Neurotensin Receptor Modulator

DOTA-NT-20.3-IPBA is a Neurotensin receptor 1 (NTR1)-targeting albumin binder with specific high-affinity binding to NTR1. DOTA-NT-20.3-IPBA is formed by the conjugation of DOTA-NT-20.3 and IPBA. DOTA-NT-20.3-IPBA can be used for positron emission tomography (PET) imaging following labeling with [⁶⁸Ga]Ga.

SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC₅₀ of 0.34 μM.

SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders.

SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders.

[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension.

JMV 7490 is a highly potent and highly hydrophilic neurotensin receptor NTS₁ probe that can be successfully labeled with ⁶⁸Ga and ¹¹¹In. JMV 7490 acts as an efflux inhibitor to reduce its efflux in NTS₁-positive cancer cells; it also serves as an internalization inducer and is efficiently and continuously internalized by NTS₁-positive cancer cells. ¹¹¹In-radiolabeled JMV 7490 shows persistent uptake in NTS₁-positive xenografts in nude mice, but no significant uptake in NTS₁-negative xenografts. JMV 7490 can be used for in vivo tracer applications of NTS1-positive tumors and supports related research on colorectal cancer.