Neurotensin Receptor Agonist

Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).

Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.

Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor (NTS1R) with an EC₅₀ of 215.50 μM. Fmoc-DL-Leu-OH triggers intracellular calcium mobilization, and its activity is blocked by selective NTS1R antagonists. Fmoc-DL-Leu-OH can be used in the research of schizophrenia.

ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC₅₀ = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions.

JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC₅₀ of 0.15 nM for inhibition of ¹²⁵I-neurotensin binding to neonatal mouse brain and an EC₅₀ of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse.

Xenopsin, a neurotensin-like octapeptide from Xenopus laevis skin. Xenopsin is an inhibitor of Tetragastrin stimulated gastric acid secretion.

NTRC-739 is a selective nonpeptide partial neurotensin receptor type 2 (NTS2) agonist with an EC₅₀ of 12 nM and a K_i of 153 nM. NTRC-739 is 161-fold selective for NTS2 versus NTS1. NTRC-739 can be used for the study of chronic pain research.

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

PD-149163 is an NTR-1 agonist. PD-149163 reverses intestinal damage through its anti-inflammatory, antioxidant, and cell proliferation promoting properties. PD-149163 has antipsychotic effects. PD-149163 is commonly used in research on mental illness and intestinal injury.

Xenopsin TFA, a neurotensin-like octapeptide from Xenopus laevis skin. Xenopsin TFA is an inhibitor of Tetragastrin stimulated gastric acid secretion.

NTRC-808 is a nonpeptide selective GPCR neurotensin receptor type 2 (NTS2) partial agonist with an EC₅₀ of 14 nM and K_i of 88 nM. NTRC-808 has higher selectivity for NTS2 than for NTS1. NTRC-808 has antipsychotic and analgesic activity.

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

SR-12062 is a Neurotensin receptor 1 (NTSR1) full agonist that modulates NTSR1 to trigger intracellular Ca²⁺ mobilization. SR-12062 can be used for the research of schizophrenia, parkinson’s disease, drug addiction.

Contulakin G is an O-glycosylated invertebrate neurotensin. Contulakin-G is a weaker agonist for the neurotensin receptor. Contulakin G is also a potent antinociceptive agent.

hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (K_i: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent.

JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC₅₀ of 0.15 nM for inhibition of [¹²⁵I]-neurotensin binding to neonatal mouse brain and an EC₅₀ of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.