Leu-enkephalin vs Larazotide

Head-to-head comparison of Leu-enkephalin (Tyr-Gly-Gly-Phe-Leu) and Larazotide (Larazotide acetate (AT-1001)) — benefits, dosing, side effects, research data, and where to buy.

Research Score

PropertyLeu-enkephalinLarazotide
CategoryPain ManagementGastrointestinal
Full NameTyr-Gly-Gly-Phe-LeuLarazotide acetate (AT-1001)
Molecular Weight555.63 DaN/A
Half-Life1-5 minutes in plasmashort; designed for local gut action
Amino Acids58
Typical Dose0.1-5 ug per animal0.5-4 mg TID (clinical studies)
RouteIntrathecal / intracerebroventricularOral
Purity≥98%≥98%
Studies Count100040
Research StatusPre-clinicalClinical

Leu-enkephalin Benefits

  • delta-opioid activity
  • endogenous analgesic model
  • receptor-selective pharmacology
  • nociception pathway research

Larazotide Benefits

  • tight-junction-support
  • reduced-permeability
  • symptom-reduction
  • barrier-protection

Leu-enkephalin Dosing

Intrathecal 0.1-5 ug per animal|Intracerebroventricular 0.1-2 ug per animal|In vitro 1-100 nM

Larazotide Dosing

0.5-4 mg orally before meals in clinical trials|typically three times daily|short-course or chronic study protocols

Leu-enkephalin Side Effects

  • sedation
  • constipation-like opioid effects
  • very short plasma stability

Larazotide Side Effects

  • headache
  • nausea
  • abdominal discomfort

Research Overview

Leu-enkephalin

Leu-enkephalin is a standard tool in opioid receptor and pain-transmission research because it helps distinguish delta- from mu-preferring signaling. Its research value is high, but its clinical utility is limited by rapid enzymatic breakdown and delivery challenges.

Larazotide

Clinical and translational studies suggest larazotide can reduce antigen passage across the epithelium and improve gut barrier function. It is one of the better-known peptides for intestinal permeability and barrier-focused gastrointestinal therapy.

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Common Stacking Partners

Leu-enkephalin stacks with:

gabapentinketamine

Larazotide stacks with:

gluten-free dietprobioticsmesalamine
opioid-peptideenkephalindelta-opioidanalgesiaIBSceliactight-junctionspermeabilitybarrier-protection