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Gene and Protein Information  |
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| class A G protein-coupled receptor | ||||||
| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 7 | 418 | 20q13.33 | NTSR1 | neurotensin receptor 1 | 43-44,70 |
| Mouse | 7 | 424 | 2 103.04 cM | Ntsr1 | neurotensin receptor 1 | 43 |
| Rat | 7 | 424 | 3q43 | Ntsr1 | neurotensin receptor 1 | 68 |
| Previous and Unofficial Names |
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| NTR1 | NTRH [8] | NTSR1 | NTR | neurotensin receptor type 1 | Levocabastin-insensitive neurotensin receptor | NT-1R | neurotensin receptor 1 (high affinity) | |
| Database Links |
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| Specialist databases | |
| GPCRdb | ntr1_human (Hs), ntr1_mouse (Mm), ntr1_rat (Rn) |
| Other databases | |
| Alphafold | P30989 (Hs), O88319 (Mm), P20789 (Rn) |
| ChEMBL Target | CHEMBL4123 (Hs), CHEMBL3570 (Mm), CHEMBL3027 (Rn) |
| Ensembl Gene | ENSG00000101188 (Hs), ENSMUSG00000027568 (Mm), ENSRNOG00000028708 (Rn) |
| Entrez Gene | 4923 (Hs), 18216 (Mm), 366274 (Rn) |
| Human Protein Atlas | ENSG00000101188 (Hs) |
| KEGG Gene | hsa:4923 (Hs), mmu:18216 (Mm), rno:366274 (Rn) |
| OMIM | 162651 (Hs) |
| Pharos | P30989 (Hs) |
| RefSeq Nucleotide | NM_002531 (Hs), NM_018766 (Mm), NM_001108967 (Rn) |
| RefSeq Protein | NP_002522 (Hs), NP_061236 (Mm), NP_001102437 (Rn) |
| UniProtKB | P30989 (Hs), O88319 (Mm), P20789 (Rn) |
| Wikipedia | NTSR1 (Hs) |
| Selected 3D Structures |
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| Associated Proteins |
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| Natural/Endogenous Ligands |
| large neuromedin N {Sp: Human} , large neuromedin N {Sp: Mouse} , large neuromedin N {Sp: Rat} |
| large neurotensin {Sp: Human} |
| neuromedin N {Sp: Human} , neuromedin N {Sp: Mouse, Rat} |
| neurotensin {Sp: Human, Mouse, Rat, Bovine} |
| Comments: Neurotensin is the most potent endogenous agonist |
| Potency order of endogenous ligands (Human) |
| neurotensin (NTS, P30990) > neuromedin N (NTS, P30990) [38] |
Download all structure-activity data for this target as a CSV file 
| Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| View species-specific agonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The sequence of neurotensin is identical for all mammalian species. Neurotensin and neuromedin N are synthesised from a common precursor [24]. Neurotensin and [125I]neurotensin bind with high affinity to NTS1 from all species [125I]-Trp11-neurotensin is specific for murine NTS1 receptors and exhibits low affinity for NTS1 receptors of human or other species [48,59]. [125I]-azidobenzoyl-neurotensin(2-13) is a photoreactive and radioactive analogue for covalent labelling of neurotensin receptors (including NTS1) from any species [15-16]. Xenopsin and contulakin-G are natural analogues of neurotensin from Xenopus laevis [5] and Conus geographus resepctively [20]. [α-bodipy]neurotensin(2-13) is a fluorescent synthetic analogue of neurotensin [7]. KH28, ABS212 and ABS-201 are able to cross the blood-brain barrier. ABS-201 and ABS212 are stable bioavailable NT analogues. |
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| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| View species-specific antagonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| SR142948A binds to both NTS1 and NTS2 with similar nanomolar affinities. SR48692 has a 10-30 times higher affinity for NTS1 than for NTS2 [35,42]. |
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| Primary Transduction Mechanisms
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| Transducer | Effector/Response |
| Gq/G11 family | Phospholipase C stimulation |
| References: 2-3,32,39,53,67,71 | |
| Secondary Transduction Mechanisms |
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| Transducer | Effector/Response |
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Gs family Gi/Go family |
Adenylyl cyclase stimulation Adenylyl cyclase inhibition Guanylate cyclase stimulation Other - See Comments |
| Comments: Binding of neurotensin to the human NTS1 receptor indicates activation of MAP kinases and stimulates transcription of Krox-24, c-fos and Elk-1 [56,58]. | |
| References: 4,14,32-33,53,73 | |
| Tissue Distribution
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| Expression Datasets |
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| Functional Assays
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| Physiological Functions
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| Physiological Consequences of Altering Gene Expression
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| Phenotypes, Alleles and Disease Models
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| Biologically Significant Variants
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| General Comments |
| A special issue of the journal "peptides" entitled "Neurotensin: Roles and Mechanisms" has recently been published [26]. |
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42. Labbé-Jullié C, Botto JM, Mas MV, Chabry J, Mazella J, Vincent JP, Gully D, Maffrand JP, Kitabgi P. (1995) [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor. Mol Pharmacol, 47 (5): 1050-6. [PMID:7746272]
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