Page last updated: 2024-08-07 16:27:34
Neurotensin receptor type 1
A neurotensin receptor type 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30989]
Synonyms
NT-R-1;
NTR1;
High-affinity levocabastine-insensitive neurotensin receptor;
NTRH
Research
Bioassay Publications (34)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 9 (26.47) | 29.6817 |
2010's | 20 (58.82) | 24.3611 |
2020's | 5 (14.71) | 2.80 |
Compounds (8)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
sr 48692 | Homo sapiens (human) | EC50 | 31.0000 | 1 | 1 |
sr 48692 | Homo sapiens (human) | Kd | 0.0184 | 7 | 7 |
neurotensin | Homo sapiens (human) | EC50 | 0.0008 | 11 | 12 |
sr 142948 | Homo sapiens (human) | Kd | 0.0004 | 1 | 1 |
sr 142948a | Homo sapiens (human) | EC50 | 45.0000 | 2 | 2 |
neurotensin | Homo sapiens (human) | EC50 | 0.0632 | 5 | 5 |
neurotensin | Homo sapiens (human) | Kd | 0.0006 | 2 | 2 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
sr 48692 | Homo sapiens (human) | Ke | 0.0360 | 1 | 1 |
sr 48527 | Homo sapiens (human) | Ke | 0.0350 | 1 | 1 |
neurotensin | Homo sapiens (human) | Activity | 0.0002 | 1 | 1 |
Imidazole-derived agonists for the neurotensin 1 receptor.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1.Bioorganic & medicinal chemistry, , Oct-15, Volume: 16, Issue:20, 2008
Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors.Bioorganic & medicinal chemistry, , 05-01, Volume: 61, 2022
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
An Alkyne-functionalized Arginine for Solid-Phase Synthesis Enabling "Bioorthogonal" Peptide Conjugation.ACS medicinal chemistry letters, , Mar-12, Volume: 11, Issue:3, 2020
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.ACS medicinal chemistry letters, , Jan-09, Volume: 11, Issue:1, 2020
[no title available]ACS medicinal chemistry letters, , Jun-13, Volume: 10, Issue:6, 2019
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018
In Search of the Optimal Macrocyclization Site for Neurotensin.ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Ligand Discovery for a Peptide-Binding GPCR by Structure-Based Screening of Fragment- and Lead-Like Chemical Libraries.ACS chemical biology, , 03-17, Volume: 12, Issue:3, 2017
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Imidazole-derived agonists for the neurotensin 1 receptor.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.ACS medicinal chemistry letters, , Jul-20, Volume: 4, Issue:9, 2013
[no title available]Journal of medicinal chemistry, , 02-25, Volume: 64, Issue:4, 2021
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.ACS medicinal chemistry letters, , Jan-09, Volume: 11, Issue:1, 2020
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Synthesis and biological effects of c(Lys-Lys-Pro-Tyr-Ile-Leu-Lys-Lys-Pro-Tyr-Ile-Leu) (JMV2012), a new analogue of neurotensin that crosses the blood-brain barrier.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1.Bioorganic & medicinal chemistry, , Oct-15, Volume: 16, Issue:20, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 18, Issue:21, 2008
Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors.Journal of medicinal chemistry, , Jul-17, Volume: 46, Issue:15, 2003
Enables
This protein enables 5 target(s):
Target | Category | Definition |
G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
G protein-coupled neurotensin receptor activity | molecular function | Combining with the tridecapeptide neurotensin to initiate a G-protein mediated change in cell activity. A G-protein is a signal transduction molecule that alternates between an inactive GDP-bound and an active GTP-bound state. [PMID:10390649] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
Located In
This protein is located in 11 target(s):
Target | Category | Definition |
endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
cytoplasmic side of plasma membrane | cellular component | The leaflet the plasma membrane that faces the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
symmetric synapse | cellular component | A synapse that lacks an electron dense postsynaptic specialization. In vertebtrates, these occur primarily on dendrite shafts and neuronal cell bodies and involve persynapses containing clusters of predominantly flattened or elongated vesicles and are typcially inhibitory. [GOC:dgh, GOC:ef] |
terminal bouton | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal bouton is a specialized region of it. [GOC:dph, GOC:mc, GOC:nln, PMID:10218156, PMID:8409967] |
dendritic spine | cellular component | A small, membranous protrusion from a dendrite that forms a postsynaptic compartment, typically receiving input from a single presynapse. They function as partially isolated biochemical and an electrical compartments. Spine morphology is variable:they can be thin, stubby, mushroom, or branched, with a continuum of intermediate morphologies. They typically terminate in a bulb shape, linked to the dendritic shaft by a restriction. Spine remodeling is though to be involved in synaptic plasticity. [GOC:nln] |
