Neurotensin receptors

The endogenous peptide neurotensin was discovered in 1973 in bovine hypothalami for its ability to induce vasodilatation.   Neurotensin is a brain and gastrointestinal peptide that acts on three subtypes of neurotensin receptors: the high affinity G-protein-coupled receptor NTS1, low affinity NTS2, and the single transmembrane receptor NTS3 (Sortilin 1).   Neurotensin is found in both the central nervous system, where it is located in neuronal synaptic vesicles, and in the gastrointestinal tract  where it is found in neuroendocrine cells, and so has a dual function as a neurotransmitter-neuromodulator in the CNS and as a hormone in the periphery.   The pharmacological roles of neurotensin through its three known receptors are numerous, neurotensin is involved in several important biological functions including analgesia and hypothermia and also food intake and glucose homeostasis.  Neurotensin receptors also have a role in promoting tumour cell proliferation, migration and  DNA synthesis.  Expression of neurotensin and its receptors has also been correlated to cancer prognosis and prediction of treatment.

Further reading

Vincent et al (1999) Neurotensin and neurotensin receptors. Trends Pharmacol Sci. 20(7) 302 PMID: 10390649

Mazella et al (2012) Neurotensin and its receptors in the control of glucose homeostasis. Front Endocrinol. 3 143 PMID: 23230428

Nikolaou et al (2020) The role of Neurotensin and its receptors in non-gastrointestinal cancers: a review. Cell Commun Signal. 18(1) 68 PMID: 32336282

Kyriatzis et al (2024) Neurotensin and Neurotensin Receptors in Stress-related Disorders: Pathophysiology & Novel Drug Targets. Curr Neuropharmacol. 22(5) 916 PMID: 37534788