pe
pep-10697 v1 CC-BY-SA-4.0

Pig spinal-cord peptide that tightens muscle and dulls pain (Neuromedin U-8, porcine)

A short peptide first found in pig spinal cord that tightens smooth muscle (like in the gut and uterus), tweaks brain signaling, and dulls pain; it also latches onto a receptor that is overactive in most pancreatic cancers. Used only as a laboratory research tool, not a medicine.

statussynthesized targetNTSR1 length8 aa refs4
status 4 / 5
prediction metrics boltz-2 2.2.1
ipTM0.954
pTM0.959
avg pLDDT52.2
ranking score0.609
STRUCTURE · PEP-10697 × NTSR1
ranking0.609
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 2.2.1 · mmCIF ↓ download
sequence8 aa
158
YFLFRPRN
overview readme

What this is

Neuromedin U-8 (NmU-8) is an 8-amino-acid peptide first isolated from porcine spinal cord in 1985. It is the shorter of two forms of Neuromedin U identified in pigs — the other, NmU-25, contains the NmU-8 sequence intact at its C-terminus. The name "neuromedin" reflects its neuronal origin, and the "U" denotes its potent ability to contract uterine smooth muscle in rats (Minamino et al. 1985). NmU-8 is a research tool used to probe the biology of Neuromedin U receptors and, in the oncology context, an oncogenic signaling axis involving the neurotensin receptor 1 (NTSR1). The stored sequence YFLFRPRN represents the backbone; the active form carries a C-terminal amide (–NH₂) on the asparagine, a post-translational modification that is essential for receptor binding and is absent from the raw sequence shown here.

History

Neuromedin U-8 and its longer sibling Neuromedin U-25 were purified by Minamino, Kangawa, and Matsuo from porcine spinal cord and reported in 1985 (Minamino et al., Biochemical and Biophysical Research Communications). Their discovery came as part of a broader search for novel neuropeptides with smooth-muscle-stimulating activity in the spinal cord — the same search that identified several other neuromedins around the same period. The "U-8" and "U-25" designations indicate peptide length (8 and 25 residues, respectively). NmU-25 contains paired arginine residues immediately upstream of the NmU-8 sequence, pointing to a common precursor that is processed by prohormone convertases. Specific G-protein-coupled receptors for Neuromedin U — NMUR1 (peripherally expressed) and NMUR2 (centrally expressed) — were not identified until around 2000, over a decade after the peptides themselves were discovered. The NmU-25 human sequence was later found to be highly conserved across mammals, with the five C-terminal residues identical across all characterized species.

What it does

Neuromedin U-8 reproduces the core biological activities of the full-length NmU-25 because its C-terminal heptapeptide (shared with NmU-25) contains all the determinants required for receptor activation. In the periphery, NmU acts on NMUR1 to contract smooth muscle — including uterine, vascular, and gastrointestinal muscle — and to modulate gastric emptying and gut motility. In the brain, NmU acts via NMUR2 to suppress food intake and increase energy expenditure; mice lacking NmU develop obesity, while mice overexpressing it are lean and eat less. Centrally, NmU activates corticotropin-releasing hormone (CRH) neurons in the hypothalamic paraventricular nucleus, triggering stress-axis responses and contributing to the suppression of appetite. NmU also modulates pain perception: mice lacking NMUR2 show impaired nociceptive responses. In addition, NmU influences dopamine circuit activity in the brain. In the oncology context, NmU has been found overexpressed in several tumor types, where it can drive cancer cell proliferation and invasion via distinct receptor-mediated pathways.

Evidence

  • Human: No clinical trials of Neuromedin U-8 have been registered on ClinicalTrials.gov. NmU-8 is used as a pharmacological research tool and is not in clinical development. Human relevance comes from studies showing that the NmU signaling axis (via NMUR1, NMUR2, and in certain cancers a GHSR1b/NTSR1 heterodimer) is conserved and that NmU overexpression is documented in human tumor samples.
  • Animal: Rodent studies have established NmU's role in energy homeostasis: central NmU administration reduces food intake and body weight; NmU-knockout mice become obese; NmU-overexpressing mice are hypophagic and lean. NMUR2-knockout mice show blunted nociceptive responses. Peripheral NmU administration decreases gastric emptying and modulates insulin secretion.
  • In vitro: NmU-8, as the minimally active fragment of NmU, is used in cell-based assays to activate NMUR1 and NMUR2 signaling (Gq/11 pathway: phospholipase C activation and intracellular calcium release; Go pathway: adenylyl cyclase inhibition). In cancer cell lines, NmU increases proliferation, migration, and invasion, with pancreatic cancer studies implicating the HGF/c-Met pathway downstream of NMUR1.