dendritic shaft | cellular component | Cylindric portion of the dendrite, directly stemming from the perikaryon, and carrying the dendritic spines. [GOC:nln] |
perikaryon | cellular component | The portion of the cell soma (neuronal cell body) that excludes the nucleus. [GOC:jl] |
membrane raft | cellular component | Any of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 23 target(s):
Target | Category | Definition |
temperature homeostasis | biological process | A homeostatic process in which an organism modulates its internal body temperature. [GOC:jl] |
negative regulation of systemic arterial blood pressure | biological process | The process that reduces the force with which blood travels through the systemic arterial circulatory system. [GOC:mtg_cardio] |
regulation of membrane depolarization | biological process | Any process that modulates the rate, frequency or extent of membrane depolarization. Membrane depolarization is the process in which membrane potential changes in the depolarizing direction from the resting potential, usually from negative to positive. [GOC:dph, GOC:tb] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |
chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
learning | biological process | Any process in an organism in which a relatively long-lasting adaptive behavioral change occurs as the result of experience. [ISBN:0582227089, ISBN:0721662544] |
adult locomotory behavior | biological process | Locomotory behavior in a fully developed and mature organism. [GOC:ai] |
positive regulation of glutamate secretion | biological process | Any process that activates or increases the frequency, rate or extent of the controlled release of glutamate. [GOC:ef] |
positive regulation of gamma-aminobutyric acid secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of gamma-aminobutyric acid. [GOC:ef] |
response to lipid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipid stimulus. [GOC:sl] |
positive regulation of apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
regulation of respiratory gaseous exchange | biological process | Any process that modulates the frequency, rate or extent of the process of gaseous exchange between an organism and its environment. [GOC:jl] |
detection of temperature stimulus involved in sensory perception of pain | biological process | The series of events involved in the perception of pain in which a temperature stimulus is received and converted into a molecular signal. [GOC:ai, GOC:dos] |
negative regulation of release of sequestered calcium ion into cytosol | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the release into the cytosolic compartment of calcium ions sequestered in the endoplasmic reticulum or mitochondria. [GOC:ai] |
positive regulation of release of sequestered calcium ion into cytosol | biological process | Any process that activates or increases the frequency, rate or extent of the release into the cytosolic compartment of calcium ions sequestered in the endoplasmic reticulum or mitochondria. [GOC:ai] |
positive regulation of inositol phosphate biosynthetic process | biological process | Any process that increases the rate, frequency or extent of inositol phosphate biosynthesis. Inositol phosphate biosynthetic processes are the chemical reactions and pathways resulting in the formation of an inositol phosphate, 1,2,3,4,5,6-cyclohexanehexol, with one or more phosphate groups attached. [GOC:dph, GOC:tb] |
D-aspartate import across plasma membrane | biological process | The directed import of D-aspartate from the extracellular region across the plasma membrane and into the cytosol. [PMID:7914198] |
inositol phosphate catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of an inositol phosphate, 1,2,3,4,5,6-cyclohexanehexol, with one or more phosphate groups attached. [GOC:mah] |
positive regulation of arachidonic acid secretion | biological process | Any process that increases the rate, frequency, or extent of arachidonic acid secretion, the controlled release of arachidonic acid from a cell or a tissue. [GOC:BHF, GOC:dph, GOC:tb] |
positive regulation of inhibitory postsynaptic potential | biological process | Any process that activates or increases the frequency, rate or extent of inhibitory postsynaptic potential (IPSP). IPSP is a temporary decrease in postsynaptic membrane potential due to the flow of negatively charged ions into the postsynaptic cell. The flow of ions that causes an IPSP is an inhibitory postsynaptic current (IPSC) and makes it more difficult for the neuron to fire an action potential. [GOC:BHF, GOC:sjp, PMID:18550748] |
L-glutamate import across plasma membrane | biological process | The directed movement of L-glutamate from outside of a cell, across the plasma membrane and into the cytosol. [GOC:dos] |