Neurotensin Receptors

neurotensin-like peptide that modulate pancreatic insulin and glucagon secretion/effects

SR 48692 (Meclinertant) is an orally bioavailable, allosteric antagonist of the neuropeptide Y receptor NTS1 (K d =3.4nM).

Kinetensin (human) is a neurotensin-like peptide isolated from pepsin-treated human plasma.

Neurotensin is a neuropeptide composed of 13 amino acids, which functions as a neurotransmitter, hormone, and neuromodulator.

neurotensin (NT) receptor antagonist

JMV 449 is a potent and long-acting neurotensin receptor (NTR) agonist peptide. JMV 449 inhibits [ 125 I]-neurotensin binding to newborn mouse brain (IC 50 =0.15nM) and contracts guinea pig ileum (EC 50 =1.9nM).

An NTS 1 agonist

AF38469 is an orally active Sortilin (SORT1; IC₅₀=330nM) receptor inhibitor.

Levocabastine is a potent and selective histamine H1 receptor antagonist with an IC50 value of 8.32 nM (Kis = 62.5, 23,500, and 1,937 nM for H1, H2, and H3, respectively) for inhibition of phosphoinositide turnover on human conjunctival epithelial cells.

Neurotensin(8-13) is the core active fragment of neurotensin and functions as a biologically active neurotensin receptor (NTSR1) agonist. By binding to NTSR1 with high affinity (Kd≈1–10nM), Neurotensin(8-13) activates the Gq/11 protein signaling pathway, thereby regulating intracellular calcium ion concentration and the activity of protein kinase C (PKC).

AF40431, the first reported small-molecule ligand of sortilin, has an IC50 of 4.4 ?M and a Kd of 0.7 ?M .

SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.

Selective NTS1 partial agonist

Potent and selective non-peptide NTS2 antagonist

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

JMV 449 acetate is a potent neurotensin receptor agonist.

Latozinemab (AL001) is a recombinant humanized monoclonal antibody against Sortilin. Latozinemab effectively binds to Sortilin with high affinity and blocks the interaction between progranulin (PGRN) and Sortilin receptors. Latozinemab has the potential to target mutations in the progranulin gene (GRN) that cause frontotemporal dementia (FTD-GRN).

[Lys8, Lys9]-Neurotensin (8-13) (JMV438) is an analogue of neurotensin that exerts its effects by activating G protein-coupled receptors NTS1 and NTS2. Its Ki values for hNTS1 and hNTS2 receptors are 0.33 nM and 0.95 nM, respectively, making it useful for pain relief research.

SR 142948 dihydrochloride is an orally active and selective non-peptide antagonist of the neurotensin receptor (NT). Its IC50 values are 1.19 nM, 0.32 nM, and 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain respectively. SR 142948 dihydrochloride inhibits NT-induced inositol phosphate formation with an IC50 value of 3.9 nM in HT-29 cells. In vivo, it blocks NT-induced hypothermia, analgesia, and turning behavior. SR 142948 dihydrochloride can penetrate the blood-brain barrier and can be used for research on psychiatric disorders.

(S)-Osanetant is the S-enantiomer of Osanetant.

Sortilin antagonist 1 (compound 44) is a sortilin antagonist with an IC50 value of 20 nM for inhibiting Neurotensin (NTS) binds to sortilin.

(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.

Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor ( NTS1R ) with an EC 50 of 215.50 μM.