Neurotensin Receptors
Neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin. Two of the receptors encoded by the NTSR1 and NTSR2 genes contain seven transmembrane helices and are G protein coupled. The third receptor has a single transmembrane domain and is encoded by the SORT1 gene. Neurotensin (NTS) is a 13-amino-acid peptide that functions as both a neurotransmitter and a hormone through the activation of the neurotensin receptor NTSR1, a G-protein-coupled receptor (GPCR). In the brain, NTS modulates the activity of dopaminergic systems, opioid-independent analgesia, and the inhibition of food intake; in the gut, NTS regulates a range of digestive processes.
Products for Neurotensin Receptors
- Cat.No. Product Name Information
- GC19023 AF38469 AF38469 is a novel, selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
- GC38586 AF40431 AF40431, the first reported small-molecule ligand of sortilin, has an IC50 of 4.4 ?M and a Kd of 0.7 ?M .
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GC17784
JMV 449
JMV 449 is a potent, long-lasting neurotensin receptor agonist
- GC61800 JMV 449 acetate JMV 449 acetate is a potent neurotensin receptor agonist.
- GC14971 Kinetensin (human) Kinetensin (human) is a neurotensin-like peptide isolated from pepsin-treated human plasma.
- GC19441 Levocabastine (hydrochloride) Levocabastine is a potent and selective histamine H1 receptor antagonist with an IC50 value of 8.32 nM (Kis = 62.5, 23,500, and 1,937 nM for H1, H2, and H3, respectively) for inhibition of phosphoinositide turnover on human conjunctival epithelial cells.
- GC18216 ML314 An NTS1 agonist
- GC16357 Neurotensin NTR1 activator
- GC36729 Neurotensin(8-13) Neurotensin (8-13) is an active fragment of Neurotensin.
- GC50164 NTRC 824 Potent and selective non-peptide NTS2 antagonist
- GC38847 SBI-553 SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
- GC61739 SORT-PGRN interaction inhibitor 1 SORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction with an IC50 of 2 μM.
- GC16683 SR 142948 neurotensin (NT) receptor antagonist
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GC69940
SR 142948 dihydrochloride
SR 142948 dihydrochloride is an orally active and selective non-peptide antagonist of the neurotensin receptor (NT). Its IC50 values are 1.19 nM, 0.32 nM, and 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain respectively. SR 142948 dihydrochloride inhibits NT-induced inositol phosphate formation with an IC50 value of 3.9 nM in HT-29 cells. In vivo, it blocks NT-induced hypothermia, analgesia, and turning behavior. SR 142948 dihydrochloride can penetrate the blood-brain barrier and can be used for research on psychiatric disorders.
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GC13242
SR 48692
nonpeptide neurotensin antagonist
- GC50096 TC NTR1 17 Selective NTS1 partial agonist
- GC67786 THX-B
- GC11333 Xenin 8 neurotensin-like peptide that modulate pancreatic insulin and glucagon secretion/effects