Phosphoramidon
Also known as: N-Phospho-Leu-Trp, Phosphoramidon disodium salt, RB 95-2886, Talopeptin
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Summary
Phosphoramidon is a naturally occurring pseudopeptide antibiotic/inhibitor isolated from Streptomyces tanashiensis. It is a classical pharmacological tool compound used extensively in research to characterize zinc metalloprotease activity, particularly neprilysin and endothelin-converting enzyme. It is not approved for clinical use and is used primarily as a reference inhibitor in biochemical and pharmacological studies.
Mechanism of Action
Potent inhibitor of zinc metalloprotease enzymes, particularly thermolysin, neprilysin (neutral endopeptidase, NEP), and endothelin-converting enzyme (ECE). Coordinates with the active-site zinc ion via its phosphoramidon moiety, blocking substrate access and enzymatic cleavage of peptide bonds.
Routes of Administration
Goals & Uses
- Inhibition of endothelin-converting enzyme (ECE)Research / Pharmacological ToolHigh
- Inhibition of neprilysin (NEP) activityResearch / Pharmacological ToolHigh
- Study of enkephalin and atrial natriuretic peptide metabolismNeuropharmacology / Cardiovascular ResearchModerate
- Characterization of thermolysin activityBiochemical ResearchHigh
Contraindications
- Human therapeutic administrationClinical UseHigh
Adverse Effects
- Broad metalloprotease inhibitionOff Target EffectsUnknown
- Cardiovascular effects (in vivo animal studies)CardiovascularUnknown
Drug Interactions
- Neprilysin substrates (ANP, BNP, enkephalins)Low
- Endothelin receptor antagonistsLow
Population Constraints
- Human useGeneral PopulationAbsolute
Regulatory Status
- European UnionUnapprovedResearch use only; no EMA authorization.
- United StatesUnapprovedResearch tool compound only; not an FDA-regulated drug for human use.
- United KingdomUnapprovedResearch use only; no MHRA authorization.
Not approved by any regulatory authority (FDA, EMA, MHRA) for human therapeutic use. Used exclusively as a research/tool compound in laboratory settings.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Phosphoramidon?
Phosphoramidon is a naturally occurring pseudopeptide antibiotic/inhibitor isolated from Streptomyces tanashiensis. It is a classical pharmacological tool compound used extensively in research to characterize zinc metalloprotease activity, particularly neprilysin and endothelin-converting enzyme. It is not approved for clinical use and is used primarily as a reference inhibitor in biochemical and pharmacological studies.
What is Phosphoramidon used for?
Phosphoramidon is educationally associated with: Inhibition of endothelin-converting enzyme (ECE), Inhibition of neprilysin (NEP) activity, Study of enkephalin and atrial natriuretic peptide metabolism, Characterization of thermolysin activity. Educational only — not medical advice.
How is Phosphoramidon administered?
Recorded routes of administration: In Vitro, Intravenous.
What are the potential side effects of Phosphoramidon?
Reported adverse effects include: Broad metalloprotease inhibition, Cardiovascular effects (in vivo animal studies). This list is not exhaustive — consult a qualified clinician.
Who should avoid Phosphoramidon?
Recorded contraindications: Human therapeutic administration. Consult a qualified clinician before use.