pe
pep-10567 v1 CC-BY-SA-4.0

Brain-pain research tool (M-15 / Galanin: Substance P chimera)

A lab-made hybrid peptide that blocks galanin's signals in the brain and spinal cord to study pain and nerve activity; used only as a lab research tool.

statussynthesized targetGALR1 length20 aa refs7
status 4 / 5
prediction metrics boltz-2 2.2.1
ipTM0.954
pTM0.919
avg pLDDT74.3
ranking score0.785
STRUCTURE · PEP-10567 × GALR1
ranking0.785
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 2.2.1 · mmCIF ↓ download
sequence20 aa
15101520
GWTLNSAGYLLGPQQFFGLM
overview readme

What this is

M-15 (also written as galanin-(1-13)-substance P-(5-11) amide) is a synthetic 20-amino-acid chimeric peptide built by fusing the front half of one neuropeptide, galanin, to the tail end of another, substance P. It was designed in the early 1990s as a research tool — the first reported high-affinity blocker of galanin's actions on neurons — and it remains a reference compound used to probe what galanin receptors do in the brain and spinal cord (Bartfai 1991; Langel 1992). The stored 20-letter sequence (GWTLNSAGYLLGPQQFFGLM) is the bare backbone; the active peptide carries a C-terminal amide inherited from the substance P portion, which is standard for this family and is not visible in the raw letter string.

History

The chimeric design strategy was introduced by Tamas Bartfai and colleagues at the Karolinska Institute, who reasoned that grafting the N-terminal recognition region of galanin onto the C-terminal "message" segment of substance P would produce a ligand that binds galanin receptors but does not transmit galanin's normal inhibitory signal (Bartfai 1991). The original 1991 report characterized M-15 as a 20-residue peptide that displaced radiolabeled galanin from binding sites in rat ventral hippocampus, midbrain, and spinal cord with an IC50 of approximately 0.1 nM (Bartfai 1991). A companion paper from the same group surveyed several related chimeras and identified galantide (galanin-(1-12)-Pro-substance P-(5-11) amide) as "the first galanin antagonist to be reported," establishing M-15 and galantide as the founding members of a small family of chimeric galanin-receptor ligands (Langel 1992). Their use as pharmacological tools was extended in the following years to dissect receptor subtypes — for example, Wynick and colleagues used M-15 to argue that the high-affinity galanin receptor on the rat anterior pituitary is distinct from the brain/gut receptor, because M-15's membrane binding there was markedly reduced (Wynick 1993).

What it does

In the brain regions where it has been tested, M-15 sits on galanin receptors without triggering galanin's usual response, and it blocks the natural peptide from doing so either. In the original characterization, M-15 reversed two well-known galanin effects: it blocked galanin's inhibition of evoked acetylcholine release in the hippocampus (measured in vivo) and it blocked galanin-induced hyperpolarization of locus coeruleus neurons in brain slices (Bartfai 1991). Because galanin tends to dampen the firing and transmitter release of the neurons it acts on, an antagonist like M-15 lifts that dampening — which is why this peptide has been a useful probe for asking what galanin is normally doing in a given circuit. M-15 is not selective among the three galanin receptor subtypes (GalR1, GalR2, GalR3) at the level of subtype pharmacology and is best understood as a galanin-receptor blocker in regions where the GalR1 subtype predominates, rather than a clean subtype-specific tool (Webling 2012; Freimann 2015).

Mechanism

M-15's design exploits a feature of galanin's pharmacology: the N-terminal portion of galanin (roughly residues 1–13) carries the bulk of the receptor-binding information, while the C-terminal portion contributes much less to affinity. Grafting that N-terminal recognition module onto the C-terminal heptapeptide of substance P (residues 5–11, amidated) produces a ligand that retains sub-nanomolar affinity for galanin binding sites — IC50 ≈ 0.1 nM against 125I-galanin in rat ventral hippocampus, midbrain, and spinal cord — but does not behave as a galanin agonist in functional assays in those regions (Bartfai 1991). The peptide is a reversible antagonist at the galanin binding site (Bartfai 1991). Across tissues, however, M-15's behavior is not uniform: in the rat anterior pituitary, membrane binding of M-15 is reduced compared with brain/gut tissue, which is part of the evidence that the pituitary galanin receptor is pharmacologically distinct (Wynick 1993). Subsequent cloning of three galanin receptor subtypes (GalR1, GalR2, GalR3) and their characterization with subtype-selective ligands has clarified that early M-15 results reflect the mixture of subtypes present in each tissue rather than a single defined target (Wang 1997; Lu 2005; Webling 2012).

Evidence

  • Human: No human clinical trials of M-15 have been published; the peptide is a preclinical research tool.
  • Animal: Reversible antagonism of galanin's inhibitory effects on hippocampal acetylcholine release in vivo and on locus coeruleus neuron firing in slices in rats (Bartfai 1991); reduced membrane binding in rat anterior pituitary used to distinguish the pituitary galanin receptor from brain/gut receptors (Wynick 1993).
  • In vitro: IC50 ≈ 0.1 nM displacement of 125I-galanin in membranes from rat ventral hippocampus, midbrain, and spinal cord (Bartfai 1991); used as a reference ligand in receptor-binding and autoradiography studies across the galanin literature (Webling 2012).

Known effects

  • Galanin receptor blockade in the central nervous system — Preclinical only; rat hippocampus, locus coeruleus, and spinal cord (Bartfai 1991).
  • Differential binding across galanin-receptor-expressing tissues — Used to argue for receptor heterogeneity (e.g., anterior pituitary vs. brain/gut) (Wynick 1993).
  • Reference antagonist in galanin pharmacology — Mechanistic and tool-compound use; not an indication (Webling 2012; Freimann 2015).

Regulatory status

  • US: Not an approved drug. No FDA filing. Research-use peptide only.
  • EU: No EMA approval; not marketed.
  • WADA: Not listed by name; as a non-approved investigational peptide that does not fall under hormone or growth-factor categories, it has no specific prohibited-list designation known to the authoring sources.

Related peptides

  • Galanin — the endogenous 29-residue (30 in humans) neuropeptide whose N-terminal 1–13 segment forms the recognition half of M-15. M-15 was built to block galanin's actions (Bartfai 1991).
  • Substance P — the tachykinin neuropeptide whose C-terminal 5–11 amide segment forms the second half of M-15. Substance P's own C-terminal amide is preserved in the chimera (Langel 1992).
  • Galantide (M-32) — the closely related chimera galanin-(1-12)-Pro-substance P-(5-11) amide; the first reported galanin antagonist and a sibling tool compound from the same design program (Langel 1992).
Hypotheses2 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 2026-06-11

Does M-15 hit all three galanin receptor subtypes equally, or does it favor one?

There are three galanin receptors with very different roles in the brain. If M-15 prefers one, researchers could use it to pin down which receptor drives memory loss or pain without confusing signals from the others.

The hypothesis
M-15 antagonizes GALR2 with higher functional selectivity relative to GALR1 than native galanin(1-13) does, because the substance P tail sterically clashes with the orthosteric pocket geometry unique to GALR1 but not GALR2, shifting the chimera's preference toward GALR2-mediated neuroprotective circuits.
Why it’s plausible
Galanin residues 1-13 are sufficient for binding all three receptor subtypes (GALR1/2/3). The C-terminal SP segment added in M-15 introduces bulky aromatic residues and a C-terminal amide that are absent in truncated galanin analogues. GALR1 and GALR2 differ substantially in their transmembrane bundle geometry and extracellular loop 2 composition, so the SP tail's steric demand would exert subtype-differential effects. Selectivity for GALR2 is therapeutically relevant because GALR2 activation is anti-apoptotic and neuroprotective in hippocampal seizure models.
Why it matters
Establishing that M-15 preferentially antagonizes one GALR subtype over another would resolve decades of ambiguity in galanin circuit studies that used M-15 as a pan-galanin blocker, and it would reveal whether the SP tail is a useful handle for engineering subtype selectivity.
Plausibility.60
Novelty.65
Impact.60
Basis · grounding1 paper · 2 computed/notes
[1]
noteM-15 used as reference galanin antagonist across brain and spinal cord, implying pan-subtype use but subtype selectivity not characterized
[2]
sequenceGalanin(1-13) segment covers all three receptor subtypes; PQQFFGLM adds bulky aromatic residues absent from native galanin
[3]
paper
Companion chimera study surveying related analogs for receptor-binding differences
doi: 10.1073/pnas.90.9.4231
openupdated 2026-06-11

Does the substance P portion of M-15 also bind the substance P receptor, on top of acting at the galanin receptor?

If M-15 acts on two pain-related receptors, some past spinal cord experiments may have credited the wrong receptor, and this dual action could be used on purpose to tackle chronic pain through two pathways at once.

The hypothesis
M-15 retains sufficient pharmacophore elements to act as a low-affinity partial agonist at the NK1 (substance P) receptor, because the PQQFFGLM C-terminal amide motif encodes the minimal SP message sequence required for NK1R recognition, potentially making M-15 a simultaneous GALR1 antagonist and NK1R modulator in the spinal dorsal horn.
Why it’s plausible
Substance P residues 5-11 (QQFFGLM-NH2) constitute the 'message' sequence with the highest NK1R-binding contribution. M-15 incorporates exactly this segment as its C-terminal half (PQQFFGLM-NH2 with amide). The galanin N-terminal 13 residues preceding it are hydrophilic and solvent-exposed in an extended conformation; NK1R has a large extracellular vestibule that could accommodate this N-terminal extension. Dual GALR1/NK1R activity in the spinal cord would represent a previously unrecognized polypharmacology that confounds interpretation of M-15 pain experiments.
Why it matters
If M-15 engages both GALR1 and NK1R in spinal nociception circuits, all pain studies using it as a galanin-specific probe would need reinterpretation, and its dual-target profile could be deliberately exploited for synergistic analgesia.
Plausibility.75
Novelty.20
Impact.55
Basis · grounding1 paper · 2 computed/notes
[1]
sequenceC-terminal PQQFFGLM-NH2 overlaps exactly with SP residues 5-11-NH2, the NK1R 'message sequence'
[2]
noteM-15 used to probe galanin receptors in spinal cord, a tissue rich in NK1R-expressing nociceptive neurons
[3]
paper
Locus coeruleus study uses M-15 in neuronal circuits where both galanin and substance P are co-expressed
doi: 10.1073/pnas.88.23.10961
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.954011857509613 boltz-2
ranking score 0.7852101922035217 boltz-2
3-letter notation
Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met
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). Brain-pain research tool (M-15 / Galanin: Substance P chimera) (pep-10567, v1). PeptideModel. https://peptidemodel.com/card/pep-10567
@peptide{pep10567,
  sequence = {GWTLNSAGYLLGPQQFFGLM},
  target   = {galr1},
  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 7 papers
discussion no comments
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