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 Isoform Specific Products
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Neurotensin Receptor Inhibitors
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Neurotensin Receptor Antagonists
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Neurotensin Receptor Related Products (71)
Related Products (71)
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Antibodies (1)
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Neurotensin Receptor Isoform Comparison
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Neurotensin
0 ImagesNeurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).
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AF38469
0 ImagesAF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
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POPG sodium
0 ImagesSynonyms: PG(16:0/18:1) sodium; 1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol) sodiumPOPG (sodium) is a negatively charged phospholipid. POPG (sodium) affects the interactions of membrane proteins with other molecules by changing the charge characteristics of the lipid environment. POPG (sodium) increases the apparent affinity of Gαq and Gβ1γ1 for activated NTS1. POPG (sodium) can interact with the positive charge of peptides. POPG sodium salt can be used in Parkinson's disease research.
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LM11A-31 dihydrochloride
0 ImagesLM11A-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.
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DOTA-NT-20.3-IPBA
0 ImagesCat. No.: HY-P11845DOTA-NT-20.3-IPBA is a Neurotensin receptor 1 (NTR1)-targeting albumin binder with specific high-affinity binding to NTR1. DOTA-NT-20.3-IPBA is formed by the conjugation of DOTA-NT-20.3 and IPBA. DOTA-NT-20.3-IPBA can be used for positron emission tomography (PET) imaging following labeling with [68Ga]Ga.
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VGD020
0 ImagesCat. No.: HY-182674CAS No.: 1322645-32-8VGD020 is a highly potent and selective Sec61 translocon inhibitor. VGD020 suppresses the expression of cell surface CD4 by inhibiting signal peptide-dependent co-translational ER translocation, interferes with the initiation of ER translocation of dengue virus polyprotein, and reduces the expression of Sortilin in breast cancer cells. VGD020 exhibits broad anti-flavivirus and anti-HIV activities. VGD020 can be used in research related to dengue virus infection, Zika virus infection, yellow fever virus infection, human immunodeficiency virus infection, and breast cancer.
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Fmoc-DL-Leu-OH
0 ImagesCat. No.: HY-W574030CAS No.: 126727-03-5Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor (NTS1R) with an EC50 of 215.50 μM. Fmoc-DL-Leu-OH triggers intracellular calcium mobilization, and its activity is blocked by selective NTS1R antagonists. Fmoc-DL-Leu-OH can be used in the research of schizophrenia.
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THX-B
0 ImagesTHX-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.
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Latozinemab
0 ImagesCat. No.: HY-P99688CAS No.: 2376132-27-1Synonyms: AL001Latozinemab (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.
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[Lys8, Lys9]-Neurotensin (8-13)
![[Lys8, Lys9]-Neurotensin (8-13)](https://file.medchemexpress.com/product_pic/hy-p2544.gif "Click to View [Lys8, Lys9]-Neurotensin (8-13) Product Detail")
0 ImagesSynonyms: JMV438[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.
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SR 142948
0 ImagesSR 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.
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SBI-810 hydrochloride
0 ImagesSBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride 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 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders.
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Levocabastine hydrochloride
0 ImagesSynonyms: R 50547 hydrochlorideLevocabastine (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).
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ML314
0 ImagesML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions.
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JMV 449 acetate
0 ImagesCat. No.: HY-P1256CPurity: 99.69%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.
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SORT-PGRN interaction inhibitor 1
0 ImagesSORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction with an IC50 of 2 μM.
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BVFP
0 ImagesBVFP 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.
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Sortilin antagonist 1
0 ImagesSortilin 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.