Mechanism

NmU-8 is an agonist at two class A GPCRs: NMUR1 (predominantly peripheral — intestine, pancreas, lung, immune tissues) and NMUR2 (predominantly central — hypothalamus, hippocampus, spinal cord). Both receptors couple to Gq/11, activating phospholipase C and raising intracellular calcium, as well as to Go, inhibiting adenylyl cyclase. The C-terminal amide on Asn-8 is required for high-affinity receptor engagement; removing it sharply reduces potency.

The platform assigns NmU-8 to NTSR1, which reflects a distinct oncogenic context: in non-small-cell lung carcinoma, NmU was found to signal not through NMUR1 or NMUR2 but through a heterodimer of the growth hormone secretagogue receptor splice variant GHSR1b and NTSR1. This heterodimer elevates cAMP (rather than calcium) and drives tumor cell proliferation. NTSR1 is independently overexpressed at high rates in pancreatic ductal adenocarcinoma (PDAC), where it promotes tumor growth and metastasis via MAPK and NF-κB signaling. The NmU/NTSR1 axis in lung cancer and the independent NTSR1-overexpression story in PDAC are thus two separate but convergent threads that make NTSR1 the relevant target anchor for this card.

Structurally, NTSR1 is a well-characterized class A GPCR. White and colleagues (Nature, 2012) resolved the crystal structure of NTSR1 in the agonist-bound state, revealing the conformational changes driving receptor activation. Deluigi and colleagues (Science Advances, 2021) extended this by solving NTSR1 complexes with small-molecule full agonists, partial agonists, and inverse agonists, providing structural determinants that distinguish each pharmacological class — work directly relevant to understanding how ligands including peptide tools like NmU-8 engage the receptor.

Known effects

  • Smooth muscle contraction — Established in vitro and in vivo (uterine, vascular, gastrointestinal)
  • Appetite suppression / anti-obesity — Preclinical (rodent models); NmU-deficient mice develop obesity; NmU-overexpressing mice are lean
  • Energy expenditure increase — Preclinical; central NmU raises body temperature and locomotor activity
  • HPA axis activation / stress response — Preclinical; NmU activates CRH neurons and elevates corticosterone
  • Pain modulation — Preclinical; NMUR2 knockout impairs nociceptive responses
  • Tumor-promoting activity (cancer context) — Preclinical and human tissue data; NmU overexpressed in pancreatic and lung cancers

Related peptides

  • Neuromedin U-25 — The 25-residue full-length form containing the NmU-8 sequence at its C-terminus; the precursor fragment from which NmU-8 is derived by prohormone convertase cleavage (Minamino et al. 1985).
  • Neurotensin — The endogenous agonist for NTSR1; a 13-residue neuropeptide. The NmU/GHSR1b/NTSR1 oncogenic axis places NmU in mechanistic proximity to neurotensin biology at the receptor level, though the two peptides are structurally unrelated.
  • Neuromedin N — A 6-residue neurotensin-related peptide encoded on the same pro-neurotensin/neuromedin N precursor as neurotensin; processed differentially by tissue-specific prohormone convertases (Kitabgi 2006). Distinct lineage from Neuromedin U.
Hypotheses5 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

Is Neuromedin U-8 incorrectly catalogued as acting on the neurotensin receptor when it actually works through its own distinct receptor family?

Correct receptor annotation is the foundation of drug development. If researchers design NmU-8-based drugs aiming at the neurotensin receptor, they would be targeting the wrong protein, wasting resources and potentially missing therapeutic opportunities in the neurology and cancer fields where the true NmU receptors are relevant.

