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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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Neurotensin receptors (nomenclature as recommended by NC-IUPHAR [5]) are activated by the endogenous tridecapeptide neurotensin (pGlu-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu) derived from a precursor (NTS, 30990), which also generates neuromedin N, an agonist at the NTS2 receptor. [3H]Neurotensin (human, mouse, rat) and [125I]neurotensin (human, mouse, rat) may be used to label NTS1 and NTS2 receptors at 0.1-0.3 and 3-5 nM concentrations respectively.
NTS1 receptor
C
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NTS2 receptor
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Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. Br J Pharmacol. 176 Suppl 1:S27-S156.
Neurotensin (NTS, P30990) appears to be a low-efficacy agonist at the NTS2 receptor [18], while the NTS1 receptor antagonist meclinertant is an agonist at NTS2 receptors [18]. An additional protein, provisionally termed NTS3 (also known as NTR3, gp95 and sortilin; ENSG00000134243), has been suggested to bind lipoprotein lipase and mediate its degradation [14]. It has been reported to interact with the NTS1 receptor [12] and the NTS2 receptor [3], and has been implicated in hormone trafficking and/or neurotensin uptake. A splice variant of the NTS2 receptor bearing 5 transmembrane domains has been identified in mouse [2] and later in rat [15]. The neurotensinergic system is implicated in various physiological and pathological processes related to neuropsychiatric and metabolic functions, cancer growth, food, and drug intake [9].