GR 64349 peptide acts as an agonist of neurokinin (NK2) receptor, which reduces NK2 response to kainate and AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid), but not to NMDA (N-methyl-D-aspartate)
CAT No: R0803
CAS No:137593-52-3
Synonyms/Alias:GR 64349;137593-52-3;136548-07-7;(3S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R)-1-[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-2-oxopyrrolidin-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-[[(2S)-2,6-diaminohexanoyl]amino]-4-oxobutanoic acid;3-Lys-8-gly-R-lactam-9-leu-neurokinin A (3-10);Neurokinin A (3-10), lys(3)-gly(8)-R-lactam-leu(9)-;Neurokinin A (3-10), lysyl(3)-glycyl(8)-R-lactam-leucine(9)-;(3R-(1(S*(S*)),3R*))-L-Lysyl-L-alpha-aspartyl-L-seryl-L-phenylalanyl-N-(1-(1-(((1-(aminocarbonyl)-3-(methylthio)propyl)amino)carbonyl)-3-methylbutyl)-2-oxo-3-pyrrolidinyl)-L-valinamide;L-Valinamide, L-lysyl-L-alpha-aspartyl-L-seryl-L-phenylalanyl-N-(1-(1-(((1-(aminocarbonyl)-3-(methylthio)propyl)amino)carbonyl)-3-methylbutyl)-2-oxo-3-pyrrolidinyl)-, (3R-(1(S*(S*)),3R*))-;DA-63889;MS-31721;G12420;
GR 64349 is a synthetic peptide compound that functions as a selective 5-HT4 receptor agonist, widely recognized for its utility in neuropharmacological and gastrointestinal research. As a member of the peptide agonist class, it is structurally designed to mimic endogenous ligands, enabling precise modulation of serotonin receptor subtypes. Its high selectivity and well-characterized activity profile make it a valuable tool for studies investigating serotonergic signaling pathways, receptor pharmacodynamics, and neurotransmitter-mediated physiological processes. The compound's unique receptor targeting capabilities have established it as a standard in experimental models seeking to elucidate the role of 5-HT4 receptors in diverse biological systems.
Receptor Pharmacology Studies: GR 64349 is extensively used in receptor binding and functional assays to delineate the pharmacological characteristics of the 5-HT4 receptor. By acting as a potent and selective agonist, it enables researchers to probe receptor-ligand interactions, assess downstream signaling events, and quantify receptor activation in both in vitro and ex vivo systems. Its specificity allows for accurate discrimination between 5-HT4-mediated effects and those mediated by other serotonin receptor subtypes, thereby facilitating a deeper understanding of serotonergic modulation in neural and peripheral tissues.
Gastrointestinal Motility Research: The compound plays a critical role in experimental investigations of gastrointestinal physiology, particularly in studies examining the regulation of motility and secretion. Through selective activation of 5-HT4 receptors in enteric neurons and smooth muscle cells, GR 64349 helps elucidate the mechanisms underlying gut transit, peristalsis, and neurotransmitter release within the enteric nervous system. Its application supports the development of mechanistic models and the identification of novel targets for modulating gastrointestinal function in preclinical settings.
Neurotransmitter Release Assays: As a functional agonist, GR 64349 is instrumental in studies measuring neurotransmitter release, especially acetylcholine, from neuronal preparations. Activation of 5-HT4 receptors by this peptide can enhance synaptic transmission and modulate neuronal excitability, providing a controlled means to investigate the dynamics of neurotransmitter release and synaptic plasticity. These insights are essential for mapping serotonergic contributions to central and peripheral nervous system activity.
Signal Transduction Pathway Analysis: Researchers utilize GR 64349 in cell-based assays to characterize the intracellular signaling cascades triggered by 5-HT4 receptor activation. The compound's defined agonist activity enables precise dissection of downstream pathways, such as cAMP production, protein kinase activation, and gene expression modulation. Such studies are fundamental for understanding the molecular basis of receptor function and for screening potential modulators of serotonergic signaling.
Peptide Ligand Development: Beyond its direct research uses, GR 64349 serves as a reference compound in the development and validation of new peptide ligands targeting serotonin receptors. Its well-established pharmacological profile provides a benchmark for evaluating the selectivity, potency, and efficacy of novel synthetic peptides or small molecules. This application is particularly relevant for structure-activity relationship studies and for advancing the design of next-generation receptor modulators in drug discovery research.
Through these diverse applications, GR 64349 has become an indispensable reagent for scientists investigating serotonin receptor biology, neurotransmission, and peptide pharmacology. Its robust and selective activity profile continues to support innovative research across neurobiology, gastroenterology, and molecular pharmacology disciplines.
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