The hypothesis
The annotated target NTSR1 for Neuromedin U-8 (YFLFRPRN) is inconsistent with the established pharmacology of this peptide, which acts through NMU1R and NMU2R rather than the neurotensin receptor; the high structure-prediction interface score (ipTM=0.95) with low pLDDT (52.2) indicates a disordered docking solution that may reflect non-specific fit rather than genuine NTSR1 ligand geometry, and the true primary target remains the NMU receptor family.
Why it’s plausible
The readme explicitly states NmU-8 acts through Neuromedin U receptors (NMU1R/NMU2R), not NTSR1. NTSR1 binds neurotensin, a 13-residue peptide with a distinct pharmacophore (pyroGlu-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu). NmU-8 (YFLFRPRN) shares the C-terminal -PRN motif with neurotensin's -RRPYIL but has different charge and hydrophobicity profiles. Critically, pLDDT=52.2 is very low, indicating the structure prediction model places most atoms with poor confidence, and a high ipTM with low pLDDT often reflects a disordered or spurious docking. This combination argues against a well-defined NTSR1 interface and suggests target misannotation.
Why it matters
If NTSR1 is a misannotated target for NmU-8, any downstream analyses or drug design efforts predicated on NmU-8/NTSR1 interaction would be founded on incorrect assumptions, and correcting the annotation to NMU1R/NMU2R would redirect the scientific value of this peptide toward the neurology and oncology applications where NmU receptor biology is active.
Plausibility.85
Novelty.50
Impact.70
Basis · grounding1 paper · 2 computed/notes
[1]
structureBoltz-2 ipTM=0.95 but pLDDT=52.2, a combination indicating high nominal interface confidence paired with very low per-residue structural confidence, consistent with a disordered docking artifact rather than a true binding pose.
[2]
noteThe readme explicitly identifies NMU1R and NMU2R as the Neuromedin U receptors, and notes the NTSR1 annotation appears in an oncology context as a secondary interaction axis rather than the primary pharmacological target.
[3]
paper
Neurotensin receptor literature (Carraway and Leeman 1973 cited therein) establishes NTSR1's natural ligand as neurotensin, a structurally distinct peptide, setting a baseline for evaluating NmU-8 as a genuine vs spurious NTSR1 ligand.
doi: 10.1038/nature11558
openupdated 2026-06-05

Could this spinal cord peptide quiet the overactive nerve pain circuits in conditions like diabetic neuropathy or post-injury chronic pain, without involving opioid receptors at all?

Neuropathic pain affects roughly 10% of adults and responds poorly to opioid drugs. A non-opioid peptide painkiller derived from the body's own spinal cord chemistry could help millions of neuropathic pain patients who currently have no good treatment options, without any addiction risk.

The hypothesis
NmU-8 (YFLFRPRN-NH2) stimulates NMU2R on spinal cord dorsal horn neurons to produce sustained antinociception in neuropathic pain models through a mechanism that does not involve opioid receptors, because NMU2R is highly expressed in superficial dorsal horn laminae that overlap with but are distinct from opioid-receptor-bearing neurons, and NmU2R activation inhibits NMDA-receptor-mediated central sensitization.
Why it’s plausible
NmU-8 was isolated from porcine spinal cord, a principal site of pain processing. NMU2R is expressed in dorsal root ganglia and spinal cord. The readme notes NmU-8's analgesic properties. Central sensitization in neuropathic pain involves NMDA receptor-mediated synaptic potentiation in the dorsal horn. NmU receptor activation in the CNS is reported to modulate nociceptive processing; if this occurs through suppression of NMDA-dependent windup rather than opioid receptor recruitment, NmU-8 analogs would be non-opioid analgesics with a mechanism directly relevant to neuropathic pain, a condition poorly served by opioids.
Why it matters
A non-opioid spinal analgesic derived from an endogenous spinal cord peptide would represent an entirely new mechanistic class for treating neuropathic pain, with no addiction liability, filling a major therapeutic gap.
Plausibility.55
Novelty.55
Impact.75
Basis · grounding3 computed/notes
[1]
noteNmU-8 was isolated from porcine spinal cord and the readme notes its analgesic properties; spinal cord is the primary site of dorsal horn pain processing, directly localizing the peptide's potential antinociceptive site of action.
[2]
sequenceYFLFRPRN contains Phe2, Leu3, Phe4 providing a hydrophobic core and Arg5 providing positive charge; this combination resembles the pharmacophore of other peptides known to modulate NMDA receptor activity indirectly through GPCR signaling.
[3]
sourceReview of neurotensin and related neuropeptide precursor processing discusses the spinal cord distribution of peptide-processing enzymes, supporting that NmU-8 would be generated at the correct anatomical site to influence spinal nociception.
openupdated 2026-06-05

Do the three fatty amino acids in a row inside NmU-8 act as a size filter, fitting into the brain receptor but being too bulky for the gut receptor?

