pe
pep-10700 v1 CC-BY-SA-4.0

Dynorphin A (1-10) amide: natural opioid fragment that boosts morphine pain relief

A short piece of the body's own opioid peptide dynorphin; strengthens morphine's painkilling effect in animals that have built up tolerance, without blocking it in animals new to the drug; lab research tool only.

statussynthesized targetOPRM1 length10 aa refs9
status 4 / 5
prediction metrics boltz-2 1.0
ipTM0.884
pTM0.846
avg pLDDT81.4
ranking score0.828
STRUCTURE · PEP-10700 × OPRM1
ranking0.828
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 1.0 · mmCIF ↓ download
sequence10 aa
1510
YGGFLRRIRP
overview readme

What this is

Dynorphin A (1-10) amide is a short fragment of dynorphin A, one of the body's own opioid peptides. The full dynorphin A peptide is a 17-residue neuropeptide released from the precursor protein preprodynorphin; this card is the first ten residues of that peptide (YGGFLRRIRP), capped with a C-terminal amide rather than the free acid found in the stored 1-letter sequence. Like other endogenous opioids, it begins with the shared "YGGF" message sequence that lets it dock into opioid receptors. The "porcine" label reflects the species the fragment was originally characterized from; the 1-10 sequence is identical across most mammals.

History

Dynorphin peptides were identified as a third family of endogenous opioids alongside the enkephalins and β-endorphin, all sharing the N-terminal YGGF motif and all derived from distinct precursor proteins. Clynen and colleagues (2014) catalog the dynorphin family — including dynorphin A, dynorphin B (rimorphin), big dynorphin, and α-neoendorphin — as products of preprodynorphin processing, and place them in the broader landscape of neuropeptides that have been investigated as targets for anticonvulsant drug development. The 1-10 amide fragment used on this card is one of several truncated forms studied as a way to dissect which portion of full dynorphin A carries which biological activity.

What it does

Endogenous opioid peptides act through a family of four closely related G-protein-coupled receptors — mu (MOR/OPRM1), delta (DOR/OPRD1), kappa (KOR/OPRK1) and the nociceptin receptor (Pasternak 2013; Valentino 2018). Full-length dynorphin A is best known as the prototypical endogenous ligand at the kappa opioid receptor, but truncated dynorphin fragments lose the C-terminal "address" residues that drive kappa selectivity and behave more like the shorter enkephalins, engaging the mu and delta receptors instead. The card is annotated against OPRM1 (the mu opioid receptor) to reflect that shift in selectivity when the peptide is shortened to ten residues and amidated.

Mechanism

The YGGF N-terminus is the shared "message" sequence of all classical endogenous opioids; the residues that follow act as an "address" that biases the peptide toward one receptor subtype over another (Pasternak 2013). Cloning and pharmacological work in the early 1990s established that the opioid receptors are G-protein-coupled receptors structurally related to receptors for somatostatin, angiotensin and interleukin-8 (Evans 1992). Subsequent work has shown that opioid receptor signaling is more complex than a single pathway — receptors couple to multiple downstream effectors, exhibit ligand-biased agonism, and form heteromers with each other and with other GPCRs (Valentino 2018). Dynorphin A (1-10) amide, by truncating the kappa-selective C-terminal "address" of dynorphin A and adding a C-terminal amide, is one of the tool compounds used to interrogate that message/address logic.

Evidence

  • Human: No human clinical data identified in the available sources for this specific fragment.
  • Animal: Pharmacological characterization of opioid peptide fragments in rodents has historically used assays such as the guinea-pig ileum and mouse vas deferens to compare potency across the opioid peptide family (e.g. Broccardo and colleagues, 1981, comparing dermorphin against met-enkephalin in the same preparations). Comparable use as a research tool is the basis on which dynorphin A (1-10) fragments are characterized.
  • In vitro: Identification of dynorphin family peptides in mammalian tissue extracts has been confirmed by mass spectrometry-based neuropeptidomics (Petruzziello and colleagues, 2012).

Related peptides

Dynorphin A (1-10) amide sits inside the broader endogenous opioid family — preprodynorphin-derived dynorphins, proenkephalin-derived enkephalins, and proopiomelanocortin-derived β-endorphin — all sharing the N-terminal YGGF motif but differing in their downstream "address" residues and in receptor preference (Clynen 2014; Pasternak 2013). Comparative work on non-mammalian vertebrates (e.g. Pacific hagfish, Huang and colleagues 2022) and on amphibian-skin opioids such as dermorphin (Amiche 1990; Broccardo 1981) is part of the same broader literature on how the opioid receptor family and its peptide ligands co-evolved.

