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

Neurotensin Receptor

The neuropeptide neurotensin (NT) exerts central actionsthat include hypothermia, analgesia, and a number of effects that involve the modulation of nigrostriatal and mesocortico-limbic dopaminergic pathways. The two neurotensin receptor subtypes known to date, NTR1 and NTR2, belong to the family of G-protein-coupled receptors with seven putative transmembrane domains (TM). The NTR1 has high affinity for neurotensin, whereas the NTR2 has lower affinity for the peptide and is selectively recognized by levocabastine, an anti-histamine H1 receptor antagonist. These receptors have widespread, though not identical, central and peripheral distributions and exhibit distinct ontogenic profiles.

It is notably reported that NTR1 activation results in significant antinociception but also causes marked hypotension and hypothermia. In sharp contrast, NTR2 has emerged as an important pain target because NTR2-selective analogues exhibit potent analgesic activity in both acute and chronic pain conditions in dose-dependent analgesic effects without inducing drop in blood pressure or body temperature.

Neurotensin Receptor Related Products (25):

Cat. No. Product Name Effect Purity
  • HY-P0251
    Neurotensin(8-13) Agonist
    Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.
  • HY-110155
    LM11A-31 dihydrochloride
    LM11A-31 dihydrochloride, a non-peptide p75NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression[1][2].
  • HY-125880
    SBI-553 Modulator 99.86%
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM[1].
  • HY-P0234
    Neurotensin Agonist 98.78%
    Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).
  • HY-12802
    AF38469 Inhibitor 99.28%
    AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
  • HY-148650
    Sortilin antagonist 1 Antagonist
    Sortilin antagonist 1 (compound 44) is a sortilin antagonist with an IC50 value of 20 nM for inhibiting Neurotensin (NTS) binds to sortilin. Neurotensin is a sortilin ligand. Sortilin antagonist 1 can be used for the research of neurological disease[1].
  • HY-P4223
    Acetyl neurotensin (8-13)
    Acetyl neurotensin (8-13) is the shortest analog of neurotensin with full binding and pharmacological activities[1].
  • HY-P99688
    Latozinemab Inhibitor
    Latozinemab (AL001) is a recombinant humanized anti-Sortilin monoclonal antibody. Latozinemab effectively binds Sortilin with a high affinity and blocks the interaction between progranulin protein (PGRN) and Sortilin receptor. Latozinemab has the potential for progranulin gene (GRN) mutations causative of Frontotemporal dementia (FTD) (FTD-GRN) research[1][2].
  • HY-14277A
    Levocabastine hydrochloride Antagonist
    Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3].
  • HY-14277
    Levocabastine Antagonist
    Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3].
  • HY-139668
    VGD071 Inhibitor
    VGD071, a sortilin-targeting compound, is a promising candidate for future studies using mouse breast cancer models.
  • HY-P3057
    [D-Trp11]-Neurotensin Modulator
    [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[1][2].
  • HY-124673
    AF40431 Inhibitor 98.00%
    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[1].
  • HY-14551B
    (S)-Osanetant Antagonist 99.25%
    (S)-Osanetant is the S-enantiomer of Osanetant. Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia[1].
  • HY-P2544
    [Lys8, Lys9]-Neurotensin (8-13) Activator 99.81%
    [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[1].
  • HY-107664A
    SR 142948 dihydrochloride Antagonist
    SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders[1][2].
  • HY-107664
    SR 142948 Antagonist
    SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders[1][2].
  • HY-P1256C
    JMV 449 acetate Agonist 99.91%
    JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse[1][2].
  • HY-P0066
    Contulakin G Agonist
    Contulakin G is an O-glycosylated invertebrate neurotensin. Contulakin-G is a weaker agonist for the neurotensin receptor. Contulakin G is also a potent antinociceptive agent[1][2].
  • HY-P1255
    Kinetensin Agonist 99.57%
    Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma.