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 |
|---|---|---|---|---|
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V69878 | (S)-Osanetant ((S)-SR142801) | 182621-58-5 | (S)-Osanetant is the S enantiomer of Osanetant. |
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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. |
|
V4017 | ML314 | 1448895-09-7 | ML314 is a novel potent small molecule agonist of NTR1 (Neurotensin 1 Receptor) with EC50 of 1.9 μM. |
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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. |
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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). |
|
V69874 | Sortilin antagonist 1 | 2691846-93-0 | Sortilin antagonist 1 (compound 44) is a sortilin antagonist that can inhibit/disrupts the binding of neurotensin (NTS) to Sortilin with IC50 of 20 nM. |
|
V2091 | Talnetant (SB 223412) | 174636-32-9 | Talnetant (formerly also known as SB 223412) is a potent and selective NK3 receptor antagonist with ki value of 1.4 nM (hNK-3-CHO); Selectivity studies versus the other neurokinin receptors (hNK-2-CHO and hNK-1-CHO) revealed that Talnetant is about 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 microM. |
|
V70845 | THX-B | 1372206-64-8 | THX-B is a potent, non-peptide antagonist of p75NTR (neurotrophin receptor p75). |
|
V69877 | VGD071 | 2826992-31-6 | VGD071, a sortilin-targeting compound, is a promising candidate active molecule for study using mouse breast cancer models. |
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