The neuropeptide neurotensin (NT) has a number of effects that involve the modulation of the nigrostriatal and mesocortico-limbic dopaminergic pathways, including hypothermia, analgesia, and other effects. The seven putative transmembrane domains (TM) family of G-protein-coupled receptors includes the two neurotensin receptor subtypes that are currently known, NTR1 and NTR2. Levocabastine, an anti-histamine H1 receptor antagonist, selectively recognizes the NTR2, which has a lower affinity for the neurotensin peptide than the NTR1. These receptors have different ontogenic profiles and widespread central and peripheral distributions, though they are not identical.
It is noteworthy that NTR1 activation not only causes significant hypotension and hypothermia but also notable antinociception. A potent analgesic activity is demonstrated by NTR2-selective analogues in both acute and chronic pain conditions, with dose-dependent analgesic effects that do not result in a drop in blood pressure or body temperature. In stark contrast, NTR2 has become a key pain target.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V86688 | (R)-Sortilin antagonist 1 | 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. |
|
V69878 | (S)-Osanetant ((S)-SR142801) | 182621-58-5 | (S)-Osanetant is the S enantiomer of Osanetant. |
|
V6718 | AF38469 | 1531634-31-7 | AF38469 is a novel, potent, selective, and orally bioavailable inhibitor of theVPS10P family sorting receptor Sortilinwith an IC50 value of 330 nM. |
|
V70847 | AF40431 | 181125-92-8 | AF40431 is the first reported small molecule ligand for sortilin, with IC50 of 4.4 µM and a Kd of 0.7 µM. |
|
V70843 | BVFP | 357158-20-4 | BVFP binds to the PGRN588-593 peptide with a Kd of 20 μM. |
|
V69875 | Contulakin G | 229180-41-0 | Contulakin G is an O-glycosylated invertebrate neurotensin. |
|
V69879 | JMV 449 | 139026-66-7 | JMV 449 is a potent neurotensin receptor agonist. |
|
V69876 | JMV 449 acetate | 141863-45-8 | JMV 449 acetate is a potent neurotensin receptor agonist. |
|
V2233 | LM11A-31 HCl | 1243259-19-9 | LM11A-31 HCl，a non-peptide p75NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist，in preventing diabetes-induced BRB breakdown. |
|
V106232 | MD01-67 | 2468971-42-6 | MD01-67 is a macrocyclic compound that selectively targets the neurotensin type 2 receptor (NTS2) with a Ki of 2.9 nM. |
|
V4017 | ML314 | 1448895-09-7 | ML314 is a novel potent small molecule agonist of NTR1 (Neurotensin 1 Receptor) with EC50 of 1.9 μM. |
|
V103964 | SBI-810 | 1849603-79-7 | SBI-810 is a functionally selective β-arrestin-biased allosteric modulator of neurotensin receptor 1 (NTSR1). |
|
V103965 | SBI-810 hydrochloride | 2772746-58-2 | SBI-810 hydrochloride is a functionally selective β-arrestin-biased allosteric modulator of neurotensin receptor 1 (NTSR1). |
|
V70846 | SORT-PGRN interaction inhibitor 1 | 100957-85-5 | SORT-PGRN interaction inhibitor 1 is a potent inhibitor of sortilin-progranulin interaction with IC50 of 2 μM. |
|
V70844 | SORT-PGRN interaction inhibitor 3 | 2691846-87-2 | SORT-PGRN interaction inhibitor 3 (Compound 13) is a SORT-PGRN interaction inhibitor (IC50= 0.17 μM). |
|
V103659 | SORT1-IN-1 | 2806762-69-4 | SORT1-IN-1 (Compound 2) is a SORT1 inhibitor. |
|
V103661 | SORT1-IN-2 | 2854233-44-4 | SORT1-IN-2 (Compound 6) is a SORT1 inhibitor. |
|
V103662 | SORT1-IN-3 | 2915675-56-6 | SORT1-IN-3 (compound 5) is a blood-brain barrier-permeable SORT1 inhibitor. |
|
V103663 | SORT1-IN-4 | 2915675-58-8 | SORT1-IN-4 (compound 6) is a blood-brain barrier-permeable SORT1 inhibitor. |
|
V103664 | SORT1-IN-5 | 3031580-91-0 | SORT1-IN-5 (compound 3) is a blood-brain barrier-permeable SORT1 inhibitor. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
