Neurotensin Receptor

Related Products

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 Related Products (28)
Antibodies (1)

By Effects:	Inhibitors (7) Agonists (8) Antagonists (8) Activator (1) Modulators (2)

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.

HY-P0234

Neurotensin	Agonist	98.78%
Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).

HY-110155

LM11A-31 dihydrochloride		≥98.0%
LM11A-31 dihydrochloride, a non-peptide p75^NTR (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. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.

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.

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.

HY-137322

THX-B	Antagonist	98.87%
THX-B is a potent and non-peptidic p75^NTR (neurotrophin receptor p75) antagonist. THX-B can be used in the research of diabetic kidney disease, neurodegenerative and inflammatory disorders.

HY-115213

SORT-PGRN interaction inhibitor 1	Inhibitor	98.94%
SORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction with an IC₅₀ of 2 μM.

HY-124673

AF40431	Inhibitor	98.00%
AF40431, the first reported small-molecule ligand of sortilin, has an IC₅₀ of 4.4 µM and a K_d of 0.7 µM . AF40431 is bound in the neurotensin-binding site of sortilin.

HY-16639

ML314	Agonist	99.82%
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.

HY-107664A

SR 142948 dihydrochloride	Antagonist	≥98.0%
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.

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.

HY-P1255

Kinetensin	Agonist	99.57%
Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma.

HY-14277A

Levocabastine hydrochloride	Antagonist	≥99.0%
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 K_i of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).

HY-P2544

[Lys8, Lys9]-Neurotensin (8-13)	Activator	99.81%
[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 K_i values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively.

HY-148650

Sortilin antagonist 1	Antagonist
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.

HY-107664

SR 142948	Antagonist
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.

HY-P1256C

JMV 449 acetate	Agonist	99.91%
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.

HY-12436

NTRC-824	Antagonist	98.02%
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 K_i of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (K_i >30 μM).

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.

HY-P4223

Acetyl neurotensin (8-13)
Acetyl neurotensin (8-13) is the shortest analog of neurotensin with full binding and pharmacological activities.

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Neurotensin Receptor

Neurotensin Receptor

Neurotensin Receptor Related Products (28)

Antibodies (1)

Neurotensin Receptor Related Products (28):