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PE-22-28

Spadin analog, TREK-1 inhibitor

A synthetic heptapeptide derived from spadin that selectively inhibits TREK-1 potassium channels, promoting neurogenesis and rapid antidepressant effects.

Molecular Profile
Formula C35H55N11O9
Mol. Weight 773.89 g/mol
Sequence Gly-Glu-Pro-Pro...
Clinical Data Trials
Scientific Data Studies
Route
Subcutaneous (SC)
300-1000 mcg
SUB
Intraperitoneal (IP, animal)
3-4 mcg/kg
INT
Oral (animal)
1 mg/kg
ORA

How It Works

How It Works: PE-22-28 functions as a potent and selective antagonist of the TREK-1 potassium channel, leading to enhanced neuronal excitability, increased serotonin signaling, and promotion of brain plasticity, which contributes to its antidepressant properties.

  • High-affinity TREK-1 blockade (IC50 = 0.12 nM), without affecting other K2P channels.
  • Stimulates hippocampal neurogenesis by increasing progenitor cell proliferation.
  • Enhances synaptogenesis through upregulation of PSD-95 expression.
  • Improves serotonergic neurotransmission, resulting in rapid antidepressant effects in behavioral models.

Pairs Well With

TB
TB-500
Systemic repair
Cu
GHK-Cu
Skin & collagen
KP
KPV
Anti-inflammatory
Ip
Ipamorelin
GH secretagogue

Latest Studies

Utility 2
pubmed Sep 12, 2017

Shortened Spadin Analogs Display Better TREK-1 Inhibition, <i>In Vivo</i> Stability and Antidepressant Activity.

Djillani. Alaeddine A; Pietri. Mariel M; Moreno. S&#xe9;bastien S; Heurteaux. Ca...

Researchers created a shorter version of the peptide spadin called PE 22-28, which blocks the TREK-1 channel much more strongly (about 500‑times lower IC50) and lasts longer in the body (up to 23 hours vs. 7 hours). In mouse tests, this new peptide reduced depressive‑like behavior, boosted brain cell growth, and increased markers of synapse formation.

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