Target intelligence / Profile preview

Neurotensin (NT)

Target
NT
Molecular classification
Peptide, Hormone, Neurotransmitter, Neuromodulator, Ligand for the neurotensin receptor (not itself a receptor), Human metabolite
01

Overview

Neurotensin is a 13-amino acid peptide that acts both as a neurotransmitter in the central nervous system and as a hormone in the gastrointestinal tract. In the brain, neurotensin modulates the activity of dopamine pathways, exerts analgesic, hypothermic, and anorectic effects, and influences pituitary hormone secretion and other neuromodulatory functions. In the gut, it is secreted from N cells of the jejuno-ileal mucosa postprandially, regulating digestive enzyme release, gastrointestinal motility, and mucosal growth. Neurotensin is synthesized as part of a larger precursor that also gives rise to neuromedin N, and exerts its physiological effects mainly through activating the neurotensin receptor 1 (NTS1), a prototypical G protein-coupled receptor. Neurotensin and its signaling are implicated in the pathogenesis of various diseases, including several cancers and CNS disorders. It is a well-established experimental and potential therapeutic target, primarily through its receptor, but presents challenges in therapeutic targeting due to its diverse effects and potential for adverse impacts, particularly on tumor growth and CNS function

Other names
NeurotensinNTSNTNeuromedin NLarge neuromedin NTail peptidepro-neurotensin/neuromedinNMN-125NNNT/N
02

Mechanism of action

Drugs targeting neurotensin or its receptor typically act by modulating signal transduction via the neurotensin (NTS1) receptor, a G protein-coupled receptor, either as agonists to mimic neurotensin's action or as antagonists to block it

03

Biological functions

Signal transduction (via neurotensin receptors, notably NTS1)Modulation of dopaminergic neurotransmissionOpioid-independent analgesia (pain control)Inhibition of food intakeRegulation of digestive processes (e.g., stimulation of pancreatic and biliary secretion, inhibition of gastric acid secretion, modulation of gut motility)Regulation of pituitary hormone secretionPromotion of cell growth (particularly in gastrointestinal and cancer cells)HypothermiaAnorexiaOther neuromodulatory effects
04

Disease associations

Cancer (promotion of growth in colon, pancreas, lung, and prostate cancer cells)Neuropsychiatric disorders (schizophrenia, Parkinson's disease, drug addiction)PainInflammationEating disordersCardiovascular disease (central control of blood pressure)Other CNS disorders
05

Safety considerations

Off-target effects due to broad distribution and pleiotropic functions, especially CNS and gastrointestinal side effectsRisk of promoting cancer cell growth if agonists are used in cancer-prone tissues
06

Interacting drugs

Neurotensin receptor agonists and antagonists under research and development (e.g., peptide and non-peptide ligands)

2 more in the full profile.

07

Biomarkers

Expression levels of neurotensin or neurotensin receptors (especially NTS1) as biomarkers for some cancers (colon, pancreas, lung, prostate)Potential CNS/neuropsychiatric biomarkers (research context)

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