Drugs that activate only the brain form of a receptor avoid the gut side effects, like muscle contractions and cramps, that plague drugs activating both versions. If this peptide is naturally CNS-selective, it could inspire cleaner drugs for central nervous system conditions including neuropathic pain, stress disorders, and potentially eating disorders.

The hypothesis
The Phe2-Leu3-Phe4 hydrophobic triad in NmU-8 (YFLFRPRN) creates a selectivity filter that favors NMU2R over NMU1R because NMU2R has a deeper hydrophobic binding cleft in its orthosteric pocket that accommodates the phenylalanine side chains, while NMU1R's shallower pocket imposes steric exclusion of the Phe4 side chain, making NmU-8 a naturally NMU2R-biased fragment.
Why it’s plausible
NMU1R and NMU2R have distinct tissue distributions and functional roles: NMU1R is peripheral (gut, immune), NMU2R is central (CNS, spinal cord). Selective NMU2R activation would target central functions including analgesia and stress response while avoiding peripheral effects on smooth muscle contraction. The NmU-8 peptide was isolated from spinal cord, a NMU2R-rich region, suggesting it may be the endogenous NMU2R-selective form generated by tissue-specific processing of the longer NmU-25. The Phe2-Leu3-Phe4 cluster would impose steric selectivity between receptor subtypes with different pocket geometries.
Why it matters
If NmU-8 is confirmed as NMU2R-selective through its Phe-Leu-Phe core, it provides a minimal pharmacophore for designing CNS-targeted NMU2R agonists for neuropathic pain and stress-related disorders without activating peripheral NMU1R-dependent smooth muscle responses.
Plausibility.45
Novelty.60
Impact.60
Basis · grounding3 computed/notes
[1]
sequenceYFLFRPRN positions Phe2, Leu3, Phe4 as consecutive hydrophobicresidues, an unusual concentration in an 8-residue peptide that would project significant steric bulk into the receptor binding pocket.
[2]
noteNmU-8 was isolated specifically from spinal cord, a tissue with high NMU2R expression, while the longer NmU-25 is more broadly distributed; tissue-specific processing generating the 8-mer in a NMU2R-rich location is consistent with NMU2R selectivity.
[3]
sourceStructural study of a related peptide-GPCR complex shows how hydrophobic residues in peptide ligands determine subtype selectivity through differential pocket depth between receptor paralogs.
openupdated 2026-06-05

Does the presence or absence of a single chemical cap on the end of this peptide determine whether it triggers a calcium signal versus a different internal messenger in cells?

If one chemical modification switches between two completely different internal cell signals, it could explain why the same receptor produces different effects in different tissues and could be exploited to design tissue-specific drugs for conditions like obesity, pain, or cancer where the NmU receptor is involved.

The hypothesis
The C-terminal amide on NmU-8 (YFLFRPRN-NH2) is not merely a stability modification but is required for productive NMU2R coupling to Gq versus Gs proteins, such that the free-acid form of YFLFRPRN preferentially activates Gs-mediated cAMP production while the amidated form selectively drives Gq-mediated calcium signaling, representing intrinsic biased agonism conferred by a single post-translational modification.
Why it’s plausible
The readme specifies that the C-terminal amide is essential for receptor binding. Amidation of neuropeptide C-termini can influence the bound peptide conformation within the receptor binding pocket, and the precise geometry of the bound C-terminus is known to influence which G-protein heterotrimer is recruited in structurally related GPCR systems. If the amide contacts a specific extracellular loop residue of NMU2R that positions the receptor toward a Gq-coupling conformation, while the carboxylate repels that contact, the two forms would be biased agonists at the same receptor. This is directly testable because the two forms differ only at the C-terminus.
Why it matters
Biased agonism controlled by a single chemical modification in an endogenous neuropeptide would have broad implications for understanding how post-translational processing generates functional diversity in neuropeptide signaling, and would make NmU-8 amide a tool for dissecting NMU2R-linked pathways in appetite, pain, and cancer.
Plausibility.40
Novelty.70
Impact.60
Basis · grounding3 computed/notes
[1]
noteThe readme explicitly states the C-terminal amide on Asn is essential for receptor binding, implying that the free-acid form is pharmacologically distinct, though the nature of this distinction at the G-protein coupling level is uncharacterized.
[2]
sequenceYFLFRPRN; the C-terminal Asn amide is the only chemical difference between the active and inactive forms, making this a minimal chemical modification with potential for large signaling consequences.
[3]
sourceStructural studies of related peptide-GPCR complexes cited in this literature show how C-terminal peptide geometry influences extracellular loop contacts that determine G-protein coupling selectivity.
openupdated 2026-06-05

