Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
CAT No: R1803
CAS No:1435786-04-1
Synonyms/Alias:Rapastinel Trifluoroacetate;1435786-04-1;GLYX-13 trifluoroacetate;Rapastinel (Trifluoroacetate);(2S)-1-[(2S)-1-[(2S,3R)-2-amino-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]pyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acid;Rapastinel TFA salt;GLYX-13 TFA salt;RapastinelTrifluoroacetate;BCWVNVCGYWOAAK-GDLIIDCZSA-N;GLXC-03841;HY-16728B;AKOS040758824;RAPASTINEL; TRIFLUOROACETIC ACID;DA-77350;MS-29761;CS-0040824;GLYX-13 trifluoroacetate, >=98% (HPLC);G14102;
Rapastinel Trifluoroacetate is a synthetic peptide compound recognized for its role as a functional modulator of the N-methyl-D-aspartate (NMDA) receptor, specifically acting as a partial agonist at the glycine site. As a cyclic tetrapeptide derivative, it exhibits unique pharmacological properties that differentiate it from conventional NMDA receptor ligands. Its well-characterized mechanism of action and selective receptor engagement have made it a subject of significant interest in neuropharmacology, synaptic plasticity research, and peptide-based drug discovery. The trifluoroacetate salt form ensures stability and solubility, supporting its utility in a variety of experimental settings. Researchers leverage the distinctive features of Rapastinel Trifluoroacetate to probe fundamental questions in neurobiology and receptor signaling.
Neuropharmacological research: Rapastinel serves as a valuable tool for investigating NMDA receptor function and its downstream signaling pathways. Its partial agonist activity at the glycine modulatory site enables the study of receptor activation dynamics and synaptic modulation under controlled experimental conditions. By selectively enhancing or modulating NMDA receptor-mediated currents, the compound aids in dissecting the molecular mechanisms underlying synaptic plasticity, long-term potentiation, and excitatory neurotransmission. Such studies are essential for elucidating the physiological roles of NMDA receptor subtypes and their contributions to neural circuit function.
Synaptic plasticity modeling: The unique pharmacological profile of this peptide allows for precise examination of synaptic plasticity phenomena, including long-term potentiation and depression in both in vitro and ex vivo systems. Researchers employ Rapastinel to simulate and analyze activity-dependent changes in synaptic strength, providing insights into the molecular basis of learning and memory. Its ability to modulate receptor activity without eliciting excitotoxic effects is particularly advantageous for experiments requiring sustained receptor engagement while minimizing confounding variables associated with receptor overstimulation.
Peptide structure-activity relationship (SAR) studies: As a structurally distinct cyclic peptide, Rapastinel is frequently utilized in SAR investigations aimed at optimizing NMDA receptor ligands. Its sequence and conformational features offer a template for the rational design of novel glycine-site modulators with improved selectivity, potency, or pharmacokinetic profiles. By systematically modifying amino acid residues or cyclization motifs, researchers can delineate the structural determinants critical for receptor binding and functional efficacy, advancing the development of next-generation peptide therapeutics and research tools.
Analytical method development: The well-defined physicochemical properties of Rapastinel Trifluoroacetate make it suitable as a reference standard or internal control in analytical protocols involving peptide quantification, receptor binding assays, or chromatographic analyses. Its stability and solubility facilitate accurate calibration and validation of bioanalytical methods, supporting high-throughput screening, quality control, and pharmacological profiling efforts in academic and industrial laboratories.
Neurodevelopmental and neurotoxicity studies: The compound's selective action on NMDA receptors provides a controlled means to investigate the role of glycine-site modulation in neurodevelopmental processes and excitotoxicity models. By applying Rapastinel in neuronal cultures or organotypic brain slices, scientists can assess the impact of NMDA receptor modulation on neuronal differentiation, maturation, and survival. Such studies contribute to a deeper understanding of receptor-mediated signaling in both physiological development and pathological conditions, offering a foundation for future research into neuroprotection and synaptic resilience.
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