Neurotensin Receptor

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

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

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

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.

Kinetensin acetate(103131-69-7 free base) is isolated from pepsin-treated human plasma. Kinetensin acetate(103131-69-7 free base) is a neurotensin-like peptide.

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

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.

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

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

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

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

[Lys8, Lys9]-Neurotensin (8-13) acetate, a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2, with Ki values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively[1].

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

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.

Substance P 1-9 aceate is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder.

NTRC-844 is a selective rat neurotensin receptor type 2 (NTS2) antagonist that shows analgesic activity in animal models of pain.

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

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).

SORT1-IN-5 (compound 3) is a SORT1 inhibitor capable of crossing the blood-brain barrier. The MSOH salt form of SORT1-IN-5 exhibits a certain degree of oral bioavailability.

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.

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].

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].

MD01-67 is a macrocyclic compound selectively targeting the neurotensin 2 receptor (NTS2), with a Ki of 2.9 nM. It exhibits analgesic activity and reduces tactile hypersensitivity in rat models of acute, sustained, and chronic inflammatory pain.

SR 142948 is a neurotensin (NT) receptor antagonist.