Sar9, Met (O2)11-Substance P

Summary

Sar9, Met(O2)11-Substance P is a metabolically stabilized analog of Substance P used primarily as a research tool. It is a potent and selective NK1 receptor agonist that resists degradation by neutral endopeptidase and other proteases, enabling sustained NK1 activation in vitro and in vivo. It is not approved for clinical use and is employed in studies of pain, neuroinflammation, nociception, and NK1 receptor pharmacology.

Mechanism of Action

Selective, full agonist at neurokinin 1 (NK1) receptors. The substitution of sarcosine at position 9 and methionine sulfone at position 11 confers resistance to enzymatic degradation while retaining high NK1 receptor binding affinity, making it a prototypical pharmacological tool for studying NK1-mediated signaling.

Routes of Administration

Goals & Uses

• NK1 receptor activation (research)Pharmacological ToolHigh
• NK1 receptor internalization assaysReceptor BiologyHigh
• Neuroinflammation studiesInflammation ResearchModerate
• Nociception and pain researchNeuroscience ResearchModerate

Contraindications

• Human therapeutic useRegulatory/safetyHigh

Adverse Effects

• HypotensionCardiovascularCommonLow blood pressure
• Nociceptive behavior (hyperalgesia/allodynia)NeurologicalCommon
• Plasma protein extravasation / edemaInflammatoryCommon

Drug Interactions

• NK1 receptor antagonists (e.g., aprepitant, L-703,606)High

Population Constraints

• General human populationRegulatory/safetyAbsolute

Regulatory Status

• European UnionUnapprovedNo EMA assessment; available solely as a laboratory research reagent.
• United StatesUnapprovedResearch chemical only; not reviewed by FDA for any therapeutic indication.
• United KingdomUnapprovedNo MHRA registration; research use only.

Not approved for human therapeutic use in any jurisdiction. Available exclusively as a research reagent from peptide synthesis suppliers. No IND or clinical trial registration is known.

Evidence & Sources

No sources recorded yet.