Could a modified version of this peptide form a near-permanent grip on its receptor, making it useful as a tool for precisely mapping where that receptor is located in the nervous system?

Scientists cannot currently measure exactly where and how densely NmU receptors sit in the pain-processing spinal cord without radioactive tracers. A non-radioactive peptide that locks onto the receptor would enable safer, more detailed maps of pain receptor distribution in human tissue, accelerating the development of targeted pain therapies.

The hypothesis
Substituting the C-terminal amide on NmU-8 (YFLFRPRN-NH2) with a boronic acid at Asn8 would preserve the hydrogen-bond-donor geometry required for NMU receptor engagement while adding covalent capture capability against Ser or Thr residues in the NMU2R binding pocket, converting NmU-8 from a reversible agonist into a slowly dissociating covalent probe for in vivo NMU2R occupancy measurement.
Why it’s plausible
Boronic acids form reversible covalent bonds with vicinal diols and can form slowly reversible dative bonds with serine and threonine hydroxyl groups at close range within protein binding pockets, a strategy used to create long-acting peptide probes. The C-terminal amide of NmU-8 is essential for receptor binding and likely contacts a polar residue in the binding pocket; an Asn-boronic acid isostere would retain the polar contact while adding covalent capture potential. This would create the first NmU2R-selective covalent chemical probe, enabling receptor occupancy studies in intact tissue without radioligand binding.
Why it matters
A covalent NMU2R probe would enable definitive receptor occupancy measurements in spinal cord tissue sections, resolving current uncertainties about the cellular localization and density of NMU2R in pain circuits, directly informing the therapeutic window for NMU2R agonist drugs.
Plausibility.40
Novelty.75
Impact.55
Basis · grounding3 computed/notes
[1]
sequenceAsn8 at the C-terminus of YFLFRPRN is the site of amidation; its carbonyl can in principle be replaced by a boronic acid isostere that retains the H-bond donor property of the amide NH2 while adding electrophilic capture capability.
[2]
noteThe readme specifies that the C-terminal amide on Asn is required for receptor binding, localizing the critical contact to the residue being modified, which ensures the modification targets the relevant interface.
[3]
structureipTM=0.9542 (the highest of all five peptides in this batch) at the annotated receptor, providing the most precise structural model of any peptide here to guide design of the C-terminal modification, even given the low pLDDT caveat for NTSR1; if applied to NMU2R the geometry would inform boronic acid placement.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.9542521238327026 boltz-2
ranking score 0.6085836291313171 boltz-2
3-letter notation
Tyr-Phe-Leu-Phe-Arg-Pro-Arg-Asn
recipeboltz-2 2.2.1
parametervalue
modelboltz-2 2.2.1
weights
hardwarevast_v100_32gb
mlx version
python
random seed1
msa strategycolabfold_local
runtime
predicted by
predicted at2026-05-22
citationbibtex
peptidemodel (2026). Pig spinal-cord peptide that tightens muscle and dulls pain (Neuromedin U-8, porcine) (pep-10697, v1). PeptideModel. https://peptidemodel.com/card/pep-10697
@peptide{pep10697,
  sequence = {YFLFRPRN},
  target   = {ntsr1},
  author   = {peptidemodel},
  year     = {2026},
  status   = {synthesized}
}
related peptides 3 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 4 papers
discussion no comments
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