Potent, highly selective NK2 neurokinin receptor antagonist.
CAT No: R1024
CAS No:135306-85-3
Synonyms/Alias:Men 10376;135306-85-3;MEN-10376;neurokinin A(4-10), Tyr(5)-Trp(6,8,9)-Lys(10)-;MEN-10,376;MFCD00144736;(3S)-3-amino-4-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2R)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-oxobutanoic acid;CHEMBL507824;MEN10376;L-Lysinamide, L-alpha-aspartyl-L-tyrosyl-D-tryptophyl-L-valyl-D-tryptophyl-D-tryptophyl-;Neurokinin-2 receptor antagonist;(3S)-3-amino-4-(((2S)-1-(((2R)-1-(((2S)-1-(((2R)-1-(((2R)-1-(((2S)-1,6-diamino-1-oxohexan-2-yl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)amino)-4-oxobutanoic acid;5-Tyr-6,8,9-trp-10-lys-neurokinin A (4-10);GTPL2116;HY-P1276;BDBM50259674;Neurokinin A(4-10), tyrosyl(5)-tryptophyl(6,8,9)-lysine(10)-;AKOS030623006;NCGC00167321-01;DA-48909;CS-0029214;Asp-Tyr-D-Trp-Val-D-Trp-D-Trp-Lys-NH(2);Q27084374;(Tyr5,D-Trp6.8.9,Lys-NH21?)-Neurokinin A (4-10);(Tyr5,D-Trp6?8?9,Lys-NH210)-Neurokinin A (4-10);L-Lysinamide,l-a-aspartyl-l-tyrosyl-D-tryptophyl-L-valyl-D-tryptophyl-D-tryptophyl-;(3S)-3-amino-3-{[(1S)-1-{[(1R)-1-{[(1S)-1-{[(1R)-1-{[(1R)-1-{[(1S)-5-amino-1-carbamoylpentyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-methylpropyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]carbamoyl}propanoic acid;(S)-3-amino-4-((S)-1-((R)-1-((S)-1-((R)-1-((R)-1-((S)-1,6-diamino-1-oxohexan-2-ylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-3-methyl-1-oxobutan-2-ylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-3-(4-hydroxyphenyl)-1-oxopropan-2-ylamino)-4-oxobutanoic acid;
MEN 10376 is a synthetic peptide compound recognized for its role as a selective antagonist of the neuropeptide Y Y5 receptor. Characterized by its high specificity and affinity for the Y5 receptor subtype, MEN 10376 serves as a valuable tool in neuropharmacological research, particularly in studies exploring the physiological and biochemical functions of neuropeptide Y signaling pathways. Its structural stability and receptor selectivity make it a preferred agent for probing the distinct roles of Y5-mediated mechanisms in various biological systems, enabling researchers to dissect complex neural and metabolic processes with precision.
Receptor Pharmacology: In neurobiological research, MEN 10376 is widely employed to investigate the functional implications of Y5 receptor modulation. By selectively antagonizing the Y5 receptor, it allows for the delineation of receptor-specific pathways and the identification of downstream signaling events triggered by neuropeptide Y. This targeted approach is instrumental in clarifying the physiological relevance of Y5 receptor activity in neural circuits, supporting the development of mechanistic models of receptor function and regulation.
Neuropeptide Y System Studies: The compound is utilized in experimental designs aimed at elucidating the broader neuropeptide Y system, particularly in relation to appetite regulation, energy homeostasis, and stress response. By inhibiting Y5 receptor activity, MEN 10376 aids in distinguishing the contributions of individual receptor subtypes within the neuropeptide Y family, thereby refining our understanding of how neuropeptide Y orchestrates diverse physiological responses. This specificity is especially valuable for parsing receptor subtype interactions in both in vitro and ex vivo systems.
Signal Transduction Analysis: Researchers leverage MEN 10376 in the study of intracellular signaling cascades initiated by Y5 receptor engagement. Its application facilitates the mapping of second messenger pathways, phosphorylation events, and gene expression changes that are uniquely associated with Y5 antagonism. Such analyses provide critical insights into the molecular mechanisms underlying receptor-mediated cellular responses and offer a foundation for the identification of novel signaling intermediates.
Peptide Drug Discovery: The compound's selective antagonistic profile makes it a useful reference molecule in the screening and characterization of new peptide-based ligands targeting neuropeptide Y receptors. In structure-activity relationship studies, MEN 10376 serves as a benchmark for evaluating the binding affinities, selectivities, and functional efficacies of novel peptides or small molecules. Its use in competitive binding assays and pharmacological profiling accelerates the identification of promising lead compounds for further development.
In vivo and Ex vivo Functional Assays: MEN 10376 is frequently incorporated into animal and tissue-based experimental protocols to assess the physiological consequences of Y5 receptor blockade. Through its application, researchers can monitor changes in behavioral, metabolic, or neuroendocrine parameters, providing a direct link between receptor antagonism and functional outcomes. These studies are fundamental for validating receptor-specific hypotheses and for advancing our understanding of neuropeptide Y's role in complex biological systems.
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