Drug intelligence / Profile preview

[D-Arg1,D-Trp5,7,9,Leu11]substance P

Development stage
Preclinical
Modality
Peptides
Administration
In Vitro, Experimental
01

Overview

**[D-Arg1,D-Trp5,7,9,Leu11]substance P** is a synthetic peptide analogue of substance P, designed as a broad-spectrum neuropeptide growth factor antagonist. It acts primarily as a potent inverse agonist and antagonist at multiple neuropeptide receptors, including the ghrelin receptor, tachykinin receptors, bradykinin receptors, CCK receptors, and bombesin receptors. This peptide inhibits constitutive ghrelin receptor activity (EC50 = 5.2 nM), blocks neuropeptide-induced calcium mobilization and mitogen-activated protein kinase activation, and induces apoptosis and inhibits tumor cell growth, particularly in small cell lung cancer models *in vitro* and *in vivo*.[2][4][5][7][9] Its mechanism is to broadly antagonize multiple neuropeptide signaling pathways implicated in cancer cell proliferation and survival. The compound is mostly used experimentally and in preclinical evaluation as a potential anticancer agent.

Other names
[D-Arg1,D-Trp5,7,9,Leu11]SP[D-Arg1,D-Trp5,7,9,Leu11]-substance P
02

Targets

TACR1 (Neurokinin‑1 Receptor)CCKAR (Cholecystokinin A receptor)GHSR (Growth hormone secretagogue receptor)BB receptors (Bombesin receptor family)Bradykinin B2 receptor

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