Larazotide vs Leu-enkephalin

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

Research Score

PropertyLarazotideLeu-enkephalin
CategoryGastrointestinalPain Management
Full NameLarazotide acetate (AT-1001)Tyr-Gly-Gly-Phe-Leu
Molecular WeightN/A555.63 Da
Half-Lifeshort; designed for local gut action1-5 minutes in plasma
Amino Acids85
Typical Dose0.5-4 mg TID (clinical studies)0.1-5 ug per animal
RouteOralIntrathecal / intracerebroventricular
Purity≥98%≥98%
Studies Count401000
Research StatusClinicalPre-clinical

Larazotide Benefits

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

Leu-enkephalin Benefits

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

Larazotide Dosing

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

Leu-enkephalin Dosing

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

Larazotide Side Effects

  • headache
  • nausea
  • abdominal discomfort

Leu-enkephalin Side Effects

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

Research Overview

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.

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.

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Common Stacking Partners

Larazotide stacks with:

gluten-free dietprobioticsmesalamine

Leu-enkephalin stacks with:

gabapentinketamine
IBSceliactight-junctionspermeabilitybarrier-protectionopioid-peptideenkephalindelta-opioidanalgesia