| Identification | Back Directory | [Name]
D-ARG-PRO-LYS-PRO-GLN-GLN-D-TRP-PHE-D-TRP-LEU-LEU-NH2 HYDROCHLORIDE | [CAS]
91224-37-2 | [Synonyms]
SPANTIDE
SPANTIDE I
(D-Arg1,D-Trp7
SPANTIDE HYDROCHLORIDE
M.W. 1497.80 C75H108N20O13
1-Arg-7,9-Trp-11-Leu-substance p
(D-ARG1,D-TRP7,9,LEU11)-SUBSTANCE P
[D-Arg1,D-Trp7,9,L-Leu11]substance P
Substance p, Arg(1)-Trp(7,9)-Leu(11)-
SUBSTANCE P, [D-ARG1, D-TRP7,9, LEU11]
(D-arg1,D-trp7,9,leu11)-substance P*acetate
D-ARG1,D-TRP7,9,LEU11]-SUBSTANCE P (SPANTIDE)
(D-Arg1,D-Trp7·9,Leu11)-Substance P, Spantide I
[D-ARG1,D-TRP7,9,LEU11]-SUBSTANCE P HYDROCHLORIDE
Substance p, arginyl(1)-tryptophyl(7,9)-leucine(11)-
D-ARG-PRO-LYS-PRO-GLN-GLN-D-TRP-PHE-D-TRP-LEU-LEU-NH2
H-D-ARG-PRO-LYS-PRO-GLN-GLN-D-TRP-PHE-D-TRP-LEU-LEU-NH2
D-ARG-PRO-LYS-PRO-GLN-GLN-D-TRP-PHE-D-TRP-LEU-LEU-NH2 HYDROCHLORIDE
D-Arg-L-Pro-L-Lys-L-Pro-L-Gln-L-Gln-D-Trp-L-Phe-D-Trp-L-Leu-L-Leu-NH2
Substance p, 1-D-arginine-7-D-tryptophan-9-D-tryptophan-11-D-leucine-
D-Arg-L-Pro-L-Lys-L-Pro-L-Glu(NH2)-L-Glu(NH2)-D-Trp-L-Phe-D-Trp-L-Leu-L-Leu-NH2
(D-Arg1,D-Trp7·9,Leu11)-Substance P H-D-Arg-Pro-Lys-Pro-Gln-Gln-D-Trp-Phe-D-Trp-Leu-Leu-NH2
L-Leucinamide, D-arginyl-L-prolyl-L-lysyl-L-prolyl-L-glutaminyl-L-glutaminyl-D-tryptophyl-L-phenylalanyl-D-tryptophyl-L-leucyl- | [Molecular Formula]
C75H108N20O13 | [MDL Number]
MFCD06801374 | [MOL File]
91224-37-2.mol | [Molecular Weight]
1497.79 |
| Chemical Properties | Back Directory | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C
| [form ]
Powder | [pka]
13.31±0.20(Predicted) | [color ]
White to off-white | [Water Solubility ]
Soluble to 1 mg/ml in water |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
|
| [IC 50]
NK1: 230 nM (Ki); NK2: 8150 nM (Ki) | [storage]
Desiccate at -20°C | [References]
[1] J C Beaujouan, et al. Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists. Br J Pharmacol. 1993 Mar;108(3):793-800. DOI:10.1111/j.1476-5381.1993.tb12880.x
[2] M Zubrzycka, et al. Comparison of antagonistic properties of substance P analogs, spantide I, II and III, on evoked tongue jerks in rats. Endocr Regul. 2000 Mar;34(1):13-8. PMID:10808247
[3] Linda D Hazlett, et al. Spantide I decreases type I cytokines, enhances IL-10, and reduces corneal perforation in susceptible mice after Pseudomonas aeruginosa infection. Invest Ophthalmol Vis Sci. 2007 Feb;48(2):797-807. DOI:10.1167/iovs.06-0882 |
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