(D-Arg1,D-Phe5,D-Trp7.9,Leu11)-Substance P

Names

[ Name ]:
(D-Arg1,D-Phe5,D-Trp7.9,Leu11)-Substance P

[Synonym ]:
AntagonistD,D-Arg-Pro-Lys-Pro-D-Phe-Gln-D-Trp-Phe-D-Trp-Leu-Leu-NH2
L-Leucinamide, D-arginyl-L-prolyl-L-lysyl-L-prolyl-D-phenylalanyl-L-glutaminyl-D-tryptophyl-L-phenylalanyl-D-tryptophyl-L-leucyl-
D-Arg-L-Pro-L-Lys-L-Pro-D-Phe-L-Gln-D-Trp-L-Phe-D-Trp-L-Leu-L-Leu-NH2
M.W. 1516.85 C79H109N19O12
D-ARG-PRO-LYS-PRO-D-PHE-GLN-D-TRP-PHE-D-TRP-LEU-LEU-NH2
D-Arginyl-L-prolyl-L-lysyl-L-prolyl-D-phenylalanyl-L-glutaminyl-D-tryptophyl-L-phenylalanyl-D-tryptophyl-L-leucyl-L-leucinamide
H-D-ARG-PRO-LYS-PRO-D-PHE-GLN-D-TRP-PHE-D-TRP-LEU-LEU-NH2
DARG-PRO-LYS-PRO-DPHE-GLN-DTRP-PHE-DTRP-LEU-LEU-NH2: DA-PKP-DF-Q-DW-F-DW-LL-NH2
Substance P-[D-Arg1,D-Phe5,D-Trp7,9,Leu11]

Biological Activity

[Description]:

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca2+ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer[1][2][3]

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Bombesin Receptor

Signaling Pathways >> MAPK/ERK Pathway >> JNK

[References]

[1]. Jarpe MB, et al. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]Substance P acts as a biased agonist toward neuropeptide and chemokine receptors. J Biol Chem. 1998 Jan 30;273(5):3097-104.

[2]. Woll PJ, Rozengurt E. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]substance P, a potent bombesin antagonist in murine Swiss 3T3 cells, inhibits the growth of human small cell lung cancer cells in vitro. Proc Natl Acad Sci U S A. 1988 Mar;85(6):1859-63.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₇₉H₁₀₉N₁₉O₁₂

[ Molecular Weight ]:
1516.831

[ Exact Mass ]:
1515.850342

[ PSA ]:
505.12000

[ LogP ]:
3.94

[ Index of Refraction ]:
1.677

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Effect of nanoconfinement on polymer dynamics: surface layers and interphases.

PLoS ONE 9(7) , e103118, (2014)

We present neutron spin echo experiments that address the much debated topic of dynamic phenomena in polymer melts that are induced by interacting with a confining surface. We find an anchored surface...

Intrarenal ghrelin receptor antagonism prevents high-fat diet-induced hypertension in male rats.

Endocrinology 155(7) , 2658-66, (2014)

Excess weight gain contributes up to 65% of the risk of primary hypertension, and the increase in blood pressure in response to high-fat diet (HFD) is preceded by significant increases in renal tubula...

Over-expression of the truncated ghrelin receptor polypeptide attenuates the constitutive activation of phosphatidylinositol-specific phospholipase C by ghrelin receptors but has no effect on ghrelin-stimulated extracellular signal-regulated kinase 1/2 activity.

Int. J. Biochem. Cell Biol. 39(4) , 752-64, (2007)

In addition to regulating growth hormone release from the pituitary, ghrelin receptors also influence cell proliferation and apoptosis. By studying mitogen-activated protein kinase activity in human e...

Related Compounds

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