FR 139317 features a peptide-based architecture used to investigate ligand-receptor contact patterns. Aromatic and charged residues support complex binding interactions. Researchers examine its conformational equilibrium to interpret structure-activity relationships. Uses include receptor mapping, motif modeling, and peptide optimization.
CAT No: R2339
CAS No:142375-60-8
Synonyms/Alias:FR 139317;142375-60-8;FR139317;2-((1-(Hexahydro-1H-azepinyl)carbonyl)amino-4-methylpentanoyl)-3-(-(1-methyl-1H-indolyl)propionyl)amino-3-(2-pyridyl)propionic acid;D-Alanine, N-((hexahydro-1H-azepin-1-yl)carbonyl)-L-leucyl-1-methyl-D-tryptophyl-3-(2-pyridinyl)-;CHEMBL352396;(2R)-2-[[(2R)-2-[[(2S)-2-(azepane-1-carbonylamino)-4-methylpentanoyl]amino]-3-(1-methylindol-3-yl)propanoyl]amino]-3-pyridin-2-ylpropanoic acid;D-Alanine, N-(N-(N-((hexahydro-1H-azepin-1-yl)carbonyl)-L-leucyl)-1-methyl-D-tryptophyl)-3-(2-pyridinyl)-;(2R)-2-(((2R)-2-(((2S)-2-(azepane-1-carbonylamino)-4-methylpentanoyl)amino)-3-(1-methylindol-3-yl)propanoyl)amino)-3-pyridin-2-ylpropanoic acid;PD 147953;Tocris-1210;GTPL998;SCHEMBL2124350;DTXSID30931419;HMS3412O03;HMS3676O03;SFA37560;BDBM50286804;AKOS024456467;NCGC00025042-01;NCGC00025042-02;AS-85708;HY-102092;G78199;SR-01000597371;SR-01000597371-1;BRD-K19318328-001-01-3;Q27077729;(2R)-2-{[(2R)-2-({(2S)-2-[(1-azepanylcarbonyl)amino]-4-methylpentanoyl}amino)-3-(1-methyl-1H-indol-3-yl)propanoyl]amino}-3-(2-pyridinyl)propanoic acid;(R)-2-((R)-2-((S)-2-(azepane-1-carboxamido)-4-methylpentanamido)-3-(1-methyl-1H-indol-3-yl)propanamido)-3-(pyridin-2-yl)propanoic acid;(R)-2-[(R)-2-{(S)-2-[(Azepane-1-carbonyl)-amino]-4-methyl-pentanoylamino}-3-(1-methyl-1H-indol-3-yl)-propionylamino]-3-pyridin-2-yl-propionic acid;D-Alanine,N-[(hexahydro-1H-azepin-1-yl)carbonyl]-L-leucyl-1-methyl-D-tryptophyl-3-(2-pyridinyl)-;N-{2-[(2-{[(Azepan-1-yl)(hydroxy)methylidene]amino}-1-hydroxy-4-methylpentylidene)amino]-1-hydroxy-3-(1-methyl-1H-indol-3-yl)propylidene}-3-pyridin-2-ylalanine;
FR 139317 is a synthetic small-molecule compound recognized for its potent and selective antagonistic activity at the serotonin 5-HT4 receptor. Characterized by its high affinity and specificity, it has become an essential tool in neuropharmacological and gastrointestinal research. Its primary utility lies in enabling detailed studies of the 5-HT4 receptor's physiological and pathophysiological roles, providing researchers with a means to dissect serotonergic signaling pathways in diverse biological systems. By modulating receptor activity, FR 139317 supports the investigation of serotonin-mediated processes, making it a valuable resource for elucidating complex neurotransmitter functions and receptor pharmacology.
Receptor pharmacology: FR 139317 is extensively employed in receptor binding and functional assays to characterize the pharmacological properties of the 5-HT4 receptor. Its selectivity allows for precise differentiation between 5-HT4-mediated effects and those mediated by other serotonin receptor subtypes. Researchers utilize it to determine receptor affinity, antagonistic potency, and downstream signaling responses in both in vitro and ex vivo systems. The compound's utility in these assays advances the understanding of receptor-ligand interactions, aiding in the mapping of receptor distribution and functional relevance in various tissues.
Neurotransmitter research: As a selective 5-HT4 antagonist, FR 139317 is instrumental in studies investigating the role of serotonin in central and peripheral nervous system function. By blocking 5-HT4 receptor activity, it enables the elucidation of serotonin's contributions to cognitive processes, synaptic plasticity, and neurochemical signaling. Researchers leverage the compound to dissect serotonergic modulation in neuronal circuits, facilitating insights into mechanisms underlying learning, memory, and mood regulation. Its use is particularly valuable in experimental models exploring neurotransmitter dynamics and receptor-mediated signaling cascades.
Gastrointestinal physiology: FR 139317 serves as a critical tool for exploring the involvement of 5-HT4 receptors in gastrointestinal motility and secretion. The compound is frequently incorporated into organ bath experiments, tissue contractility studies, and cellular assays to assess its impact on smooth muscle function and enteric neurotransmission. By selectively inhibiting 5-HT4 receptor activity, it allows researchers to delineate the receptor's role in gut motility patterns, peristalsis, and mucosal secretion, contributing to a deeper understanding of gastrointestinal physiology and serotonergic regulation in the digestive tract.
Signal transduction studies: The compound is widely utilized to investigate intracellular signaling pathways activated by 5-HT4 receptor engagement. By acting as a competitive antagonist, FR 139317 enables researchers to parse out the specific downstream effects of receptor activation, such as cyclic AMP production, protein kinase A activation, and other second messenger cascades. Its application in these studies supports the identification of key molecular targets and regulatory mechanisms, enhancing the broader understanding of G protein-coupled receptor (GPCR) signaling in health and disease.
Drug discovery and screening: FR 139317 is frequently incorporated into high-throughput screening platforms and structure-activity relationship (SAR) studies aimed at identifying novel modulators of the 5-HT4 receptor. Its well-characterized antagonist profile provides a benchmark for evaluating the efficacy and selectivity of new chemical entities. In this context, the compound aids in validating assay performance, establishing reference standards, and supporting the development of next-generation serotonergic agents for research applications. By facilitating the discovery and optimization of receptor-targeted probes, it remains a cornerstone in early-stage neuropharmacological research and compound screening initiatives.
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More