mProX™ Human NTSR2 Stable Cell Line

Kyriatzis G, et al. "Neurotensin and Neurotensin Receptors in Stress-related Disorders: ." Current neuropharmacology, 2023.
Neurotensin (NT) is a 13-amino acid neuropeptide that plays a significant role in the development of various neural and psychiatric disorders. Its effects are mediated through three known neurotensin receptors (NTSRs), which make up the neurotensinergic system in conjunction with NT. NTSR1 is the primary mediator of NT and has widespread effects in both the central nervous system (CNS) and the periphery. NTSR2 is mainly expressed in the brain, while NTSR3 has a broader expression pattern. Recent studies have shown that the neurotensinergic system is involved in stress response and stress-related disorders, including depression, anxiety, post-traumatic stress disorder (PTSD), and substance abuse. NTSR1 is mainly implicated in stress response and anxiety, whereas NTSR2 and NTSR3 are involved in depression and PTSD, respectively. Additionally, NTSR1 and NTSR2 are interrelated with substance and drug abuse and fear memory, respectively. The therapeutic potential of targeting NT and NTSRs in these disorders is supported by evidence from gene, mRNA, and protein studies, as well as behavioral and pharmacological research. The mechanisms underlying the involvement of NT and NTSRs in these pathological settings may include interactions with corticotorphin releasing factor (CRF) and pro-inflammatory mediating actions.
Pubmed: 37534788   DOI: 10.2174/1570159X21666230803101629

Kuhl T, et al. "Neurotensin(8-13) analogs as dual NTS1 and NTS2 receptor ligands with enhanced ." European journal of medicinal chemistry, 2023.
It has been suggested that neurotensin (NT) may have a role in the progression of Parkinson's disease (PD), given its modulatory interactions with the dopaminergic neurotransmitter system in the brain. NT exerts its effects on the central nervous system through interactions with its two human receptors, hNTS1 and hNTS2. As such, these receptors have potential as targets for new NT-based treatment options for PD. In this study, a computer-assisted molecular modeling approach was used to investigate the potential activity of NT(8-13) analogs designed to bind to hNTS1 and hNTS2. Experimental evidence from radioligand binding assays confirmed the importance of specific amino acid residues in positions 8 and/or 9 for binding to these receptors. Further in vitro ADME (absorption, distribution, metabolism, and excretion) profiling and in vivo studies showed that compound 10, a derivative of NT(8-13), demonstrated improved stability and ability to pass through the blood-brain barrier, while also showing promising motor and memory function improvements in a PD mouse model. These results suggest that the newly developed dual-specific NT(8-13) analogs could be a potential therapeutic option for PD and other central nervous system disorders.
Pubmed: 37094450   DOI: 10.1016/j.ejmech.2023.115386