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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-139668
    VGD071
    		Inhibitor
    VGD071, a sortilin-targeting compound, is a promising candidate for future studies using mouse breast cancer models.
    VGD071
  • 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.
    [D-Trp11]-Neurotensin
  • HY-153686
    BVFP
    		Inhibitor
    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-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.
    (S)-Osanetant
  • 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.
    Contulakin G
  • HY-149941
    hNTS1R agonist-1
    		Agonist
    hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent.
    hNTS1R agonist-1
  • HY-P1256
    JMV 449
    		Agonist
    JMV 449 is a potent neurotensin receptor agonist. JMV 449 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 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.
    JMV 449
Cat. No. Product Name / Synonyms Application Reactivity