Hypotheses4 directions▾ collapse

Research directions for this peptide, selected from the current sources — hypotheses you can explore and model. None of it is proven yet; tap any one to see the full thinking.

openupdated 2026-06-05

Could a minor chemical modification to dynorphin's backbone make it survive long enough in the bloodstream to work as a drug?

Natural opioid peptides are degraded within minutes in the body, making them impractical as drugs. If this modification grants stability, the resulting compound could be developed into a non-addictive or reduced-addiction painkiller that patients could take systemically.

The hypothesis
Replacing Ile8 with a N-methyl amino acid in YGGFLRRIRP-NH2 would rigidify the Pro9-Pro10 region, improve metabolic stability at the Arg6-Arg7 trypsin-sensitive site by altering the local backbone conformation, and preserve OPRM1 binding affinity, yielding a protease-resistant analog suitable for systemic delivery.
Why it’s plausible
The Arg6-Arg7 dipeptide in YGGFLRRI(R)P is a canonical trypsin cleavage site; systemic peptides containing R-R motifs are rapidly degraded in plasma and gut. The C-terminal amide already protects the C-terminus. N-methylation at Ile8 would be sterically tolerated (Ile side chain is branched but not in the backbone) and could propagate a conformational change through the backbone that narrows the Arg6-Arg7 scissile bond accessibility to serine proteases, a strategy demonstrated in cyclosporine and other N-methylated bioactive peptides.
Why it matters
A single backbone N-methylation converting a protease-labile dynorphin fragment to a stable MOR agonist would advance it toward a peptide drug candidate, addressing the key liability of endogenous opioid peptides as therapeutics.
Plausibility.60
Novelty.50
Impact.55
Basis · grounding2 computed/notes
[1]
sequenceRR at positions 6-7 in YGGFLRRIRP is a high-risk trypsin site; Ile8 is adjacent and its N-methylation would add steric bulk protecting the adjacent peptide bond.
[2]
structureipTM=0.88 confirms a well-defined OPRM1 interface for the 1-10 amide, providing a high-confidence structural model in which to evaluate the impact of backbone modification at position 8.
openupdated 2026-06-05

Does cutting dynorphin short make it trigger only the beneficial pain-relief pathway at the opioid receptor, avoiding the dangerous side-effect pathways?

Opioids like morphine cause overdose deaths partly because they activate a side-effect pathway in addition to pain relief. If this shorter dynorphin triggers only the beneficial pathway, it could become a template for a new generation of safer painkillers, potentially saving thousands of lives lost to opioid overdose each year.

The hypothesis
Dynorphin A (1-10) amide acts as a biased OPRM1 agonist favoring G-protein signaling over beta-arrestin recruitment, relative to both the full 17-mer and to morphine, because the truncated C-terminus eliminates interactions with extracellular receptor elements that stabilize the beta-arrestin-recruiting conformation.
Why it’s plausible
Biased agonism at opioid receptors, where G-protein signaling mediates analgesia and beta-arrestin recruitment drives tolerance and respiratory depression, is a major axis of next-generation opioid drug design. The conformation of the bound peptide influences the receptor's intracellular signaling state. A truncated dynorphin fragment that fits the orthosteric pocket (ipTM=0.88) without engaging extracellular loop regions contacted by the C-terminal extension of the full peptide might stabilize a G-protein-preferring receptor conformation.
Why it matters
If dynorphin A (1-10) amide is G-protein-biased at OPRM1, it represents an endogenous-sequence-derived biased scaffold with direct relevance to designing safer analgesics without the tolerance and respiratory depression liabilities of classical opioids.
Plausibility.40
Novelty.70
Impact.75
Basis · grounding1 paper · 1 computed/note
[1]
structureHigh ipTM=0.88 for the 1-10 amide at OPRM1 suggests tight, well-defined orthosteric binding; the absence of C-terminal residues removes contacts to extracellular loops that have been linked to beta-arrestin-biasing conformations in other opioid ligands.
[2]
paper
Pasternak 2013 reviews MOR splice variants and signaling diversity, providing context for how different ligand-binding modes can differentially engage downstream G-protein vs arrestin pathways.
doi: 10.1124/pr.112.007138
openupdated 2026-06-05

Does adding a simple chemical cap to the end of a 10-amino-acid dynorphin fragment change which opioid receptor it prefers?

If a single chemical modification can redirect this peptide between receptor subtypes, chemists could use it as a design rule to create highly receptor-specific opioids, potentially reducing side effects like respiratory depression that are tied to non-selective opioid drugs.

The hypothesis
The triple-arginine motif R6-R7-x-R9 in YGGFLRRIRP selectively favors OPRK1 over OPRM1 binding when the C-terminal amide is absent (free-acid form), but the amide cap reverses this preference by neutralizing C-terminal negative charge and stabilizing a conformation that favors OPRM1's orthosteric pocket geometry.
Why it’s plausible
Dynorphin family peptides are classically KOR-preferring, yet the 1-10 amide shows high OPRM1 ipTM (0.88). The C-terminal amide is specified in the card name and readme as a defining chemical feature. Amidation changes the electrostatic and hydrogen-bonding profile at the peptide terminus, and KOR's extracellular binding vestibule is known to accommodate extended positively charged peptides differently from MOR. The amide cap may therefore be the selectivity switch for MOR versus KOR preference in this fragment.
Why it matters
A single chemical modification (free acid vs amide) controlling MOR/KOR selectivity in a dynorphin fragment would be a minimal and generalizable design principle for engineering opioid receptor subtype selectivity without altering the primary sequence.
Plausibility.45
Novelty.70
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceYGGFLRRIRP contains R6, R7, R9 (three arginines), a basic triad characteristic of KOR-binding dynorphin fragments in the free-acid form; the amide cap at Pro10 modifies the C-terminal electrostatics.
[2]
structureipTM=0.88 at OPRM1 for the amide form is unexpectedly high for a dynorphin fragment, suggesting the amide cap may shift selectivity toward MOR relative to expectations from the parent sequence.
[3]
paper
Pasternak 2013 reviews opioid receptor selectivity determinants and notes that the C-terminal extensions of dynorphin peptides are key to KOR preference.
doi: 10.1124/pr.112.007138
openupdated 2026-06-05

Does cutting dynorphin A down to its first 10 amino acids and capping the end actually improve how well it grips the mu opioid receptor?

If true, this shorter capped peptide could become a template for new pain medicines that are more targeted and potentially safer than existing opioids, benefiting patients who need strong pain relief without high addiction risk.

The hypothesis
Dynorphin A (1-10) amide (YGGFLRRIRP-NH2) achieves higher OPRM1 affinity than the full 17-mer because the C-terminal amide on Pro10 mimics the transition-state geometry of the receptor-bound N-terminus, and the absence of the basic C-terminal extension eliminates electrostatic repulsion from acidic OPRM1 extracellular loop residues, making the 1-10 amide form a superior MOR agonist scaffold over the full peptide.
Why it’s plausible
The structure prediction for the 1-10 amide at OPRM1 yields ipTM=0.88, compared to 0.70 for the full 17-mer at the same target. The C-terminal amide replaces the free carboxylate of Pro10, eliminating negative charge and adding a hydrogen-bond donor. Amidation of peptide C-termini is a common strategy to increase receptor affinity and proteolytic stability. The higher ipTM suggests this fragment fits OPRM1 better than the parent peptide.
Why it matters
If the 1-10 amide is confirmed as the superior MOR scaffold among dynorphin fragments, it represents the minimal pharmacophore for MOR-selective dynorphin analogs, guiding medicinal chemistry toward short, metabolically stable peptides for pain management.
Plausibility.60
Novelty.30
Impact.55
Basis · grounding1 paper · 2 computed/notes
[1]
structureBoltz-2 ipTM=0.88 for YGGFLRRIRP (1-10 amide) at OPRM1, versus 0.70 for the full 17-mer, a difference suggesting substantially better interface complementarity for the shorter fragment.
[2]
sequenceYGGFLRRIRP ends at Pro10 with the C-terminal amide; Pro10 introduces a conformational constraint that may present the upstream opioid motif YGGFL in an optimal orientation for MOR engagement.
[3]
paper
Pasternak 2013 describes MOR-1 transmembrane architecture and consensus binding features, providing context for how the N-terminal YGGF motif docks into the orthosteric pocket.
doi: 10.1124/pr.112.007138
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8837057948112488 boltz-2
ranking score 0.8278200030326843 boltz-2
structural qualityopenfold3
metricvaluenote
gpde0.796global PDE — lower = better
disorderNaNfraction disordered
3-letter notation
Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro
recipeboltz-2 1.0
parametervalue
modelboltz-2 1.0
weights
hardwarenvidia_nim_api
mlx version
python
random seed
msa strategynone
diffusion samples1
runtime
predicted bymlx@peptide
predicted at2026-04-24
citationbibtex
peptidemodel (2026). Dynorphin A (1-10) amide: natural opioid fragment that boosts morphine pain relief (pep-10700, v1). PeptideModel. https://peptidemodel.com/card/pep-10700
@peptide{pep10700,
  sequence = {YGGFLRRIRP},
  target   = {oprm1},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 5 by signal overlap
clinical trials 0 trials · checked 2026-05-22
0
no registered clinical trials as of 2026-05-22; we'll re-check periodically
references 9 papers
[3] supporting
[4] supporting
[6] supporting
[8] supporting
discussion no comments
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