Y1 receptor antagonist 1 is a synthetic small molecule designed to selectively inhibit the activity of neuropeptide Y receptor subtype 1 (Y1R), a G protein-coupled receptor widely expressed in the central and peripheral nervous systems. As a potent and specific antagonist, this compound enables researchers to dissect the physiological and biochemical roles of Y1R-mediated signaling pathways. Its utility extends across neurobiology, endocrinology, and metabolic research, where the modulation of neuropeptide Y (NPY) pathways is of significant interest. By providing a targeted approach to block Y1R activation, Y1 receptor antagonist 1 serves as a valuable tool for advancing the understanding of receptor-ligand interactions, downstream signaling events, and the broader functional implications of Y1R in various biological systems.
Receptor pharmacology: In receptor binding and functional assays, Y1 receptor antagonist 1 is widely employed to characterize the pharmacological properties of Y1R. By competitively inhibiting NPY binding, it allows for the assessment of receptor specificity, ligand affinity, and antagonist potency in cell-based or membrane-based experimental systems. This approach is essential for mapping the pharmacodynamic profile of Y1R and distinguishing its contributions from those of other NPY receptor subtypes, thereby facilitating the development of more selective modulators and expanding the foundational knowledge of G protein-coupled receptor biology.
Signal transduction studies: The compound is instrumental in elucidating the downstream signaling cascades initiated by Y1R activation. In cellular models, application of the antagonist enables precise investigation of second messenger systems, such as cyclic AMP modulation, intracellular calcium flux, and kinase activation, following Y1R blockade. By comparing signaling outcomes in the presence and absence of the antagonist, researchers can delineate the specific pathways regulated by Y1R, identify cross-talk with other signaling networks, and clarify the molecular mechanisms underlying NPY-mediated physiological effects.
Neurobiological research: Y1 receptor antagonist 1 is frequently used in studies exploring the role of NPY and its receptors in neural circuits governing appetite regulation, stress response, anxiety, and circadian rhythms. By selectively inhibiting Y1R, investigators can dissect the receptor's involvement in modulating neurotransmitter release, synaptic plasticity, and neuroendocrine function. Such applications are critical for advancing the understanding of how NPY signaling influences behavior, neuroadaptation, and homeostatic processes in both in vitro and ex vivo experimental paradigms.
Metabolic pathway analysis: In metabolic research, selective antagonism of Y1R with this compound provides a means to investigate the receptor's influence on energy balance, adipogenesis, and glucose homeostasis. By blocking Y1R-mediated signaling, scientists can assess the receptor's contribution to metabolic phenotypes in cellular or animal models, evaluate its role in adipocyte differentiation, and study its impact on insulin sensitivity and nutrient partitioning. These insights are valuable for clarifying the complex interplay between neuropeptide signaling and metabolic regulation at the molecular and systemic levels.
Drug discovery and screening: Y1 receptor antagonist 1 serves as a reference compound in high-throughput screening platforms and structure-activity relationship (SAR) studies aimed at identifying novel Y1R modulators. Its well-characterized antagonistic profile makes it a benchmark for evaluating the efficacy and selectivity of new chemical entities targeting the NPY-Y1R axis. Utilization of this antagonist in assay development and compound profiling accelerates the identification of promising lead molecules, supports hit-to-lead optimization, and enhances the overall efficiency of early-stage drug discovery efforts focused on neuropeptide receptor targets.
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