[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
Biological Activity
Broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. Induces apoptosis and inhibits cancer cell growth in vitro.Technical Data
(Modifications: Arg-1 = D-Arg, Phe-5 = D-Phe, Trp-7 = Trp-9 = D-Trp, Leu-11 = C-terminal amide)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High constitutive signaling of the ghrelin receptor - identification of a potent inverse agonist.
Holst et al.
Mol.Endocrinol., 2003;17:2201 -
[D-Arg1, D-Phe5, D-Trp7,9, Leu11] Substance P acts as a biased agonist toward neuropeptide and chemokine receptors.
Jarpe et al.
J.Biol.Chem., 1998;273:3097 -
[D-Arg1, D-Phe5, D-Trp7,9, Leu11] Substance P induces apoptosis in lung cancer cells in vitro.
Reeve and Bleehen
Biochem.Biophys.Res.Commun., 1994;199:1313
Product Datasheets
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Citations for [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
The citations listed below are publications that use Tocris products. Selected citations for [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P include:
3 Citations: Showing 1 - 3
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A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity In vivo
Authors: Pastor-Cavada Et al.
Scientific Reports 2016;6:36456
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Devil's Claw to suppress appetite--ghrelin receptor modulation potential of a Harpagophytum procumbens root extract.
Authors: Torres-Fuentes Et al.
Oncotarget 2014;9:e103118
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Promiscuous dimerization of the GH secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling.
Authors: Schellekens Et al.
J Biol Chem 2013;288:181
FAQs
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