A peptide antagonist of the NK1 receptor
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Spantide I (trifluoroacetate salt)

Item No. 43079

Technical Information
Formal Name
D-arginyl-L-prolyl-L-lysyl-L-prolyl-L-glutaminyl-L-glutaminyl-D-tryptophyl-L-phenylalanyl-D-tryptophyl-L-leucyl-L-leucinamide, trifluoroacetate salt
Synonyms
  • [Arg1,Trp7,9,Leu11] Substance P
  • DADTL
  • SPA I
Molecular Formula
C75H108N20O13 • XCF3COOH
Formula Weight
Purity
≥98%
A solid
Peptide Sequence
rPKPQQwFwLL-NH2
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N[C@H](CC1=CNC2=CC=CC=C21)C(N[C@@H](CC3=CC=CC=C3)C(N[C@H](CC4=CNC5=CC=CC=C54)C(N[C@H](C(N[C@@H](CC(C)C)C(N)=O)=O)CC(C)C)=O)=O)=O)[C@@H](NC([C@@H](NC([C@H]6N(C([C@H](CCCCN)NC([C@H]7N(C([C@@H](CCCNC(N)=N)N)=O)CCC7)=O)=O)CCC6)=O)CCC(N)=O)=O)CCC(N)=O.O=C(O)C(F)(F)F
InChi Code
InChI=1S/C75H108N20O13.C2HF3O2/c1-42(2)35-55(64(80)98)89-67(101)56(36-43(3)4)90-69(103)59(39-46-41-85-51-23-11-9-20-48(46)51)93-68(102)57(37-44-17-6-5-7-18-44)91-70(104)58(38-45-40-84-50-22-10-8-19-47(45)50)92-66(100)52(27-29-62(78)96)86-65(99)53(28-30-63(79)97)87-71(105)61-26-16-34-95(61)74(108)54(24-12-13-31-76)88-72(106)60-25-15-33-94(60)73(107)49(77)21-14-32-83-75(81)82;3-2(4,5)1(6)7/h5-11,17-20,22-23,40-43,49,52-61,84-85H,12-16,21,24-39,76-77H2,1-4H3,(H2,78,96)(H2,79,97)(H2,80,98)(H,86,99)(H,87,105)(H,88,106)(H,89,101)(H,90,103)(H,91,104)(H,92,100)(H,93,102)(H4,81,82,83);(H,6,7)/t49-,52+,53+,54+,55+,56+,57+,58-,59-,60+,61+;/m1./s1
InChi Key
YZTGFYJGWVAWPR-BHCZHNAISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Spantide I is a peptide antagonist of the neurokinin-1 (NK1) receptor (Ki = 177.83 nM).1 It is selective for the NK1 receptor over NK2 and NK3 receptors (Kis = 5,000 and >10,000 nM, respectively). Spantide I induces histamine release from isolated rat mast cells (EC50 = 2.5 µM).2 It inhibits neurokinin B-induced contractions in isolated and perfused guinea pig taenia coli when used at a concentration of 10 µM. Intrathecal administration of spantide I (2 µg/animal) increases the latency to withdrawal in the tail-flick- or hot plate test but also induces hindlimb paralysis in rats.3 Spantide I (36 µg/animal per day for five days) decreases corneal P. aeruginosa levels and polymorphonuclear cell infiltration, reduces corneal Il-1β levels, and increases corneal Il-10 levels in a mouse model of corneal P. aeruginosa infection.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McLean, S., Ganong, A., Seymour, P.A., et al. Pharmacology of CP-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor. J. Pharmacol. Exp. Ther. 267(1), 472-479 (1993).

    2. Håkanson, R., Leander, S., Asano, N., et al. Spantide II, a novel tachykinin antagonist having high potency and low histamine-releasing effect. Regul. Pept. 31(1), 75-82 (1990).

    3. Post, C., and Paulsson, I. Antinociceptive and neurotoxic actions of substance P analogues in the rat’s spinal cord after intrathecal administration. Neurosci. Lett. 57(2), 159-164 (1985).

    4. Hazlett, L.D., McClellan, S.A., Barrett, R.P., 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. 48(2), 797-807 (2006).