Selective and competitive silent antagonist for the NOP opioid receptor that binds to NOP with high affinity (pKi = 10.24) and displays > 3000-fold selectivity over δ, μ and κ opioid receptors.
CAT No: R1067
CAS No:849024-68-6
Synonyms/Alias:849024-68-6;L-Glutamamide,N-(phenylmethyl)glycylglycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-arginyl-L-lysyl-L-asparaginyl-;UFP-101 TFA;AKOS024456661;DA-58867;PD079059;
UFP-101 is a synthetic peptide compound recognized for its role as a highly selective antagonist of the nociceptin/orphanin FQ peptide (NOP) receptor, which belongs to the opioid receptor family. Structurally derived from modifications of endogenous neuropeptides, UFP-101 has become an indispensable tool in neuropharmacological and receptor signaling research. Its unique ability to block the activation of NOP receptors without significant cross-reactivity with classical opioid receptors enables researchers to dissect the physiological and biochemical functions attributed specifically to the nociceptin system. As such, it serves as a critical reagent in studies aiming to elucidate the mechanisms underlying pain modulation, neurobehavioral responses, and complex signaling pathways within the central and peripheral nervous systems.
Receptor Pharmacology: UFP-101 is extensively utilized in receptor pharmacology to characterize the binding properties, functional selectivity, and downstream signaling cascades associated with the NOP receptor. By providing a highly selective blockade, it allows for the differentiation of NOP-mediated effects from those mediated by mu, delta, or kappa opioid receptors. Researchers can employ this peptide to probe receptor-ligand interactions, evaluate agonist and antagonist potency, and delineate the molecular determinants of receptor specificity, thereby advancing the understanding of opioid receptor pharmacodynamics.
Neurobiological Research: In neurobiology, UFP-101 is a valuable tool for investigating the role of the nociceptin system in modulating neuronal activity and neurochemical release. Its application in in vitro and in vivo experimental models enables the assessment of NOP receptor involvement in synaptic transmission, plasticity, and neuropeptide signaling. By selectively inhibiting NOP receptor function, scientists are able to unravel the contributions of this pathway to neural circuit regulation, stress responses, and behavioral phenotypes, providing insights into the broader neuropeptide network.
Pain Pathway Studies: The selective antagonistic action of UFP-101 on the NOP receptor makes it particularly relevant for pain research. It is frequently used to explore the mechanisms by which the nociceptin system influences nociceptive processing and pain perception. Through administration in animal models or cellular assays, the peptide helps identify the specific pathways and neurotransmitter systems modulated by NOP signaling, thereby facilitating the development of new hypotheses regarding endogenous pain regulation and the interplay between various opioid systems.
Peptide Functional Studies: UFP-101 serves as a model compound in peptide functional studies, especially those focused on structure-activity relationships and ligand-receptor interactions. Its well-characterized sequence and receptor selectivity allow researchers to investigate the effects of specific amino acid modifications on biological activity and receptor affinity. Such studies contribute to the rational design of novel peptide ligands with improved selectivity, stability, or pharmacological profiles, supporting advancements in both basic and applied peptide science.
Drug Discovery and Screening: In the context of drug discovery, UFP-101 is employed as a reference antagonist in high-throughput screening assays and preclinical research. Its use enables the validation of new NOP receptor modulators and the assessment of off-target effects in candidate compounds. By serving as a benchmark for antagonist activity, it assists medicinal chemists and pharmacologists in identifying and optimizing novel molecules with therapeutic potential targeting the nociceptin system, thereby accelerating the development of next-generation receptor modulators for research applications.
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