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-161903
    Progranulin modulator-3
    		Inducer 99.95%
    Progranulin modulator-3 (compd C40) is a brain-penetrant and orally active progranulin (PGRN) inducer. Progranulin modulator-3 can be used for neurological research.
    Progranulin modulator-3
  • 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
  • HY-124673
    AF40431
    		Inhibitor 98.09%
    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-P0253
    Xenopsin
    		Agonist 99.88%
    Xenopsin, a neurotensin-like octapeptide from Xenopus laevis skin. Xenopsin is an inhibitor of Tetragastrin stimulated gastric acid secretion.
    Xenopsin
  • HY-P1255
    Kinetensin
    		Agonist 99.89%
    Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma.
    Kinetensin
  • HY-12217
    NTRC-739
    		Agonist
    NTRC-739 is a selective nonpeptide partial neurotensin receptor type 2 (NTS2) agonist with an EC50 of 12 nM and a Ki of 153 nM. NTRC-739 is 161-fold selective for NTS2 versus NTS1. NTRC-739 can be used for the study of chronic pain research.
    NTRC-739
  • HY-107664A
    SR 142948 dihydrochloride
    		Antagonist 99.07%
    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-RS09638
    NTSR1 Human Pre-designed siRNA Set A
    		Inhibitor

    NTSR1 Human Pre-designed siRNA Set A contains three designed siRNAs for NTSR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    NTSR1 Human Pre-designed siRNA Set A
  • HY-124831
    NTRC-844
    		Antagonist
    NTRC-844 (compound 8) is a selective antagonist of neurotensin receptor type 2 (NTS2),with the EC50 of 238 nM. NTRC-844 plays an important role in analgesic animal research.
    NTRC-844
  • HY-164795
    SBI-810
    		Modulator 98.25%
    SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders.
    SBI-810
  • 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-107761
    JMV 390-1
    JMV 390-1 (Compound 6a) is a potent multipeptidase inhibitor. JMV 390-1 behaves as a full inhibitor of the major neurotensin (NT)/neuromedin N (NN) degrading enzymes in vitro with IC50 values from 30 to 60 nM. JMV 390-1 increases endogenous recovery of NT and NN from slices of mice hypothalamus depolarized with potassium.
    JMV 390-1
  • HY-P1257A
    Xenin-8 TFA
    Xenin-8 TFA, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 TFA stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM).
    Xenin-8 TFA
  • HY-153688
    SORT-PGRN interaction inhibitor 3
    		Inhibitor
    SORT-PGRN interaction inhibitor 3 (Compound 13) is a SORT-PGRN interaction inhibitor (IC50: 0.17 μM). SORT-PGRN interaction inhibitor 3 can be used for research of neurodegenerative diseases.
    SORT-PGRN interaction inhibitor 3
  • HY-107664B
    SR 142948 TFA
    		Antagonist
    SR 142948 TFA 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 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders.
    SR 142948 TFA
  • HY-RS09639
    Ntsr1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Ntsr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ntsr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Ntsr1 Mouse Pre-designed siRNA Set A
  • HY-P0253A
    Xenopsin TFA
    		Agonist
    Xenopsin TFA, a neurotensin-like octapeptide from Xenopus laevis skin. Xenopsin TFA is an inhibitor of Tetragastrin stimulated gastric acid secretion.
    Xenopsin TFA
  • HY-P4223
    Acetyl neurotensin (8-13)
    Acetyl neurotensin (8-13) is the shortest analog of neurotensin with full binding and pharmacological activities.
    Acetyl neurotensin (8-13)
  • 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).
    Levocabastine
  • HY-137525
    NTRC-808
    		Agonist
    NTRC-808 is a nonpeptide selective GPCR neurotensin receptor type 2 (NTS2) partial agonist with an EC50 of 14 nM and Ki of 88 nM. NTRC-808 has higher selectivity for NTS2 than for NTS1. NTRC-808 has antipsychotic and analgesic activity.
    NTRC-808
Cat. No. Product Name / Synonyms Application Reactivity
Neurotensin Receptor Isoform Comparison

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