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Healing & Recovery
Preclinical

PE-22-28

PE-22-28

Also known as: Spadin, PE2228, TREK-1 Channel Blocker Peptide

Overview

Key Facts

Primary Goal: Research and therapeutic applications of PE-22-28

Selectively blocks TREK-1 two-pore potassium channels, increasing neuronal excitability. TREK-1 blockade mirrors the phenotype of TREK-1 knockout mice (antidepressant, resilient to stress).

Dosing Information

Half-Life

~1-2 hours (estimated from preclinical pharmacokinetics)

Typical Dose

100–500 mcg

Frequency

Once daily

Cycle Length

4-8 weeks on, 2-4 weeks off

Administration Routes:
subcutaneous

Benefits

  • Rapid-onset antidepressant effects (days rather than weeks)
  • Promotes hippocampal neurogenesis and BDNF expression
  • Enhances cognitive function and learning in animal models
  • Anxiolytic effects without sedation or dependence
  • Improves stress resilience and behavioural adaptability
  • Synergistic with other nootropic compounds

Side Effects

Very limited adverse event data (preclinical only)mild
Injection site irritationmild
Potential for altered sleep patterns (due to neurogenesis effects)mild
Theoretical cardiovascular effects at very high doses (TREK-1 is expressed in heart)mild

Mechanism of Action

1

Selectively blocks TREK-1 two-pore potassium channels, increasing neuronal excitability

2

TREK-1 blockade mirrors the phenotype of TREK-1 knockout mice (antidepressant, resilient to stress)

3

Increases serotonin and norepinephrine transmission via TREK-1 inhibition on raphe nuclei neurons

4

Promotes hippocampal neurogenesis through increased BDNF signaling

5

Enhances synaptic plasticity and long-term potentiation in hippocampal circuits

Contraindications

Do not use this peptide if any of the following apply:

  • Cardiac arrhythmias or QT prolongation (TREK-1 expressed in cardiac tissue)
  • Concurrent use of antidepressants (potential serotonergic interaction)
  • Pregnancy or breastfeeding
  • No established human safety profile — research use only

Storage & Reconstitution

Unreconstituted (Powder)

Temperature2–8°C (36–46°F) or -20°C (-4°F) for long-term
DurationUp to 3 months

Reconstituted (Mixed)

Temperature2–8°C (36–46°F)
Duration2-4 weeks

Note: Protect from light. Do not freeze reconstituted solution.

Research Summary

Preclinical

PE-22-28 (Spadin) was discovered by researchers at the Institut de Pharmacologie Moléculaire et Cellulaire (CNRS, France) and published in Nature Medicine (2010). The team demonstrated that sortilin-derived peptides block TREK-1 channels with high selectivity, producing antidepressant effects in mice within 4 days — compared to 21+ days for fluoxetine. Follow-up studies confirmed hippocampal neurogenesis, increased BDNF expression, and enhanced 5-HT neurotransmission. Behavioural tests (forced swim, tail suspension, novelty-suppressed feeding) consistently showed antidepressant and anxiolytic activity. PE-22-28 represents a novel mechanism entirely distinct from SSRIs, SNRIs, and ketamine-like drugs. Human clinical trials have not yet been conducted.

Frequently Asked Questions

Common questions about PE-22-28

UK-Specific Information

Exclusive data points and guidance for UK residents using PE-22-28

UK Lab Testing

UK Lab Testing

Recommended labs: Medichecks, Thriva (£89-£149 for peptide safety panel)

Why this matters: UK-specific lab testing guidance not available on US competitor sites

Commonly Stacked With

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