Neurotensin Receptors

SR 48692 represents a new, potent, nonpeptide antagonist radioligand of the NT receptor that differentiates between agonist- and antagonist-receptor interactions.

ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2.

JMV 390-1 is a inhibitor of the major neurotensin and neuromedin N degrading enzymes (IC50 values are 31, 40, 52 and 58 nM for endopeptidase 24.15, endopeptidase 24.11, leucine aminopeptidase and endopeptidase 24.16 respectively).

SBI-553 is a potent and brain penetrant NTR1 allosteric modulator.

LM11A-31 is a small-molecule p75NTR modulator and proNGF antagonist.

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.

[Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist.

[Lys8, Lys9]-Neurotensin (8-13) is a neurotensin analog that primarily activates the G protein-coupled receptors NTS1 and NTS2. This compound demonstrates potent analgesic activity, with binding affinities (Ki values) of 0.33 nM and 0.95 nM for the human NTS1 and NTS2 receptors, respectively. It is utilized in research applications investigating pain modulation and neuropeptide signaling pathways.

JMV 449 acetate is a highly potent agonist of the neurotensin receptor. It demonstrates an IC50 of 0.15 nM in inhibiting 125I-neurotensin binding to neonatal mouse brain tissue and an EC50 of 1.9 nM in inducing contractions in the guinea-pig ileum. Additionally, JMV 449 acetate exhibits significant, long-lasting hypothermic and analgesic effects in mouse models, making it valuable for research in pain management and neuropharmacology.

Xenopsin is a neurotensin-like octapeptide derived from the skin of Xenopus laevis. It primarily functions as an inhibitor of Tetragastrin-stimulated gastric acid secretion, making it valuable for studies related to gastrointestinal physiology and acid regulation. Research applications include investigations into peptide signaling pathways and gastrointestinal disorders.

Acetyl neurotensin (8-13) is a neurotensin analog that retains full binding affinity and pharmacological activity. This compound is primarily utilized in research exploring neurotensin receptor interactions and their implications in various physiological processes. Its use may aid in the investigation of neuroinflammatory conditions, pain modulation, and appetite regulation.

VGD071 is a neurotensin receptor inhibitor that specifically targets sortilin. This compound exhibits potential for modulating neurotensin signaling pathways, which may be relevant in the context of breast cancer research. VGD071 is suitable for preclinical studies and investigations into the role of neurotensin receptors in tumorigenesis and cancer progression.

[D-Trp11]-Neurotensin is a neurotensin receptor modulator that acts as a selective antagonist in perfused rat hearts while exhibiting full agonistic activity in guinea pig atria and rat stomach strips. This compound has demonstrated the ability to inhibit neurotensin-induced hypotension, making it a valuable tool for studying neurotensin receptor dynamics and their physiological effects. Its diverse biological activity supports various research applications, including cardiovascular and gastrointestinal studies.

Neurotensin(8-13) TFA is an active fragment of the neuropeptide neurotensin, specifically acting as an agonist of neurotensin receptors. This compound has been shown to decrease the density of cell-surface NT1 receptors (NTR1), impacting various signaling pathways. It is useful in research applications focused on neurobiology, pharmacology, and the study of neurotensin-related pathways in health and disease.

Contulakin G is an O-glycosylated neurotensin analog that functions as an agonist of the neurotensin receptor. This compound exhibits notable antinociceptive properties, making it valuable in pain modulation research. Its unique characteristics allow for exploration in neurobiology and potential therapeutic applications targeting pain relief mechanisms.

SR 142948-C3-NHMe is a selective antagonist of the neurotensin receptor. This compound has demonstrated significant inhibitory activity against neurotensin signaling pathways, making it a valuable tool for studying neurotensin-related physiological processes. It is applicable in research focused on neuropharmacology, pain modulation, and various CNS disorders, providing insight into neurotensin's role in these conditions.

JMV 449 is a potent neurotensin receptor agonist, demonstrating an IC50 of 0.15 nM for the inhibition of [125I]-neurotensin binding in neonatal mouse brain assays. Additionally, it shows an EC50 of 1.9 nM in inducing contractions in the guinea pig ileum. JMV 449 exhibits significant hypothermic and analgesic effects in murine models, making it a valuable tool for research in pain management and neuropharmacology.

L-156903 is a potent neurotensin inhibitor that selectively disrupts the binding of neurotensin to brain tissue. This compound is valuable for studying the neurotensinergic system and its role in various neurological conditions. Its inhibitory action can contribute to research aimed at understanding the mechanisms underlying neuropsychiatric disorders and potential therapeutic interventions.