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.
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Neurotensin Receptor Inhibitors
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Neurotensin Receptor Verwandte Produkte (75)
Verwandte Produkte (75)
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Antibodies (1)
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Neurotensin Receptor Isoform Comparison
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AF40431
0 ImagesAF40431, 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.
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Xenopsin
0 ImagesXenopsin, a neurotensin-like octapeptide from Xenopus laevis skin. Xenopsin is an inhibitor of Tetragastrin stimulated gastric acid secretion.
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SBI-810
0 ImagesSBI-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.
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NTRC-739
0 ImagesNTRC-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.
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SR 142948 dihydrochloride
0 ImagesArt. -Nr.: HY-107664AReinheit: 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.
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Kinetensin
0 ImagesSynonyms: Kinetensin (human)Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma.
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NTSR1 Human Pre-designed siRNA Set A
0 ImagesArt. -Nr.: HY-RS09638NTSR1 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.
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NTRC-844
0 ImagesArt. -Nr.: HY-124831CAS. Nr.: 1811503-67-9NTRC-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.
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PD-149163
0 ImagesPD-149163 is an NTR-1 agonist. PD-149163 reverses intestinal damage through its anti-inflammatory, antioxidant, and cell proliferation promoting properties. PD-149163 has antipsychotic effects. PD-149163 is commonly used in research on mental illness and intestinal injury.
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(R)-Sortilin antagonist 1
0 ImagesArt. -Nr.: HY-148650ACAS. Nr.: 2889422-86-8(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.
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Capa-2
0 ImagesArt. -Nr.: HY-P11380CAS. Nr.: 454186-80-2Capa-2 is a neuropeptide. Capa-2 activates calcium ion influx, stimulates the production of NO, activates soluble guanylate cyclase (sGC), increases intracellular cGMP, and drives ion and fluid secretion. Capa-2 can be used in studies of diuresis.
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JMV 390-1
0 ImagesArt. -Nr.: HY-107761CAS. Nr.: 148473-36-3JMV 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.
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SORT-PGRN interaction inhibitor 3
0 ImagesArt. -Nr.: HY-153688CAS. Nr.: 2691846-87-2SORT-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.
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SR 142948 TFA
0 ImagesArt. -Nr.: HY-107664BSR 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.
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Ntsr1 Mouse Pre-designed siRNA Set A
0 ImagesArt. -Nr.: HY-RS09639Ntsr1 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.
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Acetyl neurotensin (8-13)
0 ImagesArt. -Nr.: HY-P4223CAS. Nr.: 74853-69-3Acetyl neurotensin (8-13) is the shortest analog of neurotensin with full binding and pharmacological activities.
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[D-Arg1,D-Trp5,7,9,Leu11]-Substance P
![[D-Arg1,D-Trp5,7,9,Leu11]-Substance P](https://file.medchemexpress.com/product_pic/hy-p11405.gif "Click to View [D-Arg1,D-Trp5,7,9,Leu11]-Substance P Product Detail")
0 ImagesArt. -Nr.: HY-P11405CAS. Nr.: 122481-75-8[D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is a potent inhibitor of cell growth in small cell lung cancer (SCLC). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is also a neuropeptide antagonist, capable of blocking colony formation stimulated by various neuropeptides (including vasopressin and bradykinin). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the mobilization of Ca2+ and the activation of mitogen-activated protein kinases induced by vasopressin or bradykinin. [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the growth of H-69 xenograft tumors in nude mice.
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Levocabastine
0 ImagesArt. -Nr.: HY-14277CAS. Nr.: 79516-68-0Synonyms: R 50547Levocabastine (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).
