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

Neurotensin Receptor

Neurotensin Receptor

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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 Isoform Specific Products:

Neurotensin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12802
    AF38469
    		Inhibitor 99.28%
    AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
    AF38469
  • HY-P0234
    Neurotensin
    		Agonist 98.68%
    Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).
    Neurotensin
  • HY-P0251
    Neurotensin(8-13)
    		Agonist 99.95%
    Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.
    Neurotensin(8-13)
  • HY-110155
    LM11A-31 dihydrochloride
    		≥98.0%
    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. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
    LM11A-31 dihydrochloride
  • HY-137322
    THX-B
    		Antagonist 98.87%
    THX-B is a potent and non-peptidic p75NTR (neurotrophin receptor p75) antagonist. THX-B can be used in the research of diabetic kidney disease, neurodegenerative and inflammatory disorders.
    THX-B
  • HY-148650A
    (R)-Sortilin antagonist 1
    		Antagonist
    (R)-Sortilin antagonist 1 is a sortilin antagonist that blocks the sortilin mediated apoptosis pathway by interfering with the binding of sortilin to its ligand pro-neurotrophin. (R)-Sortilin antagonist 1 can be used in the study of hearing loss.
    (R)-Sortilin antagonist 1
  • HY-14277AR
    Levocabastine hydrochloride (Standard)
    		Antagonist
    Levocabastine (hydrochloride) (Standard) is the analytical standard of Levocabastine (hydrochloride). This product is intended for research and analytical applications. 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).
    Levocabastine hydrochloride (Standard)
  • HY-P0251A
    Neurotensin(8-13) TFA
    		Agonist
    Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) TFA results in a decrease in cell-surface NT1 receptors (NTR1) density.
    Neurotensin(8-13) TFA
  • 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.
    SBI-553
  • HY-115213
    SORT-PGRN interaction inhibitor 1
    		Inhibitor 99.17%
    SORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction with an IC50 of 2 μM.
    SORT-PGRN interaction inhibitor 1
  • HY-16639
    ML314
    		Agonist 99.52%
    ML314 is a potent molecule agonist of NTR1 (EC50 = 1.9 μM); showed good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization.
    ML314
  • HY-P2544
    [Lys8, Lys9]-Neurotensin (8-13)
    		Activator 99.97%
    [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.
    [Lys8, Lys9]-Neurotensin (8-13)
  • HY-P99688
    Latozinemab
    		Inhibitor
    Latozinemab (AL001) is a recombinant human 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.
    Latozinemab
  • HY-107664A
    SR 142948 dihydrochloride
    		Antagonist 98.6%
    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.
    SR 142948 dihydrochloride
  • 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.
    AF40431
  • HY-148650
    Sortilin antagonist 1
    		Antagonist 99.63%
    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.
    Sortilin antagonist 1
  • HY-107664
    SR 142948
    		Antagonist 99.16%
    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.
    SR 142948
  • HY-P1255
    Kinetensin
    		Agonist 99.89%
    Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma.
    Kinetensin
  • HY-153686
    BVFP
    		Inhibitor 98.12%
    BVFP binds to the PGRN588–593 peptide with a Kd of 20 μM. BVFP can disrupt PGRN-SORT1 binding. BVFP also inhibits SORT1-mediated rPGRN endocytosis.
    BVFP
  • HY-12436
    NTRC-824
    		Antagonist 98.2%
    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).
    NTRC-824
Cat. No. Product Name / Synonyms Application Reactivity
Neurotensin Receptor Isoform Comparison

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