High affinity, selective ANP clearance receptor (NPR3) antagonist (Ki = 0.45 nM) that exhibits >20,000-fold selectivity for NPR3 over NPR1.
CAT No: R0974
CAS No:124833-45-0
Synonyms/Alias:N2-[[4-[(2-Naphthalenylcarbonyl)amino]phenyl]acetyl]-L-arginyl-L-isoleucyl-L-α-aspartyl-N-[(2S)-2-methylbutyl]-L-argininamide; (S)-N2-[[4-[(2-Naphthalenylcarbonyl)amino]phenyl]acetyl]-L-arginyl-L-isoleucyl-L-α-aspartyl-N-(2-methylbutyl)-L-argininamide; AP 811;
AP 811 is a synthetic peptide compound recognized for its role as a selective nociceptin/orphanin FQ (NOP) receptor agonist. Structurally designed to mimic the endogenous neuropeptide orphanin FQ, AP 811 exhibits high affinity and specificity for the NOP receptor, distinguishing it from classical opioid peptides. Its unique pharmacological profile has made it a valuable biochemical tool for investigating the physiological and molecular functions of the NOP receptor system. Researchers utilize AP 811 to elucidate complex neurobiological processes, particularly those related to pain modulation, stress response, and the regulation of neurotransmitter systems.
Receptor Pharmacology Studies: AP 811 is extensively employed in receptor binding assays and pharmacological profiling to characterize the functional properties of the NOP receptor. By selectively activating this receptor subtype, the peptide enables detailed analysis of ligand-receptor interactions, downstream signaling pathways, and receptor desensitization mechanisms. Such studies are pivotal for advancing the understanding of G protein-coupled receptor (GPCR) dynamics and for differentiating NOP-mediated effects from those mediated by classical opioid receptors.
Neuroscience Research: As a potent and selective NOP receptor agonist, AP 811 serves as a critical tool in neurophysiological investigations. It is used to dissect the role of the nociceptin system in central nervous system processes such as pain perception, anxiety, and stress adaptation. Through in vitro and ex vivo preparations, the peptide aids in mapping neural circuits and neurotransmitter release patterns influenced by NOP activation, supporting the identification of novel neurobiological pathways and modulatory mechanisms.
Signal Transduction Analysis: Researchers utilize AP 811 to probe intracellular signaling cascades initiated by NOP receptor stimulation. The peptide's selectivity allows for the isolation and quantification of specific second messenger responses, such as changes in cyclic AMP levels, calcium mobilization, and kinase activation. These studies contribute to a deeper mechanistic understanding of NOP receptor coupling to various G proteins and the resultant cellular outcomes, informing broader models of GPCR-mediated signal transduction.
Peptide Structure-Activity Relationship (SAR) Studies: AP 811 is frequently applied in structure-activity relationship analyses to elucidate critical molecular determinants of NOP receptor binding and activation. By serving as a reference ligand, it facilitates the comparative evaluation of novel peptide analogs and small-molecule modulators. Insights gained from these studies guide the rational design of new compounds with tailored receptor selectivity and efficacy, advancing the field of peptide-based drug discovery and receptor pharmacology.
Behavioral Pharmacology: In preclinical research settings, AP 811 is utilized to assess the behavioral consequences of selective NOP receptor activation. Through controlled administration in animal models, it supports the investigation of nociceptin-mediated modulation of pain thresholds, locomotor activity, and stress-induced behaviors. These applications enable researchers to parse the functional relevance of the NOP system in behavioral regulation, contributing valuable data for the broader understanding of neuropeptide signaling in complex biological systems.
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