1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Neurotensin Receptor

Neurotensin Receptor

Neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin. Two of the receptors encoded by the NTSR1 and NTSR2 genes contain seven transmembrane helices and are G protein coupled. The third receptor has a single transmembrane domain and is encoded by the SORT1 gene. Neurotensin (NTS) is a 13-amino-acid peptide that functions as both a neurotransmitter and a hormone through the activation of the neurotensin receptor NTSR1, a G-protein-coupled receptor (GPCR). In the brain, NTS modulates the activity of dopaminergic systems, opioid-independent analgesia, and the inhibition of food intake; in the gut, NTS regulates a range of digestive processes.

Neurotensin Receptor Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-12802
    AF38469 Inhibitor 99.28%
    AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
  • HY-P0234
    Neurotensin Agonist
    Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).
  • HY-125880
    SBI-553 Modulator 98.85%
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
  • HY-16639
    ML314 Agonist 99.54%
    ML314 is a potent molecule agonist of NTR1 (EC50 = 1.9 μM); showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization.
  • HY-105189
    Meclinertant Antagonist >99.0%
    Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects.
  • HY-14277A
    Levocabastine hydrochloride Antagonist >98.0%
    Levocabastine (R 50547) hydrochloride is a long acting, highly potent and selective histamine H1-receptor antagonist with anti-allergic activity. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2.
  • HY-P3057
    [D-Trp11]-Neurotensin Antagonist
    [D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension.
  • HY-P2544
    [Lys8, Lys9]-Neurotensin (8-13) Activator
    [Lys8, Lys9]-Neurotensin (8-13) (JMV438), a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2, with Ki values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively.
  • HY-P0251
    Neurotensin(8-13) Agonist >98.0%
    Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.
  • HY-124673
    AF40431 Inhibitor 99.17%
    AF40431, the first reported small-molecule ligand of sortilin, has an IC50 of 4.4 µM and a Kd of 0.7 µM . AF40431 is bound in the neurotensin-binding site of sortilin.
  • HY-P1255
    Kinetensin Agonist 99.21%
    Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma.
  • HY-12436
    NTRC-824 Antagonist >98.0%
    NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC50 of 38 nM and a Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM).
  • HY-P1256
    JMV 449 Agonist
    JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.5 nM in binding to mouse brain membranes and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.
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