neurotensinreceptor

Meclinertant (SR 48692) is a neurotensin receptor-1 (NT1) antagonist that blocks neurotensin-induced excitation and can be used to study neurological disorders.

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

SBI-553 is an effective and brain penetrant NTR1 allosteric modulator (EC50: 0.34 μM).

(±)-AC 7954 hydrochloride is a urotensin-II (UT) receptor activator.

SB 611812 is an antagonist of urotensin-II (UT) and can be used in studies about the treatment of cardiovascular disease.

SR 142948 is a neurotensin (NT) receptor antagonist.

Neurotensin(8-13) is Neurotensin (NT) fragment, Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.

Neurotensin(8-13) 3TFA is Neurotensin (NT) fragment. Neurotensin(8-13) 3TFA results in a decrease in cell-surface NT1 receptors (NTR1) density.

Latozinemab (AL001) is a potent and selective recombinant humanized monoclonal antibody against Sortilin.Latozinemab has a high affinity for Sortilin and interrupts the interaction between the granule protein precursor (PGRN) and the Sortilin receptor.Latozinemab can be used to study of dementia and Alzheimer's disease.

Compound 10, an hNTS1R agonist-1, acts as a full agonist with a strong affinity for hNTS1R (K i: 6.9 nM), showing the ability to cross the blood-brain barrier (BBB). It not only enhances motor function but also improves memory in a mouse model of Parkinson's disease (PD). Additionally, this compound is an analog of Neurotensin(8-13) and demonstrates neuroprotective properties [1].

BVFP is a PGRN-SORT1 inhibitor/SORT1 antagonist that binds to key residues 588-593 of PGRN, a multifunctional secreted glycoprotein, and SORT1, a neuronal receptor for PGRN.BVFP is able to block PGRN-SORT1 binding, restore extracellular levels of PGRN , inhibits SORT1-mediated rPGRN endocytosis, and has therapeutic potential for frontotemporal lobe dementia (FTLD-TDP).

SORT-PGRN Interaction Inhibitor 3 (Compound 13), with an IC50 value of 0.17 μM, acts as an inhibitor of the SORT-PGRN interaction, and is utilized in the study of neurodegenerative diseases [1].

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

Neurotensin is a 13 amino acid neuropeptide that is implicated in the regulation of luteinizing hormone and prolactin release and has significant interaction with the dopaminergic system.

UFP 803 acetate is a potent ligand of urotensin-II (UT) receptor. UFP-803 displays the activity of a lower residual agonist.

Urantide acetate is a selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-ind

ML314 is a brain-permeable nonpeptide β-inhibin-biased neurotensin NTR1 receptor agonist (EC50: 1.9 μM), a biased neurotensin receptor ligand for methamphetamine abuse that inhibits NTR2 and GPR35.

AF38469 is a new, specific and orally bioavailable Sortilin inhibitor (IC50: 330 nM).

LM11A-31 dihydrochloride is a water-soluble, non-peptide with high blood-brain barrier permeability.LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist.

AF40431 is the first reported small-molecule ligand of sortilin (IC50: 4.4 µM; Kd: 0.7 µM). AF40431 is bound in the neurotensin-binding site of sortilin.

NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM). NTRC-824 is an effective, selective, and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist (IC50: 38 nM and a Ki : 202 nM).

SBI-810 is a functional selective β-arrestin-biased allosteric modulator of the neurotensin receptor 1 (NTSR1). In the presence of the endogenous ligand neurotensin (NT), SBI-810 regulates NTSR1 signaling through a G protein-specific mechanism. It fully antagonizes NT-induced Gq activation and partially antagonizes NT-induced Gi1 activation, allowing NTSR1 to activate GoA and G12.

SBI-810 hydrochloride is a β-arrestin-2 (βarr2)-biased allosteric modulator of NTSR1 (neurotensin receptor 1), exerting analgesic effects through peripheral and central mechanisms by inhibiting excitatory synaptic transmission, suppressing NMDA receptor and ERK signalling in spinal nociceptive neurons, and reducing Nav1.7 expression and action potential discharge in primary sensory neurons.

SR 142948-C3-NHMe is the methylated form of SR 142948.