Leu-enkephalin vs Ziconotide

Head-to-head comparison of Leu-enkephalin (Tyr-Gly-Gly-Phe-Leu) and Ziconotide (ω-Conotoxin MVIIA (ziconotide)) — benefits, dosing, side effects, research data, and where to buy.

Research Score

PropertyLeu-enkephalinZiconotide
CategoryPain ManagementPain Management
Full NameTyr-Gly-Gly-Phe-Leuω-Conotoxin MVIIA (ziconotide)
Molecular Weight555.63 Da2639.1 Da
Half-Life1-5 minutes in plasmaapproximately 4.5 hours
Amino Acids525
Typical Dose0.1-5 ug per animal0.5-19.2 mcg/day
RouteIntrathecal / intracerebroventricularIntrathecal
Purity≥98%≥98%
Studies Count1000500
Research StatusPre-clinicalApproved

Leu-enkephalin Benefits

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

Ziconotide Benefits

  • strong non-opioid analgesia
  • effective for refractory neuropathic pain
  • opioid-sparing option
  • intrathecal delivery allows targeted action

Leu-enkephalin Dosing

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

Ziconotide Dosing

start 0.5 mcg/day intrathecal|titrate by 0.5 mcg/day no more than 2 times weekly|max 19.2 mcg/day in labeling

Leu-enkephalin Side Effects

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

Ziconotide Side Effects

  • dizziness
  • confusion
  • ataxia

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.

Ziconotide

Clinical studies and post-marketing data support ziconotide as an analgesic for severe chronic pain that does not respond to conventional therapy. Research focuses on balancing analgesic efficacy with neuropsychiatric tolerability and careful dose titration.

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Common Stacking Partners

Leu-enkephalin stacks with:

gabapentinketamine

Ziconotide stacks with:

BaclofenClonidineBupivacaine
opioid-peptideenkephalindelta-opioidanalgesiaN-type calcium channel blockerneuropathic painnon-opioidintrathecal