Kelatorphan
Also known as: H-Arg-Arg-Arg-Phe-Lys-Arg-Arg-Arg-NH2, KEL, Kelatorphan, N-[(R,S)-2-benzyl-3-(hydroxyaminocarbonyl)propanoyl]-L-alanine, RB 38A
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Summary
Kelatorphan is a synthetic, non‑natural peptide used experimentally to block multiple peptidases, especially NEP and aminopeptidase N. It is employed in vitro and in animal models to study peptide metabolism and analgesic pathways; it has no approved therapeutic indication.
Mechanism of Action
Potent competitive inhibition of neutral endopeptidase (NEP), aminopeptidase N, and related peptidases, leading to elevated endogenous opioid peptide levels.
Routes of Administration
Goals & Uses
- Reducing tolerance to exogenous opioidsResearchLow
- Study peptidase functionEnzyme BiologyHigh
- Pharmacological tool for opioid system researchResearchModerate
- Elevate endogenous enkephalin levelsAnalgesia ResearchModerate
- Analgesia via endogenous opioid potentiationPain ManagementLow
Contraindications
- Human clinical use (unapproved compound)RegulatoryHigh
Adverse Effects
- Local Injection Site ReactionsDermatologicalUnknown
- HypotensionCardiovascularUnknownLow blood pressure
- Opioid-like side effects (potential)Central Nervous SystemUnknown
Drug Interactions
- Neprilysin inhibitors (e.g., sacubitril)Moderate
- Opioid analgesics (e.g., morphine)Moderate
Population Constraints
- Human subjects (general population)Regulatory/SafetyAbsolute
Regulatory Status
- European UnionUnapprovedNo clinical authorization.
- United StatesUnapprovedResearch chemical only.
- United KingdomUnapprovedNo MHRA approval; research use only.
Not approved for human use in any jurisdiction; classified as a research chemical.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Kelatorphan?
Kelatorphan is a synthetic, non‑natural peptide used experimentally to block multiple peptidases, especially NEP and aminopeptidase N. It is employed in vitro and in animal models to study peptide metabolism and analgesic pathways; it has no approved therapeutic indication.
What is Kelatorphan used for?
Kelatorphan is educationally associated with: Reducing tolerance to exogenous opioids, Study peptidase function, Pharmacological tool for opioid system research, Elevate endogenous enkephalin levels, Analgesia via endogenous opioid potentiation. Educational only — not medical advice.
How is Kelatorphan administered?
Recorded routes of administration: Intracerebroventricular, Intraperitoneal, Intrathecal, Intravenous.
What are the potential side effects of Kelatorphan?
Reported adverse effects include: Local Injection Site Reactions, Hypotension, Opioid-like side effects (potential). This list is not exhaustive — consult a qualified clinician.
Who should avoid Kelatorphan?
Recorded contraindications: Human clinical use (unapproved compound). Consult a qualified clinician before use.