Spinorphin is an endogenous opioid heptapeptide that exhibits inhibitory effects on enkephalin-degrading enzymes. The mechanism of action of spinophin has not been fully elucidated but it has been found to act as an antagonist of the P2X3 receptor, and as a weak partial agonist/antagonist of the FP1 receptor.
CAT No: R1871
CAS No:137201-62-8
Synonyms/Alias:Spinorphin;137201-62-8;LVVYPWT;Leu-val-val-tyr-pro-trp-thr;(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoic acid;Leucyl-valyl-valyl-tyrosyl-prolyl-tryptophyl-threonine;L-Threonine, L-leucyl-L-valyl-L-valyl-L-tyrosyl-L-prolyl-L-tryptophyl-;L-Threonine, N-(N-(1-(N-(N-(N-L-leucyl-L-valyl)-L-valyl)-L-tyrosyl)-L-prolyl)-L-tryptophyl)-;CHEMBL395493;DTXSID70160105;LVV-hemorphin-4;L-leucyl-L-valyl-L-valyl-L-tyrosyl-L-prolyl-L-tryptophyl-L-threonine;(2S,3R)-2-(((2S)-2-(((2S)-1-((2S)-2-(((2S)-2-(((2S)-2-(((2S)-2-amino-4-methylpentanoyl)amino)-3-methylbutanoyl)amino)-3-methylbutanoyl)amino)-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carbonyl)amino)-3-(1H-indol-3-yl)propanoyl)amino)-3-hydroxybutanoic acid;GTPL1026;leucyl--valyl-valyl-tyrosyl-prolyl-tryptophyl-threonine;DTXCID3082596;SCHEMBL25217672;CHEBI:172845;HY-P1044;BDBM50219120;AKOS024457342;AC-33668;TS-09808;DB-230577;CS-0025001;Q7577645;
Chemical Name:(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoic acid
Spinorphin is a naturally occurring heptapeptide derived from bovine spinal cord and characterized by its distinctive sequence and opioid-modulating properties. As a member of the endogenous opioid peptide family, it is recognized for its ability to inhibit certain enkephalin-degrading enzymes, thereby modulating the activity of endogenous opioid systems. Spinorphin has garnered significant interest in neurochemical and pharmacological research due to its multifaceted roles in pain modulation, neurotransmitter release, and neuroregulatory processes. Its unique biochemical profile positions it as a valuable tool for investigations into peptide-mediated signaling pathways and the broader landscape of neuropeptide function.
Neuropharmacology research: Spinorphin serves as an important molecular probe in the study of neuropharmacological mechanisms underlying pain perception and opioid regulation. By inhibiting enzymes such as aminopeptidase N and neutral endopeptidase, it prolongs the activity of endogenous enkephalins, providing researchers with a means to dissect the roles of enkephalinergic pathways in nociceptive signaling. This enables detailed exploration of the interplay between opioid peptides and their degrading enzymes, advancing the understanding of endogenous pain control systems and their potential modulation.
Enzyme inhibition studies: The peptide is widely utilized in biochemical assays aimed at characterizing the specificity and kinetics of peptidase inhibitors. Its capacity to selectively inhibit key peptidases without directly activating opioid receptors makes it a valuable reference compound for delineating the contributions of enzymatic degradation to neuropeptide signaling. Researchers leverage its inhibitory profile to validate new assay systems, calibrate enzyme activity measurements, and benchmark novel inhibitors within the context of neuropeptidase research.
Peptide structure-activity relationship (SAR) analysis: Spinorphin's defined amino acid sequence and functional motifs make it an exemplary model for peptide SAR studies. By systematically modifying its structure, scientists can investigate how individual residues contribute to biological activity, enzymatic stability, and receptor interactions. Such studies inform the rational design of peptide analogues with tailored bioactivity, supporting the development of new research tools and advancing the field of peptide-based modulation of neurochemical pathways.
Neurotransmitter release modulation: Research employing spinorphin has revealed its capacity to influence the release of neurotransmitters in central nervous system preparations. By modulating the balance of excitatory and inhibitory signaling, the peptide provides a platform for studying the regulation of synaptic transmission and the downstream effects on neuronal communication. These insights are particularly valuable for elucidating the mechanisms governing neuropeptide-mediated control of neural circuits.
Peptide-based drug discovery platforms: Spinorphin is frequently incorporated into screening platforms for the identification and optimization of novel peptide-based modulators. Its well-characterized activity profile and established mechanism of action make it a preferred positive control or reference standard in high-throughput screening assays targeting neuropeptidase activity. Researchers in drug discovery utilize it to benchmark assay performance, validate screening protocols, and inform the selection of candidate molecules for further development in the context of neuropeptide research.
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