Name | (D-ARG1,D-TRP7·9,LEU11)-SUBSTANCE P |
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Synonyms |
M.W. 1497.80 C75H108N20O13
SPANTIDE 1-Arg-7,9-Trp-11-Leu-substance p SPANTIDE HYDROCHLORIDE Spantide I Substance P-[D-Arg1,D-Trp7,9,Leu11] |
Description | Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation[1][2][3]. |
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Related Catalog | |
Target |
NK1:230 nM (Ki) NK2:8150 nM (Ki) |
In Vivo | Spantide I (50 and 100 nM perfused through the cerebral ventricles) causes a complete respiratory arrest in all of the examined animals[2]. Spantide I (36 μg/mouse, ip daily) significantly decreases the number of perforated corneas, bacterial counts, and PMNs. Spantide I also downregulates the mRNA levels for type I cytokines (e.g., IFN-γ) as well as MIP-2, IL-6, TNF-α, and IL-1β[3]. Animal Model: Female, 8-week-old C57BL/6 (B6) and BALB/c mice[3]. Dosage: 36 μg/mouse. Administration: IP on days -1 and 0 (day of infection) and daily through 5 days pi (post infection). Result: At 3 and 5 days pi, compound-treated mice had significantly less severe ocular disease than did the PBS-treated mice. Contained significantly fewer PMNs than the corneas of PBS-treated mice at 3 and 5 days pi. Significantly reduced levels of corneal TNF-α mRNA at 3 and 5 days pi. Significantly reduced the level of IL-18 mRNA at 1 day pi. |
References |
Molecular Formula | C75H108N20O13 |
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Molecular Weight | 1497.79000 |
Exact Mass | 1496.84000 |
PSA | 548.21000 |
LogP | 7.06100 |
Storage condition | -